C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 311/58 (2006.01) A61K 31/135 (2006.01) A61K 31/275 (2006.01) A61K 31/33 (2006.01) C07C 225/20 (2006.01) C07C 255/56 (2006.01) C07D 405/04 (2006.01) C07D 407/04 (2006.01) C07D 409/04 (2006.01) C07D 413/04 (2006.01)
Patent
CA 2193367
This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by formula (I), wherein R1 and R2, independent from each other, are selected from the following: C1-6 perfluoroalkoxy, C1-6 perfluoroalkyl, C1-6 alkyl, C1-6 alkoxy, hydroxyl, C1-6 alkoxycarbonyl, nitro, cyano, halogen, C1-6 alkylsulfonamido, C1-6 perfluoroalkylsulfonamido, amino, C1-6 acylamino, C1-6 perfluoroacylamino, mono or di-C 1-12 alkylamino, C1-6 alkylsulfonyl, C6-10 arylsulfonyl, carboxyl, C1-12 mono or di-alkylaminocarbonyl, or hydrogen; a and b together form an -O- linkage, C=O, or a direct bond; R3 and R4, independent from each other, are H or C1-6 alkyl, optionally substituted by fluorine; R5 is amino or C1-12 mono alkylamine; R6 is H, C1-6 perfluoroalkyl, C1-6 alkyl, C6-10 aryl, or mono or bicyclic heteroaryl containing 1-3 heteroatoms selected from N, O, or S.
L'invention concerne de nouveaux 4-(3,4-dioxocyclobutène-1-yl)chromènes et dihydronaphthalénones et 3-(3,4-dioxocyclobutène-1-yl)indènes, ainsi que leurs sels, présentant une efficacité de relâchement des muscles lisses, leur utilisation dans le traitement de l'hypertension, ainsi que dans le traitement de maladies vascularres périphériques, de la défaillance cardiaque oedémateuse, de maladies impliquant une contraction excessive des muscles lisses des voies urinaires, telles que l'incontinence, ou des voies gastrointestinales, telles que la colopathie fonctionnelle, de l'asthme et de la perte des cheveux, ainsi que des compositions pharmaceutiques contenant les composés représentés par la formule (I) dans laquelle: R¿1? et R¿2?, indépendant l'un de l'autre, sont sélectionnés à partir de: perfluoroalcoxy C¿1-6?, perfluoroalkyle C¿1-6?, alkyle C¿1-6?, alcoxy C¿1-6?, hydroxyle, alcoxycarbonyle C¿1-6?,nitro, cyano, halogène, alkylsulfonamido C¿1-6?, perfluoroalkylsulfonamido C¿1-6?, amino, acylamino C¿1-6? perfluoroacylamino C¿1-6?, mono ou di-alkylamino C¿1-12?, alkylsulfonyle C¿1-6?, arylsulfonyle C¿6-10?, carboxyle, mono ou di-alkylaminocarbonyle C¿1-12? ou hydrogène; a et b constituent ensemble une liaison -O-, C=O ou une liaison directe; R¿3? et R¿4?, indépendant l'un de l'autre, représentent H ou alkyle C¿1-6?, éventuellement substitué par fluor; R¿5? représente amino ou mono alkylamine C¿1-12?; R¿6? représente H, perfluoroalkyle C¿1-6?, aryle C¿6-10? ou hétéroaryle mono ou bicyclique contenant 1-3 hétéroatomes sélectionnés à partir de N, O ou S.
Dollings Paul Jeffrey
Soll Richard Michael
American Home Products Corporation
Ridout & Maybee Llp
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