CA2863723C - 8-substituted 2-amino-[1,2,4]triazolo[1,5-a]pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors - Google Patents

8-substituted 2-amino-[1,2,4]triazolo[1,5-a]pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors Download PDF

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CA2863723C
CA2863723C CA2863723A CA2863723A CA2863723C CA 2863723 C CA2863723 C CA 2863723C CA 2863723 A CA2863723 A CA 2863723A CA 2863723 A CA2863723 A CA 2863723A CA 2863723 C CA2863723 C CA 2863723C
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pyrazin
triazolo
spiro
dihydro
ylamino
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French (fr)
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CA2863723A1 (en
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Carl Deutsch
Daniel Kuhn
Tatjana Ross
Lars Burgdorf
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Merck Patent GmbH
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Merck Patent GmbH
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CA2863723A 2012-02-21 2013-01-22 8-substituted 2-amino-[1,2,4]triazolo[1,5-a]pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors Active CA2863723C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12001153 2012-02-21
EP12001153.1 2012-02-21
PCT/EP2013/000189 WO2013124026A1 (en) 2012-02-21 2013-01-22 8 - substituted 2 -amino - [1,2,4] triazolo [1, 5 -a] pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors

Publications (2)

Publication Number Publication Date
CA2863723A1 CA2863723A1 (en) 2013-08-29
CA2863723C true CA2863723C (en) 2020-09-22

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CA2863723A Active CA2863723C (en) 2012-02-21 2013-01-22 8-substituted 2-amino-[1,2,4]triazolo[1,5-a]pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors

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Country Link
US (1) US9120804B2 (OSRAM)
EP (1) EP2817310B1 (OSRAM)
JP (2) JP6479476B2 (OSRAM)
CN (1) CN104114557B (OSRAM)
AR (1) AR090104A1 (OSRAM)
AU (1) AU2013224421B2 (OSRAM)
CA (1) CA2863723C (OSRAM)
ES (1) ES2674451T3 (OSRAM)
IL (1) IL233982A (OSRAM)
TW (1) TW201339165A (OSRAM)
WO (1) WO2013124026A1 (OSRAM)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2817310B1 (en) * 2012-02-21 2018-03-21 Merck Patent GmbH 8-substituted 2-amino-[1,2,4]triazolo[1,5-a]pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors
NO2699580T3 (OSRAM) 2014-01-24 2018-02-24
BR112017007164A2 (pt) * 2014-10-06 2017-12-19 A Anton Mark implantes de mama cobertos com politetrafluoroetileno expandido para minimizar reação capsular e infecção enquanto reduzindo palpabilidade
BR112018071602B1 (pt) * 2016-04-29 2024-02-27 Iomet Pharma Ltd. Compostos de imidazopiridina substituídos, sua composição e seus usos como inibidores da indolamina 2,3-dioxigenase e/ou triptofano-2,3- dioxigenase
MX378460B (es) 2016-12-22 2025-03-10 Calithera Biosciences Inc Composiciones y métodos para inhibir la actividad de la arginasa.
GB201709456D0 (en) 2017-06-14 2017-07-26 Ucb Biopharma Sprl Therapeutic agents
EP3746071A4 (en) 2018-01-29 2021-09-01 Merck Patent GmbH GCN2 INHIBITORS AND THEIR USES
CN111918651B (zh) * 2018-01-29 2024-01-30 默克专利股份有限公司 Gcn2抑制剂及其用途
CA3089240A1 (en) * 2018-02-07 2019-08-15 Insmed Incorporated Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating anca associated vasculitides
PL3758708T3 (pl) 2018-03-01 2025-03-31 Astrazeneca Ab Kompozycje farmaceutyczne zawierające (2s)-{(1s)-1-cyjano-2-[4-(3-metylo-2-okso-2,3-dihydro-1,3-benzoksazol-5-ilo)fenylo]etylo}-1,4-oksazepano-2-karboksyamid
DE112019001561T5 (de) * 2018-03-27 2020-12-10 Honda Motor Co., Ltd. Positives Elektroden-Aktivmaterial für Fluorid-Ion Sekundäre Batterien, positive Elektrode, die das Aktivmaterial verwendet, Fluorid-Ion Sekundäre Batterie und Verfahren zur Herstellung des Aktivmaterials
EP3781156A4 (en) 2018-04-16 2022-05-18 C4 Therapeutics, Inc. SPIROCYCLIC COMPOUNDS
EP3556760A1 (en) * 2018-04-19 2019-10-23 F. Hoffmann-La Roche AG Spiro compounds
EP3578561A1 (en) * 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
US11998553B2 (en) 2018-07-17 2024-06-04 Insmed Incorporated Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating lupus nephritis
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
US20230257376A1 (en) * 2020-07-14 2023-08-17 Wuhan Ll Science And Technology Development Co., Ltd. Rock inhibitor, and preparation method therefor and use thereof
JP2024518530A (ja) * 2021-05-14 2024-05-01 ビーエム ファーマ コンサルティング ピーティーワイ リミテッド ウイルス感染の予防及び治療のための二環式複素環化合物
WO2022271684A1 (en) * 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
KR102659126B1 (ko) * 2022-03-24 2024-04-19 충남대학교산학협력단 항결핵 약학조성물
IL321931A (en) 2023-01-06 2025-09-01 Insmed Inc New and reversible DPP1 inhibitors and their uses

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
PL194689B1 (pl) 1996-02-13 2007-06-29 Astrazeneca Uk Ltd Pochodne chinazoliny, ich kompozycje farmaceutyczne oraz ich zastosowania
EP0885198B1 (en) 1996-03-05 2001-12-19 AstraZeneca AB 4-anilinoquinazoline derivatives
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
EP1289952A1 (en) 2000-05-31 2003-03-12 AstraZeneca AB Indole derivatives with vascular damaging activity
CN1255391C (zh) 2000-07-07 2006-05-10 安吉奥金尼药品有限公司 作为血管破坏剂的colchinol衍生物
WO2002008213A1 (en) 2000-07-07 2002-01-31 Angiogene Pharmaceuticals Limited Colchinol derivatives as angiogenesis inhibitors
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
KR20100132550A (ko) 2008-04-16 2010-12-17 포톨라 파마슈티컬스, 인코포레이티드 syk 또는 JAK 키나제 억제제로서의 2,6-디아미노-피리미딘-5-일-카르복스아미드
US20100048557A1 (en) 2008-06-20 2010-02-25 Bing-Yan Zhu Triazolopyridine JAK Inhibitor Compounds and Methods
WO2010010184A1 (en) * 2008-07-25 2010-01-28 Galapagos Nv [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors
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
KR20120044966A (ko) * 2009-06-05 2012-05-08 세파론, 인코포레이티드 1,2,4-트리아졸로〔1,5a〕 피리딘 유도체의 제조 및 용도
US8946266B2 (en) * 2009-07-15 2015-02-03 Janssen Pharmaceuticals, Inc. Substituted triazole and imidazole derivatives as gamma secretase modulators
EP2523949B1 (en) * 2010-01-15 2014-08-20 Janssen Pharmaceuticals Inc. Novel substituted 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
JP4940370B2 (ja) * 2010-06-29 2012-05-30 キヤノン株式会社 電子写真感光体、プロセスカートリッジおよび電子写真装置
JP5951610B2 (ja) * 2010-08-27 2016-07-13 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 トリアゾロピラジン誘導体
EP2817310B1 (en) * 2012-02-21 2018-03-21 Merck Patent GmbH 8-substituted 2-amino-[1,2,4]triazolo[1,5-a]pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors

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WO2013124026A8 (en) 2014-01-09
IL233982A (en) 2017-05-29
US9120804B2 (en) 2015-09-01
JP6479476B2 (ja) 2019-03-06
CA2863723A1 (en) 2013-08-29
EP2817310A1 (en) 2014-12-31
TW201339165A (zh) 2013-10-01
AU2013224421A1 (en) 2014-10-02
CN104114557B (zh) 2017-10-24
AU2013224421B2 (en) 2017-03-02
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