AU2008321046B2 - 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors - Google Patents

4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors Download PDF

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AU2008321046B2
AU2008321046B2 AU2008321046A AU2008321046A AU2008321046B2 AU 2008321046 B2 AU2008321046 B2 AU 2008321046B2 AU 2008321046 A AU2008321046 A AU 2008321046A AU 2008321046 A AU2008321046 A AU 2008321046A AU 2008321046 B2 AU2008321046 B2 AU 2008321046B2
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pyrazol
pyrim
ino
cya
pyra
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AU2008321046A1 (en
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Yun-Long Li
James D. Rodgers
Wenqing Yao
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Incyte Holdings Corp
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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AU2008321046A 2007-11-16 2008-11-13 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors Active AU2008321046B2 (en)

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Application Number Priority Date Filing Date Title
US98860607P 2007-11-16 2007-11-16
US60/988,606 2007-11-16
PCT/US2008/083319 WO2009064835A1 (en) 2007-11-16 2008-11-13 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors

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AU2008321046A1 AU2008321046A1 (en) 2009-05-22
AU2008321046B2 true AU2008321046B2 (en) 2013-10-24

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US (1) US8309718B2 (enExample)
EP (1) EP2220068B1 (enExample)
JP (1) JP5480813B2 (enExample)
KR (1) KR101580482B1 (enExample)
CN (1) CN101910152B (enExample)
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BR (1) BRPI0820544A2 (enExample)
CA (1) CA2704599C (enExample)
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Families Citing this family (113)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
SI1966202T1 (sl) 2005-12-13 2012-01-31 Incyte Corp S heteroarilom substituirani pirolo (2,3-b)piridini in pirolo (2,3-b)pirimidini kot zaviralci janus kinaze
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
EP2173752B2 (en) 2007-06-13 2022-07-13 Incyte Holdings Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
FR2938537B1 (fr) 2008-11-14 2012-10-26 Sanofi Aventis Derives de carbamates d'alkyl-heterocycles, leur preparation et leur application en therapeutique.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
CN106967070A (zh) 2009-05-22 2017-07-21 因塞特控股公司 作为jak抑制剂的化合物
CA2762174C (en) 2009-05-22 2018-02-20 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
US20110207736A1 (en) * 2009-12-23 2011-08-25 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
AU2011214254B2 (en) * 2010-02-10 2016-06-09 Genon Biotechnologies Oy Dual activity kinase domains and uses thereof
JP5858434B2 (ja) * 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
EP3715347B1 (en) 2010-03-10 2021-12-22 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
GB201007286D0 (en) * 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
NZ603686A (en) 2010-05-21 2014-11-28 Incyte Corp Topical formulation for a jak inhibitor
PT2576541T (pt) 2010-06-04 2016-07-08 Hoffmann La Roche Derivados de aminopirimidina como moduladores de lrrk2
CA2815330A1 (en) * 2010-11-09 2012-05-18 Cellzome Limited Pyridine compounds and aza analogues thereof as tyk2 inhibitors
CA2812669C (en) 2010-11-10 2018-11-06 F. Hoffmann-La Roche Ag Pyrazole aminopyrimidine derivatives as lrrk2 modulators
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
JP5936628B2 (ja) 2011-02-18 2016-06-22 ノバルティス・ファルマ・アクチェンゲゼルシャフトＮｏｖａｒｔｉｓ Ｐｈａｒｍａ ＡＧ ｍＴＯＲ／ＪＡＫ阻害剤併用療法
US9284298B2 (en) * 2011-04-11 2016-03-15 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
TWI577676B (zh) 2011-06-20 2017-04-11 英塞特控股公司 作為ｊａｋ抑制劑之吖丁啶基苯基、吡啶基或吡基羧醯胺衍生物
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
EP2758377B1 (en) * 2011-09-22 2017-08-02 Merck Sharp & Dohme Corp. Cycloalkylnitrile pyrazole carboxamides as janus kinase inhibitors
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
CN103102359B (zh) * 2011-11-15 2016-11-09 江苏先声药业有限公司 嘧啶类化合物及其应用
WO2013082476A1 (en) 2011-11-30 2013-06-06 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
KR20150034209A (ko) 2012-06-26 2015-04-02 델 마 파마슈티컬스 인코포레이티드 디안하이드로갈락티톨, 디아세틸디안하이드로갈락티톨, 디브로모둘시톨, 또는 그의 유사체 또는 유도체를 이용하여 유전학적 다형성이 있는 환자에 있어서 티로신-키나아제-억제제 내성 악성종양, ahi1 조절곤란 또는 돌연변이를 치료하는 방법
US8809359B2 (en) * 2012-06-29 2014-08-19 Ym Biosciences Australia Pty Ltd Phenyl amino pyrimidine bicyclic compounds and uses thereof
WO2014066196A1 (en) * 2012-10-23 2014-05-01 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-substituted-4-nitrile orexin receptor antagonists
MX2015005428A (es) 2012-11-01 2015-07-21 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak).
US9499539B2 (en) * 2012-11-05 2016-11-22 Nantbioscience, Inc. Cyclic sulfonamide containing derivatives as inhibitors of hedgehog signaling pathway
SG11201503695XA (en) 2012-11-15 2015-06-29 Incyte Corp Sustained-release dosage forms of ruxolitinib
WO2014075318A1 (zh) * 2012-11-19 2014-05-22 江苏先声药业有限公司 嘧啶类化合物及其应用
JP6412503B2 (ja) 2012-11-21 2018-10-24 ピーティーシー セラピューティクス， インコーポレイテッド 置換逆ピリミジンＢｍｉ−１阻害剤
JP6397831B2 (ja) * 2013-03-06 2018-09-26 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤の製造方法及びその中間体
WO2014146249A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
WO2014186706A1 (en) * 2013-05-17 2014-11-20 Incyte Corporation Bipyrazole derivatives as jak inhibitors
EP3004057B1 (en) * 2013-06-05 2018-07-25 C&C Research Laboratories Heterocyclic derivatives and their use as stat 3 inhibitors
UA120499C2 (uk) 2013-08-07 2019-12-26 Інсайт Корпорейшн Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1
CA2922657C (en) * 2013-08-30 2022-04-12 Ptc Therapeutics, Inc. Substituted pyrimidine bmi-1 inhibitors
WO2015067630A1 (de) 2013-11-08 2015-05-14 Bayer Pharma Aktiengesellschaft Substituierte uracile und ihre verwendung
EP3071553A4 (en) 2013-11-21 2017-08-02 PTC Therapeutics, Inc. Substituted pyridine and pyrazine bmi-1 inhibitors
CN104860941B (zh) * 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
RU2715893C2 (ru) 2014-03-26 2020-03-04 Астекс Терапьютикс Лтд Комбинации ингибитора fgfr и ингибитора igf1r
SMT202100115T1 (it) 2014-03-26 2021-05-07 Astex Therapeutics Ltd Combinazioni di inibitori di fgfr e cmet per il trattamento del cancro
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
JP2017514832A (ja) 2014-04-30 2017-06-08 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ１抑制剤を調製する方法及びその新しい形態
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
WO2016105525A2 (en) * 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Novel pyrimidines as egfr inhibitors and methods of treating disorders
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
EP3327014A4 (en) * 2015-07-24 2019-01-02 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. Egfr inhibitor and pharmaceutically acceptable salt and polymorph thereof, and use thereof
LT3353177T (lt) 2015-09-23 2020-08-25 Janssen Pharmaceutica Nv Tricikliniai heterociklai, skirti vėžio gydymui
MX378230B (es) 2015-09-23 2025-03-10 Janssen Pharmaceutica Nv 1,4-benzodiazepinas biheteroarilo sustituidas y usos de las mismas para el tratamiento del cáncer.
TWI720269B (zh) * 2016-11-22 2021-03-01 財團法人生物技術開發中心 用於調節刺蝟途徑之雜芳基胺化合物及其製法及用途
MD3697789T2 (ro) 2017-10-18 2022-02-28 Incyte Corp Derivați imidazol condensați substituiți cu grupări hidroxi terțiare ca inhibitori PI3K-GAMA
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
MD3746429T2 (ro) 2018-01-30 2022-08-31 Incyte Corp Procedee pentru prepararea de (1-(3-fluoro-2-(trifluorometil)izonicotinil)piperidin-4-onă)
BR112020016628A2 (pt) 2018-02-16 2020-12-15 Incyte Corporation Inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas
HUE067471T2 (hu) 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
WO2019191679A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Biomarkers for inflammatory skin disease
CN112567247A (zh) 2018-04-13 2021-03-26 因赛特公司 用于移植物抗宿主病的生物标志物
BR112021002630A2 (pt) 2018-08-17 2021-05-11 Ptc Therapeutics, Inc. método para tratar câncer pancreático
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
EP3870177A1 (en) * 2018-10-26 2021-09-01 Arrien Pharmaceuticals LLC Pyrazolyl compounds and methods of use thereof
IL282643B2 (en) 2018-10-31 2025-08-01 Incyte Corp A selective jak1 inhibitor for use in a method of treating hematological disease
WO2020118683A1 (en) * 2018-12-14 2020-06-18 Lynk Pharmaceuticals Co. Ltd. Benzamides of pyrazolyl-amino-pyrimidinyl derivatives, and compositions and methods thereof
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
EP3956330A4 (en) 2019-04-18 2023-01-18 The Johns Hopkins University SUBSTITUTED 2-AMINO-PYRAZOLYL-[1,2,4]TRIAZOLO[1,5A]PYRIDINE DERIVATIVES AND THEIR USE
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US12428394B2 (en) 2019-06-28 2025-09-30 Chengdu Zenitar Biomedical Technology Co., Ltd. 2,4-disubstituted pyrimidine derivative, preparation method therefor and use thereof
CN112142731B (zh) * 2019-06-28 2022-07-22 成都赜灵生物医药科技有限公司 一种2，4-二取代嘧啶衍生物及其制备方法和用途
TW202115024A (zh) 2019-08-14 2021-04-16 美商英塞特公司 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物
JP2022549506A (ja) 2019-09-27 2022-11-25 ディスク・メディシン・インコーポレイテッド 骨髄線維症および関連状態を処置するための方法
US12203942B2 (en) 2019-10-10 2025-01-21 Incyte Corporation Biomarkers for graft-versus-host disease
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
PE20221905A1 (es) 2019-10-11 2022-12-23 Incyte Corp Aminas biciclicas como inhibidoras de la cdk2
PE20230251A1 (es) 2019-11-22 2023-02-07 Incyte Corp Terapia de combinacion que comprende un inhibidor de alk2 y un inhibidor de jak2
CN115413278B (zh) * 2020-03-23 2025-01-10 丸仁制药株式会社 新型嘧啶衍生物以及包含其的神经退行性疾病和癌症的预防或治疗用组合物
CN115836089A (zh) 2020-05-13 2023-03-21 迪斯克医药公司 用于治疗骨髓纤维化的抗血幼素（hjv）抗体
FI4157831T3 (fi) 2020-06-02 2024-12-02 Incyte Corp Menetelmiä jak1-estäjän valmistamiseksi
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
AU2021329301A1 (en) 2020-08-18 2023-04-13 Incyte Corporation Process and intermediates for preparing a JAK1 inhibitor
IL300555A (en) 2020-08-18 2023-04-01 Incyte Corp Process and intermediates for preparing a JAK inhibitor
CN114181199B (zh) * 2020-09-15 2023-09-26 成都赜灵生物医药科技有限公司 2，4-二取代嘧啶衍生物及其制备方法和用途
CN112142675B (zh) * 2020-10-09 2021-11-30 嘉兴特科罗生物科技有限公司 一种作为jak激酶抑制剂的小分子化合物及其用途
CN112159394B (zh) * 2020-10-09 2021-10-22 嘉兴特科罗生物科技有限公司 一种作为jak激酶抑制剂的小分子化合物及其用途
US11957661B2 (en) 2020-12-08 2024-04-16 Incyte Corporation JAK1 pathway inhibitors for the treatment of vitiligo
WO2022166916A1 (zh) * 2021-02-05 2022-08-11 深圳市塔吉瑞生物医药有限公司 取代的杂芳基衍生物及其组合物及用途
LT4333840T (lt) 2021-05-03 2026-01-12 Incyte Corporation Jak1 kelio inhibitoriai, skirti mazgelinio niežulio gydymui
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US12071439B2 (en) 2021-07-12 2024-08-27 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
WO2023060202A1 (en) * 2021-10-06 2023-04-13 Aerie Pharmaceuticals, Inc. Janus kinase inhibiting pyrazole compounds and uses thereof
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
KR20250051678A (ko) * 2022-08-22 2025-04-17 항저우 하이라이트엘엘 파마슈티컬 씨오., 엘티디. 피부과 질환의 국소 치료를 위한 jak1/jak2/tyk2 억제제
CN115594664B (zh) * 2022-11-25 2023-02-24 英矽智能科技(上海)有限公司 一类螺环衍生物作为kif18a抑制剂

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002046184A1 (en) * 2000-12-05 2002-06-13 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
WO2002092573A2 (en) * 2001-05-16 2002-11-21 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
WO2007129195A2 (en) * 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
WO1999062908A2 (en) 1998-06-04 1999-12-09 Abbott Laboratories Cell adhesion-inhibiting antinflammatory compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
PT1107964E (pt) 1998-08-11 2010-06-11 Novartis Ag Derivados de isoquinolina com actividade inibidora da angiogénese
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
EA006227B1 (ru) 1999-12-10 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА
DZ3377A1 (fr) * 1999-12-24 2001-07-05 Aventis Pharma Ltd Azaindoles
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
HU230396B1 (hu) 2000-06-28 2016-04-28 Smithkline Beecham Plc Nedves őrlési eljárás
BR0212760A (pt) 2001-09-19 2004-12-07 Aventis Pharma Sa Compostos quìmicos
CA2462657C (en) 2001-10-30 2011-04-26 Novartis Ag Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
GB0215844D0 (en) * 2002-07-09 2002-08-14 Novartis Ag Organic compounds
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
JP2006518381A (ja) 2003-02-07 2006-08-10 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ヘテロアリール置換ピロール
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
US7528138B2 (en) * 2004-11-04 2009-05-05 Vertex Pharmaceuticals Incorporated Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
AR054416A1 (es) * 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
WO2007038215A1 (en) * 2005-09-22 2007-04-05 Incyte Corporation Tetracyclic inhibitors of janus kinases
WO2007049041A1 (en) 2005-10-28 2007-05-03 Astrazeneca Ab 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer
SI1966202T1 (sl) * 2005-12-13 2012-01-31 Incyte Corp S heteroarilom substituirani pirolo (2,3-b)piridini in pirolo (2,3-b)pirimidini kot zaviralci janus kinaze
CN102633783A (zh) * 2006-02-10 2012-08-15 转化技术制药公司 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法
JP2009530261A (ja) * 2006-03-16 2009-08-27 ファイザー・プロダクツ・インク ピラゾール化合物
EP2121692B1 (en) * 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
EP2173752B2 (en) * 2007-06-13 2022-07-13 Incyte Holdings Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
CL2008001709A1 (es) * 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
AU2009223640B2 (en) * 2008-03-11 2013-07-04 Incyte Holdings Corporation Azetidine and cyclobutane derivatives as jak 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.
JOP20190230A1 (ar) * 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
CA2762174C (en) * 2009-05-22 2018-02-20 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CN106967070A (zh) * 2009-05-22 2017-07-21 因塞特控股公司 作为jak抑制剂的化合物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002046184A1 (en) * 2000-12-05 2002-06-13 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
WO2002092573A2 (en) * 2001-05-16 2002-11-21 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
WO2007129195A2 (en) * 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PILLONEL, C. Pest Manag. Sci. (2005), 61, 1069-1076 *

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