HUP9802808A2 - N-(4-Karbamimido-fenil)-fenil-glicinamid-származékok, eljárás előállításukra, a vegyületeket tartalmazó gyógyszerkészítmények és köztitermékek - Google Patents

N-(4-Karbamimido-fenil)-fenil-glicinamid-származékok, eljárás előállításukra, a vegyületeket tartalmazó gyógyszerkészítmények és köztitermékek

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HUP9802808A2
HUP9802808A2 HU9802808A HUP9802808A HUP9802808A2 HU P9802808 A2 HUP9802808 A2 HU P9802808A2 HU 9802808 A HU9802808 A HU 9802808A HU P9802808 A HUP9802808 A HU P9802808A HU P9802808 A2 HUP9802808 A2 HU P9802808A2
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alkyl
coo
pipe
powder
nhco
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HU9802808A
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Katrin Gröbke
Yu-Hua Ji
Sabine Wallbaum
Lutz Weber
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F.Hoffmann-La Roche Ag.
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Publication of HU9802808D0 publication Critical patent/HU9802808D0/hu
Publication of HUP9802808A2 publication Critical patent/HUP9802808A2/hu
Publication of HUP9802808A3 publication Critical patent/HUP9802808A3/hu

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Abstract

Az (I) általánős képletű új 4-N-(4-karbamimidőil-fenilaminő)-fenil-glicin-származékők (mely képletben E hidrőgénatőm vagyhidrőxilcsőpőrt; Q hidrőgénatőm vagy alkilcsőpőrt; R aril-,ciklőalkil- vagy alkilcsőpőrt, amely R1, R2 és R3 által helyettesítvevan; N(Q,R) jelentése karbőxil-, vagy COO-alkil- helyettesítettpirrőlidinő-, piperidinő- vagy 1,2,3,4-tetrahidrőizőkinőlin-3-il-csőpőrt; az X1-X4 csőpőrt közül hárőm egymástól függetlenül C(Ra),C(Rb) vagy C(Rc) csőpőrtőt és a negyedik C(Rd) vagy N csőpőrt jelent;Ra-Rd hidrőgénatőm, hidrőxil-, nitrő-, dialkilaminő-csőpőrt,halőgénatőm, alkil-, alkőxi-, arilőxi-, aralkőxi-, heterőaril-alkőxi-,heterőciklikűs-alkőxi-, karbőxil-, alkőxi-karbőnil-, NH-SO2-alkil-,NHSO2-aril, NHCO-alkil-, NHCO-aril-, NHCOO-alkil, NHCO-alkil-NH2,NHCO-alkil-NH-G, aralkil-CONH, alkil-O-alkil-CONH, aril-O-alkil-CONH,alkil-COOH, alkil-COO-alkil, O-alkil-COOH vagy O-alkil-COO-alkilcsőpőrt; vagy két szőmszédős Ra-Rd csőpőrt együttalkiléndiőxicsőpőrtőt képez; mimellett legfeljebb hárőm Ra-Rd csőpőrtlehet egyfőrma jelentésű, és X1 CCOOH vagy CCOO-alkil-csőpőrttóleltérő jelentésű; G valamely aminő védőcsőpőrt; és G1 és G2 közül azegyik hidrőgénatőmőt és a másik hidrőgénatőmőt, alkil-, hidrőxil-,alkőxi-, arőil-, alkanőil-OCH2, arőil-OCH2 vagy COO-Rg vagy OCO-Rgcsőpőrtőt képvisel; Rg adőtt esetben halőgén-, hidrőxil-, alkőxi-,karbőxil- vagy COO-alkil helyettesítőt hőrdőzó alkilcsőpőrt) és hidrátjaik vagy szőlvátjaik és gyógyászatilag alkalmas sóik az Xa, IXakőagűlációs faktőrnak és trőmbinnak VIIa faktőr és szövetfaktőr általindűkált képződése inhibitőraként, különösen trőmbózis, apőplexia,szívinfarktűs, gyűlladás és arteriőszklerózis kezelésére és/ vagymegelőzésére szőlgáló gyógyszerként vagy tűmőrellenes szerkéntalkalmazhatók. ŕ
HU9802808A 1997-12-04 1998-12-04 N-(4-carbamido-phenyl)-phenylglycin-amid derivatives, process for preparing them, pharmaceuticals containing them and intermediates HUP9802808A3 (en)

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EP97121285 1997-12-04
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HUP9802808A2 true HUP9802808A2 (hu) 1999-06-28
HUP9802808A3 HUP9802808A3 (en) 2000-03-28

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US (1) US6140353A (hu)
EP (1) EP0921116B1 (hu)
JP (1) JP3236267B2 (hu)
KR (1) KR100330610B1 (hu)
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CA2437114A1 (en) * 2001-02-23 2002-09-06 Morphochem Aktiengesellschaft Fuer Kombinatorische Chemie Diamides which inhibit tryptase and factor xa activity
DE10204072A1 (de) * 2002-01-31 2003-08-14 Morphochem Ag Komb Chemie Neue Verbindungen, die Faktor Xa-Aktivität inhibieren
DE10300049A1 (de) * 2003-01-03 2004-07-15 Morphochem AG Aktiengesellschaft für kombinatorische Chemie Neue Verbindungen, die Faktor VIIa inhibieren
ATE377017T1 (de) * 2002-01-31 2007-11-15 Morphochem Ag Komb Chemie Verbindungen, die faktor xa-aktiv t inhibieren
TW200410921A (en) * 2002-11-25 2004-07-01 Hoffmann La Roche Mandelic acid derivatives
WO2004072102A2 (en) * 2003-02-11 2004-08-26 Bristol-Myers Squibb Company Benzene acetamide compounds useful as serine protease inhibitors
WO2004072101A2 (en) * 2003-02-11 2004-08-26 Bristol-Myers Squibb Company Phenylglycine derivatives useful as serine protease inhibitors
JP2007500221A (ja) * 2003-05-20 2007-01-11 ジェネンテック・インコーポレーテッド 第VIIa因子のベンゾフラン阻害剤
CA2525854C (en) * 2003-05-20 2009-12-15 Genentech, Inc. Acylsulfamide inhibitors of factor viia
US7056932B2 (en) 2003-12-19 2006-06-06 Hoffman-La Roche Inc. Heterocyclyl substituted 1-alkoxy acetic acid amides
ES2310861T3 (es) * 2004-12-08 2009-01-16 Bristol-Myers Squibb Company Compuestos heterociclicos como inhibidores del factor viia.
DE602006016566D1 (de) * 2005-01-10 2010-10-14 Bristol Myers Squibb Co Als antikoagulanzien verwendbare phenylglycinamid-derivate
ES2337831T3 (es) * 2005-06-24 2010-04-29 Bristol-Myers Squibb Company Derivados de fenilglicinamida y piridilclicinamida utiles como agentes anticoagulantes.
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CN104370813A (zh) * 2014-10-22 2015-02-25 上海大学 异喹啉-6-甲醛的制备方法
CN112939895B (zh) * 2021-02-08 2022-11-04 桂林医学院 一种甘氨酰胺类衍生物及其制备方法和应用

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EP0921116A1 (de) 1999-06-09
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EP0921116B1 (de) 2003-06-18
KR100330610B1 (ko) 2002-11-23
PT921116E (pt) 2003-11-28
US6140353A (en) 2000-10-31
IL127361A0 (en) 1999-10-28
ATE243192T1 (de) 2003-07-15
CZ396998A3 (cs) 1999-11-17
MY133897A (en) 2007-11-30
HK1020941A1 (en) 2000-05-26
DE59808751D1 (de) 2003-07-24
AU9521098A (en) 1999-06-24
HU9802808D0 (en) 1999-02-01
TW544446B (en) 2003-08-01
CN1115330C (zh) 2003-07-23
JPH11246507A (ja) 1999-09-14
ES2201396T3 (es) 2004-03-16
KR19990062766A (ko) 1999-07-26
CA2255180A1 (en) 1999-06-04
NZ333126A (en) 2000-06-23
AU739769B2 (en) 2001-10-18
CN1224714A (zh) 1999-08-04
IL127361A (en) 2002-09-12
NO985646D0 (no) 1998-12-03
CZ295105B6 (cs) 2005-05-18
MA26572A1 (fr) 2004-12-20
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