EA201691471A1 - Макроциклы с гетероциклическими группами p2' как ингибиторы фактора xia - Google Patents

Макроциклы с гетероциклическими группами p2' как ингибиторы фактора xia

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Publication number
EA201691471A1
EA201691471A1 EA201691471A EA201691471A EA201691471A1 EA 201691471 A1 EA201691471 A1 EA 201691471A1 EA 201691471 A EA201691471 A EA 201691471A EA 201691471 A EA201691471 A EA 201691471A EA 201691471 A1 EA201691471 A1 EA 201691471A1
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Eurasian Patent Office
Prior art keywords
inhibitors
heterocyclic groups
compounds
xia factor
macro cycles
Prior art date
Application number
EA201691471A
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English (en)
Other versions
EA030222B1 (ru
Inventor
Джеймс Р. Корте
Индавати Де Лукка
Тианан Фанг
Ву Янг
Юфенг Ванг
Эндрю К. Дилгер
Кумар Балашанмуга Паббисетти
Уильям Р. Эвинг
Йехенг Жу
Рут Р. Векслер
Дональд Дж. П. Пинто
Майкл Дж. Орват
Леон М. II Смит
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 EA201691471A1 publication Critical patent/EA201691471A1/ru
Publication of EA030222B1 publication Critical patent/EA030222B1/ru

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    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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

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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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (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)
  • Pyridine Compounds (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы (I)или их стереоизомерам, таутомерам или фармацевтически приемлемым солям, в которых все переменные определены в настоящем документе. Данные соединения являются селективными ингибиторами фактора XIa или двойными ингибиторами FXIa и калликреина плазмы. Настоящее изобретение также относится к фармацевтическим композициям, содержащим данные соединения, и к способам лечения тромбоэмболических и/или воспалительных нарушений с их применением.
EA201691471A 2014-01-31 2015-01-30 МАКРОЦИКЛЫ С ГЕТЕРОЦИКЛИЧЕСКИМИ ГРУППАМИ P2' КАК ИНГИБИТОРЫ ФАКТОРА XIa EA030222B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461933942P 2014-01-31 2014-01-31
US201462058293P 2014-10-01 2014-10-01
PCT/US2015/013654 WO2015116886A1 (en) 2014-01-31 2015-01-30 Macrocycles with hetrocyclic p2' groups as factor xia inhibitors

Publications (2)

Publication Number Publication Date
EA201691471A1 true EA201691471A1 (ru) 2016-12-30
EA030222B1 EA030222B1 (ru) 2018-07-31

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201691471A EA030222B1 (ru) 2014-01-31 2015-01-30 МАКРОЦИКЛЫ С ГЕТЕРОЦИКЛИЧЕСКИМИ ГРУППАМИ P2' КАК ИНГИБИТОРЫ ФАКТОРА XIa

Country Status (31)

Country Link
US (2) US20170002006A1 (ru)
EP (4) EP3392249B1 (ru)
JP (6) JP6505727B2 (ru)
KR (3) KR102413453B1 (ru)
CN (4) CN106132962B (ru)
AU (4) AU2015210904C1 (ru)
BR (1) BR112016015717B1 (ru)
CA (1) CA2937739C (ru)
CL (1) CL2016001933A1 (ru)
CY (1) CY1120702T1 (ru)
DK (1) DK3099687T3 (ru)
EA (1) EA030222B1 (ru)
ES (3) ES2784841T3 (ru)
HR (1) HRP20181339T1 (ru)
HU (1) HUE040226T2 (ru)
IL (4) IL298983B2 (ru)
LT (1) LT3099687T (ru)
MX (2) MX2016009230A (ru)
MY (1) MY190429A (ru)
NZ (2) NZ723762A (ru)
PE (2) PE20161069A1 (ru)
PH (2) PH12016501249B1 (ru)
PL (1) PL3099687T3 (ru)
PT (1) PT3099687T (ru)
RS (1) RS57659B1 (ru)
SG (2) SG11201606209PA (ru)
SI (1) SI3099687T1 (ru)
TW (4) TW201613922A (ru)
UY (2) UY35971A (ru)
WO (2) WO2015116885A1 (ru)
ZA (1) ZA201606011B (ru)

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