C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 417/04 (2006.01) A61K 31/381 (2006.01) A61K 31/426 (2006.01) A61P 43/00 (2006.01) C07D 333/38 (2006.01) C07D 409/04 (2006.01) C07D 409/12 (2006.01) C07D 413/04 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01)
Patent
CA 2362390
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.
L'invention concerne des composés correspondant à la formule (I) dans laquelle X représente O, S ou NR?7¿ et R?1¿-R?7¿, Y et Z possèdent les notifications données dans la description. Elle concerne également des hydrates ou solvates de ces composés, ou des sels de ceux-ci acceptables sur le plan pharmacologique. L'invention concerne encore des procédés de préparation des composés correspondant à la formule (I). Ces nouveaux composés constituent des puissants inhibiteurs des protéases, notamment des sérines protéases du type trypsine, telles que la chymotrypsine, la trypsine, la plasmine et l'urokinase. Certains de ces composés démontrent une inhibition directe et sélective de l'urokinase, ou ils constituent des intermédiaires utiles pour former des composés possédant une telle activité.
Hoffman James B.
Illig Carl R.
Marugan Juan Jose
Rudolph M. Jonathan
Subasinghe Nalin L.
3-Dimensional Pharmaceuticals Inc.
Mbm Intellectual Property Law Llp
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