JP2016056183A5 - - Google Patents
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- Publication number
- JP2016056183A5 JP2016056183A5 JP2015246515A JP2015246515A JP2016056183A5 JP 2016056183 A5 JP2016056183 A5 JP 2016056183A5 JP 2015246515 A JP2015246515 A JP 2015246515A JP 2015246515 A JP2015246515 A JP 2015246515A JP 2016056183 A5 JP2016056183 A5 JP 2016056183A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrrolo
- pyrazol
- pyrimidin
- propanenitrile
- hydroxy
- 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.)
- Granted
Links
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25038709P | 2009-10-09 | 2009-10-09 | |
| US61/250,387 | 2009-10-09 | ||
| US31621810P | 2010-03-22 | 2010-03-22 | |
| US61/316,218 | 2010-03-22 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012533354A Division JP5946768B2 (ja) | 2009-10-09 | 2010-10-08 | ３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017172989A Division JP2017226695A (ja) | 2009-10-09 | 2017-09-08 | ３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016056183A JP2016056183A (ja) | 2016-04-21 |
| JP2016056183A5 true JP2016056183A5 (enExample) | 2016-09-01 |
| JP6251232B2 JP6251232B2 (ja) | 2017-12-20 |
Family
ID=43037845
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012533354A Active JP5946768B2 (ja) | 2009-10-09 | 2010-10-08 | ３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体 |
| JP2015246515A Active JP6251232B2 (ja) | 2009-10-09 | 2015-12-17 | ３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体 |
| JP2017172989A Pending JP2017226695A (ja) | 2009-10-09 | 2017-09-08 | ３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012533354A Active JP5946768B2 (ja) | 2009-10-09 | 2010-10-08 | ３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017172989A Pending JP2017226695A (ja) | 2009-10-09 | 2017-09-08 | ３−（４−（７Ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１Ｈ−ピラゾール−１−イル）−３−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US8486902B2 (enExample) |
| EP (1) | EP2486041B1 (enExample) |
| JP (3) | JP5946768B2 (enExample) |
| KR (3) | KR101805936B1 (enExample) |
| CN (2) | CN105541847B (enExample) |
| BR (1) | BR112012008267B1 (enExample) |
| CA (1) | CA2777114C (enExample) |
| EA (1) | EA021478B1 (enExample) |
| ES (1) | ES2435491T3 (enExample) |
| MX (1) | MX2012004180A (enExample) |
| PL (1) | PL2486041T3 (enExample) |
| PT (1) | PT2486041E (enExample) |
| WO (1) | WO2011044481A1 (enExample) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE028588T2 (hu) | 2005-12-13 | 2016-12-28 | Incyte Holdings Corp | Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok |
| 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. |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| 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. |
| WO2010083283A2 (en) | 2009-01-15 | 2010-07-22 | Incyte Corporation | Processes for preparing jak inhibitors and related intermediate compounds |
| BRPI1012108B8 (pt) | 2009-05-22 | 2021-05-25 | Incyte Corp | composto 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octa no- ou heptano-nitrila, sua composição, seus usos e processo para preparar um sal de ácido fosfórico |
| NZ596479A (en) * | 2009-05-22 | 2014-01-31 | Incyte Corp | 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 |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EA021478B1 (ru) * | 2009-10-09 | 2015-06-30 | Инсайт Корпорейшн | ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА |
| US20110207754A1 (en) * | 2010-02-18 | 2011-08-25 | Incyte Corporation | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
| CA2792508C (en) | 2010-03-10 | 2018-01-16 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| EA202091303A3 (ru) | 2010-05-21 | 2021-05-31 | Инсайт Холдингс Корпорейшн | Композиция ингибитора jak для местного применения |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| WO2012112847A1 (en) | 2011-02-18 | 2012-08-23 | Novartis Pharma Ag | mTOR/JAK INHIBITOR COMBINATION THERAPY |
| US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
| WO2013023119A1 (en) * | 2011-08-10 | 2013-02-14 | 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 |
| US9089574B2 (en) | 2011-11-30 | 2015-07-28 | 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 |
| EA201590272A1 (ru) | 2012-07-27 | 2015-05-29 | Рациофарм Гмбх | Пероральные дозированные формы для модифицированного высвобождения, содержащие руксолитиниб |
| CA2888816A1 (en) | 2012-11-01 | 2014-05-08 | Incyte Corporation | Tricyclic fused thiophene derivatives as jak inhibitors |
| KR102242077B1 (ko) | 2012-11-15 | 2021-04-20 | 인사이트 홀딩스 코포레이션 | 룩솔리티니브의 서방성 제형 |
| WO2014118388A1 (en) | 2013-02-04 | 2014-08-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for assaying jak2 activity in red blood cells and uses thereof |
| EP3489239B1 (en) | 2013-03-06 | 2021-09-15 | Incyte Holdings Corporation | Processes and intermediates for making a jak inhibitor |
| CR20190156A (es) | 2013-05-17 | 2019-05-16 | Incyte Corp | Derivados de bipirazol como inhibidores jak |
| MX376856B (es) | 2013-08-07 | 2025-03-07 | Incyte Holdings Corp | Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1). |
| SG11201609016VA (en) | 2014-04-30 | 2016-11-29 | Incyte Corp | Processes of preparing a jak1 inhibitor and new forms thereto |
| 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 |
| JP6149810B2 (ja) * | 2014-06-13 | 2017-06-21 | 株式会社島津製作所 | 代謝物解析システム及び代謝物解析方法 |
| RS63364B1 (sr) | 2014-08-11 | 2022-07-29 | Acerta Pharma Bv | Terapeutske kombinacije btk inhibitora, pd-1 inhibitora i/ili pd-l1 inhibitora |
| SMT202100674T1 (it) | 2014-08-11 | 2022-01-10 | Acerta Pharma Bv | Combinazioni terapeutiche di un inibitore di btk e un inibitore di bcl-2 |
| WO2016024232A1 (en) | 2014-08-11 | 2016-02-18 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor |
| CN105777754B (zh) | 2014-12-16 | 2019-07-26 | 北京赛林泰医药技术有限公司 | 吡咯并嘧啶化合物 |
| CA3003283A1 (en) | 2015-11-24 | 2017-06-01 | Theravance Biopharma R&D Ip, Llc | Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease |
| CN107513067A (zh) * | 2016-06-16 | 2017-12-26 | 北京赛林泰医药技术有限公司 | 含有取代环戊基的吡咯并嘧啶化合物 |
| CN107759623B (zh) * | 2016-08-23 | 2020-08-14 | 苏州旺山旺水生物医药有限公司 | Jak抑制剂的中间体及其制备方法 |
| CN110418796A (zh) | 2017-03-08 | 2019-11-05 | 施万生物制药研发Ip有限责任公司 | 托法替尼(tofacitinib)的葡萄糖苷酸前药 |
| WO2018167283A1 (en) | 2017-03-17 | 2018-09-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling |
| US20200088732A1 (en) | 2017-04-13 | 2020-03-19 | INSERM (Institut National de la Santé et de la Recherche Mèdicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma |
| CN108794480A (zh) * | 2017-04-28 | 2018-11-13 | 天津药物研究院有限公司 | 吡咯并嘧啶类化合物、其制备方法和用途 |
| BR112019024509A2 (pt) | 2017-05-23 | 2020-06-23 | Theravance Biopharma R&D Ip, Llc | Glicuronídeo de pró-fármacos dos inibidores da janus quinase |
| EP3609903A1 (en) | 2017-05-23 | 2020-02-19 | Theravance Biopharma R&D IP, LLC | Thiocarbamate prodrugs of tofacitinib |
| TW201924683A (zh) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | 用於治療骨髓增生性贅瘤的低劑量組合療法 |
| MD3746429T2 (ro) | 2018-01-30 | 2022-08-31 | Incyte Corp | Procedee pentru prepararea de (1-(3-fluoro-2-(trifluorometil)izonicotinil)piperidin-4-onă) |
| CA3091339A1 (en) | 2018-02-16 | 2019-08-22 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of cytokine-related disorders |
| WO2019191679A1 (en) | 2018-03-30 | 2019-10-03 | Incyte Corporation | Biomarkers for inflammatory skin disease |
| KR20260080448A (ko) | 2018-03-30 | 2026-06-02 | 인사이트 코포레이션 | Jak 억제제를 사용하는 화농성 한선염의 치료 |
| 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 |
| CA3108065C (en) | 2018-07-31 | 2025-10-07 | Loxo Oncology, Inc. | SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE |
| EP3847158B1 (en) * | 2018-09-06 | 2026-06-24 | Arena Pharmaceuticals, Inc. | Compounds useful in the treatment of autoimmune and inflammatory disorders |
| KR20210109522A (ko) | 2018-10-31 | 2021-09-06 | 인사이트 코포레이션 | 혈액 질환의 치료를 위한 병용 요법 |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| WO2020131627A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| US12351571B2 (en) | 2018-12-19 | 2025-07-08 | Array Biopharma Inc. | Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases |
| CA3156007A1 (en) | 2019-09-27 | 2021-04-01 | Disc Medicine, Inc. | METHODS OF TREATING MYELOFIBROSE AND ASSOCIATED CONDITIONS |
| CN110538183B (zh) * | 2019-10-09 | 2021-05-04 | 吉林大学 | 一种预防和治疗小儿湿疹的组合物及其制备方法 |
| WO2021072116A1 (en) | 2019-10-10 | 2021-04-15 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US12360120B2 (en) | 2019-10-10 | 2025-07-15 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| TW202131926A (zh) | 2019-11-22 | 2021-09-01 | 美商英塞特公司 | 包含alk2抑制劑及jak2抑制劑的組合療法 |
| AU2021273014A1 (en) | 2020-05-13 | 2022-11-17 | AbbVie Deutschland GmbH & Co. KG | Anti-hemojuvelin (HJV) antibodies for treating anemia of chronic disease |
| ES3075793T3 (en) | 2020-05-13 | 2026-08-07 | Disc Medicine Inc | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| SI4157831T1 (sl) | 2020-06-02 | 2025-02-28 | Incyte Corporation | Postopki za pripravo zaviralca jak1 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| IL300555A (en) | 2020-08-18 | 2023-04-01 | Incyte Corp | Process and intermediates for preparing a JAK inhibitor |
| CA3192055A1 (en) | 2020-08-18 | 2022-02-24 | Incyte Corporation | Process and intermediates for preparing a jak1 inhibitor |
| IL303238A (en) | 2020-12-08 | 2023-07-01 | Incyte Corp | Jak1 pathway inhibitors for the treatment of vitiligo |
| AU2022270072A1 (en) | 2021-05-03 | 2023-11-02 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of prurigo nodularis |
| CA3226714A1 (en) | 2021-07-12 | 2023-01-19 | Incyte Corporation | Process and intermediates for preparing baricitinib |
Family Cites Families (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3036390A1 (de) | 1980-09-26 | 1982-05-13 | Troponwerke GmbH & Co KG, 5000 Köln | Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen |
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| MX9800136A (es) | 1995-07-05 | 1998-03-29 | Du Pont | Pirimidinonas fungicidas. |
| PL188959B1 (pl) | 1995-07-06 | 2005-05-31 | Novartis Ag | Pirolopirymidyny i sposoby ich wytwarzania |
| AU4231299A (en) | 1998-06-04 | 1999-12-20 | Abbott Laboratories | Cell adhesion-inhibiting antinflammatory compounds |
| US6232320B1 (en) | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
| AU3951899A (en) | 1998-06-19 | 2000-01-05 | Pfizer Products Inc. | Pyrrolo(2,3-d)pyrimidine compounds |
| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| ES2342240T3 (es) | 1998-08-11 | 2010-07-02 | Novartis Ag | Derivados de isoquinolina con actividad que inhibe la angiogenia. |
| 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 |
| OA12118A (en) * | 1999-12-10 | 2006-05-04 | Pfizer Prod Inc | PyrroloÄ2,3-dÜpyrimidine compounds. |
| HUP0203895A3 (en) | 1999-12-24 | 2004-09-28 | Aventis Pharma Ltd West Mallin | Substituted azaindoles and pharmaceutical compositions containing them and their use |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| US6335342B1 (en) | 2000-06-19 | 2002-01-01 | Pharmacia & Upjohn S.P.A. | Azaindole derivatives, process for their preparation, and their use as antitumor agents |
| CA2413313C (en) | 2000-06-23 | 2011-06-14 | Mitsubishi Pharma Corporation | Antitumor effect potentiators |
| OA12292A (en) | 2000-06-26 | 2003-11-11 | Pfizer Prod Inc | PyrroloÄ2,3-dÜpyrimidine compounds as immunosuppressive agents. |
| EP1294358B1 (en) | 2000-06-28 | 2004-08-18 | Smithkline Beecham Plc | Wet milling process |
| GB0100622D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds V111 |
| WO2002060492A1 (en) | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd | Methods of inhibiting kinases |
| US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
| CA2455181C (en) | 2001-08-01 | 2010-04-06 | Merck & Co., Inc. | Benzimidazo[4,5-f]isoquinolinone derivatives |
| CN100391958C (zh) | 2001-09-19 | 2008-06-04 | 安万特医药股份有限公司 | 化合物 |
| PT1441737E (pt) | 2001-10-30 | 2006-12-29 | Dana Farber Cancer Inst Inc | Derivados de estrutura como inibidores da actividade do receptor de tirosina cinase flt3 |
| PY0228255A (es) | 2001-12-06 | 2004-06-01 | Pfizer Prod Inc | Compuestos cristalinos novedosos |
| TW200403058A (en) | 2002-04-19 | 2004-03-01 | Bristol Myers Squibb Co | Heterocyclo inhibitors of potassium channel function |
| 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 |
| US7259161B2 (en) | 2002-11-04 | 2007-08-21 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of JAK and other protein kinases |
| AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
| WO2004047843A1 (en) | 2002-11-26 | 2004-06-10 | Pfizer Products Inc. | Method of treatment of transplant rejection |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| CA2515132C (en) | 2003-02-07 | 2012-01-03 | Vertex Pharmaceuticals Incorporated | Heteroaryl substituted pyrroles useful as inhibitors of protein kinases |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| SE0301373D0 (sv) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
| SE0301372D0 (sv) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
| US20050043346A1 (en) | 2003-08-08 | 2005-02-24 | Pharmacia Italia S.P.A. | Pyridylpyrrole derivatives active as kinase inhibitors |
| PE20050952A1 (es) | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
| CA2545192A1 (en) | 2003-11-25 | 2005-06-09 | Pfizer Products Inc. | Method of treatment of atherosclerosis |
| RU2006120956A (ru) | 2003-12-17 | 2008-01-27 | Пфайзер Продактс Инк. (Us) | Пирроло{2, 3-d}пиримидиновые соединения для лечения отторжения трансплантата |
| US20050153989A1 (en) | 2004-01-13 | 2005-07-14 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
| ES2364340T3 (es) | 2004-03-30 | 2011-08-31 | Vertex Pharmaceuticals Incorporated | Azaindoles útiles como inhibidores de jak y otras proteína quinasas. |
| US20060106020A1 (en) | 2004-04-28 | 2006-05-18 | Rodgers James D | Tetracyclic inhibitors of Janus kinases |
| WO2005105988A2 (en) | 2004-04-28 | 2005-11-10 | Vertex Pharmaceuticals Incorporated | Crystal structure of human jak3 kinase domain complex and binding pockets thereof |
| WO2005105146A1 (en) | 2004-05-03 | 2005-11-10 | Novartis Ag | Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor |
| MXPA06013250A (es) | 2004-05-14 | 2007-02-28 | Abbott Lab | Inhibidores de quinasa como agentes terapeuticos. |
| PE20060426A1 (es) | 2004-06-02 | 2006-06-28 | Schering Corp | DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa |
| WO2006013114A1 (en) | 2004-08-06 | 2006-02-09 | Develogen Aktiengesellschaft | Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| UY29177A1 (es) | 2004-10-25 | 2006-05-31 | Astex Therapeutics Ltd | Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos |
| RU2007123675A (ru) | 2004-11-24 | 2008-12-27 | Новартис АГ (CH) | Комбинации ингибиторов jak |
| 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. |
| WO2006083780A2 (en) * | 2005-01-31 | 2006-08-10 | Mylan Laboratories, Inc. | Glucuronidated nebivolol |
| US8633205B2 (en) * | 2005-02-03 | 2014-01-21 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of protein kinases |
| US7019626B1 (en) * | 2005-03-03 | 2006-03-28 | Omnitek Engineering, Inc. | Multi-fuel engine conversion system and method |
| JP2008545660A (ja) | 2005-05-20 | 2008-12-18 | 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阻害剤として有用なピロロピリジン化合物 |
| US20070049591A1 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Inhibitors of MAPK/Erk Kinase |
| WO2007038215A1 (en) | 2005-09-22 | 2007-04-05 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| CN101801971A (zh) | 2005-09-30 | 2010-08-11 | 沃泰克斯药物股份有限公司 | 可用作janus激酶抑制剂的脱氮嘌呤 |
| HUE028588T2 (hu) * | 2005-12-13 | 2016-12-28 | Incyte Holdings Corp | Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok |
| WO2007076423A2 (en) | 2005-12-22 | 2007-07-05 | Smithkline Beecham Corporation | INHIBITORS OF Akt ACTIVITY |
| NZ592968A (en) | 2006-01-17 | 2012-08-31 | Vertex Pharma | Azaindoles substituted with either triazine or pyrimidine useful as inhibitors of janus kinases consisting of JAK1, JAK2, JAK3, and TYK2 |
| JP2009532475A (ja) | 2006-04-05 | 2009-09-10 | 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 | ヤヌスキナーゼの阻害剤として有用なデアザプリン |
| ES2415863T3 (es) | 2006-12-22 | 2013-07-29 | Incyte Corporation | Heterociclos sustituidos como inhibidores de Janus Quinasas |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline 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. |
| MY165582A (en) | 2008-03-11 | 2018-04-05 | Incyte Holdings Corp | 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. |
| WO2010083283A2 (en) | 2009-01-15 | 2010-07-22 | Incyte Corporation | Processes for preparing jak inhibitors and related intermediate compounds |
| NZ596479A (en) | 2009-05-22 | 2014-01-31 | Incyte Corp | 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 |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EA021478B1 (ru) * | 2009-10-09 | 2015-06-30 | Инсайт Корпорейшн | ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА |
| US20110207754A1 (en) | 2010-02-18 | 2011-08-25 | Incyte Corporation | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
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