JP2016056183A5 - - Google Patents
Download PDFInfo
- 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) | 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 (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI630207B (zh) | 2005-12-13 | 2018-07-21 | 英塞特控股公司 | 作為傑納斯激酶（ＪＡＮＵＳ ＫＩＮＡＳＥ）抑制劑之經雜芳基取代之吡咯并〔２，３-ｂ〕吡啶及吡咯并〔２，３-ｂ〕嘧啶 |
| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of 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. |
| 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. |
| TWI665200B (zh) * | 2009-01-15 | 2019-07-11 | 英塞特公司 | 製造ｊａｋ抑制劑之方法及相關中間化合物 |
| AR076794A1 (es) | 2009-05-22 | 2011-07-06 | Incyte Corp | Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen |
| EP3643312A1 (en) | 2009-05-22 | 2020-04-29 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak 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 |
| CN105541847B (zh) * | 2009-10-09 | 2019-08-16 | 因西特控股公司 | 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物 |
| CN102844317B (zh) * | 2010-02-18 | 2015-06-03 | 因西特公司 | 作为Janus激酶抑制剂的环丁烷和甲基环丁烷衍生物 |
| EP3050882B1 (en) | 2010-03-10 | 2018-01-31 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| SG10201503983QA (en) | 2010-05-21 | 2015-06-29 | Incyte Corp | Topical Formulation for a JAK Inhibitor |
| CN103415515B (zh) | 2010-11-19 | 2015-08-26 | 因塞特公司 | 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物 |
| US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
| ES2547916T3 (es) | 2011-02-18 | 2015-10-09 | Novartis Pharma Ag | Terapia de combinación de inhibidores de mTOR/JAK |
| PE20140832A1 (es) | 2011-06-20 | 2014-07-14 | Incyte Corp | Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak |
| HK1198579A1 (en) * | 2011-08-10 | 2015-04-30 | 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 |
| CN104185420B (zh) | 2011-11-30 | 2017-06-09 | 埃默里大学 | 用于治疗或预防逆转录病毒和其它病毒感染的抗病毒jak抑制剂 |
| 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 |
| AU2013337824B2 (en) | 2012-11-01 | 2018-03-08 | Incyte Holdings Corporation | Tricyclic fused thiophene derivatives as JAK inhibitors |
| PL2919766T3 (pl) | 2012-11-15 | 2021-10-04 | Incyte Holdings Corporation | Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu |
| 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 |
| CN105189509B (zh) | 2013-03-06 | 2017-12-19 | 因赛特公司 | 用于制备jak抑制剂的方法及中间体 |
| SMT202100040T1 (it) | 2013-05-17 | 2021-03-15 | Incyte Corp | Derivati di bipirazolo come inibitori di jak |
| SG10201912203XA (en) | 2013-08-07 | 2020-02-27 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| 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 |
| 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 |
| EP3179991B1 (en) | 2014-08-11 | 2021-10-06 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor and a bcl-2 inhibitor |
| AR101504A1 (es) | 2014-08-11 | 2016-12-21 | Acerta Pharma Bv | Combinaciones terapéuticas de un inhibidor de la btk, un inhibidor de la pi3k, un inhibidor de la jak-2, y/o un inhibidor de la cdk4/6 |
| SI3179992T1 (sl) | 2014-08-11 | 2022-09-30 | Acerta Pharma B.V. | Terapevtske kombinacije zaviralca BTK, zaviralca PD-1 in/ali zaviralca PD-L1 |
| 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 |
| AU2016359494B2 (en) | 2015-11-24 | 2021-01-07 | 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 |
| US10472366B2 (en) | 2017-03-08 | 2019-11-12 | 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 |
| BR112019024509A2 (pt) | 2017-05-23 | 2020-06-23 | Theravance Biopharma R&D Ip, Llc | Glicuronídeo de pró-fármacos dos inibidores da janus quinase |
| US10233174B2 (en) | 2017-05-23 | 2019-03-19 | Theravance Biopharma R&D Ip, Llc | Thiocarbamate prodrugs of tofacitinib |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| EP3746429B1 (en) | 2018-01-30 | 2022-03-09 | Incyte Corporation | Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
| KR102830476B1 (ko) | 2018-02-16 | 2025-07-08 | 인사이트 코포레이션 | 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제 |
| PT3773593T (pt) | 2018-03-30 | 2024-06-25 | Incyte Corp | Tratamento da hidradenite supurativa com inibidores de jak |
| EP3775284A1 (en) | 2018-03-30 | 2021-02-17 | Incyte Corporation | Biomarkers for inflammatory skin disease |
| SG11202010092XA (en) | 2018-04-13 | 2020-11-27 | Incyte Corp | Biomarkers for graft-versus-host disease |
| JP7286755B2 (ja) | 2018-07-31 | 2023-06-05 | ロクソ オンコロジー， インコーポレイテッド | （ｓ）－５－アミノ－３－（４－（（５－フルオロ－２－メトキシベンズアミド）メチル）フェニル）－１－（１，１，１－トリフルオロプロパン－２－イル）－１ｈ－ピラゾール－４－カルボキサミドの噴霧乾燥分散体および製剤 |
| EP3847158A1 (en) * | 2018-09-06 | 2021-07-14 | Arena Pharmaceuticals, Inc. | Compounds useful in the treatment of autoimmune and inflammatory disorders |
| IL282643B2 (en) | 2018-10-31 | 2025-08-01 | Incyte Corp | A selective jak1 inhibitor for use in a method of treating hematological disease |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| JP2022515198A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | ＦＧＦＲチロシンキナーゼの阻害剤としての置換ピラゾロ［１，５－ａ］ピリジン化合物 |
| 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 |
| US20220372135A1 (en) | 2019-09-27 | 2022-11-24 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related 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 |
| US12360120B2 (en) | 2019-10-10 | 2025-07-15 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| JP2022551649A (ja) | 2019-10-10 | 2022-12-12 | インサイト・コーポレイション | 移植片対宿主病のバイオマーカー |
| JP7717065B2 (ja) | 2019-11-22 | 2025-08-01 | インサイト コーポレーション | Ａｌｋ２阻害剤及びｊａｋ２阻害剤を含む併用療法 |
| CA3177830A1 (en) | 2020-05-13 | 2021-11-18 | Maria BECONI | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| CN115836065B (zh) | 2020-06-02 | 2025-07-01 | 因赛特公司 | 制备jak1抑制剂的方法 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| WO2022040180A1 (en) | 2020-08-18 | 2022-02-24 | Incyte Corporation | Process and intermediates for preparing a jak inhibitor |
| US11897889B2 (en) | 2020-08-18 | 2024-02-13 | Incyte Corporation | Process and intermediates for preparing a JAK1 inhibitor |
| AU2021396231A1 (en) | 2020-12-08 | 2023-06-22 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of vitiligo |
| SI4333840T1 (sl) | 2021-05-03 | 2026-01-30 | Incyte Corporation | Zaviralci poti jak1 za zdravljenje pruriga nodularisa |
| US12071439B2 (en) | 2021-07-12 | 2024-08-27 | Incyte Corporation | Process and intermediates for preparing a JAK inhibitor |
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 |
| EP0836602B1 (en) | 1995-07-05 | 2002-01-30 | E.I. Du Pont De Nemours And Company | Fungicidal pyrimidinones |
| ATE212993T1 (de) | 1995-07-06 | 2002-02-15 | Novartis Erfind Verwalt Gmbh | Pyrolopyrimidine und verfahren zu ihrer herstellung |
| US6232320B1 (en) | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
| IL139811A0 (en) | 1998-06-04 | 2002-02-10 | Abbott Lab | Cell adhesion-inhibiting antinflammatory compounds |
| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| TW505646B (en) | 1998-06-19 | 2002-10-11 | Pfizer Prod Inc | Pyrrolo [2,3-d] pyrimidine compounds |
| WO2000009495A1 (en) | 1998-08-11 | 2000-02-24 | Novartis Ag | Isoquinoline derivatives with angiogenesis inhibiting activity |
| 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 |
| PT1382339E (pt) | 1999-12-10 | 2008-02-06 | Pfizer Prod Inc | Composições que contêm derivados de pirrolo[2,3-d]- pirimidina |
| WO2001047922A2 (en) | 1999-12-24 | 2001-07-05 | Aventis Pharma Limited | Azaindoles |
| 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 |
| ATE465756T1 (de) | 2000-06-23 | 2010-05-15 | Mitsubishi Tanabe Pharma Corp | Antitumoreffekt-verstärker |
| PL359563A1 (pl) | 2000-06-26 | 2004-08-23 | Pfizer Products Inc. | Związki pirolo [2,3-d] pirymidynowe jako środki immunosupresyjne |
| DE60105023T2 (de) | 2000-06-28 | 2005-08-18 | Smithkline Beecham P.L.C., Brentford | Nassvermahlungsverfahren |
| GB0100622D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds V111 |
| JP2004528295A (ja) | 2001-01-30 | 2004-09-16 | サイトピア ピーティワイ リミテッド | キナーゼ阻害方法 |
| 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 |
| MXPA04002243A (es) | 2001-09-19 | 2004-06-29 | Aventis Pharma Sa | Compuestos quimicos. |
| CN101703509A (zh) | 2001-10-30 | 2010-05-12 | 诺瓦提斯公司 | 作为flt3受体酪氨酸激酶活性抑制剂的星形孢菌素衍生物 |
| 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 |
| AR037647A1 (es) | 2002-05-29 | 2004-12-01 | Novartis Ag | Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| WO2004041814A1 (en) | 2002-11-04 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyramidine derivatives as jak inhibitors |
| TWI335913B (en) | 2002-11-15 | 2011-01-11 | Vertex Pharma | Diaminotriazoles useful as inhibitors of protein kinases |
| 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 |
| SE0301372D0 (sv) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
| SE0301373D0 (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 |
| AR045944A1 (es) | 2003-09-24 | 2005-11-16 | Novartis Ag | Derivados de isoquinolina 1.4-disustituidas |
| CA2545192A1 (en) | 2003-11-25 | 2005-06-09 | Pfizer Products Inc. | Method of treatment of atherosclerosis |
| CA2549485A1 (en) | 2003-12-17 | 2005-07-07 | Pfizer Products Inc. | Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection |
| US20050239806A1 (en) | 2004-01-13 | 2005-10-27 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
| NZ584499A (en) | 2004-03-30 | 2011-08-26 | Vertex Pharma | Azaindoles Useful as Inhibitors of Jak and Other Protein Kinases |
| WO2005105814A1 (en) | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| US7558717B2 (en) | 2004-04-28 | 2009-07-07 | Vertex Pharmaceuticals Incorporated | Crystal structure of human JAK3 kinase domain complex and binding pockets thereof |
| KR20070006889A (ko) | 2004-05-03 | 2007-01-11 | 노파르티스 아게 | Ｓ1ｐ 수용체 작용제 및 ｊａｋ3 키나제 억제제를 포함하는조합물 |
| WO2005110410A2 (en) | 2004-05-14 | 2005-11-24 | Abbott Laboratories | Kinase inhibitors as therapeutic agents |
| 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 |
| 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 |
| 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 |
| BRPI0517887A (pt) | 2004-11-24 | 2008-10-21 | Novartis Ag | combinações de inibidores de jaks |
| 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. |
| SG175476A1 (en) * | 2005-01-31 | 2011-11-28 | Mylan Lab Inc | Glucuronidated nebivolol metabolites |
| RU2434871C2 (ru) | 2005-02-03 | 2011-11-27 | Вертекс Фармасьютикалз Инкорпорейтед | Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы |
| US7019626B1 (en) * | 2005-03-03 | 2006-03-28 | Omnitek Engineering, Inc. | Multi-fuel engine conversion system and method |
| NZ564065A (en) | 2005-05-20 | 2011-03-31 | Vertex Pharma | Pyrrolopyridines useful as inhibitors of protein kinase |
| WO2007025090A2 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase |
| JP5119154B2 (ja) | 2005-09-22 | 2013-01-16 | インサイト・コーポレイション | Ｊａｎｕｓキナーゼの四環系阻害剤 |
| EP2532667A1 (en) | 2005-09-30 | 2012-12-12 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
| TWI630207B (zh) | 2005-12-13 | 2018-07-21 | 英塞特控股公司 | 作為傑納斯激酶（ＪＡＮＵＳ ＫＩＮＡＳＥ）抑制劑之經雜芳基取代之吡咯并〔２，３-ｂ〕吡啶及吡咯并〔２，３-ｂ〕嘧啶 |
| EP1968568A4 (en) | 2005-12-22 | 2011-04-13 | Glaxosmithkline Llc | HEMMER OF NUTS ACTIVITY |
| AR060316A1 (es) | 2006-01-17 | 2008-06-11 | Vertex Pharma | Azaindoles de utilidad como inhibidores de janus quinasas |
| CN101460499A (zh) * | 2006-04-05 | 2009-06-17 | 沃泰克斯药物股份有限公司 | 可用作janus激酶抑制剂的去氮杂嘌呤 |
| 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. |
| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
| PL2288610T3 (pl) * | 2008-03-11 | 2017-12-29 | Incyte Holdings Corporation | Azetydynowe i cyklobutanowe pochodne jako inhibitory jak |
| 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. |
| TWI665200B (zh) * | 2009-01-15 | 2019-07-11 | 英塞特公司 | 製造ｊａｋ抑制劑之方法及相關中間化合物 |
| AR076794A1 (es) * | 2009-05-22 | 2011-07-06 | Incyte Corp | Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen |
| 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 |
| CN105541847B (zh) | 2009-10-09 | 2019-08-16 | 因西特控股公司 | 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物 |
| CN102844317B (zh) * | 2010-02-18 | 2015-06-03 | 因西特公司 | 作为Janus激酶抑制剂的环丁烷和甲基环丁烷衍生物 |
-
2010
- 2010-10-08 CN CN201510984778.5A patent/CN105541847B/zh active Active
- 2010-10-08 PT PT107655573T patent/PT2486041E/pt unknown
- 2010-10-08 CN CN201080049430.2A patent/CN102596960B/zh active Active
- 2010-10-08 KR KR1020187033300A patent/KR20180126619A/ko not_active Ceased
- 2010-10-08 ES ES10765557T patent/ES2435491T3/es active Active
- 2010-10-08 EA EA201200565A patent/EA021478B1/ru not_active IP Right Cessation
- 2010-10-08 KR KR1020177023122A patent/KR101921850B1/ko active Active
- 2010-10-08 KR KR1020127009995A patent/KR101805936B1/ko active Active
- 2010-10-08 PL PL10765557T patent/PL2486041T3/pl unknown
- 2010-10-08 EP EP10765557.3A patent/EP2486041B1/en active Active
- 2010-10-08 BR BR112012008267-1A patent/BR112012008267B1/pt active IP Right Grant
- 2010-10-08 JP JP2012533354A patent/JP5946768B2/ja active Active
- 2010-10-08 US US12/901,001 patent/US8486902B2/en active Active
- 2010-10-08 WO PCT/US2010/052011 patent/WO2011044481A1/en not_active Ceased
- 2010-10-08 CA CA2777114A patent/CA2777114C/en active Active
- 2010-10-08 MX MX2012004180A patent/MX2012004180A/es active IP Right Grant
-
2013
- 2013-06-13 US US13/917,124 patent/US8748401B2/en active Active
-
2014
- 2014-04-28 US US14/263,476 patent/US9512161B2/en active Active
-
2015
- 2015-12-17 JP JP2015246515A patent/JP6251232B2/ja active Active
-
2017
- 2017-09-08 JP JP2017172989A patent/JP2017226695A/ja active Pending