C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 417/04 (2006.01) A61K 31/33 (2006.01) C07D 333/38 (2006.01) C07D 409/04 (2006.01) C07D 413/04 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01)
Patent
CA 2321025
The present invention is directed to compounds of Formula (I), wherein X is O, S or NR7 and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula (I). The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
Cette invention concerne des composés de formule (I), ainsi que des hydrates, des solvates ou des sels pharmaceutiquement acceptables de ces derniers. Dans la formule (I), X représente O, S ou NR?7¿ et R?1¿-R?7¿, Y et Z sont tels que définis dans le descriptif. Cette invention concerne également des procédés de préparation des composés de formule (I). Les nouveaux composés de cette invention sont de puissants inhibiteurs de protéases, plus spécifiquement de sérine protéases du type trypsine, comme la chymotrypsine, la trypsine, la plasmine et l'urokinase. Certains composés assurent l'inhibition directe et sélective de l'urokinase, ou bien servent d'intermédiaires utiles pour former des composés possédant une telle activité.
Hoffman James B.
Illig Carl R.
Rudolph M. Jonathan
Subasinghe Nalin L.
Wilson Kenneth J.
3-Dimensional Pharmaceuticals Inc.
Mbm Intellectual Property Law Llp
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