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PE20110545A1 - Compuestos de triazolopiridina como inhibidores de jak - Google Patents

Compuestos de triazolopiridina como inhibidores de jak

Info

Publication number
PE20110545A1
PE20110545A1 PE2010001173A PE2010001173A PE20110545A1 PE 20110545 A1 PE20110545 A1 PE 20110545A1 PE 2010001173 A PE2010001173 A PE 2010001173A PE 2010001173 A PE2010001173 A PE 2010001173A PE 20110545 A1 PE20110545 A1 PE 20110545A1
Authority
PE
Peru
Prior art keywords
pyridin
phenyl
triazolo
compounds
jak inhibitors
Prior art date
Application number
PE2010001173A
Other languages
English (en)
Inventor
Bing-Yan Zhu
Michael Siu
Steven R Magnuson
Richard Pastor
He Haiying
Xiao Yisong
Xu Xing
Zhao Junping
Wendy Liu
Christopher A Hurley
Joseph P Lyssikatos
Jun Liang
Zheng Jifu
Original Assignee
Genentech Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Genentech Inc filed Critical Genentech Inc
Publication of PE20110545A1 publication Critical patent/PE20110545A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

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Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE TRIAZOLPIRIDINA DE FORMULA (I) DONDE R1 ES H, FENILO, C(O)ORa, ENTRE OTROS, DONDE Ra ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C6), ENTRE OTROS; R2 ES FENILO, HETEROARILO O HETEROCICLILO; R3, R4 Y R5 SON CADA UNO H, CH3, OCH3, CF3, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-PIPERIDIN-4-IL-4-[8-(3-TRIFLUOROMETIL-ENIL)-[1,2,4]TRIAZOLO[1,5-a]PIRIDIN-2-ILAMINO]-BENZAMIDA; [8-(3-METOXI-ENIL)-[1,2,4]TRIAZOLO[1,5-a]PIRIDIN-2-IL]-(2-METIL-PIRIDIN-4-IL)-AMINA; (3,5-DIFLUORO-FENIL)-[8-(3-METOXI-FENIL)-[1,2,4]TRIAZOLO[1,5-a]PIRIDIN-2-IL]-AMINA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LAS QUINASAS DE JANUS COMO JAK2 SIENDO UTILES EN EL TRATAMIENTO DE CANCER, DIABETES, ESCLEROSIS MULTIPLE, PSORIASIS, POLICITEMIA VERA
PE2010001173A 2008-06-20 2009-06-19 Compuestos de triazolopiridina como inhibidores de jak PE20110545A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US7450608P 2008-06-20 2008-06-20

Publications (1)

Publication Number Publication Date
PE20110545A1 true PE20110545A1 (es) 2011-08-18

Family

ID=41434469

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2010001173A PE20110545A1 (es) 2008-06-20 2009-06-19 Compuestos de triazolopiridina como inhibidores de jak

Country Status (15)

Country Link
US (4) US20100048557A1 (es)
EP (1) EP2288260A4 (es)
JP (1) JP5512665B2 (es)
KR (1) KR20110033223A (es)
CN (1) CN102131389A (es)
AU (1) AU2009259853A1 (es)
BR (1) BRPI0910021A2 (es)
CA (1) CA2727036C (es)
IL (1) IL209763A0 (es)
MX (1) MX2010014005A (es)
PE (1) PE20110545A1 (es)
RU (1) RU2560153C2 (es)
SG (1) SG178812A1 (es)
WO (1) WO2009155551A1 (es)
ZA (1) ZA201008957B (es)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2010137300A (ru) 2008-02-22 2012-03-27 Ф. Хоффманн-Ля Рош Аг (Ch) Модуляторы бета-амилоида
MX2010014005A (es) * 2008-06-20 2011-02-15 Genentech Inc Compuestos de triazolopiridina inhibidores de jak y los metodos.
SG178807A1 (en) 2008-06-20 2012-03-29 Genentech Inc Triazolopyridine jak inhibitor compounds and methods
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶，其組合物及使用其之治療方法
WO2010040661A1 (en) 2008-10-09 2010-04-15 F. Hoffmann-La Roche Ag Modulators for amyloid beta
BRPI0921348A2 (pt) 2008-11-10 2019-09-24 Hoffmann La Roche moduladores heterocíclicos da gama secretase
SG173610A1 (en) * 2009-02-13 2011-09-29 Fovea Pharmaceuticals Sa [1, 2, 4] triazolo [1, 5 -a] pyridines as kinase inhibitors
AU2011211410B2 (en) * 2009-02-13 2013-01-31 Fovea Pharmaceuticals Sa [1,2,4] triazolo [1,5-A] pyridines as kinase inhibitors
EP2438066A2 (en) * 2009-06-05 2012-04-11 Cephalon, Inc. PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a]PYRIDINE DERIVATIVES
TWI462920B (zh) * 2009-06-26 2014-12-01 葛萊伯格有限公司 用於治療退化性及發炎疾病之新穎化合物
EP2343294A1 (en) 2009-11-30 2011-07-13 Bayer Schering Pharma AG Substituted triazolopyridines
NZ601150A (en) * 2010-01-15 2014-06-27 Janssen Pharmaceuticals Inc Novel substituted bicyclic triazole derivatives as gamma secretase modulators
US20110190269A1 (en) * 2010-02-01 2011-08-04 Karlheinz Baumann Gamma secretase modulators
US8486967B2 (en) 2010-02-17 2013-07-16 Hoffmann-La Roche Inc. Heteroaryl substituted piperidines
EP2588105A1 (en) 2010-07-01 2013-05-08 Cellzome Limited Triazolopyridines as tyk2 inhibitors
CN103068828B (zh) 2010-08-27 2015-09-09 默克专利股份公司 三唑并吡嗪衍生物
AU2011328237A1 (en) 2010-11-09 2013-05-23 Cellzome Limited Pyridine compounds and aza analogues thereof as TYK2 inhibitors
JP6033230B2 (ja) * 2010-12-06 2016-11-30 セファロン、インク． 狼瘡の処置のためのヤーヌスキナーゼ２（ｊａｋ２）インヒビタ
AR086042A1 (es) * 2011-04-28 2013-11-13 Galapagos Nv Compuesto util para el tratamiento de enfermedades degenerativas e inflamatorias y composicion farmaceutica
CA2863723C (en) * 2012-02-21 2020-09-22 Carl Deutsch 8-substituted 2-amino-[1,2,4]triazolo[1,5-a]pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors
MX355164B (es) 2012-05-16 2018-04-06 Janssen Pharmaceuticals Inc Derivados de 3,4-dihidro-2h-pirido[1,2-a]pirazin-1,6-diona sustituidos utiles para el tratamiento de la enfermedad de alzheimer (inter alia).
AU2013265307B2 (en) 2012-05-24 2016-04-07 Cellzome Limited Heterocyclyl pyrimidine analogues as TYK2 inhibitors
JP6171003B2 (ja) * 2012-05-24 2017-07-26 ノバルティス アーゲー ピロロピロリジノン化合物
MX2015005428A (es) 2012-11-01 2015-07-21 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak).
CN104918938B (zh) 2012-12-20 2017-08-15 詹森药业有限公司 新颖的作为γ分泌酶调节剂的三环3，4‑二氢‑2H‑吡啶并[1，2‑a]吡嗪‑1，6‑二酮衍生物
WO2014111457A1 (en) 2013-01-17 2014-07-24 Janssen Pharmaceutica Nv Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators
CA2922770A1 (en) * 2013-09-05 2015-03-12 F. Hoffmann-La Roche Ag Triazolopyridine compounds, compositions and methods of use thereof
CA2931817A1 (en) * 2014-01-10 2015-07-16 Eli Lilly And Company Isopropyl triazolo pyridine compounds
JP6552509B2 (ja) * 2014-01-14 2019-07-31 ザ・ジョンズ・ホプキンス・ユニバーシティー 選択的ａｔｐ阻害剤をカプセル化するシクロデキストリン組成物およびその使用
US10562897B2 (en) 2014-01-16 2020-02-18 Janssen Pharmaceutica Nv Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators
CN106687462A (zh) 2014-04-30 2017-05-17 因赛特公司 Jak1抑制剂的制备方法以及其新形式
EP3204007B1 (en) 2014-10-06 2023-12-20 Apm Therapeutics 1, Inc. Triazolopyridine compounds and methods for the treatment of cystic fibrosis
EP3265464A1 (en) * 2015-03-04 2018-01-10 F. Hoffmann-La Roche AG Triazolopyridine compounds and methods of use thereof
CN107949279A (zh) * 2015-07-06 2018-04-20 得克萨斯系统大学评议会 可用作用于治疗人类癌症的抗癌剂的苯甲酰胺或苯扎明化合物
UA123633C2 (uk) 2015-11-03 2021-05-05 Тереванс Байофарма Ар Енд Ді Айпі, Елелсі Сполуки інгібітору jak-кінази для лікування респіраторного захворювання
TW201720828A (zh) 2015-11-23 2017-06-16 赫孚孟拉羅股份公司 治療性化合物及組合物以及其使用方法
CN108368112B (zh) * 2015-12-18 2021-11-02 豪夫迈·罗氏有限公司 治疗性化合物、组合物和它们的使用方法
EP3416967B1 (en) 2016-02-18 2022-02-09 F. Hoffmann-La Roche AG Therapeutic compounds, compositions and methods of use thereof
CN109476638B (zh) 2016-05-05 2021-12-28 豪夫迈·罗氏有限公司 吡唑衍生物、其组合物及治疗用途
WO2018046409A1 (en) * 2016-09-06 2018-03-15 F. Hoffmann-La Roche Ag 8-(azetidin-1-yl)-[1,2,4]triazolo[1,5-a]pyridinyl compounds, compositions and methods of use thereof
WO2018083085A1 (en) 2016-11-02 2018-05-11 F. Hoffmann-La Roche Ag PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
CA3046435A1 (en) 2016-12-29 2018-07-05 F. Hoffmann-La Roche Ag Pyrazolopyrimidine compounds and methods of use thereof
WO2018166993A2 (en) 2017-03-14 2018-09-20 F. Hoffmann-La Roche Ag Pyrazolochlorophenyl compounds, compositions and methods of use thereof
MX2019012950A (es) 2017-05-01 2019-12-16 Theravance Biopharma R&D Ip Llc Metodos de tratamiento mediante el uso de un compuesto inhibidor de jak.
CN110678467B (zh) 2017-05-22 2023-06-13 豪夫迈·罗氏有限公司 治疗化合物和组合物及其使用方法
EP3630766A1 (en) 2017-05-22 2020-04-08 H. Hoffnabb-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
JP2020524692A (ja) 2017-06-21 2020-08-20 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｉｒａｋ４調節因子としてのベンゾフラン
WO2018234342A1 (en) 2017-06-21 2018-12-27 F. Hoffmann-La Roche Ag ISOINDOLINONE DERIVATIVES AS MODULATORS OF IRAK4
JP2020524691A (ja) 2017-06-21 2020-08-20 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ＩＲＡＫ４調節因子としてのピラゾロ［１，５ａ］ピリミジン誘導体
CN111465603B (zh) * 2017-12-19 2024-01-09 勃林格殷格翰国际有限公司 作为γ-分泌酶调节剂的三唑并吡啶
MX2022012285A (es) 2018-03-30 2023-08-15 Incyte Corp Tratamiento de la hidradenitis supurativa mediante el uso de inhibidores de actividad de la cinasa janus (jak).
AU2019320945C1 (en) 2018-08-16 2021-09-30 F. Hoffmann-La Roche Ag Fused ring compounds
NZ775003A (en) 2018-11-09 2024-07-05 Hoffmann La Roche Fused ring compounds
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
WO2020257142A1 (en) 2019-06-18 2020-12-24 Genentech, Inc. Tetrazole-substituted pyrazolopyrimidine inhibitors of jak kinases and uses thereof
KR20220024405A (ko) 2019-06-18 2022-03-03 에프. 호프만-라 로슈 아게 Jak 키나제의 피라졸로피리미딘 설폰 억제제 및 그 사용
JP2022537354A (ja) * 2019-06-18 2022-08-25 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト Ｊａｋキナーゼのピラゾロピリミジンアリールエーテル阻害剤及びその使用
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
CN114728963B (zh) * 2019-11-25 2023-10-31 株式会社大熊制药 新型三唑吡啶衍生物和包括其的药物组合物
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN116057052B (zh) 2020-08-12 2024-09-03 基因泰克公司 喹唑啉化合物之合成
WO2023064458A1 (en) * 2021-10-13 2023-04-20 Yale University Selective jak2 inhibitors and methods of use
CN118574820A (zh) 2022-02-07 2024-08-30 基因泰克公司 用于合成喹唑啉化合物的方法

Family Cites Families (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4847256A (en) * 1986-10-16 1989-07-11 American Cyanamid Company 4,5-dihydro and 4,5,6,7-tetrahydropyrazolo(1,5-A)-pyrimidines
US6579857B1 (en) 1999-06-11 2003-06-17 Evanston Northwestern Healthcare Research Institute Combination cancer therapy comprising adenosine and deaminase enzyme inhibitors
US6355653B1 (en) * 1999-09-06 2002-03-12 Hoffmann-La Roche Inc. Amino-triazolopyridine derivatives
US6514989B1 (en) * 2001-07-20 2003-02-04 Hoffmann-La Roche Inc. Aromatic and heteroaromatic substituted 1,2,4-triazolo pyridine derivatives
EP1435952A1 (en) * 2001-10-08 2004-07-14 F. Hoffmann-La Roche Ag 8-amino- 1,2,4]triazolo 1,5-a]pyridine-6-carboxylic acid amide
US6693116B2 (en) * 2001-10-08 2004-02-17 Hoffmann-La Roche Inc. Adenosine receptor ligands
CA2483306A1 (en) * 2002-04-23 2003-11-06 Shionogi & Co., Ltd. Pyrazolo[1,5-a]pyrimidine derivative and nad(p)h oxidase inhibitor containing the same
US7605155B2 (en) * 2002-09-04 2009-10-20 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
US7161003B1 (en) * 2002-09-04 2007-01-09 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7119200B2 (en) * 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US8580782B2 (en) * 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
US8673924B2 (en) * 2002-09-04 2014-03-18 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
CL2003002353A1 (es) * 2002-11-15 2005-02-04 Vertex Pharma Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic
US20070270408A1 (en) * 2003-04-11 2007-11-22 Novo Nordisk A/S Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines
RS20050868A (en) * 2003-05-27 2007-08-03 Altana Pharma Ag., Pharmaceutical combinations of a proton pump inhibitor and a compound which modifies gastrointestinal motility
US7132435B2 (en) * 2003-07-25 2006-11-07 Pfizer Inc. Compounds
NZ545694A (en) 2003-12-03 2010-04-30 Ym Bioscience Australia Pty Lt Azole-based kinase inhibitors
MXPA06007640A (es) 2004-01-12 2007-04-17 Cytopia Res Pty Ltd Inhibidores de quinasa selectivos.
US7306631B2 (en) * 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
EP1765825A1 (en) * 2004-06-25 2007-03-28 Amgen Inc. Condensed triazoles and indazoles useful in treating citokines mediated diseases and other diseases
WO2006038116A2 (en) 2004-10-07 2006-04-13 Warner-Lambert Company Llc Triazolopyridine derivatives as antibacterial agents
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.
DE602006004844D1 (de) * 2005-02-03 2009-03-05 Vertex Pharma Pyrrolopyrimidine verwendbar als protein kinase inhibitoren
US20060270694A1 (en) 2005-05-03 2006-11-30 Rigel Pharmaceuticals, Inc. JAK kinase inhibitors and their uses
EP1899370A4 (en) 2005-05-12 2009-11-11 Cytopia Res Pty Ltd CRYSTALLINE STRUCTURE AND USE THEREOF
KR101312225B1 (ko) 2005-06-08 2013-09-26 리겔 파마슈티칼스, 인크. Ｊａｋ 경로의 억제를 위한 조성물 및 방법
WO2007013673A1 (en) 2005-07-29 2007-02-01 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
MX346183B (es) * 2005-12-13 2017-03-10 Incyte Holdings Corp Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas heteroarilo-sustituidas como inhibidores de cinasas janus.
EP1960372B1 (en) * 2005-12-15 2015-12-09 Rigel Pharmaceuticals, Inc. Kinase inhibitors and their uses
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
EP1993539A4 (en) 2006-03-02 2010-05-19 Glaxosmithkline Llc THIAZOLONE AS A PI3 KINASE INHIBITOR
EP1873157A1 (en) 2006-06-21 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
CN103641829A (zh) * 2006-08-30 2014-03-19 塞尔佐姆有限公司 作为激酶抑制剂的三唑衍生物
KR20090075714A (ko) 2006-10-30 2009-07-08 노파르티스 아게 소염제로서의 헤테로시클릭 화합물
WO2008129255A1 (en) * 2007-04-18 2008-10-30 Astrazeneca Ab 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer
WO2009017954A1 (en) * 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
MX2010002312A (es) 2007-08-31 2010-03-18 Merck Serono Sa Compuestos de triazolopiridina y su uso como inhibidores de cinasa reguladora de señal de apoptosis.
GB0719803D0 (en) * 2007-10-10 2007-11-21 Cancer Rec Tech Ltd Therapeutic compounds and their use
EA017218B1 (ru) * 2008-03-11 2012-10-30 Инсайт Корпорейшн Производные азетидина и циклобутана как ингибиторы jak-киназ
WO2009131687A2 (en) * 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
MX2010014005A (es) * 2008-06-20 2011-02-15 Genentech Inc Compuestos de triazolopiridina inhibidores de jak y los metodos.
SG178807A1 (en) * 2008-06-20 2012-03-29 Genentech Inc Triazolopyridine jak inhibitor compounds and methods
WO2010010188A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases.
WO2010010184A1 (en) 2008-07-25 2010-01-28 Galapagos Nv [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors
WO2010010189A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
WO2010010186A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
EP2438066A2 (en) 2009-06-05 2012-04-11 Cephalon, Inc. PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a]PYRIDINE DERIVATIVES
US8993756B2 (en) 2011-12-06 2015-03-31 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors

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