Indole derivatives as cgmp-pde inhibitors

Details Indole derivatives as cgmp-pde inhibitors Indole derivatives as cgmp-pde inhibitors

C - Chemistry, Metallurgy

07

D

C07D 403/04 (2006.01) A61K 31/395 (2006.01) C07D 209/04 (2006.01) C07D 209/08 (2006.01) C07D 209/12 (2006.01) C07D 209/14 (2006.01) C07D 209/16 (2006.01) C07D 209/30 (2006.01) C07D 209/42 (2006.01) C07D 209/52 (2006.01) C07D 209/80 (2006.01) C07D 209/88 (2006.01) C07D 401/00 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 403/00 (2006.01) C07D 403/12 (2006.01) C07D 405/00 (2006.01) C07D 405/06 (2006.01) C07D 405/12 (2006.01) C07D 409/00 (2006.01) C07D 409/06 (2006.01) C07D 413/00 (2006.01) C07D 4

Patent

CA 2217707

This invention relates to new indole derivatives of formula (I), wherein R1 is hydrogen, halogen, nitro, carboxy, protected carboxy, acyl, etc., R2 is hydrogen, halogen, lower alkenyl, acyl, etc., R3 is lower alkenyl or lower alkyl, both of which are optionally substituted with aryl optionally substituted with one or more substituent(s) selected from the group consisting of halogen, aryl, lower alkoxy, etc., and R4 is carboxy, protected carboxy, acyl, etc., in addition to their significances above, R1 and R2, together with the carbon atoms to which they are attached, represent a 4- to 7-membered carboxylic ring optionally substituted with oxo, or its pharmaceutically acceptable salt, which is useful as a medicament; and to new use of cyclic nucleotide-PDE inhibitors.

La présente invention concerne de nouveaux dérivés d'indole de formule (I), R?1¿ représentant hydrogène, halogène, nitro, carboxy, carboxy protégé, acyle, etc.; R?2¿ représentant hydrogène, halogène, alcényle inférieur, acyle, etc.; R?3¿ alcényle inférieur ou alkyle inférieur, tous deux étant éventuellement substitués avec aryle éventuellement substitué avec un ou plusieurs substituants choisis dans le groupe comprenant halogènes, aryle, alcoxy inférieur, etc., et R?4¿ représente carboxy, carboxy protégé, acyle, etc.; outre leurs significations ci-dessus, R?1¿ et R?2¿, avec les atomes de carbone auxquels ils sont fixés, représentent ensemble un noyau carbocyclique de 4 à 7 éléments, éventuellement substitué avec oxo; ou son sel acceptable sur le plan pharmaceutique, qui est utile comme médicament. L'invention concerne aussi un nouvel emploi d'inhibiteurs de PDE de nucléotides cycliques.

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