EA201100846A1 - Пиразолилзамещенные производные угольной кислоты в качестве модуляторов рецептора простациклина (pgi2), применимые для лечения связанных с ним нарушений - Google Patents

Пиразолилзамещенные производные угольной кислоты в качестве модуляторов рецептора простациклина (pgi2), применимые для лечения связанных с ним нарушений

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Publication number
EA201100846A1
EA201100846A1 EA201100846A EA201100846A EA201100846A1 EA 201100846 A1 EA201100846 A1 EA 201100846A1 EA 201100846 A EA201100846 A EA 201100846A EA 201100846 A EA201100846 A EA 201100846A EA 201100846 A1 EA201100846 A1 EA 201100846A1
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EA
Eurasian Patent Office
Prior art keywords
disease
diabetes
treatment
related disorders
pgi2
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EA201100846A
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English (en)
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EA022799B1 (ru
Inventor
Туй-Анх Тран
Джейсон Б. Ибарра
Янг-Дзун Шин
Бретт Уллман
Нин Цзоу
Сяо Цзэн
Си Цзэн
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Арена Фармасьютикалз, Инк.
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Application filed by Арена Фармасьютикалз, Инк. filed Critical Арена Фармасьютикалз, Инк.
Publication of EA201100846A1 publication Critical patent/EA201100846A1/ru
Publication of EA022799B1 publication Critical patent/EA022799B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18—One oxygen or sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Изобретение относится к производным пиразола формулы Ia и их фармацевтическим композициям, которые модулируют активность рецептора PGI2. Соединения настоящего изобретения и их фармацевтические композиции относятся к способам, применимым при лечении легочной артериальной гипертензии (РАН) и родственных нарушений; агрегации тромбоцитов; болезни коронарной артерии; инфаркта миокарда, преходящего ишемического нарушения; стенокардии; удара; ишемического повреждения при реперфузии; рестеноза; предсердной фибрилляции; образования сгустков крови при ангиопластике или операции шунтирования на коронарных артериях у индивидуума или у индивидуума, страдающего предсердной фибрилляцией; атеросклероза; атеротромбоза; астмы или ее симптома; связанного с диабетом нарушения, такого как диабетическая периферическая невропатия, диабетическая нефропатия или диабетическая ретинопатия; глаукомы или другой болезни глаз с аномальным внутриглазным давлением; гипертензии; воспаления; псориаза; псориатического артрита; ревматоидного артрита; болезни Крона; отторжения трансплантата; рассеянного склероза; системной красной волчанки (SLE); неспецифического язвенного колита; ишемического повреждения при реперфузии; рестеноза; атеросклероза; акне; диабета типа 1, диабета типа 2; сепсиса и хронического обструктивного заболевания легких (COPD).
EA201100846A 2008-11-26 2009-11-24 Пиразолилзамещенные производные угольной кислоты в качестве модуляторов рецептора простациклина (pgi2), применимые для лечения связанных с ним нарушений EA022799B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US20039308P 2008-11-26 2008-11-26
PCT/US2009/006251 WO2010068242A1 (en) 2008-11-26 2009-11-24 Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (pgi2) receptor useful for the treatment of disorders related thereto

Publications (2)

Publication Number Publication Date
EA201100846A1 true EA201100846A1 (ru) 2012-01-30
EA022799B1 EA022799B1 (ru) 2016-03-31

Family

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EA201100846A EA022799B1 (ru) 2008-11-26 2009-11-24 Пиразолилзамещенные производные угольной кислоты в качестве модуляторов рецептора простациклина (pgi2), применимые для лечения связанных с ним нарушений

Country Status (16)

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US (6) US20110224262A1 (ru)
EP (2) EP2367797A1 (ru)
JP (1) JP5603343B2 (ru)
KR (1) KR101707247B1 (ru)
CN (1) CN102292321B (ru)
AU (1) AU2009325117C1 (ru)
BR (1) BRPI0921369B8 (ru)
CA (1) CA2744124C (ru)
EA (1) EA022799B1 (ru)
HK (1) HK1257652A1 (ru)
IL (1) IL212966A (ru)
MX (1) MX2011005577A (ru)
NZ (1) NZ593002A (ru)
SG (1) SG171413A1 (ru)
WO (1) WO2010068242A1 (ru)
ZA (1) ZA201103813B (ru)

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Publication number Publication date
SG171413A1 (en) 2011-07-28
US11098034B2 (en) 2021-08-24
ZA201103813B (en) 2012-10-31
US20150191455A1 (en) 2015-07-09
AU2009325117C1 (en) 2014-12-18
MX2011005577A (es) 2011-08-03
HK1257652A1 (zh) 2019-10-25
US20140171469A1 (en) 2014-06-19
US9663500B2 (en) 2017-05-30
CN102292321A (zh) 2011-12-21
US10689372B2 (en) 2020-06-23
NZ593002A (en) 2013-08-30
EP2367797A1 (en) 2011-09-28
IL212966A0 (en) 2011-07-31
EP3342767A1 (en) 2018-07-04
AU2009325117A1 (en) 2010-06-17
EA022799B1 (ru) 2016-03-31
JP2012509936A (ja) 2012-04-26
JP5603343B2 (ja) 2014-10-08
EP3342767B1 (en) 2021-04-14
CA2744124C (en) 2018-05-01
US9012478B2 (en) 2015-04-21
BRPI0921369B1 (pt) 2020-09-29
US20110224262A1 (en) 2011-09-15
US10214518B2 (en) 2019-02-26
WO2010068242A1 (en) 2010-06-17
CN102292321B (zh) 2015-08-12
CA2744124A1 (en) 2010-06-17
AU2009325117B2 (en) 2014-07-10
KR101707247B1 (ko) 2017-02-15
US20190270731A1 (en) 2019-09-05
KR20110095914A (ko) 2011-08-25
US20180030039A1 (en) 2018-02-01
BRPI0921369B8 (pt) 2021-05-25
US20200392123A1 (en) 2020-12-17
IL212966A (en) 2015-03-31
BRPI0921369A2 (pt) 2015-12-29

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