TWI703144B - 含雜環基團之巨環fxia抑制劑 - Google Patents

含雜環基團之巨環fxia抑制劑 Download PDF

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Publication number
TWI703144B
TWI703144B TW104103315A TW104103315A TWI703144B TW I703144 B TWI703144 B TW I703144B TW 104103315 A TW104103315 A TW 104103315A TW 104103315 A TW104103315 A TW 104103315A TW I703144 B TWI703144 B TW I703144B
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independently selected
chloro
methyl
compound
preparation
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TW104103315A
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TW201615640A (zh
Inventor
詹姆士R 柯德
印達瓦提 德魯卡
方天安
武 楊
王裕豐
安德魯K 戴爾傑
庫默 巴拉夏穆葛 帕比斯提
威廉R 艾文
怡恆 朱
露斯R 衛思爾
唐諾J 皮托
麥克J 歐華
黎爾M 二世 史密斯
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美商必治妥美雅史谷比公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW104103315A 2014-01-31 2015-01-30 含雜環基團之巨環fxia抑制劑 TWI703144B (zh)

Applications Claiming Priority (2)

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US201461933948P 2014-01-31 2014-01-31
US61/933,948 2014-01-31

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TW201615640A TW201615640A (zh) 2016-05-01
TWI703144B true TWI703144B (zh) 2020-09-01

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EP (1) EP3099688B1 (cg-RX-API-DMAC7.html)
JP (1) JP6419836B2 (cg-RX-API-DMAC7.html)
CN (1) CN106459051B (cg-RX-API-DMAC7.html)
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HU (1) HUE038060T2 (cg-RX-API-DMAC7.html)
LT (1) LT3099688T (cg-RX-API-DMAC7.html)
MX (1) MX2016009385A (cg-RX-API-DMAC7.html)
NO (1) NO2760821T3 (cg-RX-API-DMAC7.html)
PL (1) PL3099688T3 (cg-RX-API-DMAC7.html)
PT (1) PT3099688T (cg-RX-API-DMAC7.html)
RS (1) RS56785B1 (cg-RX-API-DMAC7.html)
SI (1) SI3099688T1 (cg-RX-API-DMAC7.html)
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UY (1) UY35972A (cg-RX-API-DMAC7.html)
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NO2760821T3 (cg-RX-API-DMAC7.html) 2014-01-31 2018-03-10
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US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
US10160750B2 (en) 2015-06-19 2018-12-25 Bristol-Myers Squibb Company Diamide macrocycles as factor XIa inhibitors
KR102086934B1 (ko) 2015-07-29 2020-03-09 브리스톨-마이어스 스큅 컴퍼니 알킬 또는 시클로알킬 P2' 모이어티를 갖는 인자 XIa 마크로시클릭 억제제
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BR112019010511A2 (pt) 2016-11-23 2019-09-17 Bayer Ag derivados de heterociclo bicíclico fundido como pesticidas
KR102515694B1 (ko) 2017-01-10 2023-03-29 바이엘 악티엔게젤샤프트 해충 방제제로서의 헤테로사이클 유도체
WO2018130443A1 (de) 2017-01-10 2018-07-19 Bayer Aktiengesellschaft Heterocyclen-derivate als schädlingsbekämpfungsmittel
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
CN110922412A (zh) * 2018-09-20 2020-03-27 复旦大学 具有抗精神病作用药物化合物的不对称合成方法
CN113677682B (zh) * 2019-04-16 2023-05-30 华润生物医药有限公司 作为XIa因子抑制剂的大环衍生物
US20210041711A1 (en) * 2019-07-08 2021-02-11 Gary Sharp Innovations, Llc Compact Polarization-Based Collimators with High Contrast
WO2021013209A1 (zh) 2019-07-23 2021-01-28 南京明德新药研发有限公司 作为XIa因子抑制剂的大环衍生物
TW202229280A (zh) * 2020-10-12 2022-08-01 美商必治妥美雅史谷比公司 (6r,10s)-10-{4-[5-氯-2-(4-氯-1h-1,2,3-三唑-1-基)苯基]-6-側氧基-1(6h)-嘧啶基}-1-(二氟甲基)-6-甲基-1,4,7,8,9,10-六氫-11,15-(亞甲橋基)吡唑并[4,3-b][1,7]二氮雜環十四炔-5(6h)-酮之製備方法
WO2022222960A1 (zh) * 2021-04-21 2022-10-27 上海美悦生物科技发展有限公司 FXIa抑制剂及其药物组合物、制备方法和用途
TW202515882A (zh) * 2023-06-30 2025-04-16 大陸商深圳信立泰藥業股份有限公司 一種多取代的大環化合物及其製備方法與應用

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