C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 209/12 (2006.01) A61K 31/404 (2006.01) A61P 9/10 (2006.01)
Patent
CA 2509222
This invention provides indole oxo-acetyl amino acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure of Formula (I) : wherein: R1 is alkyl or optionally substituted cycloalkyl, -CH2- cycloalkyl, pyridinyl, -CH2-pyridinyl, phenyl or benzyl; R2 is hydrogen, alkyl, cycloalkyl, -CH2-cycloalkyl, or perfluoroalkyl; R3 is hydrogen, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, -CH2-cycloalkyl, -NH2, or -N02; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or -CH2- pyridinyl; R8 is hydrogen, alkyl, cycloalkyl, -CH2-cycloalkyl, perfluoroalkyl, aryl, substituted aryl, alkyl-aryl, or substituted alkyl-aryl; R9 is hydrogen, alkyl, hydroxyalkyl, 4-hydroxybenzyl, 3-indolylymethylene, 4-imidazolyl- methylene, HSCH2-, CH3SCH2CH2-, H2NC(=O)CH2-, H2NC(=O)CH2CH2-, H02CCH2-, H02CCH2CH2-, H2NCH2CH2CH2CH2-, H2NC(=NH)NHCH2CH2CH2-, or taken together with R8 as -CH2CH2CH2-; or a pharmaceutically acceptable salt or ester form thereof.
L'invention concerne des dérivés d'acide indole oxo-acétyl amino acétique utilisés comme inhibiteurs de l'inhibiteur-1 de l'activateur du plasminogène (PAI-1) servant dans le traitement de troubles fibrinolytiques, les composés ayant la structure (I), dans laquelle R¿1? est alkyle ou éventuellement cycloalkyle, -CH¿2?-cycloalkyle, pyridinyle, -CH¿2?-pyridinyle, phényle ou benzyle substitués ; R¿2? représente hydrogène, alkyle, cycloalkyle, -CH¿2?-cycloalkyle, ou perfluoroalkyle ; R¿3? représente hydrogène, halo, alkyle, perfluoroalkyle, alcoxy, cycloalkyle, -CH¿2?-cycloalkyle, -NH¿2?, ou NO¿2 ?; R¿4? représente éventuellement phényle, benzyle, benzyloxy, pyridinyle, ou CH¿2?-pyridinyle ; R¿8? représente hydrogène, alkyle, cycloalkyle, -CH¿2?-cycloalkyle, perfluoroalkyle, aryle, aryle substitué, alkyle-aryle, ou alkyle-aryle substitué ; R¿9? représente hydrogène, alkyle, hydroxyalkyle, 4-hydroxybenzyle, 3-indolylyméthylène, 4-imidazolyl-méthylène, HSCH¿2?-, CH¿3?SCH¿2?CH¿2?-, H¿2?NC(=O)CH¿2?, H¿2?NC(=O)CH 2CH2-, HO¿2?CCH¿2?-, HO¿2?CCH¿2?CH¿2?-, H¿2?NCH¿2?CH¿2?CH¿2?CH¿2?-, H¿2?NC(=NH)NHCH¿2?CH¿2?CH¿2?-, ou pris ensemble avec R¿8? en tant que CH¿2?CH¿2?CH¿2?- ; ou un sel ou une forme d'ester de ceux-ci pharmaceutiquement acceptable.
Elokdah Hassan Mahmoud
Li David Zenan
Mcfarlane Geraldine Ruth
Smart & Biggar
Wyeth
LandOfFree
Substituted indole oxo-acetyl amino acetic acid derivatives... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Substituted indole oxo-acetyl amino acetic acid derivatives..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Substituted indole oxo-acetyl amino acetic acid derivatives... will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-1667603