EA201490418A1 - Новые макроциклические соединения в качестве ингибиторов фактора xia - Google Patents

Новые макроциклические соединения в качестве ингибиторов фактора xia

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Publication number
EA201490418A1
EA201490418A1 EA201490418A EA201490418A EA201490418A1 EA 201490418 A1 EA201490418 A1 EA 201490418A1 EA 201490418 A EA201490418 A EA 201490418A EA 201490418 A EA201490418 A EA 201490418A EA 201490418 A1 EA201490418 A1 EA 201490418A1
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EA
Eurasian Patent Office
Prior art keywords
inhibitors
compounds
macrocyclic compounds
new macrocyclic
xia factor
Prior art date
Application number
EA201490418A
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English (en)
Other versions
EA024791B1 (ru
Inventor
Дональд Дж. Пинто
Джеймс Р. Корте
Пол Дж. Гиллиган
Тианан Фанг
Леон М. Смит II
Юйфэн Ван
У Ян
Вильям Р. Евинг
Original Assignee
Бристол-Майерс Сквибб Компани
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Application filed by Бристол-Майерс Сквибб Компани filed Critical Бристол-Майерс Сквибб Компани
Publication of EA201490418A1 publication Critical patent/EA201490418A1/ru
Publication of EA024791B1 publication Critical patent/EA024791B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/06—Peri-condensed systems
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Изобретение относится к соединениям формулы (Ia)или их стереоизомеру, таутомеру или фармацевтически приемлемой соли, где все переменные имеют значения, указанные в описании изобретения. Эти соединения представляют собой селективные ингибиторы фактора ХIa или двойные ингибиторы FXIa и калликреина плазмы. Это изобретение также относится к фармацевтическим композициям, содержащим эти соединения, и способам лечения тромбоэмболических и/или воспалительных заболеваний с их применением.
EA201490418A 2011-08-05 2012-08-06 НОВЫЕ МАКРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА XIa EA024791B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161515401P 2011-08-05 2011-08-05
PCT/US2012/049706 WO2013022818A1 (en) 2011-08-05 2012-08-06 Novel macrocycles as factor xia inhibitors

Publications (2)

Publication Number Publication Date
EA201490418A1 true EA201490418A1 (ru) 2014-05-30
EA024791B1 EA024791B1 (ru) 2016-10-31

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Country Status (21)

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US (4) US9221818B2 (ru)
EP (1) EP2739628B1 (ru)
JP (1) JP6158181B2 (ru)
CN (1) CN103857681B (ru)
AR (1) AR088748A1 (ru)
BR (1) BR112014002202A2 (ru)
CA (1) CA2844254A1 (ru)
CY (1) CY1119281T1 (ru)
DK (1) DK2739628T3 (ru)
EA (1) EA024791B1 (ru)
ES (1) ES2635088T3 (ru)
HR (1) HRP20171122T1 (ru)
HU (1) HUE034487T2 (ru)
LT (1) LT2739628T (ru)
MX (1) MX345763B (ru)
PL (1) PL2739628T3 (ru)
PT (1) PT2739628T (ru)
RS (1) RS56244B1 (ru)
SI (1) SI2739628T1 (ru)
TW (1) TW201311689A (ru)
WO (1) WO2013022818A1 (ru)

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BR112014002202A2 (pt) 2017-03-07
HUE034487T2 (en) 2018-02-28
MX345763B (es) 2017-02-15
JP2014521701A (ja) 2014-08-28
WO2013022818A1 (en) 2013-02-14
PL2739628T3 (pl) 2017-11-30
US9611274B2 (en) 2017-04-04
PT2739628T (pt) 2017-08-02
HRP20171122T1 (hr) 2017-10-06
US10208068B2 (en) 2019-02-19
EP2739628B1 (en) 2017-06-07
US20140221338A1 (en) 2014-08-07
JP6158181B2 (ja) 2017-07-05
CY1119281T1 (el) 2018-02-14
US20180148461A1 (en) 2018-05-31
EA024791B1 (ru) 2016-10-31
MX2014000831A (es) 2014-02-27
CA2844254A1 (en) 2013-02-14
ES2635088T3 (es) 2017-10-02
US9902742B2 (en) 2018-02-27
US20160068544A1 (en) 2016-03-10
LT2739628T (lt) 2017-08-25
US20170158712A1 (en) 2017-06-08
CN103857681A (zh) 2014-06-11
TW201311689A (zh) 2013-03-16
CN103857681B (zh) 2017-07-14
AR088748A1 (es) 2014-07-02
EP2739628A1 (en) 2014-06-11
US9221818B2 (en) 2015-12-29
DK2739628T3 (en) 2017-09-11
RS56244B1 (sr) 2017-11-30
SI2739628T1 (sl) 2017-08-31

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