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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
Authority
CL
Chile
Prior art keywords
phenyl
compounds
btk
inflammatory
pharmaceutical composition
Prior art date
Application number
CL2011002115A
Other languages
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
Original Assignee
Hoffmann La Roche
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42097405&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CL2011002115(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CL2011002115A1 publication Critical patent/CL2011002115A1/es

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    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
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    • C07D—HETEROCYCLIC COMPOUNDS
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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)

Publication Number Publication Date
CL2011002115A1 true CL2011002115A1 (es) 2012-03-30

Family

ID=42097405

Family Applications (1)

Application Number Title Priority Date Filing Date
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.

Country Status (20)

Country Link
US (1) US8299077B2 (es)
EP (1) EP2403846B1 (es)
JP (1) JP5512707B2 (es)
KR (1) KR101347978B1 (es)
CN (2) CN105001206A (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) TW201439080A (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
PT2300459E (pt) * 2008-07-02 2013-07-04 Hoffmann La Roche Novas fenilpirazinonas utilizadas como inibidores de cinase
EP3311818A3 (en) 2008-07-16 2018-07-18 Pharmacyclics, LLC Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
EP2411393B1 (en) 2009-03-23 2014-01-22 Glenmark Pharmaceuticals S.A. Fused pyrimidine-dione derivatives as trpa1 modulators
EA031737B1 (ru) 2010-06-03 2019-02-28 Фармасайкликс, Инк. Применение ингибиторов тирозинкиназы брутона (btk) для лечения лейкоза и лимфомы
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
ES2561277T3 (es) * 2010-09-01 2016-02-25 Gilead Connecticut, Inc. Piridinonas/pirazinonas, procedimiento de preparación y procedimiento de utilización de las mismas
ES2537190T3 (es) * 2010-09-01 2015-06-03 Gilead Connecticut, Inc. Piridazinonas, procedimiento de preparación y procedimientos de utilización de las mismas
KR101585753B1 (ko) 2011-05-17 2016-01-14 에프. 호프만-라 로슈 아게 브루톤 티로신 키나아제의 억제제
EP2726077A4 (en) * 2011-06-28 2014-12-10 Pharmacyclics Inc METHODS AND COMPOSITIONS FOR INHIBITING BONE RESORPTION
EP2731612A4 (en) 2011-07-13 2015-04-08 Pharmacyclics Inc BRUTON TYROSINE KINASE HEMMER
WO2013024078A1 (en) * 2011-08-17 2013-02-21 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
CN110801454A (zh) * 2011-10-19 2020-02-18 药品循环有限责任公司 布鲁顿酪氨酸激酶(btk)抑制剂的用途
BR112014010460A2 (pt) * 2011-11-03 2017-04-18 Hoffmann La Roche composto, composição farmacêutica, processo para produzir uma composição farmacêutica, método de tratamento, kit e uso de uma composição farmacêutica
JP5976828B2 (ja) * 2011-11-03 2016-08-24 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｂｔｋ活性阻害剤としてのアルキル化ピペラジン化合物
CA2854603A1 (en) * 2011-12-09 2013-06-13 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
AU2013250726B2 (en) 2012-04-20 2017-01-05 Advinus Therapeutics Limited Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
WO2013157021A1 (en) 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
EP3550031A1 (en) 2012-07-24 2019-10-09 Pharmacyclics, LLC Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
MX2015001802A (es) 2012-08-10 2015-05-07 Boehringer Ingelheim Int Compuestos heteroaromaticos como inhibidores de btk.
RU2015111133A (ru) * 2012-09-13 2016-11-10 Ф. Хоффманн-Ля Рош Аг Ингибиторы тирозинкиназы брутона
MX2015006162A (es) * 2012-11-16 2015-08-14 Hoffmann La Roche Inhibidores de la tirosina-cinasa de bruton.
CA2891634A1 (en) * 2012-11-30 2014-06-05 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
KR101737724B1 (ko) 2013-03-05 2017-05-29 에프. 호프만-라 로슈 아게 브루톤 티로신 키나아제의 억제제
EP2964642B1 (en) 2013-03-05 2017-11-15 F. Hoffmann-La Roche AG Inhibitors of bruton's tyrosine kinase
AU2014251038A1 (en) 2013-04-08 2015-11-26 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
EA028756B1 (ru) 2013-04-25 2017-12-29 Бэйджин, Лтд. Конденсированные гетероциклические соединения в качестве ингибиторов протеинкиназы
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
JP6165977B2 (ja) * 2013-07-03 2017-07-19 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ヘテロアリールピリドン及びアザ−ピリドンアミド化合物
CN105764502A (zh) 2013-07-26 2016-07-13 现代化制药公司 改善比生群及其类似物及衍生物的治疗益处的组合方法
EP3026050B1 (en) 2013-07-26 2018-11-07 Carna Biosciences Inc. Novel triazine derivative
US9415050B2 (en) 2013-08-12 2016-08-16 Pharmacyclics Llc Methods for the treatment of HER2 amplified cancer
PT3702373T (pt) 2013-09-13 2022-09-27 Beigene Switzerland Gmbh Anticorpos anti-pd1 e a sua utilização como agentes terapêuticos e de diagnóstico
US9512084B2 (en) 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
RU2646758C2 (ru) * 2013-12-05 2018-03-07 Ф. Хоффманн-Ля Рош Аг Гетероарил пиридоны и азапиридоны с электрофильной функциональностью
WO2015086636A1 (en) * 2013-12-13 2015-06-18 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
EP3119910A4 (en) 2014-03-20 2018-02-21 Pharmacyclics LLC Phospholipase c gamma 2 and resistance associated mutations
JP6526189B2 (ja) 2014-07-03 2019-06-05 ベイジーン リミテッド 抗ｐｄ−ｌ１抗体並びにその治療及び診断のための使用
JP6507234B2 (ja) * 2014-10-02 2019-04-24 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ブルトンチロシンキナーゼ（ｂｔｋ）によって介入される障害の処置における使用のためのピラゾールカルボキサミド化合物
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
WO2017002095A1 (en) 2015-07-02 2017-01-05 Acerta Pharma B.V. Solid forms and formulations of (s)-4-(8-amino-3-(1 -(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-n-(pyridin-2-yl)benzamide
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
JP6916185B2 (ja) * 2016-01-13 2021-08-11 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｔｋ阻害剤としてのイソキノロン類
JP6966044B2 (ja) * 2016-06-22 2021-11-10 シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド タンパク質キナーゼ阻害剤としての置換されているピロロ［２，３−ｄ］ピリダジン−４−オン及びピラゾロ［３，４−ｄ］ピリダジン−４−オン
CN109475536B (zh) 2016-07-05 2022-05-27 百济神州有限公司 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合
US11174243B2 (en) 2016-07-21 2021-11-16 Sunesis Pharmaceuticals, Inc. Succinate forms and compositions of Bruton's tyrosine kinase inhibitors
SG11201901141WA (en) 2016-08-16 2019-03-28 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
CN118252927A (zh) 2016-08-19 2024-06-28 百济神州有限公司 使用包含btk抑制剂的组合产品治疗癌症
CA3037364A1 (en) 2016-09-19 2018-03-22 Mei Pharma, Inc. Combination therapy
TW201831478A (zh) 2016-12-02 2018-09-01 瑞士商赫孚孟拉羅股份公司 雙環醯胺化合物及其使用方法
CN110545826A (zh) 2016-12-03 2019-12-06 朱诺治疗学股份有限公司 用于与激酶抑制剂组合使用治疗性t细胞的方法和组合物
WO2018137681A1 (en) 2017-01-25 2018-08-02 Beigene, Ltd. Crystalline forms of (s) -7- (1- (but-2-ynoyl) piperidin-4-yl) -2- (4-phenoxyphenyl) -4, 5, 6, 7-tetrahy dropyrazolo [1, 5-a] pyrimidine-3-carboxamide, preparation, and uses thereof
JP2020525411A (ja) 2017-06-26 2020-08-27 ベイジーン リミテッド 肝細胞癌のための免疫療法
KR102664604B1 (ko) 2017-07-14 2024-05-14 에프. 호프만-라 로슈 아게 이환형 케톤 화합물 및 이의 사용 방법
WO2019034009A1 (en) 2017-08-12 2019-02-21 Beigene, Ltd. BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY
AU2018360270A1 (en) 2017-10-31 2020-03-26 F. Hoffmann-La Roche Ag Bicyclic sulfones and sulfoxides and methods of use thereof
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
MX2020006587A (es) 2017-12-22 2020-12-10 Ravenna Pharmaceuticals Inc Derivados de aminopiridina como inhibidores de fosfatidilinositol fosfato cinasa.
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
EP4334311B1 (en) * 2021-05-05 2024-12-25 F. Hoffmann-La Roche AG Process for preparing btk inhibitors
CN118715209A (zh) * 2022-02-10 2024-09-27 卡尔那生物科学株式会社 氟代异喹啉化合物及其制造方法
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
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
WO2005014599A1 (en) 2003-06-04 2005-02-17 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds
RU2396259C2 (ru) * 2004-12-24 2010-08-10 Астразенека Аб Амидные производные
AR063707A1 (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 farmacéuticas que las comprenden.
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.
EP2205564B1 (en) * 2007-10-23 2014-07-30 F. Hoffmann-La Roche AG Novel kinase inhibitors
CN101952283B (zh) 2007-12-14 2013-04-17 霍夫曼-拉罗奇有限公司 咪唑并[1，2-a]吡啶和咪唑并[1，2-b]哒嗪衍生物
US7683064B2 (en) 2008-02-05 2010-03-23 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
NZ586916A (en) * 2008-02-05 2012-06-29 Hoffmann La Roche Novel pyridinones and pyridazinones
CA2728016C (en) * 2008-06-24 2017-02-28 F. Hoffmann-La Roche Ag Novel substituted pyridin-2-ones and pyridazin-3-ones
PT2300459E (pt) 2008-07-02 2013-07-04 Hoffmann La Roche Novas fenilpirazinonas utilizadas como inibidores de cinase

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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