ES2530449T3 - Inhibidores de Syk de imidazopiridinas - Google Patents

Inhibidores de Syk de imidazopiridinas Download PDF

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ES2530449T3
ES2530449T3 ES11709600T ES11709600T ES2530449T3 ES 2530449 T3 ES2530449 T3 ES 2530449T3 ES 11709600 T ES11709600 T ES 11709600T ES 11709600 T ES11709600 T ES 11709600T ES 2530449 T3 ES2530449 T3 ES 2530449T3
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pyridin
indazol
imidazo
amino
lower alkyl
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Peter Blomgren
Kevin Currie
Jeffrey Kropf
Seung Lee
Scott Mitchell
Aaron Schmitt
Jianjun Xu
Zhongdong Zhao
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Gilead Connecticut Inc
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Gilead Connecticut Inc
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Abstract

Al menos una entidad química elegida de entre compuestos de la Fórmula I:**Fórmula** y sales farmacéuticamente aceptables de los mismos, en la que R1 se elige de entre fenilo, piridinilo, pirimidinilo, piridazinilo, pirazolilo y tiazolilo, cada uno de los cuales está opcionalmente sustituido, y cada uno de los cuales está además opcionalmente condensado con un grupo heterocíclico o heteroarilo, cada uno de los cuales está opcionalmente sustituido, R2 es heteroarilo opcionalmente sustituido; y R3 se elige de entre hidrógeno o alquilo inferior, con la condición de que si R2 es 3-(4-(terc-butil)benzamido)- 2-metilfenilo, entonces R3 sea alquilo inferior, con la condición de que si R1 es 5-(morfolin-4-carbonil)-piridin- 2-ilo, entonces R3 sea alquilo inferior y con la condición además de que el compuesto de la Fórmula I no sea 1-[((6-{[6-(1H-indazol-6-il)imidazo[1,2-a]piridin-8-il]amino}piridin-3-il)oxi]-2-metilpropan-2-ol 1-((6-{[6-(1H-indazol-6-il)imidazo[1,2-a]piridin-8-il]amino}piridin-3-il)-3-metilazetidin-3-ol; 1-((6-{[6-(1H-indazol-6-il)imidazo[1,2-a]piridin-8-il]amino}piridin-3-il)azetidin-3-ol; 1-etil-N-[6-(1H-indazol-6-il)imidazo[1,2-a]piridin-8-il]-5-metil-1H-pirazol-3-amina; N-[6-(1H-indazol-6-il)imidazo[1,2-a]piridin-8-il]-6-(morfolin-4-il)piridazin-3-amina; 2-N-[6-(1H-indazol-6-il)imidazo[1,2-a]piridin-8-il]-5-N-(2-metoxietil)-5-N-metilpiridin-2,5-diamina; 2-[((6-{[6-(1H-indazol-6-il)imidazo[1,2-a]piridin-8-il]amino}piridin-3-il(metil)amino]etan-1-ol; o N-[6-(1H-indazol-6-il)-5-metilimidazo[1,2-a]piridin-8-il]-5-(morfolin-4-il)piridin-2-amina, en la que alquilo inferior tiene de 1 a 4 átomos de carbono.
ES11709600T 2010-03-11 2011-03-11 Inhibidores de Syk de imidazopiridinas Active ES2530449T3 (es)

Applications Claiming Priority (3)

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

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ES2530449T3 true ES2530449T3 (es) 2015-03-02

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

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2252617A1 (en) 2008-02-13 2010-11-24 CGI Pharmaceuticals, Inc. 6-aryl-imidaz0[l, 2-a]pyrazine derivatives, method of making, and method of use thereof
SG171991A1 (en) 2008-12-08 2011-07-28 Gilead Connecticut Inc Imidazopyrazine syk inhibitors
EA021293B1 (ru) 2008-12-08 2015-05-29 Джилид Коннектикут, Инк. ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
PT2545052E (pt) 2010-03-11 2015-02-18 Gilead Connecticut Inc Inibidores da syk à base de imidazopiridinas
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
KR20140096100A (ko) * 2011-11-03 2014-08-04 에프. 호프만-라 로슈 아게 이환 피페라진 화합물
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
WO2013188856A1 (en) * 2012-06-14 2013-12-19 Gilead Connecticut, Inc. Imidazopyrazine syk inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines 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
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為ｆｇｆｒ抑制劑之雙環雜環
ES2822285T3 (es) 2013-07-30 2021-04-30 Kronos Bio Inc Polimorfo de inhibidores de SYK
MD4684B1 (ro) * 2013-07-30 2020-03-31 Gilead Connecticut INc. Formulări pe bază de imidazopirazine în calitate de inhibitori SYK
EP3027601B1 (en) 2013-07-31 2017-10-25 Gilead Sciences, Inc. Syk inhibitors
EP3076976B1 (en) 2013-12-04 2020-09-02 Gilead Sciences, Inc. Methods for treating cancers
TWI735853B (zh) 2013-12-23 2021-08-11 美商克洛諾斯生技有限公司 脾酪胺酸激酶抑制劑
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
AU2015290000B2 (en) 2014-07-14 2018-05-17 Gilead Sciences, Inc. Combinations for treating cancers
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
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
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2017097671A1 (de) * 2015-12-10 2017-06-15 Bayer Pharma Aktiengesellschaft Substituierte perhydropyrrolo[3,4-c]pyrrol-derivate und ihre verwendung
CA3036384A1 (en) 2016-09-14 2018-03-22 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
CA3065114A1 (en) * 2017-06-14 2018-12-20 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Syk inhibitor and use method therefor
US11384082B2 (en) 2017-08-25 2022-07-12 Kronos Bio, Inc. Hydrates of polymorphs of 6-(1H-indazol-6-YL)-N-(4-morpholinophenyl)-2,3-dihydroimidazo[1,2-A]pyrazin-8-amine bisemsylate as Syk inhibitors
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CA3124569A1 (en) 2018-12-28 2020-07-02 Spv Therapeutics Inc. Cyclin-dependent kinase inhibitors
US11339168B2 (en) 2019-02-22 2022-05-24 Kronos Bio, Inc. Crystalline forms of 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as Syk inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
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
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3159348A1 (en) 2019-11-08 2021-05-14 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
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
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
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
DE4337611A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Benzoylguanidine, ihre Herstellung und ihre Verwendung in Arzneimitteln
DE4337609A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Pyrazincarboxamidderivate, 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.
US6334997B1 (en) 1994-03-25 2002-01-01 Isotechnika, Inc. Method of using deuterated calcium channel blockers
ES2293638T3 (es) 1994-03-25 2008-03-16 Isotechnika, Inc. Mejora de la eficacia de farmacos por deuteracion.
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
MXPA01007464A (es) * 1999-01-25 2003-06-06 Apoxis Sa Baff, inhibidores del mismo y su uso en la modulacion de la respuesta de celula b.
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
WO2003070732A1 (en) 2002-02-19 2003-08-28 Pharmacia & Upjohn Company Fused bicyclic-n-bridged-heteroaromatic carboxamides for the treatment of disease
JP2005530739A (ja) 2002-04-19 2005-10-13 セルラー ジェノミクス，インコーポレーテッド イミダゾ［１，２−ａ］ピラジン−８−イルアミン、生成方法、および使用方法
WO2004022562A1 (en) 2002-09-09 2004-03-18 Cellular Genomics, Inc. 6-ARYL-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
ATE378336T1 (de) * 2002-09-19 2007-11-15 Schering Corp Imidazopyridine als hemmstoffe cyclin abhängiger kinasen
KR20060010709A (ko) 2002-09-23 2006-02-02 쉐링 코포레이션 사이클린 의존성 키나제 억제제로서의 신규한 이미다조피라진
JP4799864B2 (ja) 2002-09-23 2011-10-26 シェーリング コーポレイション サイクリン依存性キナーゼインヒビターとしてのイミダゾピラジン
US7160885B2 (en) 2003-02-10 2007-01-09 Cgi Pharmaceuticals, Inc. Certain 6, 8-(heteroaryl or aryl) disubstituted imidazo[1,2-a]pyrazines as modulators of Hsp90 complex 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
US20050288295A1 (en) 2003-11-11 2005-12-29 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof
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
EP1812442A2 (en) 2004-11-10 2007-08-01 CGI Pharmaceuticals, Inc. Imidazo[1,2-a]pyrazin-8-ylamines useful as modulators of kinase activity
WO2007008541A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
WO2007058942A2 (en) 2005-11-10 2007-05-24 Schering Corporation Imidazopyrazines as protein kinase inhibitors
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
SG174086A1 (en) 2006-08-30 2011-09-29 Cellzome Ltd 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
JP5643105B2 (ja) * 2007-12-14 2014-12-17 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規イミダゾ［１，２−ａ］ピリジン及びイミダゾ［１，２−ｂ］ピリダジン誘導体
EP2252617A1 (en) 2008-02-13 2010-11-24 CGI Pharmaceuticals, Inc. 6-aryl-imidaz0[l, 2-a]pyrazine derivatives, method of making, and method of use thereof
US8338604B2 (en) * 2008-06-20 2012-12-25 Bristol-Myers Squibb Company Imidazopyridine and imidazopyrazine compounds useful as kinase inhibitors
EP2307413B1 (en) * 2008-07-15 2015-09-09 F. Hoffmann-La Roche AG Novel phenyl-imidazopyridines and pyridazines
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
SG171991A1 (en) * 2008-12-08 2011-07-28 Gilead Connecticut Inc Imidazopyrazine syk inhibitors
EA021293B1 (ru) 2008-12-08 2015-05-29 Джилид Коннектикут, Инк. ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
PT2545052E (pt) 2010-03-11 2015-02-18 Gilead Connecticut Inc Inibidores da syk à base de imidazopiridinas
US20140148430A1 (en) 2012-11-26 2014-05-29 Gilead Connecticut, Inc. Imidazopyridines syk inhibitors
ES2822285T3 (es) 2013-07-30 2021-04-30 Kronos Bio Inc Polimorfo de inhibidores de SYK
MD4684B1 (ro) 2013-07-30 2020-03-31 Gilead Connecticut INc. Formulări pe bază de imidazopirazine în calitate de inhibitori SYK
EP3027601B1 (en) 2013-07-31 2017-10-25 Gilead Sciences, Inc. Syk inhibitors
EP3076976B1 (en) 2013-12-04 2020-09-02 Gilead Sciences, Inc. Methods for treating cancers
TWI735853B (zh) 2013-12-23 2021-08-11 美商克洛諾斯生技有限公司 脾酪胺酸激酶抑制劑
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
AU2015290000B2 (en) 2014-07-14 2018-05-17 Gilead Sciences, Inc. Combinations for treating cancers
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
HK1244453A1 (zh) 2015-04-21 2018-08-10 吉利德科学公司 使用syk抑制剂对慢性移植物抗宿主病的治疗
CA3036384A1 (en) 2016-09-14 2018-03-22 Gilead Sciences, Inc. Syk inhibitors
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑

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