CL2011002115A1 - Compuestos derivados de 5-fenil-1h-piridin-2-ona y 5-fenil-pirazin-2-ona, inhibidores de la tirosina-quinasa de bruton (btk); proceso de preparación de los compuestos, compuesto intermediario, composición farmacéutica y uso en el tratamiento de enfermedades inflamatorias y/o autoinmunes. - Google Patents

Compuestos derivados de 5-fenil-1h-piridin-2-ona y 5-fenil-pirazin-2-ona, inhibidores de la tirosina-quinasa de bruton (btk); proceso de preparación de los compuestos, compuesto intermediario, composición farmacéutica y uso en el tratamiento de enfermedades inflamatorias y/o autoinmunes.

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Publication number
CL2011002115A1
CL2011002115A1 CL2011002115A CL2011002115A CL2011002115A1 CL 2011002115 A1 CL2011002115 A1 CL 2011002115A1 CL 2011002115 A CL2011002115 A CL 2011002115A CL 2011002115 A CL2011002115 A CL 2011002115A CL 2011002115 A1 CL2011002115 A1 CL 2011002115A1
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CL
Chile
Prior art keywords
phenyl
compounds
btk
inflammatory
pharmaceutical composition
Prior art date
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CL2011002115A
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English (en)
Inventor
Steven Joseph Berthel
Fariborz Firooznia
Daniel Fishlock
Jun-Bae Hong
Yan Lou
Matthew C Lucas
Thimothy D Owens
Keshab Sarma
Zachary Kevin Sweeney
Joshua Paul Gergely Taygerly
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Hoffmann La Roche
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CL2011002115A1 publication Critical patent/CL2011002115A1/es

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Abstract

COMPUESTOS DERIVADOS DE 5-FENIL-1H-PIRIDIN-2-ONA Y S-FENIL-PIRIDIN-2-ONA, INHIBIDORES DE LA TIROSINA-QUINASA DE BRUTON (BTK) DE FÓRMULA GENERAL A: PROCESO DE PREPARACIÓN DE LOS COMPUESTOS, COMPUESTO INTERMEDIARIO; COMPOSICIÓN FARMACÉUTICA Y USO EN EL<br /> TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS Y/O AUTOINMUNES.<br />  
CL2011002115A 2009-03-02 2011-08-30 Compuestos derivados de 5-fenil-1h-piridin-2-ona y 5-fenil-pirazin-2-ona, inhibidores de la tirosina-quinasa de bruton (btk); proceso de preparación de los compuestos, compuesto intermediario, composición farmacéutica y uso en el tratamiento de enfermedades inflamatorias y/o autoinmunes. CL2011002115A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US20902109P 2009-03-02 2009-03-02
US30006410P 2010-02-01 2010-02-01

Publications (1)

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CL2011002115A1 true CL2011002115A1 (es) 2012-03-30

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CL2011002115A CL2011002115A1 (es) 2009-03-02 2011-08-30 Compuestos derivados de 5-fenil-1h-piridin-2-ona y 5-fenil-pirazin-2-ona, inhibidores de la tirosina-quinasa de bruton (btk); proceso de preparación de los compuestos, compuesto intermediario, composición farmacéutica y uso en el tratamiento de enfermedades inflamatorias y/o autoinmunes.

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US (1) US8299077B2 (es)
EP (1) EP2403846B1 (es)
JP (1) JP5512707B2 (es)
KR (1) KR101347978B1 (es)
CN (2) CN102341383B (es)
AR (1) AR076066A1 (es)
AU (1) AU2010220435B2 (es)
BR (1) BRPI1009112A2 (es)
CA (1) CA2753341C (es)
CL (1) CL2011002115A1 (es)
ES (1) ES2607644T3 (es)
HK (1) HK1216887A1 (es)
IL (1) IL214351A0 (es)
MX (1) MX339583B (es)
PE (2) PE20151336A1 (es)
RU (1) RU2542585C2 (es)
SG (1) SG173816A1 (es)
TW (2) TWI519529B (es)
WO (1) WO2010100070A1 (es)
ZA (1) ZA201301679B (es)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9782405B2 (en) 2011-11-03 2017-10-10 Genentech, Inc. Heteroaryl pyridone and aza-pyrodine compounds
US11149019B2 (en) 2017-10-11 2021-10-19 Daewoong Pharmaceutical Co., Ltd. Phenylpyridine derivative and pharmaceutical composition comprising the same

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8258134B2 (en) * 2008-04-16 2012-09-04 Hoffmann-La Roche Inc. Pyridazinone glucokinase activators
PE20110164A1 (es) * 2008-07-02 2011-03-28 Hoffmann La Roche Nuevas fenilpirazinonas como inhibidores de quinasa
CA2730930C (en) 2008-07-16 2015-01-13 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
SI2411393T1 (sl) 2009-03-23 2014-03-31 Glenmark Pharmaceuticals S.A. Kondenzirani pirimidin-dionski derivati kot TRPA 1 modulatorji
CA3007787C (en) 2010-06-03 2020-03-10 Pharmacyclics Llc The use of inhibitors of bruton's tyrosine kinase (btk)
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
US8975260B2 (en) 2010-09-01 2015-03-10 Genetech, Inc Pyridazinones, method of making, and method of use thereof
CA2809836C (en) * 2010-09-01 2019-01-15 Gilead Connecticut, Inc. Pyridinones/pyrazinones, method of making, and method of use thereof for the treatment of disorders mediated by bruton's tyrosine kinase
AU2012257802A1 (en) 2011-05-17 2013-10-31 F. Hoffmann-La Roche Ag Inhibitors of Bruton's tyrosine kinase
MX2014000130A (es) * 2011-06-28 2014-05-01 Pharmacyclics Inc Procedimientos y composiciones para la inhibicion de resorcion osea.
JP2014520863A (ja) 2011-07-13 2014-08-25 ファーマサイクリックス,インク. Bruton型チロシンキナーゼの阻害剤
CA2841801A1 (en) * 2011-08-17 2013-02-21 F.Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
MX391121B (es) * 2011-10-19 2025-03-19 Pharmacyclics Llc Uso de inhibidores de la tirosina cinasa de bruton (btk).
MX2014005282A (es) * 2011-11-03 2014-05-30 Hoffmann La Roche Compuestos de 8-fluoroftalazin-1 (2h) -ona.
EP2773639B1 (en) * 2011-11-03 2017-04-26 F. Hoffmann-La Roche AG Alkylated piperazine compounds as inhibitors of btk activity
JP5832664B2 (ja) * 2011-12-09 2015-12-16 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft ブルトン型チロシンキナーゼの阻害剤
JP6182593B2 (ja) 2012-04-20 2017-08-16 アドヴィーナス セラピューティクス リミテッド 置換ヘテロ二環化合物、組成物及び医薬並びにそれらの用途
WO2013157021A1 (en) 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
CN104704129A (zh) 2012-07-24 2015-06-10 药品循环公司 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变
SG11201500499TA (en) 2012-08-10 2015-03-30 Boehringer Ingelheim Int Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors
WO2014040965A1 (en) 2012-09-13 2014-03-20 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
JP6088063B2 (ja) * 2012-11-16 2017-03-01 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft ブルトン型チロシンキナーゼの阻害剤
MX2015006457A (es) * 2012-11-30 2015-08-14 Hoffmann La Roche Inhibidores de la tirosina cinasa de bruton.
RU2618529C2 (ru) * 2013-03-05 2017-05-04 Ф. Хоффманн-Ля Рош Аг Ингибиторы тирозинкиназы брутона
EP2964642B1 (en) * 2013-03-05 2017-11-15 F. Hoffmann-La Roche AG Inhibitors of bruton's tyrosine kinase
KR20160061911A (ko) 2013-04-08 2016-06-01 데니스 엠. 브라운 최적하 투여된 화학 화합물의 치료 효과
CA2902686C (en) 2013-04-25 2017-01-24 Beigene, Ltd. Fused heterocyclic compounds as protein kinase inhibitors
CN104177338B (zh) * 2013-05-22 2018-04-03 南京勇山生物科技有限公司 一类布鲁顿激酶抑制剂
CN104211703B (zh) * 2013-05-30 2018-04-03 南京勇山生物科技有限公司 一类作为布鲁顿激酶抑制剂的稠杂环化合物
WO2015000949A1 (en) * 2013-07-03 2015-01-08 F. Hoffmann-La Roche Ag Heteroaryl pyridone and aza-pyridone amide compounds
CN112472699A (zh) 2013-07-26 2021-03-12 种族肿瘤学公司 改善比生群及衍生物的治疗益处的组合方法
DK3026050T3 (en) * 2013-07-26 2019-02-18 Carna Biosciences Inc NEW TRIAZINE DERIVATIVE
US9415050B2 (en) 2013-08-12 2016-08-16 Pharmacyclics Llc Methods for the treatment of HER2 amplified cancer
CN112552401B (zh) 2013-09-13 2023-08-25 广州百济神州生物制药有限公司 抗pd1抗体及其作为治疗剂与诊断剂的用途
US9512084B2 (en) * 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
WO2015082583A1 (en) * 2013-12-05 2015-06-11 F. Hoffmann-La Roche Ag Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality
US9802920B2 (en) * 2013-12-13 2017-10-31 Hoffman-La Roche Inc. Inhibitors of bruton's tyrosine kinase
US9885086B2 (en) 2014-03-20 2018-02-06 Pharmacyclics Llc Phospholipase C gamma 2 and resistance associated mutations
CN106604742B (zh) 2014-07-03 2019-01-11 百济神州有限公司 抗pd-l1抗体及其作为治疗剂及诊断剂的用途
CN106922146B (zh) * 2014-10-02 2020-05-26 豪夫迈·罗氏有限公司 用于治疗由布鲁顿酪氨酸激酶(btk)介导的疾病的吡唑甲酰胺化合物
CN104402828A (zh) * 2014-11-05 2015-03-11 定陶县友帮化工有限公司 一种3-氨基-4-溴-6-氯哒嗪的合成方法
TW201702218A (zh) 2014-12-12 2017-01-16 美國杰克森實驗室 關於治療癌症、自體免疫疾病及神經退化性疾病之組合物及方法
EP3042903B1 (en) 2015-01-06 2019-08-14 Impetis Biosciences Ltd. Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
HUE062258T2 (hu) 2015-07-02 2023-10-28 Acerta Pharma Bv (S)-4-(8-amino-3-(1-(but-2-inoil)pirrolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamid szilárd alakjai és készítményei
RU2608128C1 (ru) * 2015-11-12 2017-01-13 федеральное государственное бюджетное образовательное учреждение высшего образования "Ростовский государственный медицинский университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО РостГМУ Минздрава России) Способ лечения больных с х-сцепленной агаммаглобулинемией
US10570118B2 (en) * 2016-01-13 2020-02-25 Boehringer Ingelheim International Gmbh Isoquinolones as BTK inhibitors
RU2749038C2 (ru) * 2016-06-22 2021-06-03 Шанхай Фокон Фармасьютикал Ко., Лтд. Замещенные пирроло[2,3-d]пиридазин-4-оны и пиразоло[3,4-d]пиридазин-4-оны в качестве ингибиторов протеинкиназы
US10864203B2 (en) 2016-07-05 2020-12-15 Beigene, Ltd. Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer
JP7214632B2 (ja) 2016-07-21 2023-01-30 バイオジェン エムエー インク. ブルトン型チロシンキナーゼ阻害剤のコハク酸塩形態および組成物
WO2018033853A2 (en) 2016-08-16 2018-02-22 Beigene, Ltd. Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
WO2018033135A1 (en) 2016-08-19 2018-02-22 Beigene, Ltd. Use of a combination comprising a btk inhibitor for treating cancers
IL292938A (en) 2016-09-19 2022-07-01 Mei Pharma Inc Combined treatment
US11071721B2 (en) 2016-12-02 2021-07-27 Genentech, Inc. Bicyclic amide compounds and methods of use thereof
CA3045339A1 (en) 2016-12-03 2018-06-07 Juno Therapeutics, Inc. Methods and compositions for use of therapeutic t cells in combination with kinase inhibitors
US11555038B2 (en) 2017-01-25 2023-01-17 Beigene, Ltd. Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
EP3645569A4 (en) 2017-06-26 2021-03-24 BeiGene, Ltd. IMMUNOTHERAPY FOR LIVER CELL CARCINOMA
BR112020000771A2 (pt) 2017-07-14 2020-07-14 F. Hoffmann-La Roche Ag compostos de cetona bicíclica e métodos de uso dos mesmos
US11377449B2 (en) 2017-08-12 2022-07-05 Beigene, Ltd. BTK inhibitors with improved dual selectivity
AR113811A1 (es) 2017-10-31 2020-06-10 Hoffmann La Roche Sulfonas y sulfóxidos bicíclicos y métodos de uso de los mismos
WO2019108795A1 (en) 2017-11-29 2019-06-06 Beigene Switzerland Gmbh Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
CN111961035B (zh) * 2019-05-20 2022-11-01 南京科技职业学院 一类含有羟基异喹啉类结构的化合物、药物组合物以及其应用
US20220249491A1 (en) 2019-06-10 2022-08-11 Beigene Switzerland Gmbh Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
EP4545537A3 (en) * 2021-05-05 2025-07-16 F. Hoffmann-La Roche AG Process for preparing btk inhibitors
US20250145574A1 (en) * 2022-02-10 2025-05-08 Carna Biosciences, Inc. Fluoroisoquinoline compound and production method thereof
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
CN119080748A (zh) * 2024-08-29 2024-12-06 中南大学 一种靶向brd7抑瘤蛋白的增稳剂及其在制备治疗实体肿瘤药物中的应用

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
MY140868A (en) * 2004-12-24 2010-01-29 Astrazeneca Ab Amide derivatives
AR063706A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
PE20081370A1 (es) 2006-09-11 2008-11-28 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas
CN101835755B (zh) 2007-10-23 2013-12-11 霍夫曼-拉罗奇有限公司 激酶抑制剂
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
US7683064B2 (en) 2008-02-05 2010-03-23 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
PL2242749T3 (pl) * 2008-02-05 2013-09-30 Hoffmann La Roche Nowe pirydynony i pirydazynony
PH12012502374A1 (en) 2008-06-24 2014-11-12 Hoffmann La Roche Novel substituted pyridin-2-ones and pyridazin-3-ones
PE20110164A1 (es) * 2008-07-02 2011-03-28 Hoffmann La Roche Nuevas fenilpirazinonas como inhibidores de quinasa

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9782405B2 (en) 2011-11-03 2017-10-10 Genentech, Inc. Heteroaryl pyridone and aza-pyrodine compounds
US11149019B2 (en) 2017-10-11 2021-10-19 Daewoong Pharmaceutical Co., Ltd. Phenylpyridine derivative and pharmaceutical composition comprising the same

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