EA201590277A1 - Дигидропиридон р1 в качестве ингибиторов фактора xia - Google Patents

Дигидропиридон р1 в качестве ингибиторов фактора xia

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Publication number
EA201590277A1
EA201590277A1 EA201590277A EA201590277A EA201590277A1 EA 201590277 A1 EA201590277 A1 EA 201590277A1 EA 201590277 A EA201590277 A EA 201590277A EA 201590277 A EA201590277 A EA 201590277A EA 201590277 A1 EA201590277 A1 EA 201590277A1
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EA
Eurasian Patent Office
Prior art keywords
factor xia
compounds
dihydropyridon
inhibitor factor
relates
Prior art date
Application number
EA201590277A
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English (en)
Other versions
EA028581B1 (ru
Inventor
Ву Янг
Джеймс Р. Корте
Паул Дж. Гиллиган
Дональд Дж.П. Пинто Пинто
Вилльям Р. Эвинг
Эндрю К. Дилгер
Юфенг Ванг
Тианан Фанг
Кумар Б. Паббисетти
Леон М. Смит II
Original Assignee
Бристол-Маерс Сквибб Компани
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Бристол-Маерс Сквибб Компани filed Critical Бристол-Маерс Сквибб Компани
Publication of EA201590277A1 publication Critical patent/EA201590277A1/ru
Publication of EA028581B1 publication Critical patent/EA028581B1/ru

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
    • C07C53/16—Halogenated acetic acids
    • C07C53/18—Halogenated acetic acids containing fluorine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • 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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)

Abstract

Изобретение относится к соединениям формулы (V)или их стереоизомерам, таутомерам или фармацевтически приемлемым солям, где все переменные имеют значения, указанные здесь. Эти соединения представляют собой селективные ингибиторы фактора XIa 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.
EA201590277A 2012-08-03 2013-08-02 ДИГИДРОПИРИДОН Р1 В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА XIa EA028581B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261679197P 2012-08-03 2012-08-03
US201361787081P 2013-03-15 2013-03-15
PCT/US2013/053416 WO2014022767A1 (en) 2012-08-03 2013-08-02 Dihydropyridone p1 as factor xia inhibitors

Publications (2)

Publication Number Publication Date
EA201590277A1 true EA201590277A1 (ru) 2015-05-29
EA028581B1 EA028581B1 (ru) 2017-12-29

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EA201590277A EA028581B1 (ru) 2012-08-03 2013-08-02 ДИГИДРОПИРИДОН Р1 В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА XIa

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US (2) US9409908B2 (ru)
EP (1) EP2880026B1 (ru)
JP (1) JP6082463B2 (ru)
KR (1) KR20150038372A (ru)
CN (2) CN108250199B (ru)
AR (1) AR091981A1 (ru)
AU (1) AU2013296259A1 (ru)
BR (1) BR112015002081A2 (ru)
CA (1) CA2880866A1 (ru)
CY (1) CY1119004T1 (ru)
DK (1) DK2880026T3 (ru)
EA (1) EA028581B1 (ru)
ES (1) ES2623175T3 (ru)
HR (1) HRP20170506T1 (ru)
HU (1) HUE032622T2 (ru)
IL (1) IL237011A0 (ru)
LT (1) LT2880026T (ru)
MX (1) MX361759B (ru)
PL (1) PL2880026T3 (ru)
PT (1) PT2880026T (ru)
RS (1) RS55975B1 (ru)
SG (1) SG11201500271UA (ru)
SI (1) SI2880026T1 (ru)
TW (1) TW201410667A (ru)
UY (1) UY34960A (ru)
WO (1) WO2014022767A1 (ru)

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JP2019507167A (ja) 2016-03-02 2019-03-14 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因子阻害活性を有するジアミド大員環
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EP2880026A1 (en) 2015-06-10
TW201410667A (zh) 2014-03-16
UY34960A (es) 2014-01-31
CN104507924A (zh) 2015-04-08
CN104507924B (zh) 2018-01-23
PL2880026T3 (pl) 2017-08-31
HUE032622T2 (en) 2017-10-30
BR112015002081A2 (pt) 2017-07-04
EA028581B1 (ru) 2017-12-29
MX2015000892A (es) 2015-04-17
CA2880866A1 (en) 2014-02-06
US20160340360A1 (en) 2016-11-24
ES2623175T3 (es) 2017-07-10
RS55975B1 (sr) 2017-09-29
US9951071B2 (en) 2018-04-24
MX361759B (es) 2018-12-17
KR20150038372A (ko) 2015-04-08
US20150203492A1 (en) 2015-07-23
CY1119004T1 (el) 2018-01-10
AU2013296259A1 (en) 2015-03-19
CN108250199B (zh) 2021-07-16
AR091981A1 (es) 2015-03-11
US9409908B2 (en) 2016-08-09
EP2880026B1 (en) 2017-02-22
PT2880026T (pt) 2017-05-03
WO2014022767A1 (en) 2014-02-06
IL237011A0 (en) 2015-03-31
JP6082463B2 (ja) 2017-02-15
DK2880026T3 (en) 2017-06-06
SI2880026T1 (sl) 2017-04-26
CN108250199A (zh) 2018-07-06
LT2880026T (lt) 2017-04-25
SG11201500271UA (en) 2015-03-30
JP2015528022A (ja) 2015-09-24
HRP20170506T1 (hr) 2017-06-02

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