EA201200917A1 - Пролекарства ингибиторов плазменного калликреина - Google Patents

Пролекарства ингибиторов плазменного калликреина

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Publication number
EA201200917A1
EA201200917A1 EA201200917A EA201200917A EA201200917A1 EA 201200917 A1 EA201200917 A1 EA 201200917A1 EA 201200917 A EA201200917 A EA 201200917A EA 201200917 A EA201200917 A EA 201200917A EA 201200917 A1 EA201200917 A1 EA 201200917A1
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EA
Eurasian Patent Office
Prior art keywords
plasma kallikrein
procaraxes
kallikrein inhibitors
prodrugs
inhibitors
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Application number
EA201200917A
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English (en)
Inventor
Суканто Синха
Тэми Джо Чилкоут
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Эктивсайт Фармасьютикалз, Инк.
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Application filed by Эктивсайт Фармасьютикалз, Инк. filed Critical Эктивсайт Фармасьютикалз, Инк.
Publication of EA201200917A1 publication Critical patent/EA201200917A1/ru

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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
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    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 with substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • 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
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    • 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
    • C07D403/10—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 aromatic rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

Изобретение относится к пролекарствам соединений, ингибирующих активность плазменного калликреина (PK), и способам предотвращения и лечения болезней или состояний, зависящих от плазменного калликреина, например диабетического отека желтого пятна, с помощью пролекарств, имеющих формулу (I).
EA201200917A 2009-12-18 2010-12-17 Пролекарства ингибиторов плазменного калликреина EA201200917A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US28447809P 2009-12-18 2009-12-18
US34504510P 2010-05-14 2010-05-14
PCT/US2010/061122 WO2011075684A1 (en) 2009-12-18 2010-12-17 Prodrugs of inhibitors of plasma kallikrein

Publications (1)

Publication Number Publication Date
EA201200917A1 true EA201200917A1 (ru) 2012-12-28

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EA201200917A EA201200917A1 (ru) 2009-12-18 2010-12-17 Пролекарства ингибиторов плазменного калликреина

Country Status (13)

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US (1) US8609866B2 (ru)
EP (1) EP2512466A4 (ru)
JP (1) JP2013515000A (ru)
KR (1) KR20120120237A (ru)
CN (1) CN102762203A (ru)
AU (1) AU2010330743A1 (ru)
BR (1) BR112012014990A2 (ru)
CA (1) CA2783801A1 (ru)
EA (1) EA201200917A1 (ru)
IL (1) IL220429A0 (ru)
MX (1) MX2012006913A (ru)
SG (2) SG10201408429UA (ru)
WO (1) WO2011075684A1 (ru)

Cited By (11)

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RU2660421C2 (ru) * 2013-01-08 2018-07-06 Калвиста Фармасьютикалз Лимитед Бензиламиновые производные
RU2674028C2 (ru) * 2013-08-14 2018-12-04 Калвиста Фармасьютикалз Лимитед Ингибиторы ферментов
US10611758B2 (en) 2014-11-27 2020-04-07 Kalvista Pharmaceuticals Limited N-((het)arylmethyl)-heteroaryl-carboxamides compounds as kallikrein inhibitors
US10752607B2 (en) 2016-06-01 2020-08-25 Kalvista Pharmaceuticals Limited Polymorphs of N-[(6-cyano-2-fluoro)-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide as kallikrein inhibitors
US10781181B2 (en) 2014-11-27 2020-09-22 Kalvista Pharmaceuticals Limited N-((het) arylmethyl)-heteroaryl-carboxamides compounds as plasma kallikrein inhibitors
RU2739447C2 (ru) * 2016-05-31 2020-12-24 Калвиста Фармасьютикалз Лимитед Производные пиразола в качестве ингибиторов калликреина
US11230537B2 (en) 2016-06-01 2022-01-25 Kalvista Pharmaceuticals Limited Polymorphs of n-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[2-oxopyridin-1-yl)methyl]phenyl} methyl)pyrazole-4-carboxamide as iallikrein inhibitors
US11234939B2 (en) 2017-11-29 2022-02-01 Kalvista Pharmaceuticals Limited Dosage forms comprising a plasma kallikrein inhibitor
US11242333B2 (en) 2013-08-14 2022-02-08 Kalvista Pharmaceuticals Limited Inhibitors of plasma kallikrein
US11584735B2 (en) 2017-11-29 2023-02-21 Kalvista Pharmaceuticals Limited Solid forms of a plasma kallikrein inhibitor and salts thereof
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EP2697196A1 (en) * 2011-04-13 2014-02-19 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
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JP6652922B2 (ja) 2013-08-28 2020-02-26 アイオーニス ファーマシューティカルズ， インコーポレーテッドＩｏｎｉｓ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． プレカリクレイン（ｐｋｋ）発現の調節
CN105873951A (zh) 2013-10-21 2016-08-17 戴埃克斯有限公司 用于确定血浆激肽释放酶***生物标记的试验
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PE20170684A1 (es) 2014-08-04 2017-06-15 Nuevolution As Derivados de heterociclilo opcionalmente condensados de pirimidina utiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncologicas y autoinmunitarias
MA41562B1 (fr) 2015-06-03 2019-05-31 Bristol Myers Squibb Co Agonistes d'apj 4-hydroxy-3-(heteroaryl)pyridine-2-one a utiliser dans le traitement de troubles cardio-vasculaires
PL3365685T3 (pl) 2015-10-19 2021-08-02 Dyax Corp. Test immunologiczny do wykrywania rozszczepionego wielkocząsteczkowego kininogenu
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JP2023519603A (ja) 2020-03-31 2023-05-11 ヌエヴォリューション・アクティーゼルスカブ 核内受容体に対して活性な化合物
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Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2660421C2 (ru) * 2013-01-08 2018-07-06 Калвиста Фармасьютикалз Лимитед Бензиламиновые производные
US11242333B2 (en) 2013-08-14 2022-02-08 Kalvista Pharmaceuticals Limited Inhibitors of plasma kallikrein
RU2674028C2 (ru) * 2013-08-14 2018-12-04 Калвиста Фармасьютикалз Лимитед Ингибиторы ферментов
US10221161B2 (en) 2013-08-14 2019-03-05 Kalvista Pharmaceuticals Limited Inhibitors of plasma kallikrein
US10611758B2 (en) 2014-11-27 2020-04-07 Kalvista Pharmaceuticals Limited N-((het)arylmethyl)-heteroaryl-carboxamides compounds as kallikrein inhibitors
US10781181B2 (en) 2014-11-27 2020-09-22 Kalvista Pharmaceuticals Limited N-((het) arylmethyl)-heteroaryl-carboxamides compounds as plasma kallikrein inhibitors
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IL220429A0 (en) 2012-08-30
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AU2010330743A1 (en) 2012-07-05
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