CN103702999B - 作为因子xia抑制剂的环状p1连接体 - Google Patents

作为因子xia抑制剂的环状p1连接体 Download PDF

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Publication number
CN103702999B
CN103702999B CN201280037801.4A CN201280037801A CN103702999B CN 103702999 B CN103702999 B CN 103702999B CN 201280037801 A CN201280037801 A CN 201280037801A CN 103702999 B CN103702999 B CN 103702999B
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mmol
compounds
compound
chloro
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CN103702999A (zh
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P.Y.S.林
C.G.克拉克
J.R.科尔特
W.R.尤因
P.J.吉利根
Y.雍
W.杨
L.M.史密斯二世
Y.王
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P9/10Drugs 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
    • 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
    • C07D471/02Heterocyclic 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 two hetero rings
    • C07D471/06Peri-condensed systems
    • 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
    • C07D471/02Heterocyclic 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 two hetero rings
    • C07D471/08Bridged systems
    • 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
    • C07D487/06Peri-condensed systems
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06Peri-condensed 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)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201280037801.4A 2011-08-05 2012-08-06 作为因子xia抑制剂的环状p1连接体 Active CN103702999B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201510648908.8A CN105294701B (zh) 2011-08-05 2012-08-06 作为因子xia抑制剂的环状p1连接体

Applications Claiming Priority (4)

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US201161515404P 2011-08-05 2011-08-05
US61/515404 2011-08-05
US61/515,404 2011-08-05
PCT/US2012/049698 WO2013022814A1 (en) 2011-08-05 2012-08-06 Cyclic p1 linkers as factor xia inhibitors

Related Child Applications (1)

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CN103702999A CN103702999A (zh) 2014-04-02
CN103702999B true CN103702999B (zh) 2015-11-25

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US (2) US8901115B2 (OSRAM)
EP (2) EP3070087B1 (OSRAM)
JP (1) JP6113727B2 (OSRAM)
CN (2) CN103702999B (OSRAM)
AR (1) AR088423A1 (OSRAM)
ES (2) ES2563445T3 (OSRAM)
TW (1) TW201319068A (OSRAM)
WO (1) WO2013022814A1 (OSRAM)

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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
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JP6033318B2 (ja) 2011-10-14 2016-11-30 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 第XIa因子阻害剤としての置換テトラヒドロイソキノリン化合物
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JP6479763B2 (ja) 2013-03-25 2019-03-06 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 第xia因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン
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US10160750B2 (en) 2015-06-19 2018-12-25 Bristol-Myers Squibb Company Diamide macrocycles as factor XIa inhibitors
CN107922393A (zh) * 2015-07-29 2018-04-17 百时美施贵宝公司 携带非芳族p2,基团的因子xia新大环
CN107849026B (zh) 2015-07-29 2021-01-01 百时美施贵宝公司 携带烷基或环烷基p2′部分的因子xia大环抑制剂
WO2017074833A1 (en) 2015-10-29 2017-05-04 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use
CA2998902C (en) 2015-10-29 2024-03-26 Merck Sharp & Dohme Corp. Macrocyclic compounds as factor xia inhibitors
WO2017151746A1 (en) 2016-03-02 2017-09-08 Bristol-Myers Squibb Company Diamide macrocycles having factor xia inhibiting activity
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
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CN110062757B (zh) * 2017-01-18 2022-03-04 广东东阳光药业有限公司 凝血因子XIa抑制剂及其用途
WO2019011166A1 (zh) * 2017-07-14 2019-01-17 四川科伦博泰生物医药股份有限公司 大环酰胺化合物及其药物组合物和用途
WO2019204447A1 (en) * 2018-04-17 2019-10-24 The Regents Of The University Of Michigan Inhibitors of platelet function and methods for use of the same
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
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
CN115490708B (zh) * 2021-06-18 2025-01-24 苏州亚盛药业有限公司 磺酰胺类大环衍生物及其制备方法和用途
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US9108981B2 (en) 2015-08-18
US8901115B2 (en) 2014-12-02
CN105294701A (zh) 2016-02-03
AR088423A1 (es) 2014-06-11
ES2733096T3 (es) 2019-11-27
EP2739625B1 (en) 2016-01-20
JP2014521700A (ja) 2014-08-28
US20150057262A1 (en) 2015-02-26
EP2739625A1 (en) 2014-06-11
EP3070087A1 (en) 2016-09-21
US20140163002A1 (en) 2014-06-12
JP6113727B2 (ja) 2017-04-12
WO2013022814A1 (en) 2013-02-14
EP3070087B1 (en) 2019-04-10
CN105294701B (zh) 2017-10-24
CN103702999A (zh) 2014-04-02
TW201319068A (zh) 2013-05-16
ES2563445T3 (es) 2016-03-15

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