HK1161529A1 - Pyrazolopyrimidine jak inhibitor compounds and methods jak - Google Patents

Pyrazolopyrimidine jak inhibitor compounds and methods jak

Info

Publication number
HK1161529A1
HK1161529A1 HK12101703.2A HK12101703A HK1161529A1 HK 1161529 A1 HK1161529 A1 HK 1161529A1 HK 12101703 A HK12101703 A HK 12101703A HK 1161529 A1 HK1161529 A1 HK 1161529A1
Authority
HK
Hong Kong
Prior art keywords
jak
methods
pyrazolopyrimidine
inhibitor compounds
jak inhibitor
Prior art date
Application number
HK12101703.2A
Other languages
English (en)
Chinese (zh)
Inventor
Jeffrey Blaney
Paul A Gibbons
Emily Hanan
Joseph P Lyssikatos
Steven R Magnuson
Richard Pastor
Thomas E Rawson
Aihe Zhou
Bing-Yan Zhu
Original Assignee
健泰科生物技術公司
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42129330&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HK1161529(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 健泰科生物技術公司 filed Critical 健泰科生物技術公司
Publication of HK1161529A1 publication Critical patent/HK1161529A1/xx

Links

Classifications

    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • 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
    • 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
    • A61P17/06—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
    • 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
    • A61P25/28—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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
HK12101703.2A 2008-10-31 2012-02-21 Pyrazolopyrimidine jak inhibitor compounds and methods jak HK1161529A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11049708P 2008-10-31 2008-10-31
PCT/US2009/063014 WO2010051549A1 (fr) 2008-10-31 2009-11-02 Composés inhibiteurs de jak à la pyrazolopyrimidine et procédés

Publications (1)

Publication Number Publication Date
HK1161529A1 true HK1161529A1 (en) 2012-07-27

Family

ID=42129330

Family Applications (1)

Application Number Title Priority Date Filing Date
HK12101703.2A HK1161529A1 (en) 2008-10-31 2012-02-21 Pyrazolopyrimidine jak inhibitor compounds and methods jak

Country Status (20)

Country Link
US (3) US8637526B2 (fr)
EP (2) EP2348860B1 (fr)
JP (1) JP5769199B2 (fr)
KR (1) KR101686685B1 (fr)
CN (1) CN102271515B (fr)
AU (1) AU2009308675A1 (fr)
BR (1) BRPI0914404A2 (fr)
CA (1) CA2740792C (fr)
CL (1) CL2011000973A1 (fr)
CO (1) CO6361856A2 (fr)
CR (1) CR20110224A (fr)
EC (1) ECSP11011014A (fr)
ES (1) ES2545541T3 (fr)
HK (1) HK1161529A1 (fr)
IL (1) IL212085A0 (fr)
MX (1) MX2011004494A (fr)
PE (2) PE20110828A1 (fr)
RU (1) RU2539568C2 (fr)
SG (1) SG194397A1 (fr)
WO (1) WO2010051549A1 (fr)

Families Citing this family (89)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS53350B (en) 2008-09-22 2014-10-31 Array Biopharma, Inc. SUBSTITUTED COMPOUNDS OF IMIDASO [1,2-B] PYRIDASINE AS INK KINASE INHIBITORS
SI3372605T1 (sl) 2008-10-22 2022-03-31 Array Biopharma, Inc. Substituirane pirazolo(1,5-a)pirimidinske spojine kot zaviralci TRK-kinaze
UA110324C2 (en) * 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
ES2557316T3 (es) 2009-09-08 2016-01-25 F. Hoffmann-La Roche Ag Compuestos de piridín-3-il-carboxamida 4-sustituidos y métodos de utilización
EP3521291A1 (fr) 2010-05-20 2019-08-07 Array Biopharma, Inc. Composés macrocycliques comme inhibiteurs de la kinase trk
RU2604062C2 (ru) * 2010-07-13 2016-12-10 Ф.Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ПИРАЗОЛО[1,5-a]ПИРИМИДИНА И ТИЕНО[3,2-b]ПИРИМИДИНА В КАЧЕСТВЕ МОДУЛЯТОРОВ IRAK-4
SG186199A1 (en) 2010-07-29 2013-01-30 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
US9169260B2 (en) 2011-03-22 2015-10-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
WO2012178125A1 (fr) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Composés inhibiteurs de la kinase atr
LT3418281T (lt) 2012-12-07 2021-01-11 Vertex Pharmaceuticals Inc. Pirazolo[1,5-a]pirimidinai, naudotini kaip atr kinazės inhibitoriai, skirti vėžinių ligų gydymui
US20160123982A1 (en) 2013-02-04 2016-05-05 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2970289A1 (fr) * 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Composés utiles en tant qu'inhibiteurs de la kinase atr
EP2970288A1 (fr) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Composés utiles en tant qu'inhibiteurs de la kinase atr
BR112015024638A2 (pt) * 2013-03-28 2017-07-18 Takeda Pharmaceuticals Co composto, medicamento, métodos para inibir a janus cinase em um mamífero e para profilaxia ou tratamento de doença, e, uso do composto ou sal
ES2619125T3 (es) 2013-04-25 2017-06-23 Beigene, Ltd. Compuestos heterocíclicos fusionados como inhibidores de proteína cinasa
HRP20221262T1 (hr) 2013-09-13 2022-12-09 Beigene Switzerland Gmbh Protutijela anti-pd1 i njihova uporaba kao terapeutskih i dijagnostičkih sredstava
CN103539753B (zh) * 2013-10-22 2017-06-23 上海药明康德新药开发有限公司 一种3‑取代‑4‑异恶唑羧酸的合成方法
WO2015073267A1 (fr) * 2013-11-15 2015-05-21 Calitor Sciences, Llc Composés hétéroaryle substitués et méthodes d'utilisation
CN104650092B (zh) * 2013-11-16 2017-11-10 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
KR102153886B1 (ko) 2013-12-06 2020-09-09 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제 억제제로서 유용한 2-아미노-6-플루오로-n-[5-플루오로-피리딘-3-일]피라졸로[1,5-a]피리미딘-3-카복스아미드 화합물, 이의 제조 방법, 이의 상이한 고체형 및 방사성표지된 유도체
FI3636649T3 (fi) 2014-01-24 2024-05-02 Turning Point Therapeutics Inc Diaryylimakrosyklejä proteiinikinaasien modulaattoreina
PE20211782A1 (es) * 2014-05-23 2021-09-08 Hoffmann La Roche Compuestos de 5-cloro-2-difluorometoxifenil pirazolopirimidina, composiciones y metodos de uso de los mismos
PT3152212T (pt) 2014-06-05 2020-03-13 Vertex Pharma Derivados radiomarcados de um composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor de atr quinase, preparação do dito composto e diferentes formas sólidas do mesmo
RU2736219C2 (ru) 2014-06-17 2020-11-12 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации ингибиторов снк1 и atr
WO2016000619A1 (fr) 2014-07-03 2016-01-07 Beigene, Ltd. Anticorps anti-pd-l1 et leur utilisation comme agents thérapeutiques et diagnostiques
GB201414730D0 (en) 2014-08-19 2014-10-01 Tpp Global Dev Ltd Pharmaceutical compound
US20170333435A1 (en) 2014-11-06 2017-11-23 Lysosomal Therapeutics Inc. Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
EP3215509B1 (fr) 2014-11-06 2020-02-26 Lysosomal Therapeutics Inc. Pyrrolo[1,2-a]pyrimidines substituées et leur utilisation dans le traitement de troubles médicaux
FI3215511T3 (fi) * 2014-11-06 2024-05-16 Bial R&D Invest S A Substituoituja pyratsolo(1,5-a)pyrimidiinejä ja niiden käyttö lääketieteellisten häiriöiden hoitamisessa
MX2017006412A (es) 2014-11-16 2017-09-12 Array Biopharma Inc Forma cristalina de sulfato acido de (s)-n-(5-((r)-2-(2,5-difluoro fenil)-pirrolidin-1-il)-pirazolo[1,5-a]-pirimidin-3-il)-3-hidroxi pirrolidina-1-carboxamida.
JP6609631B2 (ja) * 2014-12-15 2019-11-20 シーエムジー ファーマシューティカル カンパニー，リミテッド 縮合環ヘテロアリール化合物及びｔｒｋ抑制剤としての用途
US10155765B2 (en) 2015-03-12 2018-12-18 Merck Sharp & Dohme Corp. Carboxamide inhibitors of IRAK4 activity
WO2016144846A1 (fr) * 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Inhibiteurs de l'activité d'irak4 à base de pyrazolopyrimidine
US10316044B2 (en) * 2015-07-02 2019-06-11 Tp Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
BR112018000297A2 (pt) 2015-07-06 2018-09-04 Tp Therapeutics Inc polimorfo de macrociclo de diarila
RU2728579C2 (ru) 2015-07-21 2020-07-30 Тёрнинг Поинт Терапьютикс, Инк. Хиральные диарильные макроциклы и их применение
KR20180054657A (ko) 2015-09-30 2018-05-24 버텍스 파마슈티칼스 인코포레이티드 Dna 손상제 및 atr 저해제의 병용물을 사용한 암 치료 방법
EP3156405A1 (fr) * 2015-10-13 2017-04-19 Boehringer Ingelheim International GmbH Dérivés d'éther spirocycliques de pyrazolo [1,5-a] pyrimidine-3-carboxamide
JP2018534296A (ja) 2015-10-26 2018-11-22 ロクソ オンコロジー， インコーポレイテッドＬｏｘｏ Ｏｎｃｏｌｏｇｙ， Ｉｎｃ． Ｔｒｋ阻害薬耐性がんにおける点変異およびそれに関連する方法
TW201720828A (zh) * 2015-11-23 2017-06-16 赫孚孟拉羅股份公司 治療性化合物及組合物以及其使用方法
CN105503730B (zh) * 2015-12-25 2018-06-22 山东大学 吡唑类衍生物及其制备方法与应用
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
MX2018012163A (es) 2016-04-04 2019-07-08 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirr olidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina- 1-carboxamida.
MX2018012208A (es) 2016-04-06 2019-03-28 Lysosomal Therapeutics Inc Compuestos a base de imidazo [1,5-a] pirimidinil carboxamida y su uso en el tratamiento de trastornos médicos.
EP3440080A4 (fr) 2016-04-06 2020-01-22 Lysosomal Therapeutics Inc. Composés de pyrazolo[1,5-a]pyrimidinyl carboxamide et leur utilisation dans le traitement de troubles médicaux
EP3440081A4 (fr) 2016-04-06 2019-09-18 Lysosomal Therapeutics Inc. Composés pyrrolo[1,2-a]pyrimidinyl carboxamide et leur utilisation dans le traitement de troubles médicaux
EP3452045A1 (fr) * 2016-05-04 2019-03-13 Lysosomal Therapeutics Inc. Méthodes de traitement et polythérapies faisant appel à des composés hétérobicycliques activateurs de gcase et autres composés apparentés
WO2017192931A1 (fr) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. Imidazo[1,2-a]pyridines substituées, imidazo[1,2-a]pyrazines substituées, composés apparentés et leur utilisation dans le traitement de troubles médicaux
US11168087B2 (en) 2016-05-05 2021-11-09 Bial—R&D Investments, S.A. Substituted imidazo[1,2-b]pyridazines, substituted imidazo[1,5-b]pyridazines, related compounds, and their use in the treatment of medical disorders
RS61463B1 (sr) 2016-05-18 2021-03-31 Loxo Oncology Inc Priprema (s)-n-(5-((r)-2-(2,5-difluorofenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3-il) -3-hidroksipirolidin-1-karboksamida
AU2017293423B2 (en) 2016-07-05 2023-05-25 Beigene, Ltd. Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer
EP3490564A4 (fr) 2016-07-28 2020-02-26 Turning Point Therapeutics, Inc. Inhibiteurs macrocycliques de kinases
CN116478166A (zh) 2016-08-16 2023-07-25 百济神州(苏州)生物科技有限公司 一种化合物的晶型、其制备和用途
EP3500299B1 (fr) 2016-08-19 2023-12-13 BeiGene Switzerland GmbH Combinaison de zanubrutinib avec un anticorps anti-cd20 ou anti-pd-1 pour l'utilisation dans le traitement du cancer
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
US11555038B2 (en) 2017-01-25 2023-01-17 Beigene, Ltd. Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
JP2020510061A (ja) * 2017-03-14 2020-04-02 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ピラゾロクロロフェニル化合物、組成物及びその使用方法
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
WO2018167283A1 (fr) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Procédés pour le diagnostic et le traitement d'un remodelage neuronal associé à un adénocarcinome canalaire pancréatique
WO2018189335A1 (fr) 2017-04-13 2018-10-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Procédés de diagnostic et de traitement d'un adénocarcinome canalaire pancréatique
PE20200341A1 (es) * 2017-05-22 2020-02-14 Hoffmann La Roche Composiciones y compuestos terapeuticos y metodos para utilizarlos
TW201900648A (zh) 2017-05-22 2019-01-01 瑞士商赫孚孟拉羅股份公司 治療性化合物及組成物以及其使用方法
CN110799543A (zh) 2017-06-26 2020-02-14 百济神州有限公司 肝细胞癌的免疫治疗
SG11202000714QA (en) 2017-07-28 2020-02-27 Nimbus Lakshmi Inc Tyk2 inhibitors and uses thereof
UA126158C2 (uk) 2017-07-28 2022-08-25 Тьорнінґ Поінт Терапьютикс, Інк. Макроциклічні сполуки і їх використання
US11377449B2 (en) 2017-08-12 2022-07-05 Beigene, Ltd. BTK inhibitors with improved dual selectivity
CN111801334B (zh) 2017-11-29 2023-06-09 百济神州瑞士有限责任公司 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤
PL3724191T3 (pl) 2017-12-15 2022-04-25 Pyramid Biosciences, Inc. Pochodne 5-(2-(2,5-difluorofenylo)pirolidyn-1-ylo)-3-(1h-pirazol-1-ilo)pirazolo[1,5-a]pirymidyny i pokrewne związki jako inhibitory kinaz trk do leczenia nowotworu
WO2019126121A1 (fr) 2017-12-19 2019-06-27 Tp Therapeutics, Inc. Composés macrocycliques pour le traitement de maladie
EP3849981B1 (fr) 2018-09-10 2023-02-01 Eli Lilly and Company Dérivés de pyrazolo[1,5-a]pyrimidine-3-carboxamide utiles dans le traitement du psoriasis et du lupus érythémateux disséminé
CN113271940A (zh) * 2018-10-15 2021-08-17 林伯士拉克许米公司 Tyk2抑制剂和其用途
CN109251205A (zh) * 2018-10-22 2019-01-22 上海凌凯医药科技有限公司 一种高效合成5-氯吡唑并[1,5-a]嘧啶的方法
WO2020092015A1 (fr) 2018-11-02 2020-05-07 University Of Rochester Atténuation thérapeutique d'une infection épithéliale
CN111217816B (zh) * 2018-11-27 2022-08-16 中国科学院上海药物研究所 一类flt3激酶抑制剂及其制备和应用
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
KR20220024405A (ko) * 2019-06-18 2022-03-03 에프. 호프만-라 로슈 아게 Jak 키나제의 피라졸로피리미딘 설폰 억제제 및 그 사용
EP3986899A1 (fr) 2019-06-18 2022-04-27 F. Hoffmann-La Roche AG Inhibiteurs éther-aryl-pyrazolopyrimidine de kinases jak et leurs utilisations
CN114026096A (zh) 2019-06-18 2022-02-08 豪夫迈·罗氏有限公司 四唑取代的吡唑并嘧啶类jak激酶抑制剂及其用途
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (fr) 2020-01-22 2021-07-29 Onxeo Nouvelle molécule dbait et son utilisation
TWI810520B (zh) 2020-02-12 2023-08-01 美商美國禮來大藥廠 7-(甲基胺基)吡唑并[1,5-a]嘧啶-3-甲醯胺化合物
CN113387831A (zh) * 2020-03-11 2021-09-14 苏州大学 酰胺类化合物及其在制备神经炎症抑制剂中的应用
CN113549073B (zh) * 2020-04-24 2022-07-12 成都先导药物开发股份有限公司 作为JAK抑制剂的吡唑并[1,5-a]嘧啶衍生物
WO2023057394A1 (fr) * 2021-10-04 2023-04-13 Forx Therapeutics Ag Dérivés de n,n-diméthyl-4-(7-(n-(1-méthylcyclopropyl)sulfamoyl)-imidazo[1,5-a]pyridin-5-yl)pipérazine-1-carboxamide et dérivés correspondants de pyrazolo[1,5-a]pyridine utilisés en tant qu'inhibiteurs de parg pour le traitement du cancer
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4187099A (en) 1977-11-16 1980-02-05 Monsanto Company 3-Aryl-4-isothiazolecarboxylic acid and 3-aryl-4-isoxazolecarboxylic acid derivatives and their use as herbicides
ES517193A0 (es) 1981-11-10 1983-12-01 Wellcome Found Un procedimiento para la preparacion de nuevos derivados de imidazo (4,5-c)piridina.
US4847256A (en) 1986-10-16 1989-07-11 American Cyanamid Company 4,5-dihydro and 4,5,6,7-tetrahydropyrazolo(1,5-A)-pyrimidines
US5728536A (en) 1993-07-29 1998-03-17 St. Jude Children's Research Hospital Jak kinases and regulation of Cytokine signal transduction
US6136595A (en) 1993-07-29 2000-10-24 St. Jude Children's Research Hospital Jak kinases and regulations of cytokine signal transduction
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
US5705625A (en) 1994-12-15 1998-01-06 The Johns Hopkins University School Of Medicine Nucleic Acid Encoding novel protein tyrosine kinase
US7070972B1 (en) 1995-01-13 2006-07-04 The United States Of America As Represented By The Department Of Health And Human Services Janus family kinases and identification of immune modulators
US7091020B1 (en) 1995-12-05 2006-08-15 Incyte Corporation Human Jak2 kinase
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
US6235741B1 (en) 1997-05-30 2001-05-22 Merck & Co., Inc. Angiogenesis inhibitors
FR2791562B1 (fr) 1999-03-29 2004-03-05 Oreal Composition tinctoriale contenant une pyrazolo-[1,5-a]- pyrimidine et une polyaminopyrimidine monocyclique a titre de bases d'oxydation et un coupleur, et procedes de teinture
KR100694684B1 (ko) 1999-07-02 2007-03-13 에자이 알앤드디 매니지먼트 가부시키가이샤 축합 이미다졸 화합물 및 당뇨병 치료약
PT1382339E (pt) 1999-12-10 2008-02-06 Pfizer Prod Inc Composições que contêm derivados de pirrolo[2,3-d]- pirimidina
CN100343255C (zh) 2002-04-23 2007-10-17 盐野义制药株式会社 吡唑并[1,5－a]嘧啶衍生物和含有该衍生物的NAD(P)H氧化酶抑制剂
US7161003B1 (en) 2002-09-04 2007-01-09 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
JP2006512313A (ja) 2002-10-31 2006-04-13 アムジェン インコーポレイテッド 抗炎症剤
AU2003299651A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. Tyrosine kinase inhibitors
WO2004089471A2 (fr) 2003-04-11 2004-10-21 Novo Nordisk A/S Utilisation pharmaceutique de pyrazolo[1,5-a]pyrimidines substituees
US20070270408A1 (en) 2003-04-11 2007-11-22 Novo Nordisk A/S Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines
WO2005004810A2 (fr) 2003-07-02 2005-01-20 Merck & Co., Inc. Derives arylsulfonamide
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
GB0329214D0 (en) 2003-12-17 2004-01-21 Glaxo Group Ltd Novel compounds
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
CA2563305A1 (fr) 2004-04-09 2005-11-24 University Of South Florida Polytherapies pour le cancer et des angiopathies proliferantes
WO2005105803A2 (fr) 2004-04-28 2005-11-10 Cv Therapeutics, Inc. Antagonistes du recepteur de l'adenosine a1
ES2299044T3 (es) * 2004-06-21 2008-05-16 F. Hoffmann-La Roche Ag Derivados de pirrazol-pirimidina.
EP1765825A1 (fr) 2004-06-25 2007-03-28 Amgen Inc. Triazols et indazols condenses convenant pour le traitement de maladies induites par les citokines et autres pathologies
JP5030229B2 (ja) * 2004-11-04 2012-09-19 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インヒビターとして有用なピラゾロ［１，５−ａ］ピリミジン
EP1910369A1 (fr) * 2005-07-29 2008-04-16 Astellas Pharma Inc. Hétérocycles fusionnés en tant qu inhibiteurs de lck
WO2007039797A1 (fr) 2005-10-03 2007-04-12 Pfizer Products Inc. Utilisation d'antagonistes du recepteur cannabinoide de type 1 pour traiter les inflammations et l'arthrite
CA2624500A1 (fr) 2005-10-06 2007-04-19 Schering Corporation Pyrazolopyrimidines en tant qu'inhibiteurs de la proteine kinase
CN101360499B (zh) * 2005-10-06 2015-10-07 默沙东公司 吡唑并[1,5-a]嘧啶衍生物在制备抑制蛋白激酶的药物中的用途
WO2007048064A2 (fr) 2005-10-21 2007-04-26 Exelixis, Inc. Aminopyrimidines en tant que modulateurs de caseine kinase ii (ck2)
RU2008127263A (ru) 2005-12-08 2010-01-20 Новартис АГ (CH) ПИРАЗОЛ [1,5-a] ПИРИДИН-3-КАРБОНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ EphB-И VEGFR2-КИНАЗЫ
US7274215B2 (en) * 2006-01-17 2007-09-25 M2000 Sa. Reconfigurable integrated circuits with scalable architecture including one or more adders
US8541406B2 (en) 2006-02-07 2013-09-24 Nv Remynd Thiadiazole derivatives for the treatment of neurodegenerative diseases
TW200800997A (en) 2006-03-22 2008-01-01 Astrazeneca Ab Chemical compounds
TWI419889B (zh) * 2006-07-05 2013-12-21 Mitsubishi Tanabe Pharma Corp 吡唑并〔１，５-ａ〕嘧啶化合物
AR061793A1 (es) * 2006-07-05 2008-09-24 Mitsubishi Tanabe Pharma Corp Compuesto de pirazolo[1,5-a] pirimidina y composicion farmaceutica
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
CN101522682A (zh) 2006-10-30 2009-09-02 诺瓦提斯公司 作为抗炎剂的杂环化合物
CA2670083A1 (fr) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Inhibiteurs de metalloprotease heterobicycliques
WO2009017954A1 (fr) 2007-08-01 2009-02-05 Phenomix Corporation Inhibiteurs de kinase jak2
WO2009047359A1 (fr) 2007-10-12 2009-04-16 Ingenium Pharmaceuticals Gmbh Inhibiteurs de protéine kinases
ES2734288T3 (es) 2007-11-28 2019-12-05 Dana Farber Cancer Inst Inc Inhibidores de miristato de moléculas pequeñas de Bcr-abl y métodos de uso
CA2709784A1 (fr) 2007-12-21 2009-07-09 University Of Rochester Procede permettant de modifier la duree de vie d'organismes eucaryotes
WO2010019762A1 (fr) 2008-08-13 2010-02-18 Jenrin Discovery Composés de purine en tant que bloqueurs de récepteur aux cannabinoïdes
WO2010063487A1 (fr) * 2008-12-05 2010-06-10 Merz Pharma Gmbh & Co. Kgaa Pyrazolopyrimidines, procédé pour leur préparation et leur utilisation comme médicament
CN102325765B (zh) 2009-02-06 2014-12-24 杨森制药公司 作为γ-分泌酶调节剂的取代的双环杂环化合物
TWI461425B (zh) 2009-02-19 2014-11-21 Janssen Pharmaceuticals Inc 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類
DE102009012264A1 (de) * 2009-03-11 2010-09-16 Uhde Gmbh Vorrichtung und Verfahren zur Dosierung oder Absperrung primärer Verbrennungsluft in den Primärheizraum von horizontalen Koksofenkammern
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
EP2491039A1 (fr) 2009-10-20 2012-08-29 Cellzome Limited Analogues d'hétérocyclyl pyrazolopyrimidine en tant qu'inhibiteurs de jak
KR20130001272A (ko) 2010-03-17 2013-01-03 에프. 호프만-라 로슈 아게 이미다조피리딘 및 푸린 화합물, 조성물 및 사용 방법
KR20130094693A (ko) 2010-04-30 2013-08-26 셀좀 리미티드 Ｊａｋ 저해제로서의 피라졸 화합물

Also Published As

Publication number Publication date
ES2545541T3 (es) 2015-09-11
EP2348860A1 (fr) 2011-08-03
US20120022043A1 (en) 2012-01-26
US8637526B2 (en) 2014-01-28
PE20131197A1 (es) 2013-11-06
KR20110079887A (ko) 2011-07-11
CA2740792A1 (fr) 2010-05-06
WO2010051549A1 (fr) 2010-05-06
CA2740792C (fr) 2016-06-21
IL212085A0 (en) 2011-06-30
SG194397A1 (en) 2013-11-29
EP2348860B1 (fr) 2015-05-27
CO6361856A2 (es) 2012-01-20
PE20110828A1 (es) 2011-11-22
CR20110224A (es) 2011-06-09
US20140107099A1 (en) 2014-04-17
RU2539568C2 (ru) 2015-01-20
ECSP11011014A (es) 2011-05-31
CL2011000973A1 (es) 2012-07-20
JP5769199B2 (ja) 2015-08-26
MX2011004494A (es) 2011-05-24
BRPI0914404A2 (pt) 2019-03-06
KR101686685B1 (ko) 2016-12-14
JP2012507569A (ja) 2012-03-29
CN102271515A (zh) 2011-12-07
US20160244456A1 (en) 2016-08-25
RU2011121876A (ru) 2012-12-20
EP2348860A4 (fr) 2012-10-24
CN102271515B (zh) 2014-07-02
EP2962566A1 (fr) 2016-01-06
AU2009308675A1 (en) 2010-05-06

Similar Documents

Publication Publication Date Title
HK1161529A1 (en) Pyrazolopyrimidine jak inhibitor compounds and methods jak
ZA201200490B (en) Pyrazolopyrimidine jak inhibitor compounds and methods
ZA201008957B (en) Triazolopyridine jak inhibitor compounds and methods
IL209764A0 (en) Triazolopyridine jak inhibitor compounds and methods
HRP20180718T1 (hr) Oligopeptidni spojevi i njihova upotreba
HK1172896A1 (zh) 化合物和使用方法
HK1161094A1 (en) Compounds and methods of use
GB0818241D0 (en) Compounds and their use
IL208081A0 (en) Amido - thiophene compounds and their use
ZA201007395B (en) Aryl-quinolyl compounds and their use
EP2344476A4 (fr) Inhibiteurs de jak à base de carbamates tricycliques
SI2344449T1 (sl) Aril-fenil-sulfonamido-cikloalkilne spojine in njihova uporaba
EP2379076A4 (fr) Inhibiteurs de la phosphodiestérase et utilisations de ces derniers
IL205308A0 (en) Compounds and methods
GB0801319D0 (en) Compounds and their use
GB0802195D0 (en) Compounds and their use II
GB0802194D0 (en) Compounds and their use
GB0813254D0 (en) Compounds and their use
GB0817897D0 (en) Compounds and their use
GB0805693D0 (en) Combinations of P13-delta and P13-gamma kinase inhibitor compounds

Legal Events

Date Code Title Description
PC Patent ceased (i.e. patent has lapsed due to the failure to pay the renewal fee)

Effective date: 20181031