CN114008047A - 作为XIa因子抑制剂的大环衍生物 - Google Patents

作为XIa因子抑制剂的大环衍生物 Download PDF

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Publication number
CN114008047A
CN114008047A CN202080047754.6A CN202080047754A CN114008047A CN 114008047 A CN114008047 A CN 114008047A CN 202080047754 A CN202080047754 A CN 202080047754A CN 114008047 A CN114008047 A CN 114008047A
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compound
isomer
pharmaceutically acceptable
acceptable salt
added
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CN114008047B (zh
Inventor
蔡亚仙
颜小兵
蔡哲
胡国平
丁照中
陈新海
黎健
陈曙辉
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Medshine Discovery Inc
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Medshine Discovery Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

大环衍生物、其制备方法及含有该衍生物的药物组合物，以及它们作为治疗剂，特别是作为XIa因子抑制剂和在治疗和预防血栓栓塞等疾病的药物中的用途，具体公开了式(I)所示化合物、其异构体及其药学上可接受的盐。

Description

PCT国内申请，说明书已公开。

Claims (27)

  1. PCT国内申请，权利要求书已公开。
CN202080047754.6A 2019-07-23 2020-07-23 作为XIa因子抑制剂的大环衍生物 Active CN114008047B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201910668575 2019-07-23
CN2019106685753 2019-07-23
PCT/CN2020/103692 WO2021013209A1 (zh) 2019-07-23 2020-07-23 作为XIa因子抑制剂的大环衍生物

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CN114008047A true CN114008047A (zh) 2022-02-01
CN114008047B CN114008047B (zh) 2023-03-21

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US (1) US20220281868A1 (zh)
EP (1) EP4006029A4 (zh)
JP (1) JP7286001B2 (zh)
CN (1) CN114008047B (zh)
WO (1) WO2021013209A1 (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20220144836A1 (en) * 2019-04-11 2022-05-12 Bristol-Myers Squibb Company Novel synthetic options towards the manufacture of (6r,10s)-10-{4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)-pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15-(metheno)pyrazolo[4,3-b][1,7]diazacyclotetradecin-5(6h)-one

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106459051A (zh) * 2014-01-31 2017-02-22 百时美施贵宝公司 含杂环基团的大环fxia抑制剂
CN106795161A (zh) * 2014-10-01 2017-05-31 百时美施贵宝公司 作为因子xia抑制剂的嘧啶酮
WO2018133793A1 (zh) * 2017-01-18 2018-07-26 广东东阳光药业有限公司 凝血因子XIa抑制剂及其用途

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2789622C (en) 2010-02-11 2018-04-03 Bristol-Myers Squibb Company Macrocycles as factor xia inhibitors
TW201319068A (zh) * 2011-08-05 2013-05-16 必治妥美雅史谷比公司 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑
TW201311689A (zh) 2011-08-05 2013-03-16 必治妥美雅史谷比公司 作為因子ｘｉａ抑制劑之新穎巨環化合物
LT2882734T (lt) 2012-08-03 2016-12-12 Bristol-Myers Squibb Company Dihidropiridonai, kaip xia faktoriaus slopikliai
DK2880026T3 (en) * 2012-08-03 2017-06-06 Bristol Myers Squibb Co DIHYDROPYRIDON-P1 AS A FACTOR XIA INHIBITORS
JP6464176B2 (ja) 2014-01-31 2019-02-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環
US10344039B2 (en) 2015-10-29 2019-07-09 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor XIa inhibitors, pharmaceutically acceptable compositions and their use
JP6892858B2 (ja) * 2015-10-29 2021-06-23 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 第ＸＩａ因子阻害剤

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106459051A (zh) * 2014-01-31 2017-02-22 百时美施贵宝公司 含杂环基团的大环fxia抑制剂
CN106795161A (zh) * 2014-10-01 2017-05-31 百时美施贵宝公司 作为因子xia抑制剂的嘧啶酮
WO2018133793A1 (zh) * 2017-01-18 2018-07-26 广东东阳光药业有限公司 凝血因子XIa抑制剂及其用途

Also Published As

Publication number Publication date
US20220281868A1 (en) 2022-09-08
CN114008047B (zh) 2023-03-21
WO2021013209A1 (zh) 2021-01-28
JP7286001B2 (ja) 2023-06-02
EP4006029A4 (en) 2023-06-21
EP4006029A1 (en) 2022-06-01
JP2022541927A (ja) 2022-09-28

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