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) | KR20180126619A (enExample) |
| CN (2) | CN102596960B (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 (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103214484B (zh) | 2005-12-13 | 2016-07-06 | 因塞特控股公司 | 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶 |
| 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. |
| HUE029236T2 (en) | 2007-06-13 | 2017-02-28 | Incyte Holdings Corp | (R) -3- (4- (7H-Pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanenitrile Crystalline salts of Janus kinase inhibitor |
| 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. |
| PE20211639A1 (es) | 2009-01-15 | 2021-08-24 | Incyte Holdings Corp | Procesos para preparar inhibidores de jak y compuestos intermediarios relacionado |
| MY156727A (en) * | 2009-05-22 | 2016-03-15 | 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 |
| EP2432472B1 (en) | 2009-05-22 | 2019-10-02 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak 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 |
| MX2012004180A (es) * | 2009-10-09 | 2012-07-17 | Incyte Corp | Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo. |
| CA2790070C (en) * | 2010-02-18 | 2018-03-06 | Incyte Corporation | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
| EP3354652B1 (en) | 2010-03-10 | 2020-05-06 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| AR084691A1 (es) | 2010-05-21 | 2013-06-05 | Incyte Corp | Formulacion de uso topico para un inhibidor de jak y metodo para tratar trastorno de la piel |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| WO2012112847A1 (en) | 2011-02-18 | 2012-08-23 | Novartis Pharma Ag | mTOR/JAK INHIBITOR COMBINATION THERAPY |
| MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| CA2844507A1 (en) | 2011-08-10 | 2013-02-14 | Novartis Pharma Ag | Jak pi3k/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 |
| CA3131037A1 (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 |
| CA2879603A1 (en) | 2012-07-27 | 2014-01-30 | Ratiopharm Gmbh | Oral dosage forms for modified release comprising ruxolitinib |
| JP6359546B2 (ja) | 2012-11-01 | 2018-07-18 | 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阻害薬としての三環式縮合チオフェン誘導体 |
| TWI761825B (zh) | 2012-11-15 | 2022-04-21 | 美商英塞特控股公司 | 盧梭利替尼之緩釋性劑型 |
| 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 |
| MX384910B (es) | 2013-03-06 | 2025-03-14 | Incyte Holdings Corp | Procesos e intermedios para hacer un inhibidor de jak. |
| PE20200527A1 (es) | 2013-05-17 | 2020-03-09 | Incyte Corp | Derivados del bipirazol como inhibidores jak |
| SG11201600815WA (en) | 2013-08-07 | 2016-03-30 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| BR112016025427A2 (pt) | 2014-04-30 | 2017-08-15 | Incyte Corp | processos de preparação de um inibidor de jak1 e formas do mesmo |
| 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 |
| RS62713B1 (sr) | 2014-08-11 | 2022-01-31 | Acerta Pharma Bv | Terapeutske kombinacije btk inhibitora i bcl-2 inhibitora |
| HRP20220738T1 (hr) | 2014-08-11 | 2022-08-19 | Acerta Pharma B.V. | Terapijske kombinacije inhibitora btk, inhibitora pd-1 i/ili inhibitora pd-l1 |
| US20170224819A1 (en) | 2014-08-11 | 2017-08-10 | 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 |
| US10435428B2 (en) | 2015-11-24 | 2019-10-08 | 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 |
| WO2018165250A1 (en) | 2017-03-08 | 2018-09-13 | Theravance Biopharma R&D Ip, Llc | Glucuronide prodrugs of tofacitinib |
| 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 |
| EP3610264A1 (en) | 2017-04-13 | 2020-02-19 | INSERM (Institut National de la Santé et de la Recherche Médicale) | 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 |
| JP2020520955A (ja) * | 2017-05-23 | 2020-07-16 | セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー | ヤヌスキナーゼ阻害剤のグルクロニドプロドラッグ |
| EP3609903A1 (en) | 2017-05-23 | 2020-02-19 | Theravance Biopharma R&D IP, LLC | Thiocarbamate prodrugs of tofacitinib |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| JP7393348B2 (ja) | 2018-01-30 | 2023-12-06 | インサイト・コーポレイション | (1-(3-フルオロ-2(トリフルオロメチル)イソニコチニル)ピぺリジン―4-オン)を作製するためのプロセス及び中間体 |
| UA127519C2 (uk) | 2018-02-16 | 2023-09-20 | Інсайт Корпорейшн | Інгібітори шляху jak1, призначені для лікування порушень, пов'язаних із цитокінами |
| JP7565798B2 (ja) | 2018-03-30 | 2024-10-11 | インサイト・コーポレイション | 炎症性皮膚疾患のバイオマーカー |
| CN113768934A (zh) | 2018-03-30 | 2021-12-10 | 因赛特公司 | 使用jak抑制剂治疗化脓性汗腺炎 |
| MX2020010815A (es) | 2018-04-13 | 2020-12-11 | Incyte Corp | Biomarcadores para enfermedad de injerto contra hospedero. |
| CA3224985C (en) | 2018-07-31 | 2025-11-18 | 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 |
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| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| CN113474337A (zh) | 2018-12-19 | 2021-10-01 | 奥瑞生物药品公司 | 作为fgfr抑制剂用于治疗癌症的7-((3,5-二甲氧基苯基)氨基)喹喔啉衍生物 |
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| 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 |
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| JP7802696B2 (ja) | 2020-06-02 | 2026-01-20 | インサイト・コーポレイション | Jak1阻害剤の調製プロセス |
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