C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 279/18 (2006.01) A61K 31/155 (2006.01) A61K 31/27 (2006.01) A61K 31/275 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) C07C 205/11 (2006.01) C07C 205/12 (2006.01) C07C 205/19 (2006.01) C07C 205/37 (2006.01) C07C 205/56 (2006.01) C07C 229/42 (2006.01) C07C 279/36 (2006.01) C07C 323/44 (2006.01) C07C 323/62 (2006.01) C07C 335/20 (2006.01) C07C 335/22 (2006.01) C07C 335/32 (2006.01) C07C 381/14 (2006.01) C07D 209/48 (2006.01) C07D 295/135 (2006.01)
Patent
CA 2206005
Compounds represented by the general formula (1): (see formula I) (where R1 is SR6 or NR7R8, where R6 is typically an alkyl group having 1 - 6 carbon atoms, R7 is a hydrogen atom, an alkyl group having 1 - 6 carbon atoms or a nitro group, and R8 is a hydrogen atom or an alkyl group having 1 - 6 carbon atoms; R2 and R3 are each typically a hydrogen atom or an alkyl group having 1 - 6 carbon atoms; R4 is a hydrogen atom, an alkyl group having 1 - 6 carbon atoms or an amidino group of which the amine portion may be substituted by an alkyl or nitro group; R5 is a hydrogen atom or an alkyl group having 1 - 6 carbon atoms; Y1, Y2, Y3 and Y4 which may be the same or different are each typically a hydrogen atom, a halogen atom or an alkoxy group having 1 - 6 carbon atoms; n and m are each an integer of 0 or 1), or possible stereoisomers or optically active forms of the compounds or pharmaceutically acceptable salts thereof. The compounds possess a potent nitric oxide synthase inhibiting activity and are useful as therapeutics of cerebrovascular diseases.
L'invention concerne un composé représenté par la formule générale (1), des stéréoisomères et des isomères optiques possibles de celui-ci, ainsi que ses sels acceptables sur le plan médical. Dans cette formule, R<1> représente SR6 ou NR7R8; R6 représente un alkyleC1-C6, etc; R7 représente un hydrogène, un alkyleC1-C6 ou un nitro; R8 représente un hydrogène ou un alkyleC1-C6; R2 et R3 représentent chacun un hydrogène ou un alkyleC1-C6, etc; R<4> représente un hydrogène, un alkyleC1-C6 ou amidino où le fragment amine peut être remplacé par un alkyle ou un nitro; R5 représente un hydrogène ou un alkyleC1-C6; Y1, Y2, Y3 et Y4 peuvent être identiques ou différents et chacun représente un hydrogène, un halogéno, un alcoxy C1-C6, etc; et n et m représentent chacun un 0 ou 1. Le composé a un effet puissant d'inhibition de la monoxyde d'azote synthétase et il est utile comme remède contre les troubles cérébro-vasculaires.
Honda Toshio
Kimura Nobuaki
Kitoh Yasushi
Makino Toshihiko
Nagafuji Toshiaki
Chugai Seiyaku Kabushiki Kaisha
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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