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PE20151336A1 - Inhibidores de la tirosina-quinasa de bruton - Google Patents

Inhibidores de la tirosina-quinasa de bruton

Info

Publication number
PE20151336A1
PE20151336A1 PE2015001561A PE2015001561A PE20151336A1 PE 20151336 A1 PE20151336 A1 PE 20151336A1 PE 2015001561 A PE2015001561 A PE 2015001561A PE 2015001561 A PE2015001561 A PE 2015001561A PE 20151336 A1 PE20151336 A1 PE 20151336A1
Authority
PE
Peru
Prior art keywords
compounds
tyrosine kinase
kinase inhibitors
bruton tyrosine
useful
Prior art date
Application number
PE2015001561A
Other languages
English (en)
Inventor
Steven Joseph Berthel
Daniel Fishlock
Fariborz Firooznia
Jun-Bae Hong
Yan Lou
Matthew C Lucas
Timothy 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=PE20151336(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 PE20151336A1 publication Critical patent/PE20151336A1/es

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    • C07D401/10Heterocyclic 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 two hetero rings linked by a carbon chain containing aromatic rings
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non 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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Abstract

En esta solicitud se describen compuestos de la formula general A: en la que la variable Z* tiene el significado definido antes, que inhiben la Btk. Los compuestos aqui descritos son utiles para modular la actividad de la Btk y tratar enfermedades asociadas con una actividad excesiva de la Btk. Estos compuestos son tambien utiles para tratar enfermedades inflamatorias y autoinmunes asociadas con una proliferacion aberrante de las celulas B, por ejemplo la artritis reumatoide. Se describen tambien composiciones que contienen los compuestos de la formula A y por lo menos un vehiculo, diluyente o excipiente
PE2015001561A 2009-03-02 2010-02-25 Inhibidores de la tirosina-quinasa de bruton PE20151336A1 (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
PE20151336A1 true PE20151336A1 (es) 2015-09-18

Family

ID=42097405

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2011001551A PE20120081A1 (es) 2009-03-02 2010-02-25 Derivados de 6-tert-butil-8-fluor-2-(2-hidroximetil-3-{1-metil-5-piridin-2-il-amino-6-oxo-1,6-dihidro-piridin-3-il}-fenil)-ftalazin-1-ona como inhibidores de la tirosina-quinasa de bruton
PE2015001561A PE20151336A1 (es) 2009-03-02 2010-02-25 Inhibidores de la tirosina-quinasa de bruton

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2011001551A PE20120081A1 (es) 2009-03-02 2010-02-25 Derivados de 6-tert-butil-8-fluor-2-(2-hidroximetil-3-{1-metil-5-piridin-2-il-amino-6-oxo-1,6-dihidro-piridin-3-il}-fenil)-ftalazin-1-ona como inhibidores de la tirosina-quinasa de bruton

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) PE20120081A1 (es)
RU (1) RU2542585C2 (es)
SG (1) SG173816A1 (es)
TW (2) TW201439080A (es)
WO (1) WO2010100070A1 (es)
ZA (1) ZA201301679B (es)

Families Citing this family (70)

* 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
PL2300459T3 (pl) * 2008-07-02 2013-10-31 Hoffmann La Roche Nowe fenylopirazynony jako inhibitory kinazy
MX2011000661A (es) 2008-07-16 2011-05-25 Pharmacyclics Inc Inhibidores de tirosina cinasa de bruton para el tratamiento de tumores solidos.
EA023857B1 (ru) 2009-03-23 2016-07-29 Гленмарк Фармасеутикалс С.А. Сочлененные производные пиримидиндионов в качестве модуляторов trpa1
NZ604040A (en) 2010-06-03 2015-02-27 Pharmacyclics Inc 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
KR101864908B1 (ko) * 2010-09-01 2018-06-05 질레드 코네티컷 인코포레이티드 피리다지논, 그의 제조 방법 및 사용 방법
CN106220614B (zh) 2010-09-01 2019-07-16 吉利德康涅狄格有限公司 吡啶酮/吡嗪酮、其制备方法及使用方法
AU2012257802A1 (en) 2011-05-17 2013-10-31 F. Hoffmann-La Roche Ag Inhibitors of Bruton's tyrosine kinase
US20130178483A1 (en) * 2011-06-28 2013-07-11 Pharmacyclics, Inc. Methods and Compositions for Inhibition of Bone Resorption
PH12014500122A1 (en) 2011-07-13 2014-03-24 Pharmacyclics Inc Inhibitors of bruton's tyrosine kinase
PE20140865A1 (es) * 2011-08-17 2014-07-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
EP2771010A4 (en) * 2011-10-19 2015-04-01 Pharmacyclics Inc USE OF BRUTON TYROSINE KINASE (BTK) INHIBITORS
UA111756C2 (uk) * 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
SG11201401993RA (en) * 2011-11-03 2014-05-29 Hoffmann La Roche Alkylated piperazine compounds as inhibitors of btk activity
HK1205111A1 (en) * 2011-11-03 2015-12-11 霍夫曼-拉罗奇有限公司 8-fluorophthalazin-1 (2h) - one 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
CA2869954C (en) 2012-04-20 2023-01-03 Advinus Therapeutics Limited Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof in medical conditions related to modulation of bruton's tyrosine kinase activity
WO2013157021A1 (en) 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
KR20150032340A (ko) 2012-07-24 2015-03-25 파마시클릭스, 인코포레이티드 브루톤 티로신 키나제(btk)의 억제제에 대한 내성과 관련된 돌연변이
EP2882741B1 (en) 2012-08-10 2018-10-24 Boehringer Ingelheim International GmbH Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors
EP2895473A1 (en) * 2012-09-13 2015-07-22 F. Hoffmann-La Roche AG Inhibitors of bruton's tyrosine kinase
CN104812746B (zh) * 2012-11-16 2017-03-08 弗·哈夫曼-拉罗切有限公司 布鲁顿氏酪氨酸激酶抑制剂
WO2014083026A1 (en) * 2012-11-30 2014-06-05 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
JP6089124B2 (ja) * 2013-03-05 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薬
JP2016510051A (ja) * 2013-03-05 2016-04-04 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
JP2016519684A (ja) 2013-04-08 2016-07-07 デニス エム ブラウン 準最適に投与された薬物療法の有効性を改善するための及び/又は副作用を低減するための方法および組成物
SMT201700160T1 (it) 2013-04-25 2017-05-08 Beigene Ltd Composti eterociclici fusi come inibitori di protein chinasi
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
CN110698481B (zh) * 2013-07-03 2023-02-28 豪夫迈·罗氏有限公司 杂芳基吡啶酮和氮杂-吡啶酮酰胺化合物
KR101742550B1 (ko) * 2013-07-26 2017-06-01 카나 바이오사이언스, 인코포레이션 신규 트리아진 유도체
CA2928568A1 (en) 2013-07-26 2015-01-29 Update Pharma Inc. Combinatorial methods to improve the therapeutic benefit of bisantrene
EP3033079B1 (en) 2013-08-12 2018-10-31 Pharmacyclics LLC Methods for the treatment of her2 amplified cancer
ES2792183T3 (es) 2013-09-13 2020-11-10 Beigene Switzerland Gmbh Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico
US9512084B2 (en) * 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
KR101813830B1 (ko) 2013-12-05 2017-12-29 에프. 호프만-라 로슈 아게 친전자성 작용기를 갖는 헤테로아릴 피리돈 및 아자-피리돈 화합물
US9802920B2 (en) * 2013-12-13 2017-10-31 Hoffman-La Roche Inc. Inhibitors of bruton's tyrosine kinase
JP2017509336A (ja) 2014-03-20 2017-04-06 ファーマサイクリックス エルエルシー ホスホリパーゼcガンマ2及び耐性に関連した変異
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
CN111303159A (zh) * 2014-10-02 2020-06-19 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
SI3317281T1 (sl) 2015-07-02 2020-08-31 Acerta Pharma B.V. Trdne oblike in formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin -2-il)imidazo(1,5-a)pirazin-1-il)-n-(piridin-2-il)benzamida
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
EP3402789B1 (en) * 2016-01-13 2020-03-18 Boehringer Ingelheim International Gmbh Isoquinolones as btk inhibitors
CA3028824C (en) * 2016-06-22 2023-12-12 Shanghai Fochon Pharmaceutical Co., Ltd. Substituted pyrrolo[2,3-d]pyridazin-4-ones and pyrazolo[3,4-d]pyridazin-4-ones as protein kinase inhibitors
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
CN110049976A (zh) 2016-07-21 2019-07-23 比奥根Ma公司 布鲁顿氏酪氨酸激酶抑制剂的琥珀酸盐形式和组合物
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
PT3500299T (pt) 2016-08-19 2024-02-21 Beigene Switzerland Gmbh Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro
MA46285A (fr) 2016-09-19 2019-07-31 Mei Pharma Inc Polythérapie
AR110282A1 (es) 2016-12-02 2019-03-13 Hoffmann La Roche Compuestos de amida bicíclica y uso de éstos en el tratamiento de enfermedades mediadas por rip1
MA46995A (fr) 2016-12-03 2019-10-09 Acerta Pharma Bv Méthodes et compositions pour l'utilisation de lymphocytes t thérapeutiques en association avec des inhibiteurs de kinase
CN110461847B (zh) 2017-01-25 2022-06-07 百济神州有限公司 (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途
TW202515616A (zh) 2017-06-26 2025-04-16 英屬開曼群島商百濟神州有限公司 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途
AR112274A1 (es) 2017-07-14 2019-10-09 Hoffmann La Roche Compuestos bicíclicos de cetona y sus métodos de uso
CN110997677A (zh) 2017-08-12 2020-04-10 百济神州有限公司 具有改进的双重选择性的Btk抑制剂
KR102613433B1 (ko) 2017-10-11 2023-12-13 주식회사 대웅제약 신규한 페닐피리딘 유도체 및 이를 포함하는 약학 조성물
MX2020003451A (es) 2017-10-31 2020-08-03 Hoffmann La Roche Sulfonas y sulfoxidos biciclicos y metodos 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
US11667651B2 (en) 2017-12-22 2023-06-06 Hibercell, Inc. 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
WO2020249001A1 (zh) 2019-06-10 2020-12-17 百济神州瑞士有限责任公司 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法
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
IL307819A (en) * 2021-05-05 2023-12-01 Hoffmann La Roche Process for preparing btk inhibitors
JPWO2023152888A1 (es) * 2022-02-10 2023-08-17
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
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
US7786115B2 (en) * 2004-12-24 2010-08-31 Astrazeneca Ab Amide derivatives
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.
CA2701275C (en) 2007-10-23 2016-06-21 F. Hoffmann-La Roche Ag 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
WO2009098144A1 (en) 2008-02-05 2009-08-13 F. Hoffmann-La Roche Ag Novel pyridinones and pyridazinones
US7683064B2 (en) 2008-02-05 2010-03-23 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
NZ601700A (en) * 2008-06-24 2013-02-22 Hoffmann La Roche 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives as inhibitors of Bruton's Tyrosine Kinase (Btk)
PL2300459T3 (pl) * 2008-07-02 2013-10-31 Hoffmann La Roche Nowe fenylopirazynony jako inhibitory kinazy

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