CA2937738C - Macrocyclic factor xia inhibitors condensed with heterocycles - Google Patents

Macrocyclic factor xia inhibitors condensed with heterocycles Download PDF

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Publication number
CA2937738C
CA2937738C CA2937738A CA2937738A CA2937738C CA 2937738 C CA2937738 C CA 2937738C CA 2937738 A CA2937738 A CA 2937738A CA 2937738 A CA2937738 A CA 2937738A CA 2937738 C CA2937738 C CA 2937738C
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Prior art keywords
independently
chloro
mmol
chf2
oxo
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CA2937738A
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English (en)
French (fr)
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CA2937738A1 (en
Inventor
Andrew K. Dilger
James R. Corte
Indawati De Lucca
Tianan Fang
Wu Yang
Yufeng Wang
Kumar Balashanmuga PABBISETTY
William R. Ewing
Yeheng Zhu
Ruth R. Wexler
Donald J.P. Pinto
Michael J. Orwat
Leon M. Ii Smith
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Publication of CA2937738A1 publication Critical patent/CA2937738A1/en
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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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2937738A 2014-01-31 2015-01-30 Macrocyclic factor xia inhibitors condensed with heterocycles Active CA2937738C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461933948P 2014-01-31 2014-01-31
US61/933,948 2014-01-31
PCT/US2015/013647 WO2015116882A1 (en) 2014-01-31 2015-01-30 Macrocyclic factor xia inhibitors condensed with heterocycles

Publications (2)

Publication Number Publication Date
CA2937738A1 CA2937738A1 (en) 2015-08-06
CA2937738C true CA2937738C (en) 2023-01-17

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Application Number Title Priority Date Filing Date
CA2937738A Active CA2937738C (en) 2014-01-31 2015-01-30 Macrocyclic factor xia inhibitors condensed with heterocycles

Country Status (24)

Country Link
US (3) US20170057961A1 (OSRAM)
EP (1) EP3099688B1 (OSRAM)
JP (1) JP6419836B2 (OSRAM)
CN (1) CN106459051B (OSRAM)
AR (1) AR099228A1 (OSRAM)
BR (1) BR112016016741B1 (OSRAM)
CA (1) CA2937738C (OSRAM)
CY (1) CY1120534T1 (OSRAM)
DK (1) DK3099688T3 (OSRAM)
EA (1) EA032650B1 (OSRAM)
ES (1) ES2655540T3 (OSRAM)
HR (1) HRP20172002T1 (OSRAM)
HU (1) HUE038060T2 (OSRAM)
LT (1) LT3099688T (OSRAM)
MX (1) MX2016009385A (OSRAM)
NO (1) NO2760821T3 (OSRAM)
PL (1) PL3099688T3 (OSRAM)
PT (1) PT3099688T (OSRAM)
RS (1) RS56785B1 (OSRAM)
SI (1) SI3099688T1 (OSRAM)
SM (1) SMT201800024T1 (OSRAM)
TW (1) TWI703144B (OSRAM)
UY (1) UY35972A (OSRAM)
WO (1) WO2015116882A1 (OSRAM)

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NO2760821T3 (OSRAM) 2014-01-31 2018-03-10
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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
EP3957638B1 (en) * 2019-04-16 2025-01-08 China Resources Biopharmaceutical Company Limited Macrocyclic derivatives acting as xia factor inhibitor
EP3997492A4 (en) * 2019-07-08 2023-11-15 Meta Platforms Technologies, Llc HIGH CONTRAST COLLIMATORS BASED ON COMPACT POLARIZATION
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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
TWI877478B (zh) * 2021-04-21 2025-03-21 大陸商上海美悦生物科技發展有限公司 FXIa抑制劑及其藥物組合物、製備方法和用途
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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