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)
Spanish (es)
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

Links

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—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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    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
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  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
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  • Hospice & Palliative Care (AREA)
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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 (enExample)
EP (1) EP2288260A4 (enExample)
JP (1) JP5512665B2 (enExample)
KR (1) KR20110033223A (enExample)
CN (1) CN102131389A (enExample)
AU (1) AU2009259853A1 (enExample)
BR (1) BRPI0910021A2 (enExample)
CA (1) CA2727036C (enExample)
IL (1) IL209763A0 (enExample)
MX (1) MX2010014005A (enExample)
PE (1) PE20110545A1 (enExample)
RU (1) RU2560153C2 (enExample)
SG (1) SG178812A1 (enExample)
WO (1) WO2009155551A1 (enExample)
ZA (1) ZA201008957B (enExample)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2428716T3 (es) 2008-02-22 2013-11-11 F. Hoffmann-La Roche Ag Moduladores de beta-amiloide
EP2296475A4 (en) 2008-06-20 2014-03-05 Genentech Inc TRIAZOLOPYRIDINE COMPOUNDS JAK KINASE INHIBITORS AND METHODS
AU2009259853A1 (en) * 2008-06-20 2009-12-23 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
JP5502089B2 (ja) 2008-10-09 2014-05-28 エフ．ホフマン−ラ ロシュ アーゲー アミロイドβのモジュレーター
WO2010052199A1 (en) 2008-11-10 2010-05-14 F. Hoffmann-La Roche Ag Heterocyclic gamma secretase modulators
AU2011211410B2 (en) * 2009-02-13 2013-01-31 Fovea Pharmaceuticals Sa [1,2,4] triazolo [1,5-A] pyridines as kinase inhibitors
CA2751517A1 (en) * 2009-02-13 2010-08-19 Fovea Pharmaceuticals [1, 2, 4] triazolo [1, 5 -a] pyridines as kinase inhibitors
CA2763900A1 (en) * 2009-06-05 2010-12-09 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
US9145399B2 (en) * 2010-01-15 2015-09-29 Janssen Pharmaceuticals, Inc. 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
WO2012000970A1 (en) 2010-07-01 2012-01-05 Cellzome Limited Triazolopyridines as tyk2 inhibitors
CA2809331C (en) * 2010-08-27 2018-09-25 Merck Patent Gmbh Triazolopyrazine derivatives
JP2014500254A (ja) 2010-11-09 2014-01-09 セルゾーム リミティッド Ｔｙｋ２阻害剤としてのピリジン化合物およびそのアザ類似体
WO2012078574A2 (en) 2010-12-06 2012-06-14 Cephalon, Inc. Janus kinase 2 (jak2) inhibitor for the treatment of lupus
AR086042A1 (es) * 2011-04-28 2013-11-13 Galapagos Nv Compuesto util para el tratamiento de enfermedades degenerativas e inflamatorias y composicion farmaceutica
JP6479476B2 (ja) * 2012-02-21 2019-03-06 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類
ES2585009T3 (es) 2012-05-16 2016-10-03 Janssen Pharmaceuticals, Inc. Derivados de 3,4-dihidro-2H-pirido[1,2-a]pirazina-1,6-diona sustituidos útiles para el tratamiento de (inter alia) enfermedad de Alzheimer
US9296725B2 (en) 2012-05-24 2016-03-29 Cellzome Limited Heterocyclyl pyrimidine analogues as TYK2 inhibitors
CN104321325B (zh) * 2012-05-24 2016-11-16 诺华股份有限公司 吡咯并吡咯烷酮化合物
US9181271B2 (en) 2012-11-01 2015-11-10 Incyte Holdings Corporation Tricyclic fused thiophene derivatives as JAK inhibitors
CA2889249C (en) 2012-12-20 2021-02-16 Francois Paul Bischoff Tricyclic 3,4-dihydro-2h-pyrido[1,2-a]pyrazine-1,6-dione derivatives as gamma secretase modulators
AU2014206834B2 (en) 2013-01-17 2017-06-22 Janssen Pharmaceutica Nv Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators
KR20160050080A (ko) 2013-09-05 2016-05-10 에프. 호프만-라 로슈 아게 트라이아졸로피리딘 화합물, 이의 조성물 및 사용 방법
MX2016008909A (es) * 2014-01-10 2016-10-04 Lilly Co Eli Compuestos de isopropil triazolo piridina.
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
MA39987A (fr) 2014-04-30 2017-03-08 Incyte Corp Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées
AU2015328307B2 (en) * 2014-10-06 2019-11-21 Apm Therapeutics 1, Inc. Triazolopyridine compounds and methods for the treatment of cystic fibrosis
WO2016139212A1 (en) 2015-03-04 2016-09-09 F. Hoffmann-La Roche Ag Triazolopyridine compounds and methods of use thereof
US10112948B2 (en) * 2015-07-06 2018-10-30 The Board Of Regents Of The University Of Texas System Benzamide or benzamine compounds useful as anticancer agents for the treatment of human cancers
US10100049B2 (en) 2015-11-03 2018-10-16 Theravance Biopharma R&D Ip, Llc JAK kinase inhibitor compounds for treatment of respiratory disease
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
JP6929286B2 (ja) * 2015-12-18 2021-09-01 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 治療用化合物、組成物及びその使用方法
CN108473501B (zh) 2016-02-18 2021-07-16 豪夫迈·罗氏有限公司 治疗化合物、其组合物及使用方法
WO2017191098A1 (en) 2016-05-05 2017-11-09 F. Hoffmann-La Roche Ag Pyrazole derivatives, compositions and therapeutic use thereof
CN109890817B (zh) 2016-09-06 2022-06-17 豪夫迈·罗氏有限公司 8-(氮杂环丁烷-1-基)-[1,2,4]三唑并[1,5-a]吡啶基化合物、其组合物和应用方法
WO2018083085A1 (en) 2016-11-02 2018-05-11 F. Hoffmann-La Roche Ag PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
CN110114343B (zh) 2016-12-29 2022-09-06 豪夫迈·罗氏有限公司 吡唑并嘧啶化合物及其使用方法
WO2018166993A2 (en) 2017-03-14 2018-09-20 F. Hoffmann-La Roche Ag Pyrazolochlorophenyl compounds, compositions and methods of use thereof
CA3059785A1 (en) 2017-05-01 2018-11-08 Theravance Biopharma R&D Ip, Llc Methods of treatment using a jak inhibitor compound
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
BR112019024322A2 (pt) 2017-05-22 2020-06-16 F. Hoffmann-La Roche Ag Compostos e composições terapêuticos e métodos de uso dos mesmos
CN111094292A (zh) 2017-06-21 2020-05-01 豪夫迈·罗氏有限公司 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物
JP2020524663A (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調節因子としてのイソインドリノン誘導体
EP3642199B1 (en) 2017-06-21 2022-04-27 F. Hoffmann-La Roche AG Benzofurans as irak4 modulators
EP3672971B1 (en) 2017-12-19 2021-07-14 Boehringer Ingelheim International GmbH Triazolo pyridines as modulators of gamma-secretase
SMT202400306T1 (it) 2018-03-30 2024-09-16 Incyte Corp Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
KR102495687B1 (ko) 2018-08-16 2023-02-07 에프. 호프만-라 로슈 아게 융합 고리 화합물
AR117194A1 (es) 2018-11-09 2021-07-21 Hoffmann La Roche Compuestos de anillos fusionados
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
TW202115069A (zh) 2019-06-18 2021-04-16 瑞士商赫孚孟拉羅股份公司 Ｊａｋ激酶之經四唑取代之吡唑并嘧啶抑制劑及其用途
MA56518A (fr) 2019-06-18 2022-04-27 Hoffmann La Roche Inhibiteurs de sulfone pyrazolopyrimidine de jak kinases et leurs utilisations
JP7716993B2 (ja) 2019-06-18 2025-08-01 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
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
UY38912A (es) * 2019-10-09 2021-05-31 Biocryst Pharm Inc Inhibidores del factor d del complemento para administración oral
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
JP7371253B2 (ja) * 2019-11-25 2023-10-30 デウン ファーマシューティカル カンパニー リミテッド 新規なトリアゾロピリジン誘導体およびこれを含む薬学組成物
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
IL297437A (en) 2020-05-13 2022-12-01 Disc Medicine Inc Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
CN116057052B (zh) 2020-08-12 2024-09-03 基因泰克公司 喹唑啉化合物之合成
CA3223194A1 (en) 2021-06-25 2022-12-29 Theravance Biopharma R&D Ip, Llc Imidazolo indazole compounds as jak inhibitors
WO2023064458A1 (en) * 2021-10-13 2023-04-20 Yale University Selective jak2 inhibitors and methods of use
EP4476205A1 (en) 2022-02-07 2024-12-18 Genentech Inc. Process for synthesis of quinazoline compounds

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
WO2003030904A1 (en) * 2001-10-08 2003-04-17 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
CN100343255C (zh) * 2002-04-23 2007-10-17 盐野义制药株式会社 吡唑并[1,5－a]嘧啶衍生物和含有该衍生物的NAD(P)H氧化酶抑制剂
US7161003B1 (en) * 2002-09-04 2007-01-09 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
US8673924B2 (en) * 2002-09-04 2014-03-18 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7119200B2 (en) * 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7605155B2 (en) * 2002-09-04 2009-10-20 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
AR042052A1 (es) * 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
US20070270408A1 (en) * 2003-04-11 2007-11-22 Novo Nordisk A/S Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines
AU2004243444A1 (en) * 2003-05-27 2004-12-09 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
US7737143B2 (en) 2003-12-03 2010-06-15 Ym Biosciences Australia Pty Ltd Substituted pyrazines as 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
MXPA06014637A (es) * 2004-06-25 2007-02-12 Amgen Inc Triazoles e indazoles condensados utiles en el tratamiento de enfermedades mediadas por citocinas y otras enfermedades.
JP2008515874A (ja) 2004-10-07 2008-05-15 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 抗菌薬
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.
ES2320487T3 (es) * 2005-02-03 2009-05-22 Vertex Pharmaceuticals, Inc. Pirrolopirimidinas utiles como inhibidores de proteina quinasas.
CA2604551A1 (en) 2005-05-03 2007-03-08 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
CN105348203B (zh) 2005-06-08 2018-09-18 里格尔药品股份有限公司 抑制jak途径的组合物和方法
WO2007013673A1 (en) 2005-07-29 2007-02-01 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
DK3184526T3 (en) * 2005-12-13 2019-01-14 Incyte Holdings Corp PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR
WO2007070872A1 (en) 2005-12-15 2007-06-21 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)
US20090203732A1 (en) 2006-03-02 2009-08-13 Dashyant Dhanak Thiazolones for Use as P13 Kinase Inhibitors
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
MX2009002171A (es) * 2006-08-30 2009-05-28 Cellzome Ltd Derivados de triazol como inhibidores de cinasas.
CA2667962A1 (en) 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
US20100204246A1 (en) * 2007-04-18 2010-08-12 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
KR20100075881A (ko) 2007-08-31 2010-07-05 메르크 세로노 에스. 에이. 트리아졸로피리딘 화합물 및 ａｓｋ 저해제로서 이의 용도
GB0719803D0 (en) * 2007-10-10 2007-11-21 Cancer Rec Tech Ltd Therapeutic compounds and their use
ES2602577T3 (es) * 2008-03-11 2017-02-21 Incyte Holdings Corporation Derivados de azetidina y ciclobutano como inhibidores de JAK
WO2009131687A2 (en) * 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
EP2296475A4 (en) * 2008-06-20 2014-03-05 Genentech Inc TRIAZOLOPYRIDINE COMPOUNDS JAK KINASE INHIBITORS AND METHODS
AU2009259853A1 (en) * 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine JAK inhibitor compounds and methods
WO2010010186A1 (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
WO2010010188A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases.
WO2010010189A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
CA2763900A1 (en) 2009-06-05 2010-12-09 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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