MX339139B - Metabolitos del inhibidor de janus cinasa (r)-3-(4-(7h-pirrolo[2,3 -d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo. - Google Patents
Metabolitos del inhibidor de janus cinasa (r)-3-(4-(7h-pirrolo[2,3 -d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo.Info
- Publication number
- MX339139B MX339139B MX2012004948A MX2012004948A MX339139B MX 339139 B MX339139 B MX 339139B MX 2012004948 A MX2012004948 A MX 2012004948A MX 2012004948 A MX2012004948 A MX 2012004948A MX 339139 B MX339139 B MX 339139B
- Authority
- MX
- Mexico
- Prior art keywords
- pyrrolo
- pyrazol
- pyrimidin
- cyclopentylpropanenitrile
- metabolites
- Prior art date
Links
Classifications
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Immunology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Transplantation (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Wood Science & Technology (AREA)
- Genetics & Genomics (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Zoology (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
Abstract
La presente invención provee metabolitos activos de 3-(4-(7H-pirrolo[2, 3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclope ntilpropanonitrilo que modulan la actividad de Janus cinasas y son útiles para el tratamiento de enfermedades relacionadas con la actividad de Janus cinasas que incluyen, por ejemplo, enfermedades relacionadas con el sistema inmune, trastornos cutáneos, trastornos proliferativos mieloides, cáncer y otras enfermedades.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US94369507P | 2007-06-13 | 2007-06-13 | |
PCT/US2008/066658 WO2008157207A2 (en) | 2007-06-13 | 2008-06-12 | Metabolites of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-lh-pyrazol-l-yl)-3- cyclopentylpropanenitrile |
Publications (1)
Publication Number | Publication Date |
---|---|
MX339139B true MX339139B (es) | 2016-05-13 |
Family
ID=40029276
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2009013403A MX2009013403A (es) | 2007-06-13 | 2008-06-12 | Metabolitos del inhibidor de janus cinasa (r)-3-(4-(7h-pirrolo[2,3 -d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo. |
MX2012004948A MX339139B (es) | 2007-06-13 | 2008-06-12 | Metabolitos del inhibidor de janus cinasa (r)-3-(4-(7h-pirrolo[2,3 -d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo. |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2009013403A MX2009013403A (es) | 2007-06-13 | 2008-06-12 | Metabolitos del inhibidor de janus cinasa (r)-3-(4-(7h-pirrolo[2,3 -d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo. |
Country Status (26)
Country | Link |
---|---|
US (5) | US7834022B2 (es) |
EP (1) | EP2173751B1 (es) |
JP (1) | JP5479331B2 (es) |
KR (1) | KR20100049008A (es) |
CN (1) | CN101815717B (es) |
AR (1) | AR067024A1 (es) |
AU (1) | AU2008266182B8 (es) |
BR (1) | BRPI0812563A2 (es) |
CA (1) | CA2689158C (es) |
CL (1) | CL2008001709A1 (es) |
CO (1) | CO6251255A2 (es) |
CR (1) | CR11149A (es) |
EA (1) | EA017790B1 (es) |
EC (1) | ECSP099821A (es) |
ES (1) | ES2448868T3 (es) |
GE (1) | GEP20125534B (es) |
HK (1) | HK1141020A1 (es) |
IL (1) | IL202429A0 (es) |
MX (2) | MX2009013403A (es) |
NZ (1) | NZ581801A (es) |
PL (1) | PL2173751T3 (es) |
PT (1) | PT2173751E (es) |
TW (1) | TWI426911B (es) |
UA (1) | UA99465C2 (es) |
WO (1) | WO2008157207A2 (es) |
ZA (1) | ZA200908820B (es) |
Families Citing this family (78)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20060106020A1 (en) * | 2004-04-28 | 2006-05-18 | Rodgers James D | Tetracyclic inhibitors of Janus kinases |
PT2348023E (pt) | 2005-12-13 | 2015-09-15 | Incyte Corp | Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase |
WO2008079965A1 (en) | 2006-12-22 | 2008-07-03 | 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. |
ME00960B (me) | 2007-06-13 | 2012-06-20 | Incyte Corp | Soli inhibitora janus kinaze, (r)-3-(4-(7h-pirol[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila |
EA020777B1 (ru) * | 2007-11-16 | 2015-01-30 | Инсайт Корпорейшн | 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus |
PE20091485A1 (es) | 2008-02-06 | 2009-10-26 | Novartis Ag | DERIVADOS DE PIRROLO-[2,3-d]-PIRIMIDINA COMO INHIBIDORES DE CINASAS |
EP2288610B8 (en) | 2008-03-11 | 2016-10-12 | 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 |
SG173852A1 (en) * | 2009-02-27 | 2011-09-29 | Ambit Biosciences Corp | Jak kinase modulating quinazoline derivatives and methods of use thereof |
TW201100429A (en) | 2009-05-22 | 2011-01-01 | 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 |
AR076920A1 (es) | 2009-05-22 | 2011-07-20 | Incyte Corp | 3-(4-(7h-pirrolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)octano-o heptano--nitrilo como inhibidores de jak |
WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
US20120034226A1 (en) * | 2009-09-16 | 2012-02-09 | Riken | Diagnostic method of skin inflammatory disease |
ES2435491T3 (es) * | 2009-10-09 | 2013-12-19 | Incyte Corporation | Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo |
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 |
PL2545045T3 (pl) | 2010-03-10 | 2016-08-31 | Incyte Holdings Corp | Pochodne piperydyn-4-yloazetydyny jako inhibitory JAK1 |
CN102985424B (zh) * | 2010-04-14 | 2015-03-11 | 阵列生物制药公司 | 5,7-取代的-咪唑并[1,2-c]嘧啶 |
US20110288107A1 (en) * | 2010-05-21 | 2011-11-24 | Bhavnish Parikh | Topical formulation for a jak inhibitor |
EP2611789A1 (en) | 2010-09-01 | 2013-07-10 | Ambit Biosciences Corporation | Quinazoline compounds and methods of use thereof |
KR102027394B1 (ko) * | 2010-11-02 | 2019-10-01 | 더 트러스티스 오브 콜롬비아 유니버시티 인 더 시티 오브 뉴욕 | 탈모 질환의 치료 방법 |
EP2640725B1 (en) | 2010-11-19 | 2015-01-07 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
KR20140019300A (ko) | 2010-11-19 | 2014-02-14 | 인사이트 코포레이션 | Jak 억제제로서 사이클로부틸 치환된 피롤로피리딘 및 피롤로피리미딘 유도체 |
US9993480B2 (en) | 2011-02-18 | 2018-06-12 | 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 |
JP2014521725A (ja) | 2011-08-10 | 2014-08-28 | ノバルティス・ファルマ・アクチェンゲゼルシャフト | JAKPI3K/mTOR併用療法 |
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 |
RU2014118954A (ru) * | 2011-10-12 | 2015-11-20 | Эррэй Биофарма Инк. | 5,7-ЗАМЕЩЕННЫЕ-ИМИДАЗО[1,2-c]ПИРИМИДИНЫ |
BR112014013224B1 (pt) | 2011-11-30 | 2023-03-07 | Emory University | Inibidores de jak antivirais úteis no tratamento ou prevenção de infecções retrovirais e outras infecções virais |
US10821111B2 (en) | 2011-11-30 | 2020-11-03 | Emory University | Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections |
US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
US20150197525A1 (en) | 2012-06-15 | 2015-07-16 | Concert Pharmaceuticals, Inc. | Deuterated derivatives of ruxolitinib |
EA201492287A1 (ru) | 2012-06-15 | 2015-07-30 | Консерт Фармасьютикалс, Инк. | Дейтерированные производные руксолитиниба |
WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
EA201590272A1 (ru) | 2012-07-27 | 2015-05-29 | Рациофарм Гмбх | Пероральные дозированные формы для модифицированного высвобождения, содержащие руксолитиниб |
UA117572C2 (uk) | 2012-11-01 | 2018-08-27 | Інсайт Холдинґс Корпорейшн | Трициклічні конденсовані похідні тіофену як інгібітори jak |
PT2919766T (pt) | 2012-11-15 | 2021-07-29 | Incyte Corp | Formas farmacêuticas de ruxolitinib de libertação controlada |
US8987443B2 (en) | 2013-03-06 | 2015-03-24 | Incyte Corporation | Processes and intermediates for making a JAK inhibitor |
PE20160126A1 (es) | 2013-05-17 | 2016-02-24 | Incyte Corp | Derivados del bipirazol como inhibidores jak |
CN116036089A (zh) | 2013-08-07 | 2023-05-02 | 因赛特控股公司 | Jak1抑制剂的持续释放剂型 |
SG11201601119XA (en) | 2013-08-20 | 2016-03-30 | Incyte Corp | Survival benefit in patients with solid tumors with elevated c-reactive protein levels |
EA201692011A1 (ru) | 2014-04-08 | 2017-01-30 | Инсайт Корпорейшн | Лечение b-клеточных злокачественных новообразований с применением комбинации ингибиторов jak и pi3k |
PE20170300A1 (es) | 2014-04-30 | 2017-04-19 | Incyte Corp | Procesos para preparar un inhibidor de jak 1 y nuevas formas de este |
US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
CN105218548A (zh) * | 2014-06-09 | 2016-01-06 | 上海海和药物研究开发有限公司 | 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途 |
HUE056329T2 (hu) | 2014-08-11 | 2022-02-28 | Acerta Pharma Bv | BTK-inhibitor és BCL-2-inhibitor terápiás kombinációi |
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 |
WO2016024228A1 (en) | 2014-08-11 | 2016-02-18 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor, a pd-1 inhibitor and/or a pd-l1 inhibitor |
UA119835C2 (uk) | 2016-02-24 | 2019-08-12 | Пфайзер Інк. | ПОХІДНІ ПІРАЗОЛО[1,5-а]ПІРАЗИН-4-ІЛУ ЯК JAK-ІНГІБІТОРИ |
US10561659B2 (en) | 2016-05-04 | 2020-02-18 | Concert Pharmaceuticals, Inc. | Treatment of hair loss disorders with deuterated JAK inhibitors |
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 |
WO2018041989A1 (en) | 2016-09-02 | 2018-03-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosing and treating refractory celiac disease type 2 |
WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
LT3746429T (lt) | 2018-01-30 | 2022-05-10 | Incyte Corporation | (1-(3-fluor-2-(trifluormetil)izonikotinil)piperidin-4-ono) gamybos būdai |
BR122023022247A2 (pt) | 2018-02-16 | 2024-02-20 | Incyte Corporation | Usos de inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas |
MA52655A (fr) | 2018-03-30 | 2021-02-17 | Incyte Corp | Biomarqueurs pour maladie cutanée inflammatoire |
FI3773593T3 (fi) | 2018-03-30 | 2024-06-18 | Incyte Corp | Hidradenitis suppurativan hoito jak-estäjiä käyttäen |
MA52208A (fr) | 2018-04-13 | 2021-02-17 | Incyte Corp | Biomarqueurs pour une maladie du greffon contre l'hôte |
CN117285467A (zh) | 2018-07-31 | 2023-12-26 | 罗索肿瘤学公司 | 喷雾干燥的分散体和制剂 |
KR20210109522A (ko) | 2018-10-31 | 2021-09-06 | 인사이트 코포레이션 | 혈액 질환의 치료를 위한 병용 요법 |
EP3898626A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
WO2020131674A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
KR20210142154A (ko) | 2019-03-21 | 2021-11-24 | 옹쎄오 | 암 치료를 위한 키나제 억제제와 조합된 dbait 분자 |
EP3947737A2 (en) | 2019-04-02 | 2022-02-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
AU2020256720B2 (en) * | 2019-04-12 | 2022-09-01 | PrimeGene (Beijing) Co. Ltd. | Pyrazolopyrazine derived compounds, pharmaceutical composition and use thereof |
EP3955920A1 (en) | 2019-04-16 | 2022-02-23 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels |
WO2021089791A1 (en) | 2019-11-08 | 2021-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
US11738026B2 (en) | 2019-11-22 | 2023-08-29 | Incyte Corporation | Combination therapy comprising an ALK2 inhibitor and a JAK2 inhibitor |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
TW202210471A (zh) | 2020-06-02 | 2022-03-16 | 美商英塞特公司 | 製備jak1抑制劑之方法 |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
WO2022036030A1 (en) | 2020-08-12 | 2022-02-17 | Concert Pharmaceuticals, Inc. | Process for preparing enantiomerically enriched jak inhibitors |
AU2021329303A1 (en) | 2020-08-18 | 2023-04-06 | Incyte Corporation | Process and intermediates for preparing a JAK inhibitor |
PE20231308A1 (es) | 2020-08-18 | 2023-08-24 | Incyte Corp | Proceso e intermedios para preparar un inhibidor de jak1 |
EP4259131A1 (en) | 2020-12-08 | 2023-10-18 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of vitiligo |
WO2023222565A1 (en) | 2022-05-16 | 2023-11-23 | Institut National de la Santé et de la Recherche Médicale | Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation |
Family Cites Families (83)
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 |
CN1105113C (zh) | 1995-07-05 | 2003-04-09 | 纳幕尔杜邦公司 | 杀真菌嘧啶酮 |
CA2224435C (en) | 1995-07-06 | 2008-08-05 | Novartis Ag | Pyrrolopyrimidines and processes for the preparation thereof |
US6232320B1 (en) * | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
EP1090009A2 (en) | 1998-06-04 | 2001-04-11 | Abbott Laboratories | Cell adhesion-inhibiting antinflammatory compounds |
EP1087970B1 (en) | 1998-06-19 | 2004-04-28 | 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 |
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 |
AU777911B2 (en) * | 1999-12-10 | 2004-11-04 | Pfizer Products Inc. | Pyrrolo(2,3-d)pyrimidine compounds |
NZ519121A (en) * | 1999-12-24 | 2004-05-28 | Aventis Pharma Ltd | Azaindoles useful as Syk kinase inhibitors |
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 |
DE60141963D1 (de) * | 2000-06-23 | 2010-06-10 | Mitsubishi Tanabe Pharma Corp | Antitumoreffekt-verstärker |
ES2318605T3 (es) | 2000-06-26 | 2009-05-01 | Pfizer Products Incorporated | Compuestos de pirrolo(2,3-d)pirimidina como agentes inmunosupresores. |
JP4188078B2 (ja) | 2000-06-28 | 2008-11-26 | スミスクライン ビーチャム ピー エル シー | 湿式粉砕法 |
GB0100622D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds V111 |
US20040102455A1 (en) | 2001-01-30 | 2004-05-27 | Burns Christopher John | Method of inhibiting kinases |
US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
JP4286134B2 (ja) | 2001-08-01 | 2009-06-24 | メルク エンド カムパニー インコーポレーテッド | ベンズイミダゾ[4,5−f]イソキノリノン誘導体 |
EA007983B1 (ru) | 2001-09-19 | 2007-02-27 | Авентис Фарма С.А. | Индолизины в качестве ингибиторов киназных белков |
WO2003037347A1 (en) | 2001-10-30 | 2003-05-08 | Novartis Ag | Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity |
GT200200234A (es) | 2001-12-06 | 2003-06-27 | 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 |
EP1562938B1 (en) | 2002-11-04 | 2007-08-29 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyrimidine derivatives as jak inhibitors |
AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
EP1572213A1 (en) | 2002-11-26 | 2005-09-14 | 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 |
AU2004212421B2 (en) | 2003-02-07 | 2009-08-20 | Vertex Pharmaceuticals Incorporated | Heteroaryl substituted pyrolls 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 |
PE20050952A1 (es) | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
MXPA06005882A (es) | 2003-11-25 | 2006-06-27 | Pfizer Prod Inc | Metodo de tratamiento de la aterosclerosis. |
CA2549485A1 (en) | 2003-12-17 | 2005-07-07 | Pfizer Products Inc. | Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection |
US20050165029A1 (en) * | 2004-01-13 | 2005-07-28 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
CN101676285A (zh) | 2004-03-30 | 2010-03-24 | 沃泰克斯药物股份有限公司 | 用作jak和其它蛋白激酶抑制剂的氮杂吲哚 |
US20060106020A1 (en) | 2004-04-28 | 2006-05-18 | Rodgers James D | 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 |
AU2005237254B2 (en) | 2004-05-03 | 2010-02-04 | Novartis Ag | Combinations comprising a S1P receptor agonist and a JAK3 kinase inhibitor |
EP1753428A4 (en) | 2004-05-14 | 2010-09-15 | Abbott Lab | INHIBITORS OF KINASES 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 |
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 |
MX2007006204A (es) | 2004-11-24 | 2007-06-20 | Novartis Ag | Combinaciones que comprenden inhibidores de jak y cuando menos uno de entre inhibidores de bcr-abl, flt-3, fak o raf cinasa. |
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. |
AU2006221065A1 (en) * | 2005-02-03 | 2006-09-14 | Vertex Pharmaceuticals Incorporated | Pyrrolopyrimidines useful as inhibitors of protein kinase |
ATE540948T1 (de) | 2005-05-20 | 2012-01-15 | Vertex Pharma | Pyrrolopyridine als proteinkinasehemmer |
US20070049591A1 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Inhibitors of MAPK/Erk Kinase |
EP2270014A1 (en) * | 2005-09-22 | 2011-01-05 | Incyte Corporation | Azepine 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 |
US20130137681A1 (en) | 2005-12-13 | 2013-05-30 | Incyte Corporation | HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS |
PT2348023E (pt) * | 2005-12-13 | 2015-09-15 | Incyte Corp | Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase |
WO2007076423A2 (en) | 2005-12-22 | 2007-07-05 | Smithkline Beecham Corporation | INHIBITORS OF Akt ACTIVITY |
TW201412738A (zh) | 2006-01-17 | 2014-04-01 | Vertex Pharma | 適合作為傑納斯激酶(janus kinase)抑制劑之氮雜吲哚 |
MX2008012860A (es) | 2006-04-05 | 2009-01-07 | Vertex Pharma | Desazapurinas de utilidad como inhibidores de janus cinasas. |
WO2008079965A1 (en) | 2006-12-22 | 2008-07-03 | Incyte Corporation | Substituted heterocycles as janus kinase inhibitors |
ME00960B (me) | 2007-06-13 | 2012-06-20 | Incyte Corp | Soli inhibitora janus kinaze, (r)-3-(4-(7h-pirol[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila |
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. |
EA020777B1 (ru) | 2007-11-16 | 2015-01-30 | Инсайт Корпорейшн | 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus |
EP2288610B8 (en) | 2008-03-11 | 2016-10-12 | 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 |
TW201100429A (en) | 2009-05-22 | 2011-01-01 | 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 |
AR076920A1 (es) | 2009-05-22 | 2011-07-20 | Incyte Corp | 3-(4-(7h-pirrolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)octano-o heptano--nitrilo como inhibidores de jak |
WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
ES2435491T3 (es) | 2009-10-09 | 2013-12-19 | Incyte Corporation | Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo |
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 |
PL2545045T3 (pl) | 2010-03-10 | 2016-08-31 | Incyte Holdings Corp | Pochodne piperydyn-4-yloazetydyny jako inhibitory JAK1 |
US20110288107A1 (en) | 2010-05-21 | 2011-11-24 | Bhavnish Parikh | Topical formulation for a jak inhibitor |
EP2640725B1 (en) | 2010-11-19 | 2015-01-07 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
KR20140019300A (ko) | 2010-11-19 | 2014-02-14 | 인사이트 코포레이션 | Jak 억제제로서 사이클로부틸 치환된 피롤로피리딘 및 피롤로피리미딘 유도체 |
US9993480B2 (en) | 2011-02-18 | 2018-06-12 | 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 |
JP2014521725A (ja) | 2011-08-10 | 2014-08-28 | ノバルティス・ファルマ・アクチェンゲゼルシャフト | JAKPI3K/mTOR併用療法 |
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 |
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