EA201291038A1 - Соединения пиразола в качестве ингибиторов jak - Google Patents

Соединения пиразола в качестве ингибиторов jak

Info

Publication number
EA201291038A1
EA201291038A1 EA201291038A EA201291038A EA201291038A1 EA 201291038 A1 EA201291038 A1 EA 201291038A1 EA 201291038 A EA201291038 A EA 201291038A EA 201291038 A EA201291038 A EA 201291038A EA 201291038 A1 EA201291038 A1 EA 201291038A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
jak inhibitors
pyrazol compounds
relates
pyrazol
Prior art date
Application number
EA201291038A
Other languages
English (en)
Inventor
Ричард Джон Хэррисон
Сэлли Оксенфорд
Эндру Хобсон
Найджель Рэмсден
Воррэн Миллер
Original Assignee
Целльзом Лимитид
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 Целльзом Лимитид filed Critical Целльзом Лимитид
Publication of EA201291038A1 publication Critical patent/EA201291038A1/ru

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
    • A61K31/495—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
    • 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
    • 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

Abstract

Bзобретение относится к соединениям формулы (I)в которой R, R, R, Rимеют значения, указанные в описании и формуле изобретения. Указанные соединения пригодны в качестве ингибиторов JAK для лечения или профилактики иммунологических, воспалительных, аутоимунных, аллергических, а также иммунологически обусловленных заболеваний. Настоящее изобретение также относится к фармацевтическим композициям, включающим указанные соединения, к получению подобных соединений, а также к их применению в качестве лекарственных препаратов.
EA201291038A 2010-04-30 2011-04-18 Соединения пиразола в качестве ингибиторов jak EA201291038A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10161632 2010-04-30
PCT/EP2011/056158 WO2011134831A1 (en) 2010-04-30 2011-04-18 Pyrazole compounds as jak inhibitors

Publications (1)

Publication Number Publication Date
EA201291038A1 true EA201291038A1 (ru) 2013-05-30

Family

ID=42711762

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201291038A EA201291038A1 (ru) 2010-04-30 2011-04-18 Соединения пиразола в качестве ингибиторов jak

Country Status (12)

Country Link
US (1) US20130131043A1 (ru)
EP (1) EP2566867A1 (ru)
JP (1) JP2013525392A (ru)
KR (1) KR20130094693A (ru)
CN (1) CN103180322A (ru)
BR (1) BR112012027803A2 (ru)
CA (1) CA2797772A1 (ru)
EA (1) EA201291038A1 (ru)
MX (1) MX2012012328A (ru)
SG (1) SG184989A1 (ru)
WO (1) WO2011134831A1 (ru)
ZA (1) ZA201208125B (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20131197A1 (es) 2008-10-31 2013-11-06 Genentech Inc Compuestos de pirazolopirimidina como inhibidores de jak y composiciones farmaceuticas que los contienen
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
WO2012035039A1 (en) 2010-09-15 2012-03-22 F. Hoffmann-La Roche Ag Azabenzothiazole compounds, compositions and methods of use
JP2013542966A (ja) * 2010-11-19 2013-11-28 エフ．ホフマン−ラ ロシュ アーゲー ピラゾロピリジンならびにｔｙｋ２阻害剤としてのピラゾロピリジン及びそれらの使用
CN104169272A (zh) 2011-12-23 2014-11-26 赛尔佐姆有限公司 作为激酶抑制剂的嘧啶-2,4-二胺衍生物
US20160222014A1 (en) * 2013-09-10 2016-08-04 Asana Biosciences, Llc Compounds for regulating fak and/or src pathways
SG11201609830RA (en) 2014-05-23 2016-12-29 Hoffmann La Roche 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds which are jak inhibitors
EP3630766A1 (en) 2017-05-22 2020-04-08 H. Hoffnabb-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
KR20200085779A (ko) * 2017-12-05 2020-07-15 주식회사 오스코텍 Lrrk2 억제제로서의 피롤로(피라졸로)피리미딘 유도체
CN110446713B (zh) * 2018-06-06 2022-05-24 杭州澳津生物医药技术有限公司 一种吡唑嘧啶衍生物及其用途和药物组合物
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
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
JP2022532877A (ja) * 2019-05-08 2022-07-20 ビマラン バイオサイエンシーズ，インク． Ｊａｋ阻害剤
TW202110849A (zh) * 2019-05-27 2021-03-16 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
US11697648B2 (en) 2019-11-26 2023-07-11 Theravance Biopharma R&D Ip, Llc Fused pyrimidine pyridinone compounds as JAK inhibitors

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ337750A (en) 1997-02-12 2001-08-31 Univ Michigan Protein markers for lung cancer and use thereof
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
KR100838617B1 (ko) 1999-02-10 2008-06-16 아스트라제네카 아베 혈관형성 억제제로서의 퀴나졸린 유도체
EE05330B1 (et) 1999-11-05 2010-08-16 Astrazeneca Ab Kinasoliini derivaadid kui VEGF-i inhibiitorid
PT1235830E (pt) 1999-12-10 2004-04-30 Pfizer Prod Inc Compostos de pirrolo¬2,3-d|pirimidina como inibidores das proteina cinases
MY130363A (en) 2000-02-15 2007-06-29 Sugen Inc "pyrrole substituted 2-indolinone protein kinase inhibitors"
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
EP1704145B1 (en) * 2004-01-12 2012-06-13 YM BioSciences Australia Pty Ltd Selective kinase inhibitors
UA87494C2 (en) * 2004-03-30 2009-07-27 Вертекс Фармасьютикалс Инкорпорейтед Azaindoles useful as inhibitors of jak and other protein kinases
AU2006205851A1 (en) * 2005-01-14 2006-07-20 Janssen Pharmaceutica N.V. 5-membered annelated heterocyclic pyrimidines as kinase inhibitors
PL1891446T3 (pl) 2005-06-14 2013-08-30 Cellzome Gmbh Sposób identyfikacji nowych związków oddziałujących z enzymami
EP1931675B1 (en) * 2005-10-06 2015-01-14 Merck Sharp & Dohme Corp. Pyrazolo(1, 5a) pyrimidines as protein kinase inhibitors
GB0605691D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
EP1862802B1 (en) 2006-06-01 2008-12-10 Cellzome Ag Methods for the identification of ZAP-70 interacting molecules and for the purification of ZAP-70
JP2009544592A (ja) 2006-07-21 2009-12-17 ノバルティス アクチエンゲゼルシャフト Ｊａｋキナーゼ阻害剤としての２，４−ジ（アリールアミノ）−ピリミジン−５−カルボキサミド化合物
CA2669686A1 (en) 2006-11-16 2008-05-22 Pharmacopeia, Llc 7-substituted purine derivatives for immunosuppression
JP2010516812A (ja) 2007-01-30 2010-05-20 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 有糸***キナーゼの調節剤
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
CA2714177A1 (en) 2008-02-06 2009-08-13 Novartis Ag Pyrrolo [2,3-d] pyridines and use thereof as tyrosine kinase inhibitors
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.
WO2010118986A1 (en) 2009-04-14 2010-10-21 Cellzome Limited Fluoro substituted pyrimidine compounds as jak3 inhibitors
EP2475648A1 (en) 2009-09-11 2012-07-18 Cellzome Limited Ortho substituted pyrimidine compounds as jak inhibitors

Also Published As

Publication number Publication date
CN103180322A (zh) 2013-06-26
JP2013525392A (ja) 2013-06-20
KR20130094693A (ko) 2013-08-26
SG184989A1 (en) 2012-11-29
WO2011134831A1 (en) 2011-11-03
BR112012027803A2 (pt) 2016-08-09
ZA201208125B (en) 2013-08-28
CA2797772A1 (en) 2011-11-03
US20130131043A1 (en) 2013-05-23
MX2012012328A (es) 2013-05-06
EP2566867A1 (en) 2013-03-13

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