CN103168039B - 咪唑并吡啶类syk抑制剂 - Google Patents

咪唑并吡啶类syk抑制剂 Download PDF

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Publication number
CN103168039B
CN103168039B CN201180023252.0A CN201180023252A CN103168039B CN 103168039 B CN103168039 B CN 103168039B CN 201180023252 A CN201180023252 A CN 201180023252A CN 103168039 B CN103168039 B CN 103168039B
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base
pyridine
alkyl
imidazo
indazole
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Expired - Fee Related
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Chinese (zh)
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CN103168039A (zh
Inventor
P·布洛姆格伦
K·S·柯里
J·E·克罗普夫
S·H·李
S·A·米切尔
A·C·施密特
许建军
Z·赵
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Gilead Sciences Inc
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Gilead Sciences Inc
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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CN201180023252.0A 2010-03-11 2011-03-11 咪唑并吡啶类syk抑制剂 Expired - Fee Related CN103168039B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US31277110P 2010-03-11 2010-03-11
US61/312,771 2010-03-11
US31322310P 2010-03-12 2010-03-12
US61/313,223 2010-03-12
PCT/US2011/028194 WO2011112995A1 (en) 2010-03-11 2011-03-11 Imidazopyridines syk inhibitors

Publications (2)

Publication Number Publication Date
CN103168039A CN103168039A (zh) 2013-06-19
CN103168039B true CN103168039B (zh) 2016-08-03

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CN201180023252.0A Expired - Fee Related CN103168039B (zh) 2010-03-11 2011-03-11 咪唑并吡啶类syk抑制剂

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US (3) US9562056B2 (pt-PT)
EP (1) EP2545052B1 (pt-PT)
JP (3) JP5938352B2 (pt-PT)
KR (1) KR101717809B1 (pt-PT)
CN (1) CN103168039B (pt-PT)
AU (3) AU2011226689B2 (pt-PT)
BR (1) BR112012022943A2 (pt-PT)
CA (1) CA2792769C (pt-PT)
ES (1) ES2530449T3 (pt-PT)
HK (1) HK1180689A1 (pt-PT)
MX (1) MX350010B (pt-PT)
NZ (1) NZ602362A (pt-PT)
PT (1) PT2545052E (pt-PT)
WO (1) WO2011112995A1 (pt-PT)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5496915B2 (ja) 2008-02-13 2014-05-21 シージーアイ ファーマシューティカルズ,インコーポレーテッド 6−アリール−イミダゾ[1,2−a]ピラジン誘導体、その製造方法、及びその使用方法
JP5696052B2 (ja) 2008-12-08 2015-04-08 ギリアード コネチカット, インコーポレイテッド イミダゾピラジンsyk阻害剤
HUE030427T2 (en) 2008-12-08 2017-05-29 Gilead Connecticut Inc Imidazopyrazine Syk inhibitors
NZ602362A (en) 2010-03-11 2014-11-28 Gilead Connecticut Inc Imidazopyridines syk inhibitors
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
RU2628616C2 (ru) * 2011-11-03 2017-08-21 Ф. Хоффманн-Ля Рош Аг Бициклические соединения пиперазина
CN107383009B (zh) 2012-06-13 2020-06-09 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
US20130338142A1 (en) * 2012-06-14 2013-12-19 Gilead Connecticut, Inc. Imidazopyrazine syk inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
CN102898426B (zh) * 2012-11-15 2015-04-22 江苏先声药业有限公司 抑制igf-1r酪氨酸激酶活性的吡啶并吡唑类衍生物
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
SG11201508328PA (en) 2013-04-19 2015-11-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
TW201602108A (zh) 2013-07-30 2016-01-16 吉李德康乃狄克公司 脾酪胺酸激酶(Syk)抑制劑之多晶型
AP2016009007A0 (en) 2013-07-30 2016-01-31 Gilead Connecticut Inc Formulation of syk inhibitors
US9376441B2 (en) 2013-07-31 2016-06-28 Gilead Sciences, Inc. Substituted pyrrolidines as SYK inhibitors
PT3076976T (pt) 2013-12-04 2020-12-07 Kronos Bio Inc Métodos para tratar cancros
UY35898A (es) 2013-12-23 2015-07-31 Gilead Sciences Inc ?compuestos inhibidores de syk y composiciones que los comprenden?.
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
WO2015157955A1 (en) * 2014-04-17 2015-10-22 Abbvie Inc. Heterocyclic btk inhibit ors
TW201617074A (zh) * 2014-07-14 2016-05-16 吉李德科學股份有限公司 Syk(脾酪胺酸激酶)抑制劑
KR20170029580A (ko) 2014-07-14 2017-03-15 길리애드 사이언시즈, 인코포레이티드 암을 치료하기 위한 조합물
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CN107438607B (zh) 2015-02-20 2021-02-05 因赛特公司 作为fgfr抑制剂的双环杂环
EP3386993A1 (de) * 2015-12-10 2018-10-17 Bayer Pharma Aktiengesellschaft Substituierte perhydropyrrolo[3,4-c]pyrrol-derivate und ihre verwendung
EP3512519A1 (en) 2016-09-14 2019-07-24 Gilead Sciences, Inc. Syk inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JP7299167B2 (ja) * 2017-06-14 2023-06-27 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド Syk阻害薬及びその使用方法
KR102399996B1 (ko) 2017-08-25 2022-05-20 길리애드 사이언시즈, 인코포레이티드 Syk 억제제의 다형체
AU2019262195B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
CA3099116A1 (en) 2018-05-04 2019-11-07 Incyte Corporation Salts of an fgfr inhibitor
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. PYRROLE AND PYRAZOLE COMPOUNDS AND METHODS OF USE THERE
JP2022521413A (ja) 2019-02-22 2022-04-07 クロノス バイオ インコーポレイテッド Syk阻害剤としての縮合ピラジンの固体形態
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN110183471B (zh) * 2019-05-21 2022-02-15 江苏大学 一种哌嗪类衍生物及制备方法及应用
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP2022552324A (ja) 2019-10-14 2022-12-15 インサイト・コーポレイション Fgfr阻害剤としての二環式複素環
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN112010879B (zh) * 2020-09-15 2021-07-02 山西大学 一种Zn功能配合物及其制备方法和应用
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Fgfr阻害剤としての三環式ヘテロ環
CN113636973B (zh) * 2021-09-07 2023-04-07 山东铂源药业股份有限公司 一种4-(6-氨基吡啶-3-基)哌嗪-1-羧酸叔丁酯的工业化制备方法

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
FR2607813B1 (fr) 1986-12-05 1989-03-31 Montpellier I Universite Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
US5137876A (en) 1990-10-12 1992-08-11 Merck & Co., Inc. Nucleoside antiviral and anti-inflammatory compounds and compositions and methods for using same
DE4327027A1 (de) 1993-02-15 1994-08-18 Bayer Ag Imidazoazine
DE4337609A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Pyrazincarboxamidderivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
DE4337611A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Benzoylguanidine, ihre Herstellung und ihre Verwendung in Arzneimitteln
FR2711993B1 (fr) 1993-11-05 1995-12-01 Rhone Poulenc Rorer Sa Médicaments contenant des dérivés de 7H-imidazol[1,2-a]pyrazine-8-one, les nouveaux composés et leur préparation.
ATE372966T1 (de) 1994-03-25 2007-09-15 Isotechnika Inc Verbesserung der effektivität von arzneimitteln duren deuterierung
US6334997B1 (en) 1994-03-25 2002-01-01 Isotechnika, Inc. Method of using deuterated calcium channel blockers
FR2723373B1 (fr) 1994-08-02 1996-09-13 Rhone Poulenc Rorer Sa Forme purifiee de streptogramines, sa preparation et les compositions pharmaceutiques qui la contiennent
JPH11505524A (ja) 1995-05-01 1999-05-21 藤沢薬品工業株式会社 イミダゾ1,2−aピリジンおよびイミダゾ1,2−aピリデジン誘導体、および骨吸収阻害剤としてのその用途
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
SE9704404D0 (sv) 1997-11-28 1997-11-28 Astra Ab New compounds
KR100834809B1 (ko) * 1999-01-25 2008-06-05 바이오겐 아이덱 엠에이 인코포레이티드 Baff, 관련 차단제 및 면역 반응에서 b 세포와면역글로불린을 촉진 및 억제하는데에 있어서 이들의 용도
DE19948434A1 (de) 1999-10-08 2001-06-07 Gruenenthal Gmbh Substanzbibliothek enthaltend bicyclische Imidazo-5-amine und/oder bicyclische Imidazo-3-amine
JP2001302667A (ja) * 2000-04-28 2001-10-31 Bayer Ag イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体
GB0018473D0 (en) 2000-07-27 2000-09-13 Merck Sharp & Dohme Therapeutic agents
DE10050663A1 (de) 2000-10-13 2002-04-18 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]pyridin-, -pyrimidin- und pyrazin-3-yl-amin-Derivaten zur Herstellung von Medikamenten zur NOS-Inhibierung
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
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
BR0307735A (pt) 2002-02-19 2005-01-25 Upjohn Co Carboxamidas heteroaromáticas com ligação-n em ponte biciclìcas fundidas para o tratamento de doença
KR20050008691A (ko) 2002-04-19 2005-01-21 셀룰러 지노믹스 아이엔씨 이미다조[1,2-a]피라진-8-일 아민, 그의 제조방법 및사용방법
AU2003270489A1 (en) 2002-09-09 2004-03-29 Cellular Genomics, Inc. 6-ARYL-IMIDAZO(1,2-a)PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
KR20050052500A (ko) * 2002-09-19 2005-06-02 쉐링 코포레이션 사이클린 의존성 키나제 억제제로서의 이미다조피리딘
TW200412967A (en) 2002-09-23 2004-08-01 Schering Corp Novel imidazopyrazines as cyclin dependent kinase inhibitors
KR20050057520A (ko) 2002-09-23 2005-06-16 쉐링 코포레이션 사이클린 의존성 키나제 억제제로서의 이미다조피라진
WO2004072081A1 (en) 2003-02-10 2004-08-26 Cellular Genomics, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity
AR043002A1 (es) 2003-02-18 2005-07-13 Altana Pharma Ag Imidazopirazinas 6-substituidos
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7405295B2 (en) 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US20060183746A1 (en) 2003-06-04 2006-08-17 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
WO2005005429A1 (en) 2003-06-30 2005-01-20 Cellular Genomics, Inc. Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-ylamines and methods of inhibition of bruton’s tyrosine kinase by such compounds
WO2005019220A2 (en) 2003-08-11 2005-03-03 Cellular Genomics Inc. Substituted imidazo[1,2-a]pyrazines as modulators of kinase activity
US7144907B2 (en) * 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
WO2005047290A2 (en) * 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
WO2005085252A1 (en) 2004-03-04 2005-09-15 Biofocus Discovery Limited Imidazo ‘1,2-a’ pyrazine compounds which interact with protein kinases
US7713973B2 (en) 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
BRPI0517619A (pt) 2004-11-10 2008-10-14 Cgi Pharmaceuticals Inc entidades quìmicas de imidazo[1,2-a] pirazin-8-ilaminas, suas composições farmacêuticas, uso dos referidos compostos na preparação de medicamento, processo de preparação de medicamento e métodos de utilização dos referidos compostos
WO2007008541A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
JP2009515882A (ja) 2005-11-10 2009-04-16 シェーリング コーポレイション プロテインキナーゼを阻害するための方法
AR056785A1 (es) 2005-11-10 2007-10-24 Schering Corp COMPUESTOS DE IMIDAZO[1,2-A]PIRAZINAS, uTILES COMO INHIBIDORES, REGULADORES O MODULADORES DE PROTEINQUINASAS
AU2007291190A1 (en) * 2006-08-30 2008-03-06 Cellzome Limited Triazole derivatives as kinase inhibitors
US7951818B2 (en) * 2006-12-01 2011-05-31 Galapagos Nv Imidazolopyridine compounds useful for the treatment of degenerative and inflammatory diseases
WO2009077334A1 (en) 2007-12-14 2009-06-25 F. Hoffmann-La Roche Ag Novel imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives
JP5496915B2 (ja) 2008-02-13 2014-05-21 シージーアイ ファーマシューティカルズ,インコーポレーテッド 6−アリール−イミダゾ[1,2−a]ピラジン誘導体、その製造方法、及びその使用方法
JP2011525183A (ja) * 2008-06-20 2011-09-15 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ阻害剤として有用なイミダゾピリジンおよびイミダゾピラジン化合物
CN102066370B (zh) * 2008-07-15 2014-05-14 霍夫曼-拉罗奇有限公司 苯基-咪唑并吡啶类和哒嗪类
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
WO2010038257A1 (ja) * 2008-09-30 2010-04-08 株式会社アドバンテスト プログラマブルデバイス、およびデータ書込方法
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
JP5696052B2 (ja) 2008-12-08 2015-04-08 ギリアード コネチカット, インコーポレイテッド イミダゾピラジンsyk阻害剤
HUE030427T2 (en) 2008-12-08 2017-05-29 Gilead Connecticut Inc Imidazopyrazine Syk inhibitors
NZ602362A (en) 2010-03-11 2014-11-28 Gilead Connecticut Inc Imidazopyridines syk inhibitors
US20140148430A1 (en) 2012-11-26 2014-05-29 Gilead Connecticut, Inc. Imidazopyridines syk inhibitors
AP2016009007A0 (en) 2013-07-30 2016-01-31 Gilead Connecticut Inc Formulation of syk inhibitors
TW201602108A (zh) 2013-07-30 2016-01-16 吉李德康乃狄克公司 脾酪胺酸激酶(Syk)抑制劑之多晶型
US9376441B2 (en) 2013-07-31 2016-06-28 Gilead Sciences, Inc. Substituted pyrrolidines as SYK inhibitors
PT3076976T (pt) 2013-12-04 2020-12-07 Kronos Bio Inc Métodos para tratar cancros
UY35898A (es) 2013-12-23 2015-07-31 Gilead Sciences Inc ?compuestos inhibidores de syk y composiciones que los comprenden?.
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
TW201617074A (zh) 2014-07-14 2016-05-16 吉李德科學股份有限公司 Syk(脾酪胺酸激酶)抑制劑
KR20170029580A (ko) 2014-07-14 2017-03-15 길리애드 사이언시즈, 인코포레이티드 암을 치료하기 위한 조합물
TW201639573A (zh) 2015-02-03 2016-11-16 吉李德科學股份有限公司 有關治療癌症之合併治療
JP2018513173A (ja) 2015-04-21 2018-05-24 ギリアード サイエンシーズ, インコーポレイテッド Syk阻害剤を用いた慢性移植片対宿主病の処置
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
EP3512519A1 (en) 2016-09-14 2019-07-24 Gilead Sciences, Inc. Syk inhibitors

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