EA201490859A1 - Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона - Google Patents

Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона

Info

Publication number
EA201490859A1
EA201490859A1 EA201490859A EA201490859A EA201490859A1 EA 201490859 A1 EA201490859 A1 EA 201490859A1 EA 201490859 A EA201490859 A EA 201490859A EA 201490859 A EA201490859 A EA 201490859A EA 201490859 A1 EA201490859 A1 EA 201490859A1
Authority
EA
Eurasian Patent Office
Prior art keywords
thyrosinkinase
bluton
inhibitors
piperazine compounds
alkylated piperazine
Prior art date
Application number
EA201490859A
Other languages
English (en)
Other versions
EA027561B1 (ru
Inventor
Джеймс Джон Кроуфорд
Венди Б. Янг
Original Assignee
Ф.Хоффманн-Ля Рош Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ф.Хоффманн-Ля Рош Аг filed Critical Ф.Хоффманн-Ля Рош Аг
Publication of EA201490859A1 publication Critical patent/EA201490859A1/ru
Publication of EA027561B1 publication Critical patent/EA027561B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • 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
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

Предложены алкилированные соединения пиперазина формулы I, включая их стереоизомеры, таутомеры и фармацевтически приемлемые соли, используемые для ингибирования киназы Btk и для лечения иммунных расстройств, таких как воспаление, опосредованное киназой Btk. Раскрыты способы применения соединений формулы I для диагностики in vitro, in situи in vivoи для лечения таких расстройств в клетках млекопитающих или связанных с ними патологических состояний.
EA201490859A 2011-11-03 2012-11-02 Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона EA027561B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161555395P 2011-11-03 2011-11-03
PCT/US2012/063198 WO2013067277A1 (en) 2011-11-03 2012-11-02 Alkylated piperazine compounds as inhibitors of btk activity

Publications (2)

Publication Number Publication Date
EA201490859A1 true EA201490859A1 (ru) 2014-09-30
EA027561B1 EA027561B1 (ru) 2017-08-31

Family

ID=47146780

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201490859A EA027561B1 (ru) 2011-11-03 2012-11-02 Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона

Country Status (22)

Country Link
US (3) US8729072B2 (ru)
EP (1) EP2773639B1 (ru)
JP (2) JP5976828B2 (ru)
KR (1) KR101716011B1 (ru)
CN (1) CN104024255B (ru)
AR (1) AR088642A1 (ru)
AU (1) AU2012332368A1 (ru)
BR (1) BR112014010439A2 (ru)
CA (1) CA2853970A1 (ru)
CL (1) CL2014001158A1 (ru)
CO (1) CO6950475A2 (ru)
CR (1) CR20140187A (ru)
EA (1) EA027561B1 (ru)
IL (1) IL232280A0 (ru)
IN (1) IN2014CN03265A (ru)
MA (1) MA35725B1 (ru)
MX (1) MX2014005289A (ru)
PE (1) PE20141686A1 (ru)
SG (1) SG11201401993RA (ru)
TW (1) TW201326171A (ru)
WO (1) WO2013067277A1 (ru)
ZA (1) ZA201403158B (ru)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013021374A2 (en) 2011-08-05 2013-02-14 Mitraltech Ltd. Techniques for percutaneous mitral valve replacement and sealing
UA111756C2 (uk) * 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
JP5976828B2 (ja) * 2011-11-03 2016-08-24 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｂｔｋ活性阻害剤としてのアルキル化ピペラジン化合物
KR101815360B1 (ko) 2013-07-03 2018-01-04 에프. 호프만-라 로슈 아게 헤테로아릴 피리돈 및 아자-피리돈 아마이드 화합물
EP3077384B1 (en) 2013-12-05 2017-09-06 F. Hoffmann-La Roche AG Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality
JP6879740B2 (ja) 2013-12-13 2021-06-02 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
AU2014361800B2 (en) 2013-12-13 2020-05-07 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
WO2015151006A1 (en) 2014-03-29 2015-10-08 Lupin Limited Substituted purine compounds as btk inhibitors
AU2015240465B2 (en) 2014-04-04 2020-02-27 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
WO2015170266A1 (en) 2014-05-07 2015-11-12 Lupin Limited Substituted pyrimidine compounds as btk inhibitors
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
WO2016065138A1 (en) 2014-10-22 2016-04-28 Dana-Farber Cancer Institute, Inc. Thiazolyl-containing compounds for treating proliferative diseases
JP6368043B2 (ja) 2014-10-27 2018-08-01 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 三環式ラクタム化合物の製造法
CN105837576B (zh) 2015-01-14 2019-03-26 湖北生物医药产业技术研究院有限公司 Btk抑制剂
ES2907988T3 (es) * 2015-03-10 2022-04-27 Aurigene Discovery Tech Ltd Compuestos de 1,2,4-oxadiazol y tiadiazol como inmunomoduladores
EP4049660A1 (en) 2016-02-29 2022-08-31 F. Hoffmann-La Roche AG Dosage form compositions comprising an inhibitor of bruton's tyrosine kinase
JP2020511462A (ja) 2016-12-03 2020-04-16 ジュノー セラピューティクス インコーポレイテッド キナーゼ阻害剤との組み合わせで治療用ｔ細胞を使用するための方法および組成物
TWI766176B (zh) * 2016-12-15 2022-06-01 瑞士商赫孚孟拉羅股份公司 製備btk抑制劑之方法
CN107445981B (zh) * 2017-08-25 2018-06-22 牡丹江医学院 一种用于防治***的活性化合物
CN113939292A (zh) 2019-02-25 2022-01-14 广州麓鹏制药有限公司 Btk及其突变体的抑制剂
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
US20220363689A1 (en) 2019-10-05 2022-11-17 Newave Pharmaceutical Inc. Inhibitor of btk and mutants thereof
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
EP4107154A4 (en) 2020-02-20 2024-02-28 Hutchison Medipharma Ltd HETEROARYL HETEROCYCLIC COMPOUNDS AND THEIR USES
CN115715291A (zh) * 2020-06-18 2023-02-24 上海华汇拓医药科技有限公司 布鲁顿酪氨酸激酶抑制剂及其制备方法
IL301275A (en) 2020-09-21 2023-05-01 Hutchison Medipharma Ltd Heterocyclic heteroaryl compounds and their uses
US20230382900A1 (en) 2020-10-30 2023-11-30 Newave Pharmaceutical Inc. Inhibitors of btk
US20240058457A1 (en) 2020-12-20 2024-02-22 Newave Pharmaceutical Inc. Btk degrader
WO2023143491A1 (zh) * 2022-01-28 2023-08-03 和记黄埔医药（上海）有限公司 7,8-二氢-2h-环戊二烯并吡咯并吡嗪酮化合物的合成方法

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US5583024A (en) 1985-12-02 1996-12-10 The Regents Of The University Of California Recombinant expression of Coleoptera luciferase
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
JPH08336393A (ja) 1995-04-13 1996-12-24 Mitsubishi Chem Corp 光学活性なγ−置換−β−ヒドロキシ酪酸エステルの製造法
US6602677B1 (en) 1997-09-19 2003-08-05 Promega Corporation Thermostable luciferases and methods of production
CA2453113A1 (en) 2001-07-12 2003-01-23 Avecia Limited Microencapsulated catalyst, methods of preparation and methods of use thereof
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
WO2005005429A1 (en) 2003-06-30 2005-01-20 Cellular Genomics, Inc. Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-ylamines and methods of inhibition of bruton’s tyrosine kinase by such compounds
CA2587192A1 (en) 2004-11-10 2006-05-18 Cgi Pharmaceuticals, Inc. Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity
KR101357524B1 (ko) 2005-03-10 2014-02-03 질레드 코네티컷 인코포레이티드 특정 치환된 아미드, 그의 제조 방법, 및 사용 방법
AU2006302415B2 (en) 2005-10-07 2012-09-13 Exelixis, Inc. Azetidines as MEK inhibitors for the treatment of proliferative diseases
AR063946A1 (es) 2006-09-11 2009-03-04 Cgi Pharmaceuticals Inc Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
PE20080839A1 (es) 2006-09-11 2008-08-23 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas
US7838523B2 (en) 2006-09-11 2010-11-23 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
CL2008002793A1 (es) * 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
US8426441B2 (en) 2007-12-14 2013-04-23 Roche Palo Alto Llc Inhibitors of bruton's tyrosine kinase
US7683064B2 (en) 2008-02-05 2010-03-23 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
AU2009244291B2 (en) 2008-05-06 2014-02-13 Genentech, Inc. Substituted amides, method of making, and use as Btk inhibitors
EP2297142B1 (en) 2008-06-24 2015-10-14 F. Hoffmann-La Roche AG Novel substituted pyridin-2-ones and pyridazin-3-ones
RU2507202C2 (ru) * 2008-07-02 2014-02-20 Ф.Хоффманн-Ля Рош Аг Новые фенилпиразиноны в качестве ингибиторов киназы
JP5318952B2 (ja) 2008-07-15 2013-10-16 エフ．ホフマン−ラ ロシュ アーゲー 新規なフェニル−イミダゾピリジン類及びピリダジン類
US8598174B2 (en) 2008-11-12 2013-12-03 Genetech, Inc. Pyridazinones, method of making, and method of use thereof
US8299077B2 (en) * 2009-03-02 2012-10-30 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
SG175287A1 (en) 2009-04-24 2011-11-28 Hoffmann La Roche Inhibitors of bruton's tyrosine kinase
WO2010126960A1 (en) * 2009-04-29 2010-11-04 Locus Pharmaceuticals, Inc. Pyrrolotriazine compounds
DK2473049T3 (en) * 2009-09-04 2019-04-01 Biogen Ma Inc INHIBITORS OF BRUTON'S TYROSINKINASE
CA3034600C (en) 2010-05-07 2020-11-10 Genentech, Inc. Pyridone and aza-pyridone compounds and methods of use
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
US9249123B2 (en) 2010-09-01 2016-02-02 Genentech, Inc. Pyridinones/pyrazinones, method of making, and method of use thereof
JP5842004B2 (ja) 2010-09-01 2016-01-13 ジーアイリード コネチカット インコーポレーテッドＧｉｌｅａｄ Ｃｏｎｎｅｃｔｉｃｕｔ，Ｉｎｃ． ピリダジノン、その製造方法及びその使用方法
KR101585753B1 (ko) 2011-05-17 2016-01-14 에프. 호프만-라 로슈 아게 브루톤 티로신 키나아제의 억제제
PE20140865A1 (es) 2011-08-17 2014-07-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
JP5976828B2 (ja) * 2011-11-03 2016-08-24 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｂｔｋ活性阻害剤としてのアルキル化ピペラジン化合物
UA111756C2 (uk) * 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона

Also Published As

Publication number Publication date
JP2014532763A (ja) 2014-12-08
SG11201401993RA (en) 2014-05-29
EA027561B1 (ru) 2017-08-31
TW201326171A (zh) 2013-07-01
MX2014005289A (es) 2014-05-30
US20140221365A1 (en) 2014-08-07
EP2773639A1 (en) 2014-09-10
US8946213B2 (en) 2015-02-03
US9115152B2 (en) 2015-08-25
MA35725B1 (fr) 2014-12-01
CA2853970A1 (en) 2013-05-10
JP2016028045A (ja) 2016-02-25
IN2014CN03265A (ru) 2015-07-03
AR088642A1 (es) 2014-06-25
KR20140090227A (ko) 2014-07-16
US8729072B2 (en) 2014-05-20
ZA201403158B (en) 2017-09-27
CN104024255A (zh) 2014-09-03
CL2014001158A1 (es) 2014-09-12
PE20141686A1 (es) 2014-11-08
IL232280A0 (en) 2014-06-30
CO6950475A2 (es) 2014-05-20
CN104024255B (zh) 2017-01-18
JP5976828B2 (ja) 2016-08-24
BR112014010439A2 (pt) 2017-04-18
KR101716011B1 (ko) 2017-03-13
AU2012332368A1 (en) 2014-05-22
WO2013067277A1 (en) 2013-05-10
US20150094302A1 (en) 2015-04-02
US20130116245A1 (en) 2013-05-09
EP2773639B1 (en) 2017-04-26
CR20140187A (es) 2014-06-20

Similar Documents

Publication Publication Date Title
EA201490859A1 (ru) Алкилированные соединения пиперазина в качестве ингибиторов тирозинкиназы брутона
MX2014005285A (es) Compuestos biciclicos de piperazina.
TR201909849T4 (tr) Btk etkinliği inhibitörleri olarak heteroaril piridon ve aza-piridon bileşikleri.
MX2014005282A (es) Compuestos de 8-fluoroftalazin-1 (2h) -ona.
MY160349A (en) Pyridone and aza-pyridone compounds and methods of use
EA201390879A1 (ru) Трициклические ингибиторы pi3k и способы их применения
MX2014014828A (es) Compuestos de 5-azaindazol y metodos de uso.
BR112013020329A2 (pt) compostos heterocíclicos como inibidores da pi3-quinase
EA201590624A1 (ru) Циклические эфиры пиразол-4-ил-гетероциклил-карбоксамидных соединений и способы их применения
MX2015018038A (es) Compuestos de heteroaril-piridona y aza-piridona-amida.
MX2016007171A (es) Compuestos de heteroaril piridona y azapiridona con funcionalidad electrofila.
MX340013B (es) Compuestos de benzoxazepina selectivos para fosfatidilinositol 3-cinasa (pi3k) p110 delta y metodos de uso.
EA201290957A1 (ru) Пиразол-4-илгетероциклилкарбоксамидные соединения и способы их применения
MX355852B (es) Compuestos de pirazolo [3,4-c] piridina y métodos de uso.
PH12014501947A1 (en) Serine/threonine kinase inhibitors
UA111933C2 (uk) Піролопіридини як інгібітори кінази
CR11757A (es) Compuestos de triazina como inhibidores mtor y quinasa pi3
CR11690A (es) Pirazolo (3,4-b) piridinas como inhibidores de raf
ECSP10010510A (es) Compuestos del inhibidor de raf y métodos de uso de los mismos
MX370906B (es) Inhibidores de serina/treonina cinasa.
EA201301301A1 (ru) Производные тиазола
SG178899A1 (en) Raf inhibitor compounds and methods of use thereof
MX361157B (es) Compuestos inhibidores de pi3k de dioxino- y oxazin-[2,3-d]pirimid ina y métodos de uso.
MX2017000544A (es) Compuestos de quinoxalina, metodo para preparar los mismos y uso de los mismos.
NZ620928A (en) Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU