EA018573B1 - Ингибиторы тирозинкиназы брутона - Google Patents
Ингибиторы тирозинкиназы брутона Download PDFInfo
- Publication number
- EA018573B1 EA018573B1 EA200900351A EA200900351A EA018573B1 EA 018573 B1 EA018573 B1 EA 018573B1 EA 200900351 A EA200900351 A EA 200900351A EA 200900351 A EA200900351 A EA 200900351A EA 018573 B1 EA018573 B1 EA 018573B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- phenoxyphenyl
- pyrazolo
- pyrimidin
- amino
- tyrosine kinase
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
- A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2887—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against CD20
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
- C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
Abstract
В изобретении приведены описания соединений, образующих ковалентные связи с тирозинкиназой Брутона (Btk). Кроме того, описаны необратимые ингибиторы Btk, а также способы получения таких соединений. Также описаны фармацевтические композиции, содержащие такие соединения, а также способы применения ингибиторов Btk отдельно или в комбинации с другими терапевтическими агентами для лечения аутоиммунных заболеваний или состояний, гетероиммунных заболеваний или состояний, рака, включая лимфому, и воспалительных заболеваний или состояний.
Description
(57) В изобретении приведены описания соединений, образующих ковалентные связи с тирозинкиназой Брутона (В(к). Кроме того, описаны необратимые ингибиторы В!к, а также способы получения таких соединений. Также описаны фармацевтические композиции, содержащие такие соединения, а также способы применения ингибиторов В!к отдельно или в комбинации с другими терапевтическими агентами для лечения аутоиммунных заболеваний или состояний, гетероиммунных заболеваний или состояний, рака, включая лимфому, и воспалительных заболеваний или состояний.
018573 Β1
Claims (15)
- ФОРМУЛА ИЗОБРЕТЕНИЯ1. Соединение формулы Ό, имеющее структуру1г-АгНа к7 формула Ώ, где Ьа представляет собой О;Аг представляет собой фенил;Υ представляет собой незамещенный пиперидинил, незамещенный пирролидинил или незамещенный циклогексил;Ζ представляет собой С(=О), ЯНС(=О) или 8(=О)2;Р- и К8 представляют собой Н или вместе образуют связь;Кб представляет собой Н, или его фармацевтически приемлемая соль.
- 2. Соединение по п.1, отличающееся тем, что Υ представляет собой циклогексил.
- 3. Соединение по п.1, отличающееся тем, что Υ представляет собой пиперидиновое кольцо.
- 4. Соединение по п.1, отличающееся тем, что Υ представляет собой пирролидиновое кольцо.
- 5. Соединение, выбранное из1 -(3 -(4-амино-3 -(4-феноксифенил)-1Н-пиразоло [3,4-б]пиримидин-1-ил)пиперидин-1 -ил)проп-2-ин1-она;1 -(3 -(4-амино-3 -(4-феноксифенил)-1Н-пиразоло [3,4-б]пиримидин-1-ил)пиперидин-1 -ил)проп-2-ен-1- она;1 -(3 -(4-амино-3 -(4-феноксифенил)-1Н-пиразоло [3,4-б]пиримидин-1-ил)пиперидин-1 ил)сульфонилэтена;№((1к,4к)-4-(4-амино-3-(4-феноксифенил)-1Н-пиразоло[3,4-б]пиримидин-1ил)циклогексил)акриламида;1 -((К)-3-(4-амино-3 -(4-феноксифенил)-1Н-пиразоло [3,4-б]пиримидин-1 -ил)пирролидин-1 -ил)проп-2- ен-1-она;1 -((8)-3 -(4-амино-3 -(4-феноксифенил)-1Н-пиразоло [3,4-б]пиримидин-1ил)пирролидин-1 -ил)проп-2ен-1-она;1 -((К)-3-(4-амино-3 -(4-феноксифенил)-1Н-пиразоло [3,4-б]пиримидин-1 -ил)пиперидин-1-ил)проп-2ен-1-она;- 55 0185731 -((8)-3 -(4-амино-3 -(4-феноксифенил)-1Н-пиразоло [3,4-й]пиримидин-1-ил)пиперидин-1 -ил)проп-2ен-1-она и1 -(3 -(4-амино-3 -(4-феноксифенил)-1Н-пиразоло [3,4-й]пиримидин-1-ил)пирролидин-1 -ил)проп-2-ен1-она.
- 6. Фармацевтическая композиция, содержащая терапевтически эффективное количество соединения по любому из пп.1-5, представляющего собой ингибитор тирозинкиназы Брутона, и фармацевтически приемлемый эксципиент.
- 7. Ингибированная тирозинкиназа, включающая тирозинкиназу Брутона, связанную с ингибитором, имеющим структуру где Ьа представляет собой О;Аг представляет собой фенил;Υ представляет собой незамещенный пиперидинил, незамещенный пирролидинил или незамещенный циклогексил;Ζ представляет собой С(=О), ΝΗ0(=Ο) или 8(=О)2;К.7 и К8 представляют собой Н или вместе образуют связь;Кб представляет собой Н и \АЛЛЛ указывает точку соединения между ингибитором и тирозинкиназой.
- 8. Ингибированная тирозинкиназа по п.7, отличающаяся тем, что инибитор ковалентно связан с цистеиновым остатком на тирозинкиназе.
- 9. Композиция, содержащая терапевтически эффективное количество соединения по п.1, образующего ковалентную связь с цистеиновой боковой цепью тирозинкиназы Брутона, для использования в лечении рака.
- 10. Композиция по п.9, отличающаяся тем, что в соединении формулы ИΥ представляет собой незамещенный пиперидинил или незамещенный пирролидинил;Ζ представляет собой С(=О), ΝΗί.’(=Ο) или 8(=О)2;К- и К8 представляют собой Н или вместе образуют связь;К6 представляет собой Н.
- 11. Соединение, имеющее структуру или его фармацевтически приемлемая соль.или его фармацевтически приемлемая соль.- 56 018573
- 13. Фармацевтическая композиция, содержащая терапевтически эффективное количество соединения по п.11, представляющего собой ингибитор тирозинкиназы Брутона, и фармацевтически приемлемый эксципиент.
- 14. Фармацевтическая композиция, содержащая терапевтически эффективное количество соединения по п.11, для использования в лечении рака.
- 15. Применение соединения по п.11 в изготовлении лекарственного средства для лечения Вклеточного пролиферативного нарушения.
- 16. Применение по п.15, где В-клеточное пролиферативное нарушение выбрано из лимфомы, миеломы или лейкемии.
473 474 475 476 477 478 479 480 481 482 <1 ВТК I т Г: Υ М Л N О С Е Е нмх V т Е Υ м Л К о С Е Е ТЕС V I Е Г м Е К. о С Е I. так V т Е Е м Е N о ε I, Б ПК V Ё Е Е м Е И а С Б 5 ки I I 9 Б м Г Е о С Б Б &ЬВ2 V т 0 Б М Е Υ Ст с Е Б ЕЙ1В4 V т 9 Б м Р II а с Б Б 1АКЗ V м Е Υ Е Р я □ с Ь К ВЕК V т Е Υ Е Р 5 о с Б Б БСК I т Е Υ м Е N о 8 Б V ΕΥΝ I τ Е Υ м А К □ 8 Е Е 8ΥΚ V М Е м А Е Б а Ё Е N Фиг. 1Фиг. 2- 57 018573-β-1 !мг/кг_ -О- з мг/кг-Ο- ίο мг/кг *-3Ο мг/кгУровни в плазме после введения последней дозыДоза (мг/кг) Концентрация(мкМ) 0.5 ч 2 ч ΐ 0.066 0.049 3 0.250 0.135 ю 0.635 0.070 | зо 1-720 -З103 Фиг. 5- 58 018573Фиг. 7
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US82672006P | 2006-09-22 | 2006-09-22 | |
US82859006P | 2006-10-06 | 2006-10-06 | |
PCT/US2006/049626 WO2008039218A2 (en) | 2006-09-22 | 2006-12-28 | Inhibitors of bruton's tyrosine kinase |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200900351A1 EA200900351A1 (ru) | 2009-10-30 |
EA018573B1 true EA018573B1 (ru) | 2013-09-30 |
Family
ID=39225888
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200900351A EA018573B1 (ru) | 2006-09-22 | 2006-12-28 | Ингибиторы тирозинкиназы брутона |
EA201300246A EA024255B1 (ru) | 2006-09-22 | 2006-12-28 | Синтез ингибиторов тирозинкиназы брутона |
EA201000599A EA020001B1 (ru) | 2006-09-22 | 2006-12-28 | Ингибиторы тирозинкиназы брутона |
Family Applications After (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201300246A EA024255B1 (ru) | 2006-09-22 | 2006-12-28 | Синтез ингибиторов тирозинкиназы брутона |
EA201000599A EA020001B1 (ru) | 2006-09-22 | 2006-12-28 | Ингибиторы тирозинкиназы брутона |
Country Status (28)
Country | Link |
---|---|
US (48) | US7514444B2 (ru) |
EP (11) | EP2526933B1 (ru) |
JP (4) | JP4934197B2 (ru) |
KR (4) | KR101315610B1 (ru) |
CN (4) | CN101805341B (ru) |
AT (1) | ATE531263T1 (ru) |
AU (2) | AU2006348662B8 (ru) |
BR (2) | BRPI0622054B8 (ru) |
CA (3) | CA2663116C (ru) |
CY (11) | CY1112513T1 (ru) |
DK (7) | DK2526934T3 (ru) |
EA (3) | EA018573B1 (ru) |
ES (8) | ES2564647T3 (ru) |
FR (1) | FR15C0029I2 (ru) |
HK (3) | HK1140107A1 (ru) |
HU (10) | HUE031334T2 (ru) |
IL (1) | IL197550A0 (ru) |
LT (7) | LT2529621T (ru) |
LU (3) | LU92692I2 (ru) |
MX (3) | MX2009003122A (ru) |
NL (1) | NL300728I1 (ru) |
NZ (3) | NZ595230A (ru) |
PL (8) | PL2530083T3 (ru) |
PT (7) | PT2526933E (ru) |
SG (2) | SG166093A1 (ru) |
SI (8) | SI2530083T1 (ru) |
WO (1) | WO2008039218A2 (ru) |
ZA (4) | ZA200901784B (ru) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2655388C2 (ru) * | 2012-01-31 | 2018-05-28 | Фармасайкликс Элэлси | Соединения пуринона в качестве ингибиторов киназ |
RU2711106C2 (ru) * | 2018-06-06 | 2020-01-15 | Общество с ограниченной ответственностью "АКСЕЛЬФАРМ" | Кристаллическая μ-модификация 1-[(3R)-3-[4-амино-3-(4-фенокси-фенил)-1Н-пиразоло[3,4-d]пиримидин-1-ил]-1-пиперидил]-2-пропенил-1-она, способ её получения и фармацевтическая композиция на её основе |
RU2721774C1 (ru) * | 2016-11-24 | 2020-05-22 | Шанхай Инститьют Оф Материя Медика, Чайниз Академи Оф Сайенсез | ПИРИМИДО[5,4-b]ИНДОЛИЗИНОВОЕ ИЛИ ПИРИМИДО[5,4-b]ПИРРОЛИЗИНОВОЕ СОЕДИНЕНИЕ, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ |
Families Citing this family (509)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2005230818B2 (en) | 2004-04-02 | 2010-11-25 | Osi Pharmaceuticals, Inc. | 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors |
EP1906950A4 (en) * | 2005-06-21 | 2008-09-24 | Infinity Discovery Inc | ANSAMYCIN FORMULATIONS AND METHODS OF USE |
EP2027087A2 (en) * | 2006-05-18 | 2009-02-25 | MannKind Corporation | Intracellular kinase inhibitors |
BRPI0714963A2 (pt) * | 2006-08-16 | 2013-07-30 | Novartis Ag | processo de fabricaÇço de dispersÕes sàlidas de compostos terapÊuticos altamente cristalinos |
SI2530083T1 (sl) | 2006-09-22 | 2016-09-30 | Pharmacyclics Llc | Inhibitorji Bruton tirozin kinaze |
ES2403546T3 (es) * | 2006-11-03 | 2013-05-20 | Pharmacyclics, Inc. | Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización |
US8809273B2 (en) * | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
ES2562215T3 (es) | 2007-03-28 | 2016-03-03 | Pharmacyclics Llc | Inhibidores de la tirosina quinasa de Bruton |
US20080255080A1 (en) * | 2007-04-12 | 2008-10-16 | Wright James L | Hydroquinone Ansamycin Formulations |
US7989465B2 (en) * | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
TWI552752B (zh) * | 2007-10-19 | 2016-10-11 | 賽基艾維洛米斯研究股份有限公司 | 雜芳基化合物及其用途 |
US20110046144A1 (en) * | 2008-01-18 | 2011-02-24 | Mulvihill Mark J | Imidazopyrazinol derivatives for the treatment of cancers |
WO2009143051A1 (en) * | 2008-05-19 | 2009-11-26 | Osi Pharmaceuticals, Inc. | Substituted imidazopyr-and imidazotri-azines |
US20090301928A1 (en) * | 2008-06-05 | 2009-12-10 | United Comb & Novelty Corporation | Packaging For Lipped Containers |
US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
JP2011526299A (ja) | 2008-06-27 | 2011-10-06 | アビラ セラピューティクス, インコーポレイテッド | ヘテロアリール化合物およびそれらの使用 |
US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
ES2552681T3 (es) * | 2008-07-15 | 2015-12-01 | F. Hoffmann-La Roche Ag | Nuevas fenil-imidazopiridinas y piridazinas |
AU2009270856B2 (en) * | 2008-07-16 | 2013-07-25 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors |
AU2013245503B2 (en) * | 2008-07-16 | 2015-09-24 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors |
CN102405284B (zh) * | 2008-09-05 | 2016-01-20 | 新基阿维罗米克斯研究公司 | 设计不可逆抑制剂的算法 |
JP5583680B2 (ja) * | 2008-10-15 | 2014-09-03 | インフィニティー ファーマスーティカルズ インコーポレイテッド | アンサマイシンヒドロキノン組成物 |
WO2010043633A1 (en) * | 2008-10-15 | 2010-04-22 | Palau Pharma, S. A. | 2h-pyrazolo [4,3-d]pyrimidin-5-amine derivatives as h4 histamine receptor antagonists for the treatment of allergic, immunological and inflammatory diseases |
US9095592B2 (en) * | 2008-11-07 | 2015-08-04 | The Research Foundation For The State University Of New York | Bruton's tyrosine kinase as anti-cancer drug target |
US8426428B2 (en) * | 2008-12-05 | 2013-04-23 | Principia Biopharma, Inc. | EGFR kinase knockdown via electrophilically enhanced inhibitors |
CA2752826A1 (en) | 2009-04-20 | 2010-10-28 | OSI Pharmaceuticals, LLC | Preparation of c-pyrazine-methylamines |
WO2010126960A1 (en) * | 2009-04-29 | 2010-11-04 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
US9908884B2 (en) | 2009-05-05 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | EGFR inhibitors and methods of treating disorders |
JP2012526138A (ja) * | 2009-05-07 | 2012-10-25 | オーエスアイ・ファーマシューティカルズ,エルエルシー | 副腎皮質癌を治療するためのosi−906の使用 |
JP5699149B2 (ja) * | 2009-09-04 | 2015-04-08 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | Bruton型チロシンキナーゼ阻害薬 |
AU2010292116A1 (en) * | 2009-09-11 | 2012-05-03 | Cylene Pharmaceuticals Inc. | Pharmaceutically useful heterocycle-substituted lactams |
NZ620174A (en) | 2009-09-16 | 2016-08-26 | Celgene Avilomics Res Inc | Protein kinase conjugates and inhibitors |
US7965498B2 (en) | 2009-09-30 | 2011-06-21 | Apple Inc. | Cover glass to housing interface system |
US7741330B1 (en) * | 2009-10-12 | 2010-06-22 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase |
EP2937345B1 (en) | 2009-12-29 | 2018-03-21 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
AU2010339456A1 (en) | 2009-12-30 | 2012-07-05 | Celgene Avilomics Research, Inc. | Ligand-directed covalent modification of protein |
WO2011110478A1 (en) * | 2010-03-08 | 2011-09-15 | Ratiopharm Gmbh | Dabigatran etexilate-containing pharmaceutical composition |
US9371567B2 (en) * | 2010-04-19 | 2016-06-21 | The Translational Genomics Research Institute | Methods and kits to predict therapeutic outcome of BTK inhibitors |
NZ603643A (en) * | 2010-05-31 | 2014-07-25 | Ono Pharmaceutical Co | Purinone derivative |
EP2575818A4 (en) * | 2010-06-03 | 2013-11-06 | Pharmacyclics Inc | USE OF INHIBITORS OF BRUTON TYROSINE KINASE (BTK) |
US20120053189A1 (en) * | 2010-06-28 | 2012-03-01 | Pharmacyclics, Inc. | Btk inhibitors for the treatment of immune mediated conditions |
CA2804648C (en) | 2010-07-09 | 2019-01-22 | The Walter And Eliza Hall Institute Of Medical Research | Protein kinase inhibitors and methods of treatment |
EP2603081B1 (en) | 2010-08-10 | 2016-10-05 | Celgene Avilomics Research, Inc. | Besylate salt of a btk inhibitor |
CA2808543C (en) * | 2010-08-20 | 2016-01-26 | Hutchison Medipharma Limited | Pyrrolopyrimidine compounds and uses thereof |
JP5956999B2 (ja) | 2010-11-01 | 2016-07-27 | セルジーン アヴィロミクス リサーチ, インコーポレイテッド | ヘテロアリール化合物およびその使用 |
RU2644151C2 (ru) | 2010-11-01 | 2018-02-08 | Селджен Авиломикс Рисерч, Инк. | Гетероциклические соединения и их применение |
EP2637502B1 (en) | 2010-11-10 | 2018-01-10 | Celgene CAR LLC | Mutant-selective egfr inhibitors and uses thereof |
AU2012221828C1 (en) | 2011-02-23 | 2015-10-01 | Pfizer Inc. | Imidazo[5,1-f][1,2,4]triazines for treatment of neurological disorders |
EP2710005B1 (en) | 2011-05-17 | 2016-10-05 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
US20140107151A1 (en) * | 2011-05-17 | 2014-04-17 | Principia Biophama Inc. | Tyrosine kinase inhibitors |
US9376438B2 (en) | 2011-05-17 | 2016-06-28 | Principia Biopharma, Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
ES2770550T3 (es) * | 2011-05-17 | 2020-07-02 | Univ California | Inhibidores de quinasa |
WO2013003629A2 (en) * | 2011-06-28 | 2013-01-03 | Pharmacyclics, Inc. | Methods and compositions for inhibition of bone resorption |
CA2840687C (en) | 2011-07-01 | 2020-04-28 | Dana-Farber Cancer Institute, Inc. | Discovery of a somatic mutation in myd88 gene in lymphoplasmacytic lymphoma |
CA2841111A1 (en) | 2011-07-08 | 2013-01-17 | Novartis Ag | Novel pyrrolo pyrimidine derivatives |
KR20140048968A (ko) * | 2011-07-13 | 2014-04-24 | 파마시클릭스, 인코포레이티드 | 브루톤형 티로신 키나제의 억제제 |
EP2548877A1 (en) * | 2011-07-19 | 2013-01-23 | MSD Oss B.V. | 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors |
DK3689878T3 (da) * | 2011-07-19 | 2021-11-08 | Merck Sharp & Dohme | 4-imidazopyridazin-1-yl-benzamider og 4-imidazotriazin-1-yl-benzamider som btk-inhibitorer |
PL3409278T3 (pl) | 2011-07-21 | 2021-02-22 | Sumitomo Pharma Oncology, Inc. | Heterocykliczne inhibitory kinazy białkowej |
EP2771010A4 (en) * | 2011-10-19 | 2015-04-01 | Pharmacyclics Inc | USE OF INHIBITORS OF BRUTON TYROSINE KINASE (BTK) |
WO2013063401A1 (en) | 2011-10-28 | 2013-05-02 | Celgene Avilomics Research, Inc. | Methods of treating a bruton's tyrosine kinase disease or disorder |
GB2496135B (en) | 2011-11-01 | 2015-03-18 | Valirx Plc | Inhibitors of the interaction between a Src family kinase and an androgen receptor or estradiol receptor for treatment of endometriosis |
UA111756C2 (uk) * | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
WO2013067260A1 (en) * | 2011-11-03 | 2013-05-10 | Genentech, Inc. | Bicyclic piperazine compounds |
US9212381B2 (en) * | 2011-11-10 | 2015-12-15 | President And Fellows Of Harvard College | Methods and compositions for labeling polypeptides |
WO2013074986A1 (en) | 2011-11-17 | 2013-05-23 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
RU2750538C2 (ru) | 2011-11-29 | 2021-06-29 | Оно Фармасьютикал Ко., Лтд. | Гидрохлорид производного пуринона |
US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
ES2672367T3 (es) | 2012-01-09 | 2018-06-14 | X-Chem, Inc. | Derivados de triptolina que tienen actividad inhibidora de quinasas y sus usos |
US9458162B2 (en) * | 2012-01-31 | 2016-10-04 | Nanjing Allgen Pharma Co. Ltd. | Cyclic molecules as bruton's tyrosine kinase inhibitors |
TW201336847A (zh) * | 2012-02-07 | 2013-09-16 | Taiho Pharmaceutical Co Ltd | 喹啉基吡咯并嘧啶化合物或其鹽 |
CA2861980C (en) * | 2012-02-23 | 2016-11-08 | Taiho Pharmaceutical Co., Ltd. | Quinolylpyrrolopyrimidyl fused-ring compound or salt thereof |
CN103312670A (zh) | 2012-03-12 | 2013-09-18 | 西安西电捷通无线网络通信股份有限公司 | 一种认证方法及*** |
ES2698298T3 (es) | 2012-03-15 | 2019-02-04 | Celgene Car Llc | Sales de un inhibidor de quinasa receptor de factor de crecimiento epidérmico |
CN104302178B (zh) | 2012-03-15 | 2018-07-13 | 西建卡尔有限责任公司 | 表皮生长因子受体激酶抑制剂的固体形式 |
WO2013148603A1 (en) | 2012-03-27 | 2013-10-03 | Takeda Pharmaceutical Company Limited | Cinnoline derivatives as as btk inhibitors |
US9353062B2 (en) | 2012-04-04 | 2016-05-31 | Hangzhouderenyucheng Biotechnology Ltd | Substituted quinolines as bruton's tyrosine kinases inhibitors |
EP2836214B1 (en) | 2012-04-11 | 2018-06-27 | Acerta Pharma B.V. | Bruton's tyrosine kinase inhibitors for hematopoietic mobilization |
WO2013154778A1 (en) | 2012-04-11 | 2013-10-17 | Dana-Farber Cancer Institute, Inc. | Host targeted inhibitors of dengue virus and other viruses |
CN103374001B (zh) * | 2012-04-19 | 2015-10-28 | 山东轩竹医药科技有限公司 | 咪唑并三嗪类mTOR抑制剂 |
BR112014029718A2 (pt) * | 2012-05-31 | 2017-06-27 | Pharmascience Inc | inibidores da proteína quinase |
KR20220093389A (ko) * | 2012-06-04 | 2022-07-05 | 파마싸이클릭스 엘엘씨 | 브루톤 타이로신 키나아제 저해제의 결정 형태 |
AR091273A1 (es) * | 2012-06-08 | 2015-01-21 | Biogen Idec Inc | Inhibidores de pirimidinil tirosina quinasa |
EP2861599B1 (en) * | 2012-06-18 | 2019-12-18 | Principia Biopharma Inc. | Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment of cancer and autoimmune diseases |
US20150140085A1 (en) | 2012-06-29 | 2015-05-21 | Principia Biopharma Inc. | Formulations comprising ibrutinib |
JP6575950B2 (ja) | 2012-07-24 | 2019-09-18 | ファーマサイクリックス エルエルシー | Bruton型チロシンキナーゼ(Btk)阻害剤に対する耐性を伴う変異 |
ES2682043T3 (es) * | 2012-07-30 | 2018-09-18 | Concert Pharmaceuticals Inc. | Ibrutinib deuterado |
WO2014022569A1 (en) * | 2012-08-03 | 2014-02-06 | Principia Biopharma Inc. | Treatment of dry eye |
MX2015001802A (es) | 2012-08-10 | 2015-05-07 | Boehringer Ingelheim Int | Compuestos heteroaromaticos como inhibidores de btk. |
CN103121999A (zh) * | 2012-08-29 | 2013-05-29 | 苏州迪飞医药科技有限公司 | 一种酪氨酸激酶抑制剂pci-32765的合成方法 |
EP2890691B1 (en) | 2012-08-31 | 2018-04-25 | Principia Biopharma Inc. | Benzimidazole derivatives as itk inhibitors |
ME03455B (me) * | 2012-09-10 | 2020-01-20 | Principia Biopharma Inc | Jedinjenja pirazolopirimidina kao inhibitori kinaze |
CH706997A1 (en) | 2012-09-20 | 2014-03-31 | Ferag Ag | Access control on operating modules of a control unit. |
WO2014063068A1 (en) | 2012-10-18 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
GEP201606597B (en) | 2012-11-02 | 2017-01-10 | Pfizer | Bruton's tyrosine kinase inhibitors |
MX2015005633A (es) * | 2012-11-02 | 2016-02-03 | Pharmacyclics Inc | Terapia adyuvante con inhibidores de quinasa de la familia tec. |
PE20151495A1 (es) * | 2012-11-15 | 2015-10-23 | Pharmacyclics Inc | Compuestos de pirrolopirimidina como inhibidores de quinasas |
CN104918935B (zh) | 2012-11-16 | 2017-07-28 | 百时美施贵宝公司 | 二氢吡唑gpr40调节剂 |
CN103848810A (zh) * | 2012-11-30 | 2014-06-11 | 北京赛林泰医药技术有限公司 | 鲁顿酪氨酸激酶抑制剂 |
EP2935226A4 (en) | 2012-12-21 | 2016-11-02 | Celgene Avilomics Res Inc | HETEROARYL COMPOUNDS AND USES THEREOF |
CN104869983A (zh) * | 2012-12-21 | 2015-08-26 | 泰华制药工业有限公司 | 醋酸格拉替雷的透粘膜给药 |
WO2014113942A1 (en) * | 2013-01-23 | 2014-07-31 | Merck Sharp & Dohme Corp. | Btk inhibitors |
WO2014113932A1 (en) * | 2013-01-23 | 2014-07-31 | Merck Sharp & Dohme Corp. | Btk inhibitors |
WO2014114185A1 (en) | 2013-01-23 | 2014-07-31 | Merck Sharp & Dohme Corp. | Btk inhibitors |
KR20150119012A (ko) | 2013-02-08 | 2015-10-23 | 셀진 아빌로믹스 리서치, 인코포레이티드 | Erk 억제제 및 이의 용도 |
US20140357636A1 (en) * | 2013-02-21 | 2014-12-04 | Wayne Rothbaum | Treatment of Skeletal-Related Disorders |
EP2960241A4 (en) | 2013-02-22 | 2016-07-13 | Taiho Pharmaceutical Co Ltd | PROCESS FOR PREPARING TRICYCLIC COMPOUNDS AND TRICYCLIC COMPOUNDS MADE ACCORDING TO THE SAID MANUFACTURING METHOD |
JO3377B1 (ar) | 2013-03-11 | 2019-03-13 | Takeda Pharmaceuticals Co | مشتقات بيريدينيل وبيريدينيل مندمج |
WO2014165253A1 (en) * | 2013-03-12 | 2014-10-09 | Nbip, Llc | Compositions and methods for preventing infection of a wound and for advancing the healing process |
CN103142601A (zh) * | 2013-03-13 | 2013-06-12 | 杭州雷索药业有限公司 | Pci-32765在制备抗血管生成类药物中的应用 |
KR20160006668A (ko) * | 2013-03-14 | 2016-01-19 | 파마싸이클릭스 엘엘씨 | 브루톤 티로신 키나제 억제제와 cyp3a4 억제제의 배합물 |
WO2014151620A1 (en) | 2013-03-14 | 2014-09-25 | Boehringer Ingelheim International Gmbh | 5-thiazolecarboxamide dervatives and their use as btk inhibitors |
ES2738493T3 (es) | 2013-03-14 | 2020-01-23 | Tolero Pharmaceuticals Inc | Inhibidores de JAK2 y ALK2 y métodos para su uso |
WO2014152114A1 (en) | 2013-03-15 | 2014-09-25 | Boehringer Ingelheim International Gmbh | Heteroaromatic compounds as btk inhibitors |
HUE058914T2 (hu) * | 2013-03-15 | 2022-09-28 | Janssen Pharmaceutica Nv | Gyógyszer elõállítására szolgáló eljárások és köztitermékek |
US9156847B2 (en) * | 2013-03-15 | 2015-10-13 | Janssen Pharmaceutica Nv | Processes and intermediates for preparing a medicament |
US10138256B2 (en) | 2013-03-15 | 2018-11-27 | Celgene Car Llc | MK2 inhibitors and uses thereof |
UY35468A (es) | 2013-03-16 | 2014-10-31 | Novartis Ag | Tratamiento de cáncer utilizando un receptor quimérico de antígeno anti-cd19 |
MX369503B (es) * | 2013-04-08 | 2019-11-11 | Pharmacyclics Llc | Combinaciones que comprenden ibrutinib y abt-199 para tratar trastornos proliferativos de células b y métodos de uso de las mismas. |
WO2014168986A1 (en) | 2013-04-08 | 2014-10-16 | Brown Dennis M | Therapeutic benefit of suboptimally administered chemical compounds |
US8957080B2 (en) | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
KR101793807B1 (ko) | 2013-04-25 | 2017-11-03 | 베이진 엘티디 | 단백질 키나제 억제제로서의 융합된 헤테로시클릭 화합물 |
GB2513615A (en) | 2013-05-01 | 2014-11-05 | Cancer Rec Tech Ltd | Medical use |
GB201309085D0 (en) | 2013-05-20 | 2013-07-03 | Redx Pharma Ltd | Compounds |
WO2014187319A1 (en) | 2013-05-21 | 2014-11-27 | Jiangsu Medolution Ltd | Substituted pyrazolopyrimidines as kinases inhibitors |
US9637487B2 (en) | 2013-07-02 | 2017-05-02 | Pharmacyclics Llc | Purinone compounds as kinase inhibitors |
BR112015029972A2 (pt) | 2013-07-03 | 2017-07-25 | Hoffmann La Roche | composto, composição farmacêutica, processo para a preparação de uma composição farmacêutica, método para o tratamento de uma doença, conjunto e utilização de um composto |
WO2015013579A1 (en) | 2013-07-26 | 2015-01-29 | Update Pharma Inc. | Compositions to improve the therapeutic benefit of bisantrene |
JP6800750B2 (ja) | 2013-08-02 | 2020-12-16 | ファーマサイクリックス エルエルシー | 固形腫瘍の処置方法 |
EP2832358A1 (en) | 2013-08-02 | 2015-02-04 | Bionsil S.r.l. | Pharmaceutical kit for use in the treatment of colon and colorectal cancer |
WO2015023703A1 (en) | 2013-08-12 | 2015-02-19 | Pharmacyclics, Inc. | Methods for the treatment of her2 amplified cancer |
US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
EP4130044A1 (en) | 2013-09-13 | 2023-02-08 | BeiGene Switzerland GmbH | Anti-pd1 antibodies and their use as therapeutics and diagnostics |
AU2014324595B2 (en) | 2013-09-30 | 2018-12-20 | Beijing Innocare Pharma Tech Co., Ltd | Substituted nicotinimide inhibitors of BTK and their preparation and use in the treatment of cancer, inflammation and autoimmune disease |
BR112016006978A2 (pt) * | 2013-09-30 | 2017-08-01 | Pharmacyclics Llc | inibidores de tirosina quinase de bruton |
WO2015054197A1 (en) * | 2013-10-10 | 2015-04-16 | Acetylon Pharmaceuticals, Inc. | Hdac inhibitors, alone or in combination with btk inhibitors, for treating non-hodgkin's lymphoma |
WO2015057992A1 (en) | 2013-10-16 | 2015-04-23 | Izumi Raquel | Btk inhibitors for hematopoietic mobilization |
CA2927917C (en) | 2013-10-18 | 2022-08-09 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of proliferative diseases |
AU2014337044A1 (en) | 2013-10-18 | 2016-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
US20160272645A1 (en) * | 2013-10-18 | 2016-09-22 | Medivation Technologies, Inc. | Heterocyclic Compounds and Methods of Use |
US20210317140A1 (en) | 2013-10-18 | 2021-10-14 | Medivation Technologies, Inc. | Heterocyclic Compounds and Methods of Use |
EP3060218A4 (en) * | 2013-10-25 | 2017-07-19 | Pharmacyclics LLC | Methods of treating and preventing graft versus host disease |
TWI617309B (zh) * | 2013-10-25 | 2018-03-11 | 製藥公司 | 使用布魯頓氏酪胺酸激酶抑制劑之治療及免疫療法 |
US9636340B2 (en) | 2013-11-12 | 2017-05-02 | Ayyappan K. Rajasekaran | Kinase inhibitors |
WO2015071432A1 (en) | 2013-11-14 | 2015-05-21 | Sandoz Ag | Pharmaceutical compositions of ibrutinib |
US20150141438A1 (en) * | 2013-11-15 | 2015-05-21 | Pharmacyclics, Inc. | Methods for delaying or preventing the onset of type 1 diabetes |
CN103626774B (zh) * | 2013-11-20 | 2015-11-04 | 苏州明锐医药科技有限公司 | 伊鲁替尼的制备方法 |
CA2833867A1 (en) | 2013-11-21 | 2015-05-21 | Pharmascience Inc. | Protein kinase inhibitors |
CN103694241A (zh) * | 2013-11-27 | 2014-04-02 | 苏州晶云药物科技有限公司 | Pci-32765的新晶型a及其制备方法 |
US9512084B2 (en) | 2013-11-29 | 2016-12-06 | Novartis Ag | Amino pyrimidine derivatives |
WO2015084857A1 (en) * | 2013-12-02 | 2015-06-11 | Pharmacyclics, Inc. | Methods of treating and preventing alloantibody driven chronic graft versus host disease |
SI3077395T1 (en) | 2013-12-05 | 2018-03-30 | Pfizer Inc. | Pyrrolo (2,3-d) pyrimidinyl, pyrrolo (2,3-b) pyrazinyl and pyrrolo (2,3-d) pyridinyl acrylamides |
WO2015083008A1 (en) | 2013-12-05 | 2015-06-11 | Acerta Pharma B.V. | Therapeutic combination of a pi3k inhibitor and a btk inhibitor |
WO2015082583A1 (en) | 2013-12-05 | 2015-06-11 | F. Hoffmann-La Roche Ag | Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality |
JP6878004B2 (ja) * | 2013-12-13 | 2021-05-26 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | リンパ形質細胞性リンパ腫を処置する方法 |
CA2932351A1 (en) | 2013-12-13 | 2015-06-18 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
US9834554B2 (en) | 2013-12-20 | 2017-12-05 | Merck Sharp & Dohme Corp. | BTK inhibitors |
EP3082809B1 (en) * | 2013-12-20 | 2021-01-20 | Merck Sharp & Dohme Corp. | Btk inhibitors |
US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
US10272083B2 (en) | 2014-01-21 | 2019-04-30 | Acerta Pharma B.V. | Methods of treating chronic lymphocytic leukemia and small lymphocytic leukemia using a BTK inhibitor |
CN106008515A (zh) * | 2014-01-29 | 2016-10-12 | 苏州晶云药物科技有限公司 | 依鲁替尼的新晶型及其制备方法 |
JP6486954B2 (ja) | 2014-01-29 | 2019-03-20 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Btk阻害剤としてのピラゾール化合物 |
JP6162904B2 (ja) * | 2014-02-03 | 2017-07-12 | カディラ ヘルスケア リミティド | 新規複素環式化合物 |
ES2841248T3 (es) | 2014-02-21 | 2021-07-07 | Principia Biopharma Inc | Sales y forma sólida de un inhibidor de BTK |
JP6526065B2 (ja) | 2014-02-28 | 2019-06-05 | ニンバス ラクシュミ, インコーポレイテッド | Tyk2阻害剤およびその使用 |
WO2015143400A1 (en) | 2014-03-20 | 2015-09-24 | Pharmacyclics, Inc. | Phospholipase c gamma 2 and resistance associated mutations |
GB201404987D0 (en) * | 2014-03-20 | 2014-05-07 | Redx Pharma Ltd | Compounds |
WO2015146159A1 (en) | 2014-03-25 | 2015-10-01 | Ono Pharmaceutical Co., Ltd. | Prophylactic agent and/or therapeutic agent for diffuse large b-cell lymphoma |
WO2015151006A1 (en) * | 2014-03-29 | 2015-10-08 | Lupin Limited | Substituted purine compounds as btk inhibitors |
WO2015185998A2 (en) | 2014-04-11 | 2015-12-10 | Acerta Pharma B.V. | Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bone marrow x kinase |
WO2015181633A2 (en) | 2014-04-11 | 2015-12-03 | Acerta Pharma B.V. | Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bruton's tyrosine kinase |
CN105017256A (zh) | 2014-04-29 | 2015-11-04 | 浙江导明医药科技有限公司 | 多氟化合物作为布鲁顿酪氨酸激酶抑制剂 |
CN105085474B (zh) | 2014-05-07 | 2018-05-18 | 北京赛林泰医药技术有限公司 | 鲁顿酪氨酸激酶抑制剂 |
CN105085529A (zh) * | 2014-05-15 | 2015-11-25 | 广东东阳光药业有限公司 | 依鲁替尼新晶型及其制备方法 |
CN104086551B (zh) * | 2014-06-06 | 2016-09-21 | 人福医药集团股份公司 | 化合物及其制备方法和用途 |
GB201410430D0 (en) * | 2014-06-11 | 2014-07-23 | Redx Pharma Ltd | Compounds |
TW201613644A (en) | 2014-06-17 | 2016-04-16 | Acerta Pharma Bv | Therapeutic combinations of a BTK inhibitor, a PI3K inhibitor, and/or a JAK-2 inhibitor |
CN104945404B (zh) * | 2014-06-25 | 2018-09-14 | 广东东阳光药业有限公司 | 一种n-丙烯羰基哌啶衍生物的制备方法 |
TW201613919A (en) | 2014-07-02 | 2016-04-16 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
CN105294571B (zh) * | 2014-07-03 | 2019-04-23 | 浙江九洲药业股份有限公司 | 一种依鲁替尼中间体及其制备方法和用途 |
KR102130600B1 (ko) | 2014-07-03 | 2020-07-08 | 베이진 엘티디 | Pd-l1 항체와 이를 이용한 치료 및 진단 |
BR112017000470B1 (pt) * | 2014-07-07 | 2022-11-29 | Jiangsu Hengrui Medicine Co., Ltd | Compostos, composição farmacêutica e uso do composto ou da composição |
WO2016008411A1 (en) * | 2014-07-18 | 2016-01-21 | Beigene, Ltd. | 5-amino-4-carbamoyl-pyrazole compounds as selective and irreversible t790m over wt-egfr kinase inhibitors and use thereof |
WO2016019237A2 (en) * | 2014-07-31 | 2016-02-04 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
AU2015296215A1 (en) * | 2014-08-01 | 2017-03-23 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
WO2016020901A1 (en) | 2014-08-07 | 2016-02-11 | Acerta Pharma B.V. | Methods of treating cancers, immune and autoimmune diseases, and inflammatory diseases based on btk occupancy and btk resynthesis rate |
KR20170033358A (ko) | 2014-08-07 | 2017-03-24 | 파마싸이클릭스 엘엘씨 | 브루톤 티로신 키나아제 저해제의 신규한 제제 |
CN105461720B (zh) * | 2014-08-08 | 2019-08-06 | 南京圣和药业股份有限公司 | 吗啉类酪氨酸激酶抑制剂 |
CN106714909A (zh) | 2014-08-08 | 2017-05-24 | 药品循环有限责任公司 | 布鲁顿氏酪氨酸激酶抑制剂组合及其用途 |
US20170231995A1 (en) | 2014-08-11 | 2017-08-17 | Acerta Pharma B.V. | BTK Inhibitors to Treat Solid Tumors Through Modulation of the Tumor Microenvironment |
PL3179991T3 (pl) | 2014-08-11 | 2022-02-14 | Acerta Pharma B.V. | Kombinacje terapeutyczne inhibitora btk i inhibitora bcl-2 |
DK3179992T3 (da) | 2014-08-11 | 2022-07-11 | Acerta Pharma Bv | Terapeutisk kombination af en btk-inhibitor, en pd-1-inhibitor og/eller en pd-l1-inhibitor |
TW201618773A (zh) | 2014-08-11 | 2016-06-01 | 艾森塔製藥公司 | Btk抑制劑、pi3k抑制劑、jak-2抑制劑、及/或cdk4/6抑制劑的治療組合物 |
AU2015303835B2 (en) | 2014-08-12 | 2020-04-09 | Monash University | Lymph directing prodrugs |
DK3179858T3 (da) | 2014-08-13 | 2019-07-22 | Celgene Car Llc | Forme og sammensætninger af en ERK-inhibitor |
WO2016025720A1 (en) | 2014-08-14 | 2016-02-18 | Assia Chemical Industries Ltd. | Solid state forms of ibrutinib |
CN106922146B (zh) | 2014-10-02 | 2020-05-26 | 豪夫迈·罗氏有限公司 | 用于治疗由布鲁顿酪氨酸激酶(btk)介导的疾病的吡唑甲酰胺化合物 |
EP3715346B1 (en) | 2014-10-22 | 2024-01-03 | Dana-Farber Cancer Institute, Inc. | Thiazolyl-containing compounds for treating proliferative diseases |
ME03807B (me) | 2014-10-24 | 2021-04-20 | Bristol Myers Squibb Co | Jedinjenja indol karboksamida korisna kao inhibitori kinaze |
EP3212645B1 (en) | 2014-10-27 | 2018-11-28 | F.Hoffmann-La Roche Ag | Process for making tricyclic lactam compounds |
US20170327504A1 (en) * | 2014-10-30 | 2017-11-16 | Sandoz Ag | Synthesis of Substituted 1H-Pyrazolo[3,4-D]Pyrimidines |
WO2016079693A1 (en) | 2014-11-19 | 2016-05-26 | Sun Pharmaceutical Industries Limited | A process for the preparation of ibrutinib |
WO2016079216A1 (en) | 2014-11-20 | 2016-05-26 | Sandoz Ag | Physical forms of ibrutinib, a bruton's kinase inhibitor |
CN104447761A (zh) * | 2014-11-27 | 2015-03-25 | 广东东阳光药业有限公司 | 一种吡唑衍生物的制备方法 |
AR102871A1 (es) * | 2014-12-03 | 2017-03-29 | Pharmacyclics Llc | Métodos de tratamiento de fibrosis |
WO2016088074A1 (en) * | 2014-12-03 | 2016-06-09 | Dr. Reddy’S Laboratories Limited | Process for the preparation of amorphous ibrutinib |
CN104478884A (zh) * | 2014-12-05 | 2015-04-01 | 广东东阳光药业有限公司 | 一种中间体的制备方法 |
WO2016087994A1 (en) | 2014-12-05 | 2016-06-09 | Acerta Pharma B.V. | Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment |
TW201702218A (zh) | 2014-12-12 | 2017-01-16 | 美國杰克森實驗室 | 關於治療癌症、自體免疫疾病及神經退化性疾病之組合物及方法 |
BR112017013022A2 (pt) | 2014-12-18 | 2018-02-27 | Principia Biopharma Inc | métodos para tratar uma doença inflamatória e/ou autoimune aguda num mamífero que a necessite onde a terapia de corticosteróides é utilizada como terapia de primeira ou segunda linha e/ou para tratar uma doença inflamatória e/ou autoimune num mamífero que a necessite, onde a terapia de corticosteróides é utilizada como terapia de manutenção de primeira ou segunda linha e/ou para eliminar ou reduzir dose terapêutica de corticosteróides utilizado no tratamento de uma doença inflamatória e/ou autoimune num mamífero que a necessite, onde a terapia de corticosteróides é utilizada como terapia de manutenção crônica de primeira ou segunda linha e/ou de tratamento de uma doença autoimune e/ou inflamatória num mamífero que a necessite |
KR102559719B1 (ko) | 2014-12-18 | 2023-07-26 | 에프. 호프만-라 로슈 아게 | 테트라하이드로-피리도[3,4-b]인돌 에스트로겐 수용체 조절제 및 이의 용도 |
WO2016105528A2 (en) | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
WO2016106628A1 (en) | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Btk inhibitors |
WO2016106652A1 (en) * | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Biarylether imidazopyrazine btk inhibitors |
WO2016106629A1 (en) * | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Btk inhibitors |
WO2016106624A1 (en) | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Tertiary alcohol imidazopyrazine btk inhibitors |
CN105820168B (zh) * | 2015-01-09 | 2018-12-04 | 上海医药工业研究院 | 一种依鲁替尼中间体的制备方法 |
MA41350A (fr) * | 2015-01-14 | 2017-11-21 | Janssen Pharmaceutica Nv | Synthèse d'un inhibiteur de la tyrosine kinase de bruton |
WO2016115869A1 (zh) | 2015-01-21 | 2016-07-28 | 中国科学院合肥物质科学研究院 | Flt3激酶的新型抑制剂及其用途 |
WO2016123504A1 (en) * | 2015-01-30 | 2016-08-04 | Pharmacyclics Llc | Btk inhibitor combinations and multidrug-resistance |
CZ201584A3 (cs) | 2015-02-09 | 2016-08-17 | Zentiva, K.S. | Sůl Ibrutinib sulfátu |
RU2712440C2 (ru) * | 2015-02-12 | 2020-01-29 | Шанхай Дьюд Медикал Сайенс Энд Текнолоджи Ко., Лтд | Способ получения ибрутиниба |
WO2016132383A1 (en) | 2015-02-18 | 2016-08-25 | Mylan Laboratories Limited | Process for the preparation of ibrutinib |
ES2930585T3 (es) | 2015-02-27 | 2022-12-19 | Nimbus Lakshmi Inc | Inhibidores de TYK2 y usos de los mismos |
DK3265084T3 (da) | 2015-03-03 | 2024-02-12 | Pharmacyclics Llc | Farmaceutiske formuleringer af Bruton's tyrosinkinase-hæmmer |
US10045990B2 (en) | 2015-03-04 | 2018-08-14 | Arizona Board Of Regents On Behalf Of Arizona State University | ERBB4 inhibitors and methods of use thereof |
CN106146508A (zh) * | 2015-03-19 | 2016-11-23 | 浙江导明医药科技有限公司 | 优化的联合用药及其治疗癌症和自身免疫疾病的用途 |
US9717745B2 (en) | 2015-03-19 | 2017-08-01 | Zhejiang DTRM Biopharma Co. Ltd. | Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases |
MA41828A (fr) | 2015-03-27 | 2018-01-30 | Pharmacyclics Llc | Co-cristaux d'un inhibiteur de la tyrosine kinase de bruton |
AU2016243529B2 (en) | 2015-03-27 | 2021-03-25 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
MA41827A (fr) | 2015-03-27 | 2018-01-30 | Pharmacyclics Llc | Formes solvatées d'un inhibiteur de la tyrosine kinase de bruton |
ES2733460T3 (es) * | 2015-04-02 | 2019-11-29 | Ratiopharm Gmbh | Co-cristales de Ibrutinib |
WO2016161248A1 (en) * | 2015-04-02 | 2016-10-06 | Tolero Pharmaceuticals, Inc. | Targeting pim kinases in combination with btk inhibition |
CN106146511A (zh) * | 2015-04-03 | 2016-11-23 | 安润医药科技(苏州)有限公司 | 吡唑并嘧啶衍生物、制备方法、药物组合物及用途 |
UA125681C2 (uk) | 2015-04-06 | 2022-05-18 | Янссен Фармацевтика Нв | Композиції, які містять ібрутиніб |
CN105906621A (zh) * | 2015-04-06 | 2016-08-31 | 四川百利药业有限责任公司 | 用作fgfr抑制剂的乙醇类化合物 |
US10253086B2 (en) | 2015-04-08 | 2019-04-09 | Novartis Ag | CD20 therapies, CD22 therapies, and combination therapies with a CD19 chimeric antigen receptor (CAR)-expressing cell |
CN106146512B (zh) * | 2015-04-09 | 2018-07-17 | 北京睿创康泰医药研究院有限公司 | 依鲁替尼的制备方法 |
ES2955554T3 (es) | 2015-04-09 | 2023-12-04 | Ono Pharmaceutical Co | Proceso para producir un derivado de purinona |
KR20170134462A (ko) * | 2015-04-13 | 2017-12-06 | 다이이찌 산쿄 가부시키가이샤 | Mdm2 저해제와 btk 저해제의 병용 치료법 |
CN106146482B (zh) * | 2015-04-14 | 2020-06-23 | 宁波文达医药科技有限公司 | 布鲁顿酪氨酸激酶抑制剂 |
WO2016170545A1 (en) * | 2015-04-22 | 2016-10-27 | Msn Laboratories Private Limited | Process for the preparation of 1-[(3r)-3-[4-amino-3-(4-phenoxyphenvl)-1h- pvrazolo[3,4-d]pyriniidin-1-y1]-1-piperidinvl]-2-propen-1-one and its polymorphs thereof |
US20180289685A1 (en) | 2015-04-30 | 2018-10-11 | Bayer Pharma Aktiengesellschaft | Combinations of inhibitors of irak4 with inhibitors of btk |
EP3195865A1 (de) | 2016-01-25 | 2017-07-26 | Bayer Pharma Aktiengesellschaft | Kombinationen von irak4 inhibitoren und btk inhibitoren |
RS59605B1 (sr) | 2015-05-26 | 2020-01-31 | Morphosys Ag | Kombinacija anti-cd19 antitela i inhibitora brutonove tirozin kinaze i njene upotrebe |
RS62290B1 (sr) | 2015-06-03 | 2021-09-30 | Principia Biopharma Inc | Inhibitori tirozinske kinaze |
US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
US9394312B1 (en) * | 2015-06-14 | 2016-07-19 | Mark Quang Nguyen | Ibrutinib prodrugs, pharmaceutical compositions thereof, and methods of use |
RU2719477C2 (ru) | 2015-06-22 | 2020-04-17 | Оно Фармасьютикал Ко., Лтд. | Соединение, ингибирующее brk |
US20180305350A1 (en) | 2015-06-24 | 2018-10-25 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
CZ2015442A3 (cs) * | 2015-06-26 | 2017-01-04 | Zentiva, K.S. | Ibrutinib hemisulfát |
WO2016207172A1 (en) * | 2015-06-26 | 2016-12-29 | Sandoz Gmbh | Preparation of pure amorphous ibrutinib |
WO2017004134A1 (en) | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
WO2017001658A1 (en) | 2015-07-02 | 2017-01-05 | F. Hoffmann-La Roche Ag | Benzoxazepin oxazolidinone compounds and methods of use |
TWI649326B (zh) | 2015-07-02 | 2019-02-01 | 瑞士商赫孚孟拉羅股份公司 | 苯并氧氮呯噁唑啶酮化合物及其製備方法 |
PT3954690T (pt) | 2015-07-02 | 2023-06-06 | Acerta Pharma Bv | Formas sólidas e formulações de (s)-4-(8-amino-3-(1-(but- 2-inoil)pirrolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n- (piridin-2-il)benzamida |
ITUB20152576A1 (it) * | 2015-07-29 | 2017-01-29 | Laboratorio Chimico Int S P A | Procedimento per la preparazione di ibrutinib e nuovo intermedio di sintesi. |
WO2017029586A1 (en) * | 2015-08-19 | 2017-02-23 | Sun Pharmaceutical Industries Limited | Crystalline forms of ibrutinib |
US20190008859A1 (en) | 2015-08-21 | 2019-01-10 | Acerta Pharma B.V. | Therapeutic Combinations of a MEK Inhibitor and a BTK Inhibitor |
EP3344254A1 (en) | 2015-08-31 | 2018-07-11 | Pharmacyclics LLC | Btk inhibitor combinations for treating multiple myeloma |
JP6802263B2 (ja) | 2015-09-02 | 2020-12-16 | ニンバス ラクシュミ, インコーポレイテッド | Tyk2阻害剤およびその使用 |
US11738087B2 (en) | 2015-09-08 | 2023-08-29 | Monash University | Lymph directing prodrugs |
AU2016319125B2 (en) | 2015-09-09 | 2021-04-08 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
CN105753863B (zh) * | 2015-09-11 | 2018-07-31 | 东莞市真兴贝特医药技术有限公司 | 氧代二氢咪唑并吡啶类化合物及其应用 |
US10683308B2 (en) | 2015-09-11 | 2020-06-16 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
CA2904270A1 (en) * | 2015-09-11 | 2017-03-11 | Pharmascience Inc. | Protein kinase inhibitors |
MA44909A (fr) | 2015-09-15 | 2018-07-25 | Acerta Pharma Bv | Association thérapeutique d'un inhibiteur du cd19 et d'un inhibiteur de la btk |
US20190022092A1 (en) | 2015-09-15 | 2019-01-24 | Acerta Pharma B.V. | Therapeutic Combinations of a BTK Inhibitor and a GITR Binding Molecule, a 4-1BB Agonist, or an OX40 Agonist |
EA201890730A1 (ru) | 2015-09-16 | 2018-10-31 | Локсо Онколоджи, Инк. | Производные пиразолопиримидина в качестве ингибиторов btk для лечения злокачественного новообразования |
ES2900482T3 (es) | 2015-10-01 | 2022-03-17 | Gilead Sciences Inc | Combinación de un inhibidor de Btk y un inhibidor de punto de control para el tratamiento del cáncer |
CN106608877B (zh) * | 2015-10-21 | 2018-11-13 | 新发药业有限公司 | 一种依鲁替尼中间体4-氨基-3-(4-苯氧基)苯基-1H-吡唑并[3,4-d]嘧啶的制备方法 |
PT3364958T (pt) | 2015-10-23 | 2023-04-10 | Navitor Pharm Inc | Moduladores de interação sestrina-gator2 e utilizações dos mesmos |
US9834561B2 (en) | 2015-10-28 | 2017-12-05 | Scinopharm Taiwan, Ltd. | Process for preparing ibrutinib and its intermediates |
DK3377484T3 (da) * | 2015-11-17 | 2023-11-27 | Merck Patent Gmbh | Fremgangsmåder til behandling af multipel sklerose under anvendelse af pyrimidin- og pyridinforbindelser med btk- inhiberende aktivitet |
CN105294696A (zh) * | 2015-11-19 | 2016-02-03 | 上海创诺医药集团有限公司 | 依鲁替尼新晶型及其制备方法 |
CA2950640A1 (en) | 2015-12-04 | 2017-06-04 | Portola Pharmaceuticals, Inc. | Cerdulatinib for treating hematological cancers |
EP4012415A3 (en) | 2015-12-04 | 2022-12-07 | Juno Therapeutics, Inc. | Methods and compositions related to toxicity associated with cell therapy |
JO3794B1 (ar) | 2015-12-10 | 2021-01-31 | Janssen Pharmaceutica Nv | المركبات متعددة الحلقات كمثبطات لتيروزين كيناز بروتون |
JO3793B1 (ar) | 2015-12-10 | 2021-01-31 | Janssen Pharmaceutica Nv | مثبطات تيروزين كاينيز بروتون وأساليب استخدامها |
WO2017106352A1 (en) | 2015-12-14 | 2017-06-22 | Raze Therapeutics, Inc. | Caffeine inhibitors of mthfd2 and uses thereof |
CN108368086B (zh) | 2015-12-16 | 2021-01-08 | 勃林格殷格翰国际有限公司 | 可用于治疗自身免疫疾病的二吡唑基衍生物 |
PE20220502A1 (es) | 2015-12-16 | 2022-04-07 | Loxo Oncology Inc | Compuestos utiles como inhibidores de cinasa |
JP6916185B2 (ja) | 2016-01-13 | 2021-08-11 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Btk阻害剤としてのイソキノロン類 |
HUE052893T2 (hu) | 2016-01-13 | 2021-05-28 | Acerta Pharma Bv | Antifolát és BTK-gátló terápiás kombinációi |
WO2017125423A1 (en) | 2016-01-19 | 2017-07-27 | Janssen Pharmaceutica Nv | Formulations/compositions comprising a btk inhibitor |
EP3405178A1 (en) | 2016-01-19 | 2018-11-28 | Janssen Pharmaceutica NV | Formulations/compositions comprising a btk inhibitor |
US10793566B2 (en) | 2016-01-21 | 2020-10-06 | Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. | Bruton's tyrosine kinase inhibitors |
MX2018008815A (es) * | 2016-01-21 | 2019-03-28 | Zibo Biopolar Changsheng Pharmaceutical Co Ltd | Inhibidores de tirosina quinasa de bruton. |
CN105732638B (zh) * | 2016-01-22 | 2018-01-30 | 成都倍特药业有限公司 | 一种具有螺环或桥环结构的布鲁顿酪氨酸激酶抑制剂及其制备方法 |
CN106995446B (zh) * | 2016-01-22 | 2021-07-02 | 山东新时代药业有限公司 | 布鲁顿酪氨酸激酶抑制剂制备方法 |
WO2017134684A2 (en) | 2016-02-01 | 2017-08-10 | Natco Pharma Limited | An improved process for the preparation of ibrutinib |
WO2017134685A2 (en) * | 2016-02-02 | 2017-08-10 | Sun Pharma Advanced Research Company Limited | Novel hydrazino compounds as btk inhibitors |
WO2017134588A1 (en) | 2016-02-04 | 2017-08-10 | Shilpa Medicare Limited | Process for the preparation of ibrutinib |
CN108602834B (zh) * | 2016-02-05 | 2021-01-08 | 北京盛诺基医药科技股份有限公司 | 一种布鲁顿酪氨酸激酶抑制剂 |
GB2558514A (en) * | 2016-02-09 | 2018-07-18 | Azad Pharmaceutical Ingredients Ag | Process for the synthesis of stable amorphous ibrutinib |
CA3015172A1 (en) | 2016-02-18 | 2017-08-24 | Privo Technologies, Inc. | Two-stage microparticle-based therapeutic delivery system and method |
CN105646499A (zh) * | 2016-03-01 | 2016-06-08 | 孙霖 | 依鲁替尼晶型g及制备方法 |
CN105646498A (zh) * | 2016-03-01 | 2016-06-08 | 孙霖 | 依鲁替尼晶型f及制备方法 |
RS62271B1 (sr) | 2016-03-09 | 2021-09-30 | Raze Therapeutics Inc | Inhibitori 3-fosfoglicerat dehidrogenaze i njihova upotreba |
EP3426244B1 (en) | 2016-03-09 | 2023-06-07 | Raze Therapeutics, Inc. | 3-phosphoglycerate dehydrogenase inhibitors and uses thereof |
KR102416971B1 (ko) | 2016-03-11 | 2022-07-04 | 엔젤 파마슈티칼 컴퍼니, 리미티드 | 브루톤형 티로신 키나제를 조절하기 위한 화합물 및 방법 |
WO2017163257A1 (en) * | 2016-03-21 | 2017-09-28 | Ind-Swift Laboratories Limited | Process for preparing pure lh-pyrazolo[3,4-d] pyrimidine derivative |
AU2017240609B2 (en) | 2016-03-31 | 2021-07-15 | Takeda Pharmaceutical Company Limited | Isoquinolinyl triazolone complexes |
CZ2016196A3 (cs) | 2016-04-06 | 2017-10-18 | Zentiva, K.S. | Pevné formy Ibrutinibu |
CA3019394A1 (en) | 2016-04-08 | 2017-10-12 | X4 Pharmaceuticals, Inc. | Methods for treating cancer |
RS63609B1 (sr) | 2016-04-15 | 2022-10-31 | Cancer Research Tech Ltd | Heterociklična jedinjenja kao inhibitori ret kinaze |
JP6943876B2 (ja) | 2016-04-15 | 2021-10-06 | キャンサー・リサーチ・テクノロジー・リミテッドCancer Research Technology Limited | Retキナーゼ阻害剤としての複素環化合物 |
US11813261B2 (en) | 2016-04-19 | 2023-11-14 | Acetylon Pharmaceuticals, Inc. | HDAC inhibitors, alone or in combination with BTK inhibitors, for treating chronic lymphocytic leukemia |
AU2017258510A1 (en) * | 2016-04-29 | 2018-10-11 | Dana-Farber Cancer Institute, Inc. | HCK as a therapeutic target in MYD88 mutated diseases |
CZ2016276A3 (cs) | 2016-05-11 | 2017-11-22 | Zentiva, K.S. | Pevné formy volné báze ibrutinibu |
DK3458053T3 (da) | 2016-05-20 | 2022-02-21 | Biohaven Therapeutics Ltd | Anvendelse af riluzol, riluzolprodrugs eller riluzolanaloger med immunterapier til cancerbehandling |
CN105859728B (zh) * | 2016-05-26 | 2018-06-08 | 江苏中邦制药有限公司 | 一种依鲁替尼的制备方法 |
WO2017205843A1 (en) | 2016-05-27 | 2017-11-30 | Tg Therapeutics, Inc. | Combination of anti-cd20 antibody, p13 kinase-delta selective inhibitor, and btk inhibitor to treat b-cell proliferative disorders |
CN109311876B (zh) | 2016-06-16 | 2022-05-03 | 豪夫迈·罗氏有限公司 | 杂芳基***受体调节剂及其用途 |
JP2019521983A (ja) | 2016-06-16 | 2019-08-08 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | テトラヒドロ−ピリド[3,4−b]インドールエストロゲン受容体モジュレーター及びその使用 |
US11091489B2 (en) * | 2016-06-20 | 2021-08-17 | Novartis Ag | Crystalline forms of a triazolopyrimidine compound |
WO2017223229A1 (en) | 2016-06-21 | 2017-12-28 | X4 Pharmaceuticals, Inc. | Cxcr4 inhibitors and uses thereof |
EP3808748A1 (en) | 2016-06-21 | 2021-04-21 | X4 Pharmaceuticals, Inc. | Substituted piperidines as cxcr4-inhibitors |
CN109641838A (zh) | 2016-06-21 | 2019-04-16 | X4 制药有限公司 | Cxcr4抑制剂及其用途 |
CN106117214A (zh) * | 2016-06-29 | 2016-11-16 | 上海创诺医药集团有限公司 | 依鲁替尼新晶型及其制备方法 |
JP7129704B2 (ja) | 2016-06-29 | 2022-09-02 | プリンシピア バイオファーマ インコーポレイテッド | 2-[3-[4-アミノ-3-(2-フルオロ-4-フェノキシ-フェニル)ピラゾロ[3,4-d]ピリミジン-1-イル]ピペリジン-1-カルボニル]-4-メチル-4-[4-(オキセタン-3-イル)ピペラジン-1-イル]ペント-2-エネニトリルの放出調節製剤 |
WO2018000250A1 (zh) * | 2016-06-29 | 2018-01-04 | 上海创诺医药集团有限公司 | 依鲁替尼新晶型及其制备方法 |
RU2714206C1 (ru) | 2016-06-30 | 2020-02-13 | Даевунг Фармасьютикал Ко., Лтд. | Пиразолопиримидиновые производные в качестве ингибитора киназы |
WO2018002958A1 (en) | 2016-06-30 | 2018-01-04 | Sun Pharma Advanced Research Company Limited | Novel hydrazide containing compounds as btk inhibitors |
AU2017293423B2 (en) | 2016-07-05 | 2023-05-25 | Beigene, Ltd. | Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer |
ES2965081T3 (es) * | 2016-07-07 | 2024-04-11 | Daewoong Pharmaceutical Co Ltd | Derivados 4-aminopirazolo[3,4-d]pirimidinil-azabiciclo y composición farmacéutica que comprende dichos derivados |
CN107641123A (zh) * | 2016-07-20 | 2018-01-30 | 南京亿华药业有限公司 | 一种依鲁替尼及其关键中间体的制备新方法 |
RU2019104758A (ru) | 2016-07-21 | 2020-08-21 | Байоджен Ма Инк. | Сукцинатные формы и композиции ингибиторов тирозинкиназы брутона |
WO2018033853A2 (en) | 2016-08-16 | 2018-02-22 | Beigene, Ltd. | Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
CN108368119B (zh) * | 2016-08-17 | 2019-04-23 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制酪氨酸激酶活性的稠合双环类化合物 |
WO2018033135A1 (en) | 2016-08-19 | 2018-02-22 | Beigene, Ltd. | Use of a combination comprising a btk inhibitor for treating cancers |
IL292938A (en) | 2016-09-19 | 2022-07-01 | Mei Pharma Inc | Combined treatment |
CN109790121B (zh) * | 2016-10-06 | 2024-01-05 | 詹森药业有限公司 | 用于制备btk抑制剂的方法和中间体 |
CA3039202A1 (en) | 2016-10-14 | 2018-04-19 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
CA3040840A1 (en) | 2016-10-17 | 2018-04-26 | Daiichi Sankyo Company, Limited | Combined use of mdm2 inhibitor and dna methyltransferase inhibitor for cancer treatment |
WO2018075937A1 (en) | 2016-10-21 | 2018-04-26 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
MX2019005029A (es) | 2016-11-03 | 2019-10-24 | Juno Therapeutics Inc | Terapia de combinación de una terapia de células t y un inhibidor de tirosina cinasa de bruton (btk). |
EP3538091A4 (en) | 2016-11-08 | 2020-06-10 | Navitor Pharmaceuticals, Inc. | PHENYL AMINO PIPERIDINE MTORC INHIBITORS AND USES THEREOF |
WO2018090792A1 (zh) * | 2016-11-15 | 2018-05-24 | 杭州和正医药有限公司 | 一种选择性布鲁顿酪氨酸激酶抑制剂及其应用 |
AU2017368050A1 (en) | 2016-11-29 | 2019-06-20 | Puretech Lyt, Inc. | Exosomes for delivery of therapeutic agents |
US10183024B2 (en) | 2016-12-02 | 2019-01-22 | Apotex Inc. | Crystalline forms of ibrutinib |
US11590167B2 (en) | 2016-12-03 | 2023-02-28 | Juno Therapeutic, Inc. | Methods and compositions for use of therapeutic T cells in combination with kinase inhibitors |
WO2018106636A1 (en) | 2016-12-05 | 2018-06-14 | Raze Therapeutics, Inc. | Shmt inhibitors and uses thereof |
BR112019012604A2 (pt) * | 2016-12-21 | 2019-11-26 | Acerta Pharma Bv | composto da fórmula (i) ou fórmula (ii), uso de um composto, métodos para tratar um distúrbio hiperproliferativo, um distúrbio inflamatório, um distúrbio imune, ou um distúrbio autoimune e para tratar um câncer de tumor sólido, e, composição farmacêutica. |
US11730819B2 (en) | 2016-12-23 | 2023-08-22 | Bicycletx Limited | Peptide derivatives having novel linkage structures |
WO2018127699A1 (en) | 2017-01-06 | 2018-07-12 | Bicyclerd Limited | Compounds for treating cancer |
WO2018137681A1 (en) | 2017-01-25 | 2018-08-02 | Beigene, Ltd. | Crystalline forms of (s) -7- (1- (but-2-ynoyl) piperidin-4-yl) -2- (4-phenoxyphenyl) -4, 5, 6, 7-tetrahy dropyrazolo [1, 5-a] pyrimidine-3-carboxamide, preparation, and uses thereof |
WO2018151849A1 (en) | 2017-02-17 | 2018-08-23 | Privo Technologies, Inc. | Particle-based multi-layer therapeutic delivery device and method |
EP3585789A1 (en) | 2017-02-24 | 2020-01-01 | Gilead Sciences, Inc. | Inhibitors of bruton's tyrosine kinase |
WO2018156895A1 (en) | 2017-02-24 | 2018-08-30 | Gilead Sciences, Inc. | Inhibitors of bruton's tyrosine kinase |
EP4338802A2 (en) | 2017-03-08 | 2024-03-20 | Takeda Pharmaceutical Company Limited | Tyk2 inhibitors, uses, and methods for production thereof |
CN108570036A (zh) * | 2017-03-09 | 2018-09-25 | 北京赛林泰医药技术有限公司 | 一种btk抑制剂的多晶型物及其制备方法 |
GB201703876D0 (en) | 2017-03-10 | 2017-04-26 | Berlin-Chemie Ag | Pharmaceutical combinations |
EP3595777A4 (en) * | 2017-03-14 | 2021-01-20 | Dana-Farber Cancer Institute, Inc. | SENSITIZATION OF SMALL MOLECULES TO BAX ACTIVATION FOR INDUCTION OF CELLULAR DEATH |
EP3375778A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aryl-piperidine derivatives |
EP3375784A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aza-dihydro-acridone derivatives |
AU2018237123B2 (en) * | 2017-03-22 | 2022-08-04 | Xibin Liao | Bruton's tyrosine kinase inhibitors |
WO2018191146A1 (en) | 2017-04-10 | 2018-10-18 | Navitor Pharmaceuticals, Inc. | Heteroaryl rheb inhibitors and uses thereof |
GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
CA3058682A1 (en) | 2017-04-20 | 2018-10-25 | Apotex Inc. | Processes for the preparation of acalabrutinib and intermediates thereof |
CN107043366B (zh) * | 2017-04-25 | 2020-05-26 | 中国药科大学 | 4-氨基嘧啶类化合物、其制备方法及医药用途 |
CN110809467B (zh) | 2017-04-26 | 2023-03-10 | 纳维托制药有限公司 | Sestrin-gator2相互作用的调节剂及其用途 |
US10857196B2 (en) | 2017-04-27 | 2020-12-08 | Bicycletx Limited | Bicyclic peptide ligands and uses thereof |
US10478403B1 (en) | 2017-05-03 | 2019-11-19 | Privo Technologies, Inc. | Intraoperative topically-applied non-implantable rapid release patch |
MA48781A (fr) | 2017-06-02 | 2020-04-08 | Juno Therapeutics Inc | Articles de fabrication et procédés liés à la toxicité associée à la thérapie cellulaire |
BR112019025403A2 (pt) | 2017-06-02 | 2020-08-18 | Juno Therapeutics Inc | artigos de fabricação e métodos para tratamento usando terapia celular adotiva |
CN109111446B (zh) | 2017-06-22 | 2021-11-30 | 上海度德医药科技有限公司 | 一种具有药物活性的杂芳基化合物 |
CA3066518A1 (en) | 2017-06-26 | 2019-01-03 | Beigene, Ltd. | Immunotherapy for hepatocellular carcinoma |
US10899798B2 (en) | 2017-06-26 | 2021-01-26 | Bicyclerd Limited | Bicyclic peptide ligands with detectable moieties and uses thereof |
JP2020526194A (ja) | 2017-06-29 | 2020-08-31 | ジュノー セラピューティクス インコーポレイテッド | 免疫療法薬と関連する毒性を評価するためのマウスモデル |
KR102384924B1 (ko) * | 2017-07-12 | 2022-04-08 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
WO2019013562A1 (ko) | 2017-07-12 | 2019-01-17 | 주식회사 대웅제약 | 신규한 1h-피라졸로피리딘 유도체 및 이를 포함하는 약학 조성물 |
CN111194317A (zh) | 2017-07-28 | 2020-05-22 | 林伯士拉克许米公司 | Tyk2抑制剂与其用途 |
WO2019034009A1 (en) | 2017-08-12 | 2019-02-21 | Beigene, Ltd. | BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY |
WO2019034868A1 (en) | 2017-08-14 | 2019-02-21 | Bicyclerd Limited | CONJUGATES PEPTIDE BICYCLIC-LIGAND PPR-A AND USES THEREOF |
WO2019034866A1 (en) | 2017-08-14 | 2019-02-21 | Bicyclerd Limited | BICYCLIC PEPTIDE LIGANDS CONJUGATES AND USES THEREOF |
US11883497B2 (en) | 2017-08-29 | 2024-01-30 | Puretech Lyt, Inc. | Lymphatic system-directing lipid prodrugs |
AU2018324037A1 (en) | 2017-08-29 | 2020-04-16 | Monash University | Lymphatic system-directing lipid prodrugs |
US20210071258A1 (en) | 2017-09-01 | 2021-03-11 | Juno Therapeutics, Inc. | Gene expression and assessment of risk of developing toxicity following cell therapy |
JP7366031B2 (ja) | 2017-09-22 | 2023-10-20 | カイメラ セラピューティクス, インコーポレイテッド | タンパク質分解剤およびそれらの使用 |
WO2019060693A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES THEREOF |
EA037031B1 (ru) * | 2017-10-06 | 2021-01-28 | Асерта Фарма Б.В. | Имидазопиразиновые ингибиторы тирозинкиназы брутона |
KR102613433B1 (ko) * | 2017-10-11 | 2023-12-13 | 주식회사 대웅제약 | 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물 |
TW201922256A (zh) | 2017-10-27 | 2019-06-16 | 中國大陸商浙江導明醫藥科技有限公司 | 治療淋巴樣惡性疾病之方法 |
US11564946B2 (en) | 2017-11-01 | 2023-01-31 | Juno Therapeutics, Inc. | Methods associated with tumor burden for assessing response to a cell therapy |
US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
CZ2017787A3 (cs) | 2017-12-08 | 2019-06-19 | Zentiva, K.S. | Farmaceutické kompozice obsahující ibrutinib |
US11304954B2 (en) | 2017-12-19 | 2022-04-19 | Puretech Lyt, Inc. | Lipid prodrugs of mycophenolic acid and uses thereof |
US11608345B1 (en) | 2017-12-19 | 2023-03-21 | Puretech Lyt, Inc. | Lipid prodrugs of rapamycin and its analogs and uses thereof |
GB201721265D0 (en) | 2017-12-19 | 2018-01-31 | Bicyclerd Ltd | Bicyclic peptide ligands specific for EphA2 |
TWI825046B (zh) | 2017-12-19 | 2023-12-11 | 英商拜西可泰克斯有限公司 | Epha2特用之雙環胜肽配位基 |
WO2019126378A1 (en) | 2017-12-19 | 2019-06-27 | Ariya Therapeutics, Inc. | Lipid prodrugs of mycophenolic acid and uses thereof |
BR112020012997A2 (pt) | 2017-12-26 | 2020-12-01 | Kymera Therapeutics, Inc. | degradadores de irak e usos dos mesmos |
WO2019127008A1 (zh) * | 2017-12-26 | 2019-07-04 | 清华大学 | 一种靶向降解btk的化合物及其应用 |
CN108220261B (zh) * | 2017-12-29 | 2021-05-14 | 安徽联创生物医药股份有限公司 | 酮还原酶、核酸、重组表达载体、重组表达菌株及应用 |
WO2019140387A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
US11485743B2 (en) | 2018-01-12 | 2022-11-01 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
WO2019142207A1 (en) | 2018-01-20 | 2019-07-25 | Natco Pharma Limited | Pharmaceutical compositions comprising ibrutinib |
CA3089769A1 (en) | 2018-01-29 | 2019-08-01 | Merck Patent Gmbh | Gcn2 inhibitors and uses thereof |
SG11202006701TA (en) | 2018-01-29 | 2020-08-28 | Merck Patent Gmbh | Gcn2 inhibitors and uses thereof |
CN112189009B (zh) | 2018-02-27 | 2023-09-29 | 阿塔克斯生物制药有限公司 | 作为tcr-nck相互作用的抑制剂的色烯衍生物 |
US11013741B1 (en) | 2018-04-05 | 2021-05-25 | Sumitomo Dainippon Pharma Oncology, Inc. | AXL kinase inhibitors and use of the same |
CA3095580A1 (en) | 2018-04-13 | 2019-10-17 | Sumitomo Dainippon Pharma Oncology, Inc. | Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer |
HUE058746T2 (hu) | 2018-04-24 | 2022-09-28 | Merck Patent Gmbh | Antiproliferációs vegyületek és felhasználásuk |
WO2019209757A1 (en) | 2018-04-24 | 2019-10-31 | Vertex Pharmaceuticals Incorporated | Pteridinone compounds and uses thereof |
KR102106821B1 (ko) | 2018-04-27 | 2020-05-06 | 재단법인대구경북과학기술원 | 이브루티닙을 유효성분으로 포함하는 퇴행성 뇌질환의 예방 또는 치료용 약학적 조성물 |
WO2019208805A1 (ja) | 2018-04-27 | 2019-10-31 | 小野薬品工業株式会社 | Btk阻害活性を有する化合物を有効成分として含む自己免疫疾患の予防および/または治療剤 |
AU2019261986A1 (en) | 2018-05-03 | 2020-11-26 | Juno Therapeutics, Inc. | Combination therapy of a chimeric antigen receptor (CAR) T cell therapy and a kinase inhibitor |
TW202014412A (zh) | 2018-05-04 | 2020-04-16 | 美商普托拉製藥有限公司 | 賽度替尼(cerdulatinib)之固體型式 |
EP3575300A1 (en) | 2018-05-31 | 2019-12-04 | Apotex Inc. | Novel crystalline forms of ibrutinib |
IL259810A (en) | 2018-06-04 | 2018-07-31 | Yeda Res & Dev | Mitogen-activated protein kinase kinase 7 inhibitors |
MA52874A (fr) | 2018-06-15 | 2021-04-21 | Janssen Pharmaceutica Nv | Formulations/compositions comprenant de l'ibrutinib |
US10980784B2 (en) | 2018-06-15 | 2021-04-20 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
GB201810316D0 (en) | 2018-06-22 | 2018-08-08 | Bicyclerd Ltd | Peptide ligands for binding to EphA2 |
US11180531B2 (en) | 2018-06-22 | 2021-11-23 | Bicycletx Limited | Bicyclic peptide ligands specific for Nectin-4 |
WO2020010177A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Tricyclic crbn ligands and uses thereof |
CA3103995A1 (en) | 2018-07-26 | 2020-01-30 | Sumitomo Dainippon Pharma Oncology, Inc. | Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same |
KR102545594B1 (ko) | 2018-07-31 | 2023-06-21 | 록쏘 온콜로지, 인코포레이티드 | (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제 |
WO2020045941A1 (ko) | 2018-08-27 | 2020-03-05 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
US10548889B1 (en) | 2018-08-31 | 2020-02-04 | X4 Pharmaceuticals, Inc. | Compositions of CXCR4 inhibitors and methods of preparation and use |
WO2020043321A1 (en) * | 2018-08-31 | 2020-03-05 | Stichting Katholieke Universiteit | Synergistic combinations of amino acid depletion agent sensitizers (aadas) and amino acid depletion agents (aada), and therapeutic methods of use thereof |
EP3846793B1 (en) | 2018-09-07 | 2024-01-24 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
CN110964016B (zh) * | 2018-09-29 | 2021-05-28 | 南京药捷安康生物科技有限公司 | 氨基降茨烷衍生物及其制备方法与应用 |
CA3115088A1 (en) | 2018-10-15 | 2020-04-23 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
JP2022512779A (ja) | 2018-10-23 | 2022-02-07 | バイスクルテクス・リミテッド | 二環式ペプチドリガンドおよびその使用 |
US11345654B2 (en) | 2018-10-24 | 2022-05-31 | Navitor Pharmaceuticals, Inc. | Polymorphic compounds and uses thereof |
CN111170986A (zh) | 2018-11-13 | 2020-05-19 | 北京睿熙生物科技有限公司 | 布鲁顿酪氨酸激酶的抑制剂 |
CN109293630A (zh) * | 2018-11-15 | 2019-02-01 | 山东大学 | 含取代吡唑类化合物及其制备方法与应用 |
CN109369654A (zh) * | 2018-11-20 | 2019-02-22 | 山东大学 | 1,3-二取代-4-氨基吡唑并嘧啶类化合物及其制备方法和应用 |
US11053241B2 (en) | 2018-11-30 | 2021-07-06 | Nimbus Lakshmi, Inc. | TYK2 inhibitors and uses thereof |
KR20210117260A (ko) | 2018-11-30 | 2021-09-28 | 주노 쎄러퓨티크스 인코퍼레이티드 | 입양 세포 요법을 사용한 치료방법 |
US20220031746A1 (en) | 2018-11-30 | 2022-02-03 | Juno Therapeutics, Inc. | Methods for dosing and treatment of b cell malignancies in adoptive cell therapy |
WO2020113233A1 (en) | 2018-11-30 | 2020-06-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
WO2020132561A1 (en) | 2018-12-20 | 2020-06-25 | C4 Therapeutics, Inc. | Targeted protein degradation |
EP3670659A1 (en) | 2018-12-20 | 2020-06-24 | Abivax | Biomarkers, and uses in treatment of viral infections, inflammations, or cancer |
EP3669867A1 (en) | 2018-12-21 | 2020-06-24 | Synthon B.V. | Pharmaceutical composition comprising ibrutinib |
US10688050B1 (en) | 2018-12-21 | 2020-06-23 | Synthon B.V. | Pharmaceutical composition comprising ibrutinib |
JPWO2020130125A1 (ja) | 2018-12-21 | 2021-11-04 | 第一三共株式会社 | 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ |
AU2020206884A1 (en) | 2019-01-09 | 2021-08-05 | Beth Israel Deaconess Medical Center, Inc. | Modulators of Pin1 activity and uses thereof |
CN111454268B (zh) * | 2019-01-18 | 2023-09-08 | 明慧医药(上海)有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
CA3126034A1 (en) | 2019-01-23 | 2020-07-30 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
WO2020167990A1 (en) | 2019-02-12 | 2020-08-20 | Tolero Pharmaceuticals, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
WO2020165600A1 (en) | 2019-02-14 | 2020-08-20 | Bicycletx Limited | Bicyclic peptide ligand sting conjugates and uses thereof |
WO2020170270A1 (en) * | 2019-02-19 | 2020-08-27 | Msn Laboratories Private Limited, R&D Center | Novel crystalline polymorphs of 1-[(3r)-3-[4-amino-3-(4-phenoxyphenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one and process for preparation thereof |
CN114364798A (zh) | 2019-03-21 | 2022-04-15 | 欧恩科斯欧公司 | 用于治疗癌症的Dbait分子与激酶抑制剂的组合 |
EP3946462A1 (en) | 2019-04-02 | 2022-02-09 | BicycleTX Limited | Bicycle toxin conjugates and uses thereof |
SG11202110829YA (en) | 2019-04-05 | 2021-10-28 | Kymera Therapeutics Inc | Stat degraders and uses thereof |
MX2021014246A (es) | 2019-05-21 | 2022-01-06 | Janssen Pharmaceutica Nv | Procedimientos y productos intermedios para preparar un inhibidor de btk. |
WO2020234379A1 (en) | 2019-05-21 | 2020-11-26 | Janssen Pharmaceutica Nv | Processes and intermediates for preparing a btk inhibitor |
US10937541B2 (en) | 2019-05-28 | 2021-03-02 | PAIGE.AI, Inc. | Systems and methods for processing images to prepare slides for processed images for digital pathology |
CA3141826A1 (en) | 2019-05-31 | 2020-12-03 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
WO2021038540A1 (en) | 2019-08-31 | 2021-03-04 | Sun Pharma Advanced Research Company Limited | Cycloalkylidene carboxylic acids and derivatives as btk inhibitors |
WO2021050992A1 (en) | 2019-09-11 | 2021-03-18 | Vincere Biosciences, Inc. | Usp30 inhibitors and uses thereof |
WO2021050964A1 (en) | 2019-09-13 | 2021-03-18 | Nimbus Saturn, Inc. | Hpk1 antagonists and uses thereof |
BR112022008287A2 (pt) | 2019-11-01 | 2022-07-26 | Navitor Pharm Inc | Métodos de tratamento usando um modulador de mtorc1 |
AU2020378630A1 (en) | 2019-11-08 | 2022-05-26 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
CA3163680A1 (en) | 2019-12-05 | 2021-06-10 | David John O'neill | Rapamycin analogs and uses thereof |
CN115398231A (zh) | 2019-12-06 | 2022-11-25 | 朱诺治疗学股份有限公司 | 与治疗b细胞恶性肿瘤的细胞疗法相关的毒性和反应的相关方法 |
WO2021127283A2 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
JP2023509366A (ja) | 2019-12-17 | 2023-03-08 | カイメラ セラピューティクス, インコーポレイテッド | Irak分解剤およびそれらの使用 |
JP2023509394A (ja) | 2019-12-23 | 2023-03-08 | カイメラ セラピューティクス, インコーポレイテッド | Smarca分解剤およびそれらの使用 |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
WO2021164697A1 (zh) * | 2020-02-18 | 2021-08-26 | 深圳市塔吉瑞生物医药有限公司 | 取代的酰胺衍生物及其组合物及用途 |
CN115151537A (zh) | 2020-02-26 | 2022-10-04 | 株式会社大熊制药 | 制备杂环胺衍生物的方法 |
AR121506A1 (es) | 2020-03-03 | 2022-06-08 | Pic Therapeutics Inc | Inhibidores del eif4e y sus usos |
IL296451A (en) | 2020-03-19 | 2022-11-01 | Kymera Therapeutics Inc | mdm2 joints and their uses |
TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
CN114057724A (zh) * | 2020-07-29 | 2022-02-18 | 鲁南制药集团股份有限公司 | 一种btk抑制剂 |
AU2021327130A1 (en) | 2020-08-17 | 2023-03-02 | Bicycletx Limited | Bicycle conjugates specific for Nectin-4 and uses thereof |
WO2022043251A1 (en) | 2020-08-28 | 2022-03-03 | Synthon B.V. | Pharmaceutical composition comprising ibrutinib |
US20240024325A1 (en) * | 2020-08-28 | 2024-01-25 | Emory University | Methods of Managing Cocaine or Other Drug Addictions |
WO2022120353A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
AU2021392040A1 (en) | 2020-12-02 | 2023-06-29 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
CN112574216B (zh) * | 2020-12-16 | 2022-03-08 | 天津济坤医药科技有限公司 | 一种化合物及其制备方法以及其在制备治疗抗癌药物中的应用 |
US20240092785A1 (en) | 2021-01-21 | 2024-03-21 | Synthon B.V. | Process for making ibrutinib |
EP4288427A1 (en) | 2021-02-02 | 2023-12-13 | Liminal Biosciences Limited | Gpr84 antagonists and uses thereof |
WO2022167445A1 (en) | 2021-02-02 | 2022-08-11 | Liminal Biosciences Limited | Gpr84 antagonists and uses thereof |
TW202245789A (zh) | 2021-02-15 | 2022-12-01 | 美商凱麥拉醫療公司 | Irak4降解劑及其用途 |
JP2024509192A (ja) | 2021-03-05 | 2024-02-29 | ニンバス サターン, インコーポレイテッド | Hpk1アンタゴニスト及びその使用 |
KR20230172548A (ko) | 2021-04-16 | 2023-12-22 | 이케나 온콜로지, 인코포레이티드 | Mek 억제제 및 이의 용도 |
US20220387340A1 (en) * | 2021-06-01 | 2022-12-08 | Privo Technologies, Inc. | Enhanced Two-Stage Microparticle-Based Localized Therapeutic Delivery System |
US11433072B1 (en) | 2021-06-10 | 2022-09-06 | Hikma Pharmaceuticals USA, Inc. | Oral dosage forms of ibrutinib |
WO2022260667A1 (en) | 2021-06-10 | 2022-12-15 | Hikma Pharmaceuticals Usa Inc. | Oral dosage forms of ibrutinib |
CN113583001A (zh) * | 2021-07-13 | 2021-11-02 | 江苏君若药业有限公司 | 依鲁替尼的制备 |
WO2023014817A1 (en) | 2021-08-03 | 2023-02-09 | Syros Pharmaceuticals, Inc. | Compositions and methods for treating lymphomas with a cdk7 inhibitor in combination with a btk inhibitor |
CN115702898B (zh) * | 2021-08-04 | 2024-02-09 | 成都倍特药业股份有限公司 | 一种btk抑制剂固体制剂及其制备方法 |
IL310924A (en) | 2021-08-25 | 2024-04-01 | Pic Therapeutics Inc | EIF4E inhibitors and their uses |
WO2023028238A1 (en) | 2021-08-25 | 2023-03-02 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
WO2023071973A1 (en) * | 2021-10-26 | 2023-05-04 | Shenzhen Targetrx, Inc. | Fused bicyclic compound for inhibiting activity of tyrosine kinase |
WO2023104808A1 (en) | 2021-12-10 | 2023-06-15 | Synthon B.V. | Pharmaceutical composition comprising ibrutinib |
WO2023114984A1 (en) | 2021-12-17 | 2023-06-22 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
WO2023173053A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
WO2023173057A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
CN114605418B (zh) * | 2022-03-15 | 2023-09-05 | 广东医科大学附属医院 | 一类具有抗肿瘤活性的依鲁替尼丙烯酰胺类衍生物及其合成方法与应用 |
WO2023211889A1 (en) | 2022-04-25 | 2023-11-02 | Ikena Oncology, Inc. | Polymorphic compounds and uses thereof |
WO2023220655A1 (en) | 2022-05-11 | 2023-11-16 | Celgene Corporation | Methods to overcome drug resistance by re-sensitizing cancer cells to treatment with a prior therapy via treatment with a t cell therapy |
WO2023230205A1 (en) | 2022-05-25 | 2023-11-30 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
US11814439B1 (en) | 2022-06-01 | 2023-11-14 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
US11884740B1 (en) | 2022-06-01 | 2024-01-30 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
US11807689B1 (en) | 2022-06-01 | 2023-11-07 | Tg Therapeutics, Inc. | Anti-CD20 antibody compositions |
US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
WO2023242384A1 (en) | 2022-06-17 | 2023-12-21 | Krka, D.D., Novo Mesto | Crystalline form of ibrutinib |
WO2023249980A1 (en) * | 2022-06-22 | 2023-12-28 | Genzyme Corporation | Methods of making modified btk inhibitors |
WO2024028365A1 (en) | 2022-08-02 | 2024-02-08 | Liminal Biosciences Limited | Substituted pyridone gpr84 antagonists and uses thereof |
WO2024028363A1 (en) | 2022-08-02 | 2024-02-08 | Liminal Biosciences Limited | Heteroaryl carboxamide and related gpr84 antagonists and uses thereof |
WO2024028364A1 (en) | 2022-08-02 | 2024-02-08 | Liminal Biosciences Limited | Aryl-triazolyl and related gpr84 antagonists and uses thereof |
CN115417827B (zh) * | 2022-09-30 | 2023-05-26 | 中国药科大学 | 6-氨基-1,3,5-三嗪类化合物及其合成方法和应用 |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU95113966A (ru) * | 1992-12-17 | 1997-08-10 | Пфайзер Инк. | Пиразолопиримидины, фармацевтическая композиция и способ лечения |
US20040006083A1 (en) * | 2001-03-22 | 2004-01-08 | Hirst Gavin C. | Pyrazolopyrimidines as therapeutic agents |
US20060079494A1 (en) * | 2004-09-27 | 2006-04-13 | Santi Daniel V | Specific kinase inhibitors |
Family Cites Families (158)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3598123A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
US3993073A (en) | 1969-04-01 | 1976-11-23 | Alza Corporation | Novel drug delivery device |
US3598122A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
US3710795A (en) | 1970-09-29 | 1973-01-16 | Alza Corp | Drug-delivery device with stretched, rate-controlling membrane |
US4069307A (en) | 1970-10-01 | 1978-01-17 | Alza Corporation | Drug-delivery device comprising certain polymeric materials for controlled release of drug |
US3731683A (en) | 1971-06-04 | 1973-05-08 | Alza Corp | Bandage for the controlled metering of topical drugs to the skin |
US3742951A (en) | 1971-08-09 | 1973-07-03 | Alza Corp | Bandage for controlled release of vasodilators |
US3996934A (en) | 1971-08-09 | 1976-12-14 | Alza Corporation | Medical bandage |
BE795384A (fr) | 1972-02-14 | 1973-08-13 | Ici Ltd | Pansements |
US3921636A (en) | 1973-01-15 | 1975-11-25 | Alza Corp | Novel drug delivery device |
US3993072A (en) | 1974-08-28 | 1976-11-23 | Alza Corporation | Microporous drug delivery device |
US4151273A (en) | 1974-10-31 | 1979-04-24 | The Regents Of The University Of California | Increasing the absorption rate of insoluble drugs |
US3972995A (en) | 1975-04-14 | 1976-08-03 | American Home Products Corporation | Dosage form |
US4077407A (en) | 1975-11-24 | 1978-03-07 | Alza Corporation | Osmotic devices having composite walls |
US4031894A (en) | 1975-12-08 | 1977-06-28 | Alza Corporation | Bandage for transdermally administering scopolamine to prevent nausea |
US4060084A (en) | 1976-09-07 | 1977-11-29 | Alza Corporation | Method and therapeutic system for providing chemotherapy transdermally |
US4201211A (en) | 1977-07-12 | 1980-05-06 | Alza Corporation | Therapeutic system for administering clonidine transdermally |
JPS5562012A (en) | 1978-11-06 | 1980-05-10 | Teijin Ltd | Slow-releasing preparation |
US4230105A (en) | 1978-11-13 | 1980-10-28 | Merck & Co., Inc. | Transdermal delivery of drugs |
US4229447A (en) | 1979-06-04 | 1980-10-21 | American Home Products Corporation | Intraoral methods of using benzodiazepines |
CA1146866A (en) | 1979-07-05 | 1983-05-24 | Yamanouchi Pharmaceutical Co. Ltd. | Process for the production of sustained release pharmaceutical composition of solid medical material |
US4291015A (en) | 1979-08-14 | 1981-09-22 | Key Pharmaceuticals, Inc. | Polymeric diffusion matrix containing a vasodilator |
US4327725A (en) | 1980-11-25 | 1982-05-04 | Alza Corporation | Osmotic device with hydrogel driving member |
US4476116A (en) | 1982-12-10 | 1984-10-09 | Syntex (U.S.A.) Inc. | Polypeptides/chelating agent nasal compositions having enhanced peptide absorption |
US5116817A (en) | 1982-12-10 | 1992-05-26 | Syntex (U.S.A.) Inc. | LHRH preparations for intranasal administration |
US4596795A (en) | 1984-04-25 | 1986-06-24 | The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services | Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives |
US4624848A (en) | 1984-05-10 | 1986-11-25 | Ciba-Geigy Corporation | Active agent containing hydrogel devices wherein the active agent concentration profile contains a sigmoidal concentration gradient for improved constant release, their manufacture and use |
GB8518301D0 (en) | 1985-07-19 | 1985-08-29 | Fujisawa Pharmaceutical Co | Hydrodynamically explosive systems |
US5011692A (en) | 1985-12-28 | 1991-04-30 | Sumitomo Pharmaceuticals Company, Limited | Sustained pulsewise release pharmaceutical preparation |
US4755386A (en) | 1986-01-22 | 1988-07-05 | Schering Corporation | Buccal formulation |
US5312325A (en) | 1987-05-28 | 1994-05-17 | Drug Delivery Systems Inc | Pulsating transdermal drug delivery system |
US4968509A (en) | 1987-07-27 | 1990-11-06 | Mcneilab, Inc. | Oral sustained release acetaminophen formulation and process |
US5033252A (en) | 1987-12-23 | 1991-07-23 | Entravision, Inc. | Method of packaging and sterilizing a pharmaceutical product |
US5052558A (en) | 1987-12-23 | 1991-10-01 | Entravision, Inc. | Packaged pharmaceutical product |
JPH01167840A (ja) | 1987-12-24 | 1989-07-03 | Konica Corp | 新規な写真用シアンカプラー |
IL92966A (en) | 1989-01-12 | 1995-07-31 | Pfizer | Hydrogel-operated release devices |
US5739136A (en) | 1989-10-17 | 1998-04-14 | Ellinwood, Jr.; Everett H. | Intraoral dosing method of administering medicaments |
US5017381A (en) | 1990-05-02 | 1991-05-21 | Alza Corporation | Multi-unit pulsatile delivery system |
US5633009A (en) | 1990-11-28 | 1997-05-27 | Sano Corporation | Transdermal administration of azapirones |
DE69222847T3 (de) | 1991-04-16 | 2005-09-15 | Nippon Shinyaku Co., Ltd. | Verfahren zur herstellung einer festen dispersion |
US5229135A (en) | 1991-11-22 | 1993-07-20 | Prographarm Laboratories | Sustained release diltiazem formulation |
KR100274734B1 (ko) | 1991-11-22 | 2000-12-15 | 제이코버스 코넬리스 레이서 | 리제드로네이트 지연-방출성 조성물 |
US5340591A (en) | 1992-01-24 | 1994-08-23 | Fujisawa Pharmaceutical Co., Ltd. | Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine |
US5461140A (en) | 1992-04-30 | 1995-10-24 | Pharmaceutical Delivery Systems | Bioerodible polymers for solid controlled release pharmaceutical compositions |
US5260068A (en) | 1992-05-04 | 1993-11-09 | Anda Sr Pharmaceuticals Inc. | Multiparticulate pulsatile drug delivery system |
US5281420A (en) | 1992-05-19 | 1994-01-25 | The Procter & Gamble Company | Solid dispersion compositions of tebufelone |
US5323907A (en) | 1992-06-23 | 1994-06-28 | Multi-Comp, Inc. | Child resistant package assembly for dispensing pharmaceutical medications |
AU4198793A (en) | 1992-07-24 | 1994-01-27 | Takeda Chemical Industries Ltd. | Microparticle preparation and production thereof |
US5700485A (en) | 1992-09-10 | 1997-12-23 | Children's Medical Center Corporation | Prolonged nerve blockade by the combination of local anesthetic and glucocorticoid |
WO1994008568A1 (en) | 1992-10-16 | 1994-04-28 | Nippon Shinyaku Co., Ltd. | Method of manufacturing wax matrices |
US5260069A (en) | 1992-11-27 | 1993-11-09 | Anda Sr Pharmaceuticals Inc. | Pulsatile particles drug delivery system |
TW370529B (en) * | 1992-12-17 | 1999-09-21 | Pfizer | Pyrazolopyrimidines |
GB9226855D0 (en) | 1992-12-23 | 1993-02-17 | Erba Carlo Spa | Vinylene-azaindole derivatives and process for their preparation |
US5686105A (en) | 1993-10-19 | 1997-11-11 | The Procter & Gamble Company | Pharmaceutical dosage form with multiple enteric polymer coatings for colonic delivery |
US6326469B1 (en) | 1994-04-22 | 2001-12-04 | Sugen, Inc. | Megakaryocytic protein tyrosine kinases |
US5665378A (en) | 1994-09-30 | 1997-09-09 | Davis; Roosevelt | Transdermal therapeutic formulation |
US5530012A (en) | 1994-12-22 | 1996-06-25 | Bristol-Myers Squibb Co. | 3-alkoxybenzylpiperidine derivatives as melatonergic agents |
US5567441A (en) | 1995-03-24 | 1996-10-22 | Andrx Pharmaceuticals Inc. | Diltiazem controlled release formulation |
CA2220451A1 (en) | 1995-05-17 | 1996-11-21 | Cedars-Sinai Medical Center | Methods and compositions for improving digestion and absorption in the small intestine |
US5593997A (en) | 1995-05-23 | 1997-01-14 | Pfizer Inc. | 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors |
SE9502244D0 (sv) | 1995-06-20 | 1995-06-20 | Bioglan Ab | A composition and a process for the preparation thereof |
US5837284A (en) | 1995-12-04 | 1998-11-17 | Mehta; Atul M. | Delivery of multiple doses of medications |
US5858401A (en) | 1996-01-22 | 1999-01-12 | Sidmak Laboratories, Inc. | Pharmaceutical composition for cyclosporines |
CH690773A5 (de) | 1996-02-01 | 2001-01-15 | Novartis Ag | Pyrrolo(2,3-d)pyrimide und ihre Verwendung. |
US6923983B2 (en) | 1996-02-19 | 2005-08-02 | Acrux Dds Pty Ltd | Transdermal delivery of hormones |
US6929801B2 (en) | 1996-02-19 | 2005-08-16 | Acrux Dds Pty Ltd | Transdermal delivery of antiparkinson agents |
US6458373B1 (en) | 1997-01-07 | 2002-10-01 | Sonus Pharmaceuticals, Inc. | Emulsion vehicle for poorly soluble drugs |
AU748884B2 (en) | 1997-03-19 | 2002-06-13 | Abbott Gmbh & Co. Kg | Pyrrolo(2,3d)pyrimidines and their use as tyrosine kinase inhibitors |
US5840329A (en) | 1997-05-15 | 1998-11-24 | Bioadvances Llc | Pulsatile drug delivery system |
US6391452B1 (en) | 1997-07-18 | 2002-05-21 | Bayer Corporation | Compositions for nasal drug delivery, methods of making same, and methods of removing residual solvent from pharmaceutical preparations |
US5869090A (en) | 1998-01-20 | 1999-02-09 | Rosenbaum; Jerry | Transdermal delivery of dehydroepiandrosterone |
DE69918089T2 (de) * | 1998-04-17 | 2005-07-14 | Parker Hughes Institute, St. Paul | Btk inhibitoren und verfahren zur identifizierung und verwendung |
US6303652B1 (en) | 1998-08-21 | 2001-10-16 | Hughes Institute | BTK inhibitors and methods for their identification and use |
US6998233B2 (en) | 1998-06-26 | 2006-02-14 | Sunesis Pharmaceuticals, Inc. | Methods for ligand discovery |
US20050287596A9 (en) | 1998-06-26 | 2005-12-29 | Braisted Andrew C | Novel ligands and libraries of ligands |
US6335155B1 (en) | 1998-06-26 | 2002-01-01 | Sunesis Pharmaceuticals, Inc. | Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules |
US6946144B1 (en) | 1998-07-08 | 2005-09-20 | Oryxe | Transdermal delivery system |
ES2307482T3 (es) | 1999-02-10 | 2008-12-01 | Pfizer Products Inc. | Dispersiones farmaceuticas solidas. |
US6306897B1 (en) | 1999-03-19 | 2001-10-23 | Parker Hughes Institute | Calanolides for inhibiting BTK |
US6600744B1 (en) * | 1999-03-23 | 2003-07-29 | Alcatel Canada Inc. | Method and apparatus for packet classification in a data communication system |
US6395300B1 (en) | 1999-05-27 | 2002-05-28 | Acusphere, Inc. | Porous drug matrices and methods of manufacture thereof |
US6921763B2 (en) | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
CZ2002936A3 (cs) | 1999-09-17 | 2002-10-16 | Abbott Gmbh & Co. Kg | Pyrazolopyrimidiny jako terapeutické prostředky |
US6506769B2 (en) | 1999-10-06 | 2003-01-14 | Boehringer Ingelheim Pharmaceuticals, Inc. | Heterocyclic compounds useful as inhibitors of tyrosine kinases |
WO2001025238A2 (en) | 1999-10-06 | 2001-04-12 | Boehringer Ingelheim Pharmaceuticals, Inc. | Heterocyclic compounds useful as inhibitors of tyrosine kinases |
WO2001041754A2 (en) | 1999-11-30 | 2001-06-14 | Parker Hughes Institute | Inhibitors of collagen-induced platelet aggregation |
JP2003532632A (ja) | 1999-12-17 | 2003-11-05 | アライアッド・ファーマシューティカルズ・インコーポレーテッド | 新規の複素環 |
GB0005345D0 (en) | 2000-03-06 | 2000-04-26 | Mathilda & Terence Kennedy Ins | Methods of treating sepsis septic shock and inflammation |
JP2004533209A (ja) | 2000-10-23 | 2004-11-04 | ブリストル−マイヤーズ スクイブ カンパニー | ブルトンチロシンキナーゼおよびブルトンチロシンキナーゼ媒体のモデュレーターおよびその同定方法および骨粗鬆症および関連疾患状態の治療および予防におけるその使用 |
AU2002232492A1 (en) | 2000-12-06 | 2002-06-18 | Pharmacia Corporation | Rapidly dispersing pharmaceutical composition comprising effervescent agents |
US6465014B1 (en) | 2001-03-21 | 2002-10-15 | Isp Investments Inc. | pH-dependent sustained release, drug-delivery composition |
US8306897B2 (en) | 2001-05-04 | 2012-11-06 | Stockshield, Inc. | Method and system for insuring against investment loss |
ITMI20010995A1 (it) * | 2001-05-15 | 2002-11-15 | Getters Spa | Dispensatori di cesio e processo per il loro uso |
FI20011237A0 (fi) * | 2001-06-12 | 2001-06-12 | Nokia Corp | Tiedonsiirtomenetelmä ja -järjestely |
WO2003000187A2 (en) | 2001-06-21 | 2003-01-03 | Ariad Pharmaceuticals, Inc. | Novel pyrazolo-and pyrrolo-pyrimidines and uses thereof |
CA2810339A1 (en) | 2001-08-10 | 2003-02-20 | Novartis Ag | Use of c-src inhibitors alone or in combination with sti571 for the treatment of leukaemia |
WO2003016338A1 (en) | 2001-08-15 | 2003-02-27 | Parker Hughes Institute | Crystal structure of the btk kinase domain |
US6960563B2 (en) | 2001-08-31 | 2005-11-01 | Morton Grove Pharmaceuticals, Inc. | Spontaneous emulsions containing cyclosporine |
IL161409A0 (en) | 2001-11-21 | 2004-09-27 | Sunesis Pharmaceuticals Inc | Methods for ligand discovery |
US6961787B2 (en) * | 2002-01-07 | 2005-11-01 | Intel Corporation | Method and apparatus for updating task files |
US20050084905A1 (en) | 2002-03-21 | 2005-04-21 | Prescott John C. | Identification of kinase inhibitors |
GB2388594A (en) | 2002-05-16 | 2003-11-19 | Bayer Ag | Imidazo-triazine PDE 4 inhibitors |
EP1529046A1 (en) | 2002-08-08 | 2005-05-11 | Boehringer Ingelheim Pharmaceuticals Inc. | Substituted benzimidazole compounds |
GB0303910D0 (en) | 2003-02-20 | 2003-03-26 | Merck Sharp & Dohme | Therapeutic agents |
WO2005000197A2 (en) | 2003-04-11 | 2005-01-06 | The Regents Of The University Of California | Selective serine/threonine kinase inhibitors |
US20050008640A1 (en) | 2003-04-23 | 2005-01-13 | Wendy Waegell | Method of treating transplant rejection |
EP1473039A1 (en) | 2003-05-02 | 2004-11-03 | Centre National De La Recherche Scientifique (Cnrs) | Use of inhibitors and antisense oligonucleotides of BTK for the treatment of proliferative mastocytosis |
WO2005014599A1 (en) | 2003-06-04 | 2005-02-17 | Cellular Genomics, Inc. | Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds |
US7393848B2 (en) | 2003-06-30 | 2008-07-01 | Cgi Pharmaceuticals, Inc. | Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds |
US8131475B2 (en) | 2003-09-03 | 2012-03-06 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Methods for identifying, diagnosing, and predicting survival of lymphomas |
CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
WO2005060956A1 (en) | 2003-12-12 | 2005-07-07 | University Of Maryland, Baltimore | IMMUNOMODULATORY COMPOUNDS THAT TARGET AND INHIBIT THE pY+3 BINDING SITE OF TYROSENE KINASE p56 LCK SH2 DOMAIN |
US20070281907A1 (en) | 2003-12-22 | 2007-12-06 | Watkins William J | Kinase Inhibitor Phosphonate Conjugates |
JP2007519742A (ja) | 2004-01-26 | 2007-07-19 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼの阻害剤として有用な組成物 |
WO2005074603A2 (en) | 2004-02-03 | 2005-08-18 | Abbott Laboratories | Aminobenzoxazoles as therapeutic agents |
ITMI20041314A1 (it) | 2004-06-30 | 2004-09-30 | Nuvera Fuel Cells Europ Srl | Dispositivo di raffreddamento per celle a combustibili a membrana |
KR20070063562A (ko) | 2004-09-28 | 2007-06-19 | 얀센 파마슈티카 엔.브이. | 치환 디피페리딘 ccr2 길항제 |
JP2008519843A (ja) * | 2004-11-10 | 2008-06-12 | シージーアイ ファーマスーティカル インコーポレーテッド | 特定のイミダゾ[1,2−a]ビラジン−8−イラミンズ、その生成方法及びそれに関する使用方法 |
GB0425035D0 (en) * | 2004-11-12 | 2004-12-15 | Novartis Ag | Organic compounds |
KR101357524B1 (ko) * | 2005-03-10 | 2014-02-03 | 질레드 코네티컷 인코포레이티드 | 특정 치환된 아미드, 그의 제조 방법, 및 사용 방법 |
KR20080025039A (ko) | 2005-05-13 | 2008-03-19 | 아이알엠 엘엘씨 | 단백질 키나제 억제제로서의 화합물 및 조성물 |
PE20070100A1 (es) | 2005-06-22 | 2007-03-10 | Plexxikon Inc | DERIVADOS DE PIRROLO[2,3-b]PIRIDINA COMO MODULADORES DE QUINASAS |
US20070065449A1 (en) | 2005-09-16 | 2007-03-22 | Claire Verschraegen | Method of treating cancer, especially soft tissue sarcoma utilizing gemcitabine in combination with docetaxel and anti-VEGF therapy (bevacizumab) |
CA2629314A1 (en) | 2005-11-12 | 2007-05-24 | Boehringer Ingelheim International Gmbh | Tec kinase inhibitors |
JP2009523724A (ja) | 2006-01-13 | 2009-06-25 | ファーマサイクリクス,インコーポレイテッド | チロシンキナーゼ阻害剤およびその使用方法 |
JP2009525468A (ja) | 2006-01-30 | 2009-07-09 | ザ・スクリプス・リサーチ・インステイチユート | 循環腫瘍細胞の検出方法および哺乳類対象における癌の診断方法 |
KR20090017498A (ko) * | 2006-04-04 | 2009-02-18 | 더 리젠트스 오브 더 유니이버시티 오브 캘리포니아 | Pi3 키나제 길항물질 |
EP2027087A2 (en) * | 2006-05-18 | 2009-02-25 | MannKind Corporation | Intracellular kinase inhibitors |
SI2530083T1 (sl) | 2006-09-22 | 2016-09-30 | Pharmacyclics Llc | Inhibitorji Bruton tirozin kinaze |
ES2403546T3 (es) * | 2006-11-03 | 2013-05-20 | Pharmacyclics, Inc. | Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización |
NL2000640C2 (nl) | 2007-03-05 | 2008-09-08 | Stichting Wetsus Ct Of Excelle | Werkwijze en systeem voor het zuiveren van een vloeistof. |
ES2562215T3 (es) | 2007-03-28 | 2016-03-03 | Pharmacyclics Llc | Inhibidores de la tirosina quinasa de Bruton |
US20120065201A1 (en) | 2007-03-28 | 2012-03-15 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
US8809273B2 (en) | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
US20090010911A1 (en) | 2007-04-06 | 2009-01-08 | Iowa State University Research Foundation, Inc. | Methods and compositions for affecting cyclophilin a regulation of kinases in modulating cellular activities |
US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
TWI552752B (zh) | 2007-10-19 | 2016-10-11 | 賽基艾維洛米斯研究股份有限公司 | 雜芳基化合物及其用途 |
EP2426109B1 (en) | 2007-10-23 | 2013-12-18 | F. Hoffmann-La Roche AG | Novel kinase inhibitors |
US8426441B2 (en) | 2007-12-14 | 2013-04-23 | Roche Palo Alto Llc | Inhibitors of bruton's tyrosine kinase |
US20150152115A1 (en) | 2007-12-27 | 2015-06-04 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
JP2011526299A (ja) | 2008-06-27 | 2011-10-06 | アビラ セラピューティクス, インコーポレイテッド | ヘテロアリール化合物およびそれらの使用 |
AU2009270856B2 (en) | 2008-07-16 | 2013-07-25 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors |
WO2010126960A1 (en) | 2009-04-29 | 2010-11-04 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
TWI380514B (en) * | 2009-07-09 | 2012-12-21 | Hon Hai Prec Ind Co Ltd | Electronic connector and electronic device using the same |
NZ620174A (en) | 2009-09-16 | 2016-08-26 | Celgene Avilomics Res Inc | Protein kinase conjugates and inhibitors |
US7741330B1 (en) | 2009-10-12 | 2010-06-22 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase |
US20120071497A1 (en) | 2010-06-03 | 2012-03-22 | Pharmacyclics, Inc. | Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase |
EP2575818A4 (en) | 2010-06-03 | 2013-11-06 | Pharmacyclics Inc | USE OF INHIBITORS OF BRUTON TYROSINE KINASE (BTK) |
LT2975042T (lt) | 2010-06-23 | 2019-01-25 | Hanmi Science Co., Ltd. | Naujieji kondensuoti pirimidino dariniai, skirti tirozino kinazės aktyvumo slopinimui |
EP2603081B1 (en) | 2010-08-10 | 2016-10-05 | Celgene Avilomics Research, Inc. | Besylate salt of a btk inhibitor |
US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
US8501724B1 (en) | 2012-01-31 | 2013-08-06 | Pharmacyclics, Inc. | Purinone compounds as kinase inhibitors |
KR20220093389A (ko) | 2012-06-04 | 2022-07-05 | 파마싸이클릭스 엘엘씨 | 브루톤 타이로신 키나아제 저해제의 결정 형태 |
JP6575950B2 (ja) | 2012-07-24 | 2019-09-18 | ファーマサイクリックス エルエルシー | Bruton型チロシンキナーゼ(Btk)阻害剤に対する耐性を伴う変異 |
AU2014273946B2 (en) | 2013-05-30 | 2020-03-12 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using PI3 kinase isoform modulators |
JP6800750B2 (ja) | 2013-08-02 | 2020-12-16 | ファーマサイクリックス エルエルシー | 固形腫瘍の処置方法 |
TWI617309B (zh) | 2013-10-25 | 2018-03-11 | 製藥公司 | 使用布魯頓氏酪胺酸激酶抑制劑之治療及免疫療法 |
CN106008515A (zh) | 2014-01-29 | 2016-10-12 | 苏州晶云药物科技有限公司 | 依鲁替尼的新晶型及其制备方法 |
-
2006
- 2006-12-28 SI SI200632078A patent/SI2530083T1/sl unknown
- 2006-12-28 NZ NZ595230A patent/NZ595230A/xx unknown
- 2006-12-28 EA EA200900351A patent/EA018573B1/ru active Protection Beyond IP Right Term
- 2006-12-28 PL PL12166295.1T patent/PL2530083T3/pl unknown
- 2006-12-28 US US11/617,645 patent/US7514444B2/en active Active
- 2006-12-28 SI SI200631929T patent/SI2526933T1/sl unknown
- 2006-12-28 EP EP12166301.7A patent/EP2526933B1/en active Active
- 2006-12-28 KR KR1020097008224A patent/KR101315610B1/ko active Protection Beyond IP Right Term
- 2006-12-28 PL PL12166302T patent/PL2529622T3/pl unknown
- 2006-12-28 HU HUE12166298A patent/HUE031334T2/hu unknown
- 2006-12-28 LT LTEP12166298.5T patent/LT2529621T/lt unknown
- 2006-12-28 LT LTEP12166295.1T patent/LT2530083T/lt unknown
- 2006-12-28 CN CN2010101622704A patent/CN101805341B/zh active Active
- 2006-12-28 SI SI200632029T patent/SI2526934T1/sl unknown
- 2006-12-28 WO PCT/US2006/049626 patent/WO2008039218A2/en active Application Filing
- 2006-12-28 HU HUE12166295A patent/HUE028086T2/en unknown
- 2006-12-28 NZ NZ601278A patent/NZ601278A/xx unknown
- 2006-12-28 EP EP12166295.1A patent/EP2530083B1/en active Active
- 2006-12-28 ES ES12166305.8T patent/ES2564647T3/es active Active
- 2006-12-28 SI SI200632124A patent/SI2529621T1/sl unknown
- 2006-12-28 DK DK12166305.8T patent/DK2526934T3/en active
- 2006-12-28 HU HUE12166300A patent/HUE033182T2/en unknown
- 2006-12-28 CA CA2663116A patent/CA2663116C/en active Active
- 2006-12-28 KR KR1020107006332A patent/KR20100051863A/ko not_active Application Discontinuation
- 2006-12-28 HU HUE06850039A patent/HUE029095T2/en unknown
- 2006-12-28 DK DK12166298.5T patent/DK2529621T3/en active
- 2006-12-28 PT PT121663017T patent/PT2526933E/pt unknown
- 2006-12-28 ES ES12166298.5T patent/ES2617150T3/es active Active
- 2006-12-28 SG SG201006601-7A patent/SG166093A1/en unknown
- 2006-12-28 MX MX2009003122A patent/MX2009003122A/es active IP Right Grant
- 2006-12-28 PL PL12166305.8T patent/PL2526934T4/pl unknown
- 2006-12-28 EP EP06850039.6A patent/EP2081435B1/en active Active
- 2006-12-28 AU AU2006348662A patent/AU2006348662B8/en active Active
- 2006-12-28 SI SI200632084A patent/SI2081435T1/sl unknown
- 2006-12-28 BR BRPI0622054A patent/BRPI0622054B8/pt active IP Right Grant
- 2006-12-28 LT LTEP12166300.9T patent/LT2526771T/lt unknown
- 2006-12-28 AT AT10155834T patent/ATE531263T1/de active
- 2006-12-28 PT PT10155834T patent/PT2201840E/pt unknown
- 2006-12-28 SI SI200632256T patent/SI2529622T1/en unknown
- 2006-12-28 ES ES12166300.9T patent/ES2616789T3/es active Active
- 2006-12-28 EP EP12166296A patent/EP2532234A1/en not_active Withdrawn
- 2006-12-28 ES ES12166301.7T patent/ES2537399T3/es active Active
- 2006-12-28 DK DK06850039.6T patent/DK2081435T3/en active
- 2006-12-28 EA EA201300246A patent/EA024255B1/ru unknown
- 2006-12-28 PL PL10155834T patent/PL2201840T3/pl unknown
- 2006-12-28 CN CN201210200042.0A patent/CN102746305B/zh active Active
- 2006-12-28 EP EP12166302.5A patent/EP2529622B1/en not_active Revoked
- 2006-12-28 EP EP12151943A patent/EP2443929A1/en not_active Withdrawn
- 2006-12-28 EP EP12166305.8A patent/EP2526934B1/en active Active
- 2006-12-28 JP JP2009529166A patent/JP4934197B2/ja active Active
- 2006-12-28 SI SI200631249T patent/SI2201840T1/sl unknown
- 2006-12-28 DK DK10155834.4T patent/DK2201840T3/da active
- 2006-12-28 SI SI200632148A patent/SI2526771T1/sl unknown
- 2006-12-28 DK DK12166301.7T patent/DK2526933T3/en active
- 2006-12-28 KR KR1020127034005A patent/KR101464424B1/ko active IP Right Grant
- 2006-12-28 EA EA201000599A patent/EA020001B1/ru unknown
- 2006-12-28 CN CN201210217024.3A patent/CN102887900B/zh active Active
- 2006-12-28 NZ NZ575650A patent/NZ575650A/en not_active IP Right Cessation
- 2006-12-28 BR BRPI0622277-3A patent/BRPI0622277A2/pt not_active Application Discontinuation
- 2006-12-28 HU HUE12166305A patent/HUE028712T2/en unknown
- 2006-12-28 CA CA2847852A patent/CA2847852A1/en not_active Abandoned
- 2006-12-28 HU HUE12166301A patent/HUE025459T2/hu unknown
- 2006-12-28 CA CA3180977A patent/CA3180977A1/en active Pending
- 2006-12-28 MX MX2012014021A patent/MX347525B/es unknown
- 2006-12-28 SG SG10201503235VA patent/SG10201503235VA/en unknown
- 2006-12-28 EP EP12166306A patent/EP2532235A1/en not_active Withdrawn
- 2006-12-28 ES ES10155834T patent/ES2376424T3/es active Active
- 2006-12-28 EP EP12166298.5A patent/EP2529621B1/en active Active
- 2006-12-28 DK DK12166300.9T patent/DK2526771T3/en active
- 2006-12-28 PL PL12166298T patent/PL2529621T3/pl unknown
- 2006-12-28 PL PL06850039.6T patent/PL2081435T3/pl unknown
- 2006-12-28 EP EP10155834A patent/EP2201840B1/en active Active
- 2006-12-28 PL PL12166301T patent/PL2526933T3/pl unknown
- 2006-12-28 PT PT121663025T patent/PT2529622T/pt unknown
- 2006-12-28 PT PT68500396T patent/PT2081435T/pt unknown
- 2006-12-28 HU HUE12166302A patent/HUE036897T2/hu unknown
- 2006-12-28 PT PT121662985T patent/PT2529621T/pt unknown
- 2006-12-28 EP EP12166300.9A patent/EP2526771B1/en active Active
- 2006-12-28 ES ES12166302.5T patent/ES2673973T3/es active Active
- 2006-12-28 PL PL12166300T patent/PL2526771T3/pl unknown
- 2006-12-28 DK DK12166302.5T patent/DK2529622T3/en active
- 2006-12-28 LT LTEP12166302.5T patent/LT2529622T/lt unknown
- 2006-12-28 KR KR1020147002658A patent/KR101479913B1/ko active IP Right Grant
- 2006-12-28 ES ES06850039.6T patent/ES2585902T3/es active Active
- 2006-12-28 CN CN2006800564385A patent/CN101610676B/zh active Active
- 2006-12-28 PT PT121662951T patent/PT2530083T/pt unknown
- 2006-12-28 PT PT121663009T patent/PT2526771T/pt unknown
- 2006-12-28 ES ES12166295.1T patent/ES2584331T3/es active Active
-
2007
- 2007-03-28 US US11/692,870 patent/US7732454B2/en active Active
- 2007-12-26 US US11/964,285 patent/US7825118B2/en active Active
-
2008
- 2008-03-27 US US12/594,805 patent/US8883435B2/en active Active
-
2009
- 2009-01-20 US US12/356,498 patent/US8088781B2/en active Active
- 2009-03-12 IL IL197550A patent/IL197550A0/en active Protection Beyond IP Right Term
- 2009-03-12 ZA ZA2009/01784A patent/ZA200901784B/en unknown
- 2009-03-20 MX MX2019012657A patent/MX2019012657A/es unknown
- 2009-07-07 US US12/499,005 patent/US8008309B2/en active Active
- 2009-07-07 US US12/499,002 patent/US8501751B2/en active Active
- 2009-07-07 US US12/499,008 patent/US20100022561A1/en not_active Abandoned
- 2009-09-14 HK HK10106827.4A patent/HK1140107A1/xx unknown
- 2009-09-14 HK HK09108393.7A patent/HK1129274A1/zh unknown
-
2010
- 2010-03-18 AU AU2010201052A patent/AU2010201052B2/en active Active
- 2010-03-19 US US12/727,703 patent/US20100324050A1/en not_active Abandoned
- 2010-07-08 JP JP2010155965A patent/JP5193256B2/ja active Active
- 2010-08-31 US US12/873,205 patent/US7960396B2/en active Active
- 2010-09-21 US US12/887,428 patent/US8236812B2/en active Active
- 2010-10-19 US US12/907,759 patent/US8952015B2/en active Active
- 2010-10-22 ZA ZA2010/07561A patent/ZA201007561B/en unknown
-
2011
- 2011-01-21 US US13/011,258 patent/US8232280B2/en active Active
- 2011-02-03 ZA ZA2011/00893A patent/ZA201100893B/en unknown
- 2011-06-15 US US13/161,238 patent/US8158786B2/en active Active
- 2011-06-16 US US13/162,449 patent/US20110281322A1/en not_active Abandoned
- 2011-09-29 US US13/249,066 patent/US8735403B2/en active Active
- 2011-12-06 US US13/312,606 patent/US8497277B2/en active Active
- 2011-12-16 US US13/328,718 patent/US8476284B2/en active Active
- 2011-12-22 US US13/335,719 patent/US8735404B2/en active Active
- 2011-12-29 US US13/340,556 patent/US8741908B2/en active Active
- 2011-12-29 US US13/340,409 patent/US8748438B2/en active Active
-
2012
- 2012-01-27 CY CY20121100100T patent/CY1112513T1/el unknown
- 2012-01-30 US US13/361,730 patent/US8563563B2/en active Active
- 2012-01-30 US US13/361,726 patent/US8658653B2/en active Active
- 2012-01-30 US US13/361,733 patent/US8399470B2/en active Active
- 2012-03-06 JP JP2012049524A patent/JP5635544B2/ja active Active
- 2012-04-18 US US13/450,158 patent/US8748439B2/en active Active
- 2012-05-15 US US13/472,292 patent/US8691546B2/en active Active
- 2012-05-23 US US13/479,053 patent/US8697711B2/en active Active
- 2012-06-18 US US13/526,163 patent/US8552010B2/en active Active
- 2012-06-18 US US13/526,161 patent/US8703780B2/en active Active
- 2012-07-05 US US13/542,440 patent/US8754091B2/en active Active
- 2012-09-20 ZA ZA2012/07075A patent/ZA201207075B/en unknown
- 2012-10-17 US US13/654,173 patent/US8957079B2/en active Active
- 2012-12-28 JP JP2012286719A patent/JP5718890B2/ja active Active
-
2013
- 2013-03-22 US US13/849,399 patent/US8975266B2/en active Active
- 2013-04-24 HK HK13104973.8A patent/HK1178144A1/xx unknown
- 2013-05-09 US US13/890,498 patent/US9133198B2/en active Active
- 2013-07-26 US US13/952,531 patent/US8759516B2/en active Active
- 2013-09-20 US US14/033,344 patent/US9127012B2/en active Active
- 2013-11-06 US US14/073,543 patent/US9133201B2/en active Active
- 2013-11-06 US US14/073,594 patent/US9409911B2/en active Active
- 2013-11-13 US US14/079,508 patent/US9133202B2/en active Active
- 2013-11-14 US US14/080,640 patent/US9181257B2/en active Active
- 2013-11-14 US US14/080,649 patent/US9212185B2/en active Active
-
2014
- 2014-01-10 US US14/152,886 patent/US9266893B2/en active Active
- 2014-01-15 US US14/156,247 patent/US9193735B2/en active Active
- 2014-07-24 US US14/340,483 patent/US9206189B2/en active Active
-
2015
- 2015-02-03 US US14/613,309 patent/US20150306103A1/en not_active Abandoned
- 2015-04-03 CY CY2015016C patent/CY2015016I2/el unknown
- 2015-04-03 NL NL300728C patent/NL300728I1/nl unknown
- 2015-04-03 LT LTPA2015017C patent/LTC2201840I2/lt unknown
- 2015-04-03 FR FR15C0029C patent/FR15C0029I2/fr active Active
- 2015-04-07 LU LU92662C patent/LU92692I2/xx unknown
- 2015-04-08 HU HUS1500018C patent/HUS1500018I1/hu unknown
- 2015-05-20 CY CY20151100453T patent/CY1116295T1/el unknown
-
2016
- 2016-02-12 US US15/042,734 patent/US20170007611A1/en not_active Abandoned
- 2016-03-07 CY CY20161100196T patent/CY1117587T1/el unknown
- 2016-07-26 CY CY20161100734T patent/CY1117840T1/el unknown
- 2016-08-03 CY CY20161100765T patent/CY1117897T1/el unknown
- 2016-11-15 CY CY2016041C patent/CY2016041I2/el unknown
- 2016-11-23 LU LU93321C patent/LU93321I2/fr unknown
- 2016-11-23 HU HUS1600049C patent/HUS1600049I1/hu unknown
- 2016-11-24 LT LTPA2016034C patent/LTPA2016034I1/lt unknown
- 2016-12-27 CY CY20161101348T patent/CY1119209T1/el unknown
-
2017
- 2017-02-22 CY CY20171100248T patent/CY1118666T1/el unknown
- 2017-03-24 HU HUS1700012C patent/HUS1700012I1/hu unknown
- 2017-03-30 LU LU00011C patent/LUC00011I2/fr unknown
- 2017-03-30 LT LTPA2017009C patent/LTPA2017009I1/lt unknown
- 2017-03-31 CY CY2017012C patent/CY2017012I2/el unknown
- 2017-05-08 US US15/588,947 patent/US20180085372A1/en not_active Abandoned
-
2018
- 2018-04-17 CY CY20181100404T patent/CY1120135T1/el unknown
-
2019
- 2019-05-20 US US16/417,043 patent/US20200108072A1/en not_active Abandoned
-
2021
- 2021-02-19 US US17/180,391 patent/US20220008424A1/en not_active Abandoned
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU95113966A (ru) * | 1992-12-17 | 1997-08-10 | Пфайзер Инк. | Пиразолопиримидины, фармацевтическая композиция и способ лечения |
US20040006083A1 (en) * | 2001-03-22 | 2004-01-08 | Hirst Gavin C. | Pyrazolopyrimidines as therapeutic agents |
US20060079494A1 (en) * | 2004-09-27 | 2006-04-13 | Santi Daniel V | Specific kinase inhibitors |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2655388C2 (ru) * | 2012-01-31 | 2018-05-28 | Фармасайкликс Элэлси | Соединения пуринона в качестве ингибиторов киназ |
RU2721774C1 (ru) * | 2016-11-24 | 2020-05-22 | Шанхай Инститьют Оф Материя Медика, Чайниз Академи Оф Сайенсез | ПИРИМИДО[5,4-b]ИНДОЛИЗИНОВОЕ ИЛИ ПИРИМИДО[5,4-b]ПИРРОЛИЗИНОВОЕ СОЕДИНЕНИЕ, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ |
AU2017366529B2 (en) * | 2016-11-24 | 2021-08-19 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Pyrimido(5,4-b)indolizine or pyrimido(5,4-b)pyrrolizine compound, preparation method and use thereof |
RU2711106C2 (ru) * | 2018-06-06 | 2020-01-15 | Общество с ограниченной ответственностью "АКСЕЛЬФАРМ" | Кристаллическая μ-модификация 1-[(3R)-3-[4-амино-3-(4-фенокси-фенил)-1Н-пиразоло[3,4-d]пиримидин-1-ил]-1-пиперидил]-2-пропенил-1-она, способ её получения и фармацевтическая композиция на её основе |
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
EA018573B1 (ru) | Ингибиторы тирозинкиназы брутона | |
ES2547916T3 (es) | Terapia de combinación de inhibidores de mTOR/JAK | |
JP5528807B2 (ja) | 複合薬剤 | |
US20180186785A1 (en) | Proteolysis Targeting Chimera Compounds and Methods of Preparing and Using Same | |
EP3154957B1 (en) | Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases | |
CY1122336T1 (el) | Eνωσεις πυρρολιου ως αναστολεις πρωτεϊνικων κινασων εrκ και φαρμακευτικες συνθεσεις που περιεχουν αυτες τις ενωσεις | |
US7468380B2 (en) | Nitrogen-containing aromatic derivatives | |
WO2016145935A1 (zh) | 优化的联合用药及其治疗癌症和自身免疫疾病的用途 | |
JP5523829B2 (ja) | 複合薬剤 | |
US20060281771A1 (en) | Synergistic modulation of flt3 kinase using aminoquinoline and aminoquinazoline kinase modulators | |
KR20200108298A (ko) | 벤즈아미드 화합물 | |
US8071768B2 (en) | Alkylquinoline and alkylquinazoline kinase modulators | |
JP2016514134A (ja) | Betブロモドメイン阻害剤およびこれを用いる治療方法 | |
UA86614C2 (ru) | Соединение, которое имеет активность ингибитора киназ, фармацевтическая композиция, которая включает указанное соединение, и их применение для приготовления лекарственного препарата | |
MA29791B1 (fr) | Composes therapeutiques. | |
CN102647904A (zh) | 新型三环蛋白激酶调节剂 | |
TW201536786A (zh) | 新穎縮合嘧啶化合物或其鹽 | |
NZ736048A (en) | The use of inhibitors of bruton’s tyrosine kinase (btk) | |
UY28496A1 (es) | Compuestos de bencimidazolona que tienen actividad agonista del receptor 5-ht4 | |
JP2010505931A (ja) | 複合薬剤 | |
JP2008533142A (ja) | α7ニューロンニコチン性受容体リガンドおよび抗精神病薬組成物 | |
AU2017220738A1 (en) | Carboxamide derivatives useful as RSK inhibitors | |
SG158863A1 (en) | Intravenous formulations of pde-5 inhibitors | |
BRPI0612076A2 (pt) | modulação sinergìstica de flt3 cinase empregando-se moduladores de aminopirimidinas cinase | |
KR20160047521A (ko) | 세포 증식성 질환의 치료를 위한 alk 억제제 및 cdk 억제제의 조합물 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
ND4A | Extension of term of a eurasian patent | ||
PD4A | Registration of transfer of a eurasian patent in accordance with the succession in title | ||
PD4A | Registration of transfer of a eurasian patent in accordance with the succession in title | ||
TC4A | Change in name of a patent proprietor in a eurasian patent |