AU2012311504B2 - Pyrazolo[4,3-C]pyridine derivatives as kinase inhibitors - Google Patents

Pyrazolo[4,3-C]pyridine derivatives as kinase inhibitors Download PDF

Info

Publication number
AU2012311504B2
AU2012311504B2 AU2012311504A AU2012311504A AU2012311504B2 AU 2012311504 B2 AU2012311504 B2 AU 2012311504B2 AU 2012311504 A AU2012311504 A AU 2012311504A AU 2012311504 A AU2012311504 A AU 2012311504A AU 2012311504 B2 AU2012311504 B2 AU 2012311504B2
Authority
AU
Australia
Prior art keywords
alkyl
alkynyl
alkenyl
methyl
optionally substituted
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
AU2012311504A
Other languages
English (en)
Other versions
AU2012311504A1 (en
Inventor
Claudio Dagostin
Nigel Ramsden
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cellzome Ltd
Original Assignee
Cellzome Ltd
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 Cellzome Ltd filed Critical Cellzome Ltd
Publication of AU2012311504A1 publication Critical patent/AU2012311504A1/en
Application granted granted Critical
Publication of AU2012311504B2 publication Critical patent/AU2012311504B2/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2012311504A 2011-09-20 2012-09-20 Pyrazolo[4,3-C]pyridine derivatives as kinase inhibitors Expired - Fee Related AU2012311504B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11182020 2011-09-20
EP11182020.5 2011-09-20
PCT/EP2012/068504 WO2013041605A1 (en) 2011-09-20 2012-09-20 Pyrazolo[4,3-c]pyridine derivatives as kinase inhibitors

Publications (2)

Publication Number Publication Date
AU2012311504A1 AU2012311504A1 (en) 2014-04-10
AU2012311504B2 true AU2012311504B2 (en) 2016-03-24

Family

ID=46924422

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012311504A Expired - Fee Related AU2012311504B2 (en) 2011-09-20 2012-09-20 Pyrazolo[4,3-C]pyridine derivatives as kinase inhibitors

Country Status (9)

Country Link
US (1) US20140323504A1 (enExample)
EP (1) EP2760863A1 (enExample)
JP (1) JP2014531449A (enExample)
KR (1) KR20140063700A (enExample)
CN (1) CN103874699A (enExample)
AU (1) AU2012311504B2 (enExample)
CA (1) CA2849340A1 (enExample)
RU (1) RU2014115476A (enExample)
WO (1) WO2013041605A1 (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2758402B9 (en) * 2011-09-22 2016-09-14 Pfizer Inc Pyrrolopyrimidine and purine derivatives
WO2014022569A1 (en) * 2012-08-03 2014-02-06 Principia Biopharma Inc. Treatment of dry eye
SI2892900T1 (en) 2012-09-10 2018-01-31 Principia Biopharma Inc. Pyrazolopyrimidine compounds as kinase inhibitors
RS58361B1 (sr) * 2013-07-31 2019-03-29 Merck Patent Gmbh Piridini, pirimidini i pirazini, kao inhibitori btk i njihova upotreba
WO2015038417A1 (en) * 2013-09-10 2015-03-19 Asana Biosciences, Llc Compounds for regulating fak and/or src pathways
CN112353806A (zh) 2014-02-21 2021-02-12 普林斯匹亚生物制药公司 Btk抑制剂的盐和固体形式
SG11201704808VA (en) 2014-12-18 2017-07-28 Principia Biopharma Inc Treatment of pemphigus
WO2016210165A1 (en) 2015-06-24 2016-12-29 Principia Biopharma Inc. Tyrosine kinase inhibitors
CN106831779B (zh) * 2015-11-28 2019-07-19 南昌弘益药业有限公司 一类jak激酶抑制剂的新化合物
CN115054586B (zh) 2016-06-29 2024-08-02 普林斯匹亚生物制药公司 改性的释放制剂
WO2018011681A1 (en) 2016-07-14 2018-01-18 Pfizer Inc. Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
CN110885331B (zh) * 2018-09-11 2021-07-09 中国药科大学 一种6-氨基-1H-吡唑并[3，4-d]嘧啶类JAK激酶抑制剂的制备与应用
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
CA3139277A1 (en) * 2019-05-08 2020-11-12 Vimalan Biosciences, Inc. Jak inhibitors
TWI899080B (zh) * 2019-05-27 2025-10-01 大陸商迪哲（江蘇）醫藥股份有限公司 Ｄｎａ依賴性蛋白激酶抑制劑
US20210106584A1 (en) 2019-10-14 2021-04-15 Principia Biopharma Inc. Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
US11697648B2 (en) 2019-11-26 2023-07-11 Theravance Biopharma R&D Ip, Llc Fused pyrimidine pyridinone compounds as JAK inhibitors
WO2021147953A1 (zh) * 2020-01-21 2021-07-29 江苏先声药业有限公司 嘧啶并五元环类衍生物及其应用
US11814390B2 (en) 2020-01-22 2023-11-14 Principia Biopharma Inc. Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1H-pyrazolo[3,4-D]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
WO2022237844A1 (zh) * 2021-05-12 2022-11-17 微境生物医药科技(上海)有限公司 含吡嗪结构的吡咯并嘧啶衍生物
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010129053A2 (en) * 2009-05-05 2010-11-11 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
WO2011048082A1 (en) * 2009-10-20 2011-04-28 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2280930C (en) 1997-02-12 2010-04-06 The Regents Of The University Of Michigan Protein markers for lung cancer and use thereof
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
PT1154774E (pt) 1999-02-10 2005-10-31 Astrazeneca Ab Derivados de quinazolina como inibidores de angiogenese
KR100881105B1 (ko) 1999-11-05 2009-02-02 아스트라제네카 아베 Ｖｅｇｆ 억제제로서의 퀴나졸린 유도체
DE60037345T2 (de) 1999-12-10 2008-11-13 Pfizer Products Inc., Groton Pyrrolo(2,3-d)pyrimidin-Verbindungen
JP3663382B2 (ja) 2000-02-15 2005-06-22 スージェン・インコーポレーテッド ピロール置換２−インドリノン蛋白質キナーゼ阻害剤
CN1918158B (zh) * 2004-02-14 2011-03-02 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
GB0427604D0 (en) 2004-12-16 2005-01-19 Novartis Ag Organic compounds
PL1891446T3 (pl) 2005-06-14 2013-08-30 Cellzome Gmbh Sposób identyfikacji nowych związków oddziałujących z enzymami
GB0605691D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
ES2318616T3 (es) 2006-06-01 2009-05-01 Cellzome Ag Metodos para la identificacion de moleculas que interactuan con zap-70 y para la purificacion de zap-70.
WO2008009458A1 (en) 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
BRPI0622030A2 (pt) 2006-11-16 2014-04-22 Pharmacopeia Llc Derivados de purina 7-substituída, para imunossupressão
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US20090274698A1 (en) 2007-07-06 2009-11-05 Shripad Bhagwat Combination anti-cancer therapy
PE20091485A1 (es) 2008-02-06 2009-10-26 Novartis Ag DERIVADOS DE PIRROLO-[2,3-d]-PIRIMIDINA COMO INHIBIDORES DE CINASAS
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
GB0903759D0 (en) 2009-03-04 2009-04-15 Medical Res Council Compound
CA2758614A1 (en) 2009-04-14 2010-10-21 Cellzome Limited Fluoro substituted pyrimidine compounds as jak3 inhibitors
US8846673B2 (en) 2009-08-11 2014-09-30 Bristol-Myers Squibb Company Azaindazoles as kinase inhibitors and use thereof
US9040545B2 (en) 2010-08-20 2015-05-26 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as selective JAK inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010129053A2 (en) * 2009-05-05 2010-11-11 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
WO2011048082A1 (en) * 2009-10-20 2011-04-28 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors

Also Published As

Publication number Publication date
US20140323504A1 (en) 2014-10-30
WO2013041605A1 (en) 2013-03-28
CN103874699A (zh) 2014-06-18
AU2012311504A1 (en) 2014-04-10
CA2849340A1 (en) 2013-03-28
KR20140063700A (ko) 2014-05-27
RU2014115476A (ru) 2015-10-27
JP2014531449A (ja) 2014-11-27
EP2760863A1 (en) 2014-08-06

Similar Documents

Publication Publication Date Title
AU2012311504B2 (en) Pyrazolo[4,3-C]pyridine derivatives as kinase inhibitors
KR101864589B1 (ko) 특정한 단백질 키나아제 억제제
WO2013017480A1 (en) Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
KR20140047092A (ko) Jak 억제제로서의 헤테로시클릴 피리미딘 유사체
AU2018300218B2 (en) ASK1 inhibiting pyrrolopyrimidine and pyrrolopyridine derivatives
WO2013085802A1 (en) Pyrrolopyrimidines as janus kinase inhibitors
CA2797772A1 (en) Pyrazole compounds as jak inhibitors
CA2860095A1 (en) Pyrimidine-2,4-diamine derivatives as kinase inhibitors
TW202411229A (zh) 用於治療發炎性病症之新穎化合物及其醫藥組合物
US20160083376A1 (en) Certain protein kinase inhibitors
JP2013534233A (ja) 選択的ｊａｋ阻害剤としてのヘテロシクリルピラゾロピリミジン類似体
US20140296234A1 (en) Pyrimidine derivatives as mtor inhibitors
JP2014510122A (ja) ｍＴＯＲ阻害剤としてのジヒドロピロロピリミジン誘導体
WO2012143320A1 (en) (7h-pyrrolo[2,3-d]pyrimidin-2-yl)amine compounds as jak3 inhibitors
CN120858100A (zh) 抑制性化合物
JP2015504914A (ja) Ｍｔｏｒ阻害剤としてのピリミドオキサゾシン誘導体
WO2013017479A1 (en) Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
CN116249696B (zh) 嘧啶酮类化合物及其用途
HK40091563B (zh) 嘧啶酮类化合物及其用途
HK40091563A (zh) 嘧啶酮类化合物及其用途

Legal Events

Date Code Title Description
MK25 Application lapsed reg. 22.2i(2) - failure to pay acceptance fee