CN103415520B8 - 吡咯并六元杂芳环类衍生物、其制备方法及其在医药上的应用 - Google Patents

吡咯并六元杂芳环类衍生物、其制备方法及其在医药上的应用 Download PDF

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CN103415520B8
CN103415520B8 CN201280011688.2A CN201280011688A CN103415520B8 CN 103415520 B8 CN103415520 B8 CN 103415520B8 CN 201280011688 A CN201280011688 A CN 201280011688A CN 103415520 B8 CN103415520 B8 CN 103415520B8
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hetero
hexahydric
pyrrol
analog derivative
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CN103415520A (zh
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张学军
董庆
刘柏年
朱耀平
李晓涛
兰炯
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Shanghai Hengrui Pharmaceutical Co Ltd
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Abstract

本发明涉及吡咯并六元杂芳环类衍生物、其制备方法及其在医药上的应用。具体而言，本发明涉及一种通式(I)所示的新的吡啶并六元杂芳环类衍生物、其制备方法及含有该衍生物的药物组合物以及其作为治疗剂，特别是作为JAK抑制剂和免疫抑制剂的用途，其中通式(I)的各取代基与说明书中的定义相同。
CN201280011688.2A 2011-12-21 2012-12-19 吡咯并六元杂芳环类衍生物、其制备方法及其在医药上的应用 Active CN103415520B8 (zh)

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CN201280011688.2A CN103415520B8 (zh) 2011-12-21 2012-12-19 吡咯并六元杂芳环类衍生物、其制备方法及其在医药上的应用

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CN2011104340719 2011-12-21
CN201110434071 2011-12-21
CN201110434071.9 2011-12-21
CN201280011688.2A CN103415520B8 (zh) 2011-12-21 2012-12-19 吡咯并六元杂芳环类衍生物、其制备方法及其在医药上的应用
PCT/CN2012/086922 WO2013091539A1 (zh) 2011-12-21 2012-12-19 吡咯并六元杂芳环类衍生物、其制备方法及其在医药上的应用

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Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY198512A (en) * 2012-07-17 2023-09-01 Glaxosmithkline Ip No 2 Ltd Indolecarbonitriles as selective androgen receptor modulators
ES2647525T3 (es) * 2013-02-22 2017-12-22 Pfizer Inc. Derivados de pirrolo[2,3-d]pirimidina como inhibidores de janus cinasas (JAK)
HUE036533T2 (hu) * 2013-06-07 2018-07-30 Jiangsu Hengrui Medicine Co Janus-kináz (JAK) gátló biszulfátja és eljárás annak elõállítására
ES2707739T3 (es) 2013-09-26 2019-04-04 Cadent Therapeutics Inc Moduladores negativos de octahidro-ciclopenta[c]pirrol selectivo de NR2B
UA117040C2 (uk) * 2013-12-05 2018-06-11 Пфайзер Інк. ПІРОЛО[2,3-d]ПІРИМІДИНІЛ-, ПІРОЛО[2,3-b]ПІРАЗИНІЛ- ТА ПІРОЛО[2,3-d]ПІРИДИНІЛАКРИЛАМІДИ
KR101710127B1 (ko) * 2014-08-29 2017-02-27 한화제약주식회사 야누스인산화효소 억제제로서의 치환된 N-(피롤리딘-3-일)-7H-피롤로[2,3-d]피리미딘-4-아민
JO3579B1 (ar) 2014-09-26 2020-07-05 Luc Therapeutics Inc مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول
CN105566327A (zh) * 2014-10-09 2016-05-11 江苏恒瑞医药股份有限公司 一种jak激酶抑制剂的硫酸氢盐的i型结晶及其制备方法
KR102522895B1 (ko) * 2014-11-05 2023-04-17 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 Jak 키나아제 억제제 바이설페이트의 결정형 및 이의 제조방법
CN105712998B (zh) * 2014-12-05 2019-12-13 上海润诺生物科技有限公司 氮杂吲哚类衍生物、其制备方法及其在医药上的应用
AU2016271904B2 (en) * 2015-05-29 2018-05-10 Wuxi Fortune Pharmaceutical Co.,Ltd Janus kinase inhibitor
RU2744432C2 (ru) * 2016-02-19 2021-03-09 Цзянсу Хэнжуй Медицин Ко., Лтд. Фармацевтическая композиция, включающая ингибитор янус-киназы или его фармацевтически приемлемую соль
CN107098908B (zh) * 2016-02-23 2021-01-08 欣凯医药科技(上海)有限公司 一种吡咯并嘧啶类化合物的制备方法和应用
BR112019008812A2 (pt) 2016-11-23 2019-07-16 Jiangsu Hengrui Medicine Co método de preparação para e intermediário de derivado de pirrolo anel heteroaromático de seis elementos
AU2017379281A1 (en) 2016-12-22 2019-08-08 Bayer Aktiengesellschaft Substituted heteroaryl pyrrolones and salts thereof and use thereof as herbicidal active substances
EP3558986A1 (de) 2016-12-22 2019-10-30 Bayer CropScience Aktiengesellschaft Substituierte 1,2,4-thiadiazolylpyrrolone und 1,2,4-thiadiazolylhydantoine sowie deren salze und ihre verwendung als herbizide wirkstoffe
CN108779122B (zh) * 2017-01-20 2021-01-15 江苏恒瑞医药股份有限公司 一种jak激酶抑制剂的硫酸氢盐的晶型及其制备方法
EP3686196B1 (en) * 2017-09-20 2024-06-12 Hangzhou Innogate Pharma Co., Ltd. Polycyclic compound acting as ido inhibitor and/or ido-hdac dual inhibitor
TWI717658B (zh) * 2017-11-20 2021-02-01 大陸商江蘇恒瑞醫藥股份有限公司 局部給藥的藥物組合物及其製備方法
US20200390100A1 (en) 2017-12-19 2020-12-17 Bayer Aktiengesellschaft Substituted n-heterocyclyl- and n-heteroaryl-tetrahydropyrimidinones and the salts thereof, and the use of same as herbicidal active substances
US11365188B2 (en) 2018-03-21 2022-06-21 Xibin Liao JAK inhibitors
WO2020052575A1 (zh) * 2018-09-12 2020-03-19 江苏恒瑞医药股份有限公司 Jak激酶抑制剂与egfr抑制剂联合在制备治疗肿瘤疾病的药物中的用途
US20210379052A1 (en) * 2018-09-27 2021-12-09 Shenzhen Chipscreen Biosciences Co., Ltd. Quinoline derivative having indoleamine-2,3-dioxygenase inhibitory activity
CN111205290B (zh) * 2018-11-22 2021-10-08 江苏恒瑞医药股份有限公司 一种jak激酶抑制剂的结晶形式及其制备方法
CN111320633B (zh) * 2018-12-14 2022-09-27 中国医药研究开发中心有限公司 吡咯/咪唑并六元杂芳环类化合物及其制备方法和医药用途
EP3939979A4 (en) 2019-03-14 2022-04-06 Shanghai Synergy Pharmaceutical Sciences Co., Ltd KINASE JAK INHIBITOR, METHOD FOR PREPARING IT AND ITS APPLICATIONS IN THE FIELD OF MEDICINE
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
CN110028509B (zh) * 2019-05-27 2020-10-09 上海勋和医药科技有限公司 作为选择性jak2抑制剂的吡咯并嘧啶类化合物、其合成方法及用途
CA3152021A1 (en) * 2019-08-26 2021-03-04 Chemwerth, Inc. Substituted (7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino compounds useful as jak1 inhibitors
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
CN114829362A (zh) * 2019-12-10 2022-07-29 成都倍特药业股份有限公司 一种可用作shp2抑制剂的含氮杂原子的六元并五元芳环衍生物
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
JP2023068213A (ja) * 2020-03-31 2023-05-17 慶應義塾 炎症性腸疾患処置剤、及び、アミド化合物又はその塩
WO2021201126A1 (ja) * 2020-03-31 2021-10-07 富士フイルム株式会社 アミド化合物又はその塩、医薬組成物、及び、ヒストン脱アセチル化酵素阻害剤
CN113698404B (zh) * 2020-05-21 2023-06-16 江苏恒瑞医药股份有限公司 一种低溶剂残留的六氢环戊并[c]吡咯-2(1H)-甲酰胺化合物及其制备方法
JP2023536102A (ja) 2020-07-28 2023-08-23 アーキュティス・バイオセラピューティクス・インコーポレーテッド Ｊａｋ阻害剤およびラウレス－４を含有する局所配合物
MX2023005106A (es) 2020-10-29 2023-05-23 Arcutis Biotherapeutics Inc Metodos para tratar lesiones de vitiligo que tienen eficacia mejorada.
US11628177B2 (en) 2020-11-17 2023-04-18 Arcutis Biotherapeutics, Inc. Compositions and methods for deep dermal drug delivery
TW202227452A (zh) * 2020-12-04 2022-07-16 大陸商廣州費米子科技有限責任公司 氮雜並環化合物、其製備方法、抑制酪氨酸激酶的方法、藥物組成物及其用途
TW202237614A (zh) * 2020-12-11 2022-10-01 大陸商江蘇恒瑞醫藥股份有限公司 Jak抑制劑在腎臟疾病中的應用
CN114099514A (zh) * 2020-12-29 2022-03-01 上海岸阔医药科技有限公司 预防或治疗egfr功能异常相关的副作用的方法
CN118043051A (zh) * 2021-08-12 2024-05-14 江苏恒瑞医药股份有限公司 用于治疗或预防抗宿主病的吡咯并六元杂芳物
WO2023029943A1 (zh) * 2021-09-03 2023-03-09 星药科技(北京)有限公司 一种芳杂环化合物及其制备方法和用途
CA3240662A1 (en) 2021-12-15 2023-06-22 Herbert R. Brinkman Stable formulations of shr0302
WO2023151069A1 (zh) * 2022-02-14 2023-08-17 湖南南新制药股份有限公司 吡咯并[2,3-d]六元杂芳环衍生物、其制备方法和药物用途
WO2024114814A1 (en) * 2022-12-02 2024-06-06 Onquality Pharmaceuticals China Ltd Jak inhibitors, pharmaceutical compositions, and therapeutic applications

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1439010A (zh) * 2000-06-26 2003-08-27 辉瑞产品公司 吡咯并[2,3－d]嘧啶化合物作为免疫抑制剂
CN1798559A (zh) * 2003-04-04 2006-07-05 诺瓦提斯公司 用于治疗气管疾病的喹啉－2－酮衍生物
WO2009054941A1 (en) * 2007-10-25 2009-04-30 Merck & Co., Inc. Therapeutic compounds

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0278659A (ja) * 1988-09-12 1990-03-19 Shionogi & Co Ltd アザビシクロアルカン類化合物
US5521193A (en) 1992-06-24 1996-05-28 G. D. Searle & Co. Benzimidazole compounds
US5527910A (en) * 1992-12-30 1996-06-18 Cheil Foods & Chemicals, Inc. Pyridone carboxylic acid compounds and their uses for treating infectious diseases caused by bacteria
EA005852B1 (ru) * 1998-06-19 2005-06-30 Пфайзер Продактс Инк. ПИРРОЛО[2,3-d]ПИРИМИДИНЫ
CN1195755C (zh) 1999-12-10 2005-04-06 辉瑞产品公司 吡咯并[2,3－d]嘧啶化合物
OA12316A (en) * 2000-01-24 2006-05-15 Warner Lambert Co 3-Aminoquinazolin-2,4-dione antibacterial agents.
JP4516064B2 (ja) * 2003-04-04 2010-08-04 ノバルティス アーゲー 気道疾患の処置のためのキノリン−２−オン誘導体
WO2004103980A1 (en) 2003-05-21 2004-12-02 Biovitrum Ab Inhibitors of 11-beta-hydroxy steroid dehydrogenase type i
US7381738B2 (en) * 2004-02-19 2008-06-03 Bristol-Myers Squibb Company Substituted bicycloalkylamine derivatives as modulators of chemokine receptor activity
EP1778688A1 (en) * 2004-07-22 2007-05-02 Glaxo Group Limited Antibacterial agents
AR054416A1 (es) * 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
CA2588220A1 (en) * 2004-12-23 2006-06-29 Pfizer Products Inc. Heteroaromatic derivatives useful as anticancer agents
US8633205B2 (en) * 2005-02-03 2014-01-21 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of protein kinases
EP2251341A1 (en) * 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
CN101230058A (zh) * 2007-01-23 2008-07-30 上海恒瑞医药有限公司 双环氮杂烷类衍生物、其制备方法及其在医药上的用途
BRPI0822143A2 (pt) 2008-01-23 2019-09-24 Jiangsu Hansoh Pharmaceutical Cio Ltd derivados de dicicloaza-alcano, processos de preparação e usos médicos dos mesmos
TW200944523A (en) * 2008-02-08 2009-11-01 Organon Nv (Dihydro)pyrrolo[2,1-a]isoquinolines
US20120028990A1 (en) * 2009-04-16 2012-02-02 Msd K.K 3 aryl or heteroaryl-substituted indole derivative
TWI466885B (zh) 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
CN102020643A (zh) * 2009-09-22 2011-04-20 上海恒瑞医药有限公司 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用
US9273028B2 (en) * 2010-10-29 2016-03-01 Biogen Ma Inc. Heterocyclic tyrosine kinase inhibitors
EP2686321B1 (en) * 2011-03-17 2016-11-16 Bristol-Myers Squibb Company Pyrrolopyridazine jak3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases
WO2012171863A1 (en) 2011-06-16 2012-12-20 Boehringer Ingelheim International Gmbh New selective ccr2 antagonists

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1439010A (zh) * 2000-06-26 2003-08-27 辉瑞产品公司 吡咯并[2,3－d]嘧啶化合物作为免疫抑制剂
CN1798559A (zh) * 2003-04-04 2006-07-05 诺瓦提斯公司 用于治疗气管疾病的喹啉－2－酮衍生物
WO2009054941A1 (en) * 2007-10-25 2009-04-30 Merck & Co., Inc. Therapeutic compounds

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