NO960629L - (Ikke-peptid endothelin-antagonister I). Substituerte 2 (5H) furanon-,2 (5H) tiofenon- og 2 (5H) pyrrolonderivater, deres fremstilling og deres anvendelse som endetholin-antagonister - Google Patents

(Ikke-peptid endothelin-antagonister I). Substituerte 2 (5H) furanon-,2 (5H) tiofenon- og 2 (5H) pyrrolonderivater, deres fremstilling og deres anvendelse som endetholin-antagonister

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Publication number
NO960629L
NO960629L NO960629A NO960629A NO960629L NO 960629 L NO960629 L NO 960629L NO 960629 A NO960629 A NO 960629A NO 960629 A NO960629 A NO 960629A NO 960629 L NO960629 L NO 960629L
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substituted
unsubstituted
alkyl
substituents
carbon atoms
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NO960629A
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English (en)
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NO960629D0 (no
Inventor
Kent Alan Berryman
Annette Marian Doherty
Jeremy John Edmunds
William Chester Patt
Mark Stephen Plummer
Joseph Thomas Repine
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Warner Lambert Co
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Publication of NO960629L publication Critical patent/NO960629L/no
Publication of NO960629D0 publication Critical patent/NO960629D0/no

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Abstract

Forbindelser med formel (I) eller en tautomer åpenkjedet ketosyre-form derav, eller et farmasøytisk akseptabelt salt derav, hvor: R! er alkyl, usubstituert eller substituert, rettkjedet eller forgrenet, med l til 12 karbonatomer, cyklo- alkyl, usubstituert eller substituert med 3 til 12 karbon- atomer, fenyl substituert med l til 5 substituenter, naftyl usubstituert eller substituert med l til 5 substituent- er, eller heteroaryl usubstituert eller substituert med l til 5 substituenter; R2 er alkyl, usubstituert eller substituert, rettkjedet eller forgrenet, med fra l til 12 karbonatomer, cykloalkyl, usubstituert eller substituert med 3 til 12 karbonatomer, aryl som er usubstituert eller substituert med l til 5 substituenter, heteroaryl som er usubstituert eller substituert med l til 3 substituenter, R3 er alkyl, usubstit- uert eller substituert, rettkjedet eller forgrenet, med fra l til 12 karbonatomer, cykloalkyl, usubstituert eller substit- uert med 3 til 12 karbonatomer, aryl som er usubstituert eller substituert med l til 5 substituenter, heteroaryl som er usubstituert eller substituert med l til 3 substituenter, R« er hydrogen, hydroksy, halogen, SRS/ OR5, hvor R5 er alkyl eller substituert alkyl med l til 7 karbonatomer, NR6R7, hvor R, og R7 uavhengig av hverandre, er hydrogen, alkyl, substituert alkyl, substituert eller usubstituert fenyl, og (CH2)nOR5, hvor n er et heltall fra l til 3; X er oksygen, S eller NR,, hvor R, er hydrogen, alkyl eller substituert alkyl, med det forbehold at når R! er monosubstituert fenyl og substituenten er p-metoksy, da er R3 ikke usubstituert fenyl, monosubstituert fenyl eller mesityl, og med det ytterligere forbehold at når R, er alkyl- substituert, da er substituenten ikke oksygen i a-stillingen til furanonringen, og med det ytterligere forbehold at R^ og R3 ikke begge er alkyl eller alkyl substituert i samme molekyl, deres anvendelse som ikke-peptid-antagonister av endothelin I, så vel som fremgangsmåter for fremstilling av farmasøytiske blandinger av disse, som er anvendelige ved behandling av forhøyede nivåer av endothelin, akutt og kronisk nyresvikt, hypertensjonr myokardinfarkt, myokardischemi, cerebral vaso- spasme, cerebral ischemi, cerebral infarktasjon, cirrhose, septisk sjokk, kongestiv hjertesvikt, endotoksisk sjokk, subaraknoidalblødning, arytmier, astma, preeklampsi, atero- sklerotiske lidelser inklusivt Raynauds fenomen og restenose, angina, kreft, pulmonal hypertensjon, ischemisk sykdom, skade av maveslimhinne, blødningssjokk, ischemisk tarmsykdom, slag og diabetes.
NO960629A 1993-08-19 1996-02-16 (Ikke-peptid endothelin-antagonister I). Substituerte 2 (5H) furanon-,2 (5H) tiofenon- og 2 (5H) pyrrolonderivater, deres fremstilling og deres anvendelse som endetholin-antagonister NO960629D0 (no)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US10975193A 1993-08-19 1993-08-19
US21757894A 1994-03-24 1994-03-24
US27888294A 1994-07-26 1994-07-26
PCT/US1994/009091 WO1995005376A1 (en) 1993-08-19 1994-08-09 Substituted 2(5h)furanone, 2(5h)thiophenone and 2(5h)pyrrolone derivatives, their preparation and their use as endothelin antagonists

Publications (2)

Publication Number Publication Date
NO960629L true NO960629L (no) 1996-02-16
NO960629D0 NO960629D0 (no) 1996-02-16

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NO960629A NO960629D0 (no) 1993-08-19 1996-02-16 (Ikke-peptid endothelin-antagonister I). Substituerte 2 (5H) furanon-,2 (5H) tiofenon- og 2 (5H) pyrrolonderivater, deres fremstilling og deres anvendelse som endetholin-antagonister

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US (2) US5691373A (no)
EP (1) EP0714391A1 (no)
JP (1) JPH09501920A (no)
KR (1) KR960703901A (no)
AU (1) AU693110B2 (no)
CA (1) CA2165567A1 (no)
CZ (1) CZ40996A3 (no)
FI (1) FI960671A (no)
HU (1) HUT74179A (no)
NO (1) NO960629D0 (no)
NZ (1) NZ271833A (no)
SK (1) SK20396A3 (no)
WO (1) WO1995005376A1 (no)

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KR960703901A (ko) 1996-08-31
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US5691373A (en) 1997-11-25
WO1995005376A1 (en) 1995-02-23
NZ271833A (en) 1997-08-22
EP0714391A1 (en) 1996-06-05
AU7561794A (en) 1995-03-14
FI960671A (fi) 1996-04-19
CA2165567A1 (en) 1995-02-23
US6017916A (en) 2000-01-25
AU693110B2 (en) 1998-06-25
HU9600365D0 (en) 1996-04-29
HUT74179A (en) 1996-11-28
JPH09501920A (ja) 1997-02-25
SK20396A3 (en) 1997-03-05
CZ40996A3 (en) 1996-09-11

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