C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
167/211, 167/270
C07C 211/40 (2006.01) A61K 31/13 (2006.01) A61K 31/395 (2006.01) C07C 215/08 (2006.01) C07C 215/42 (2006.01) C07D 295/03 (2006.01) C07D 295/033 (2006.01)
Patent
CA 2037721
ABSTRACT A substituted-amine compound of the following formula : Image Image wherein a group of the formula : is cyclo(lower)alkyl or cyclo(lower)alkenyl, R1 and R2 are each hydrogen, lower alkyl, cyclo(lower)alkyl or aryl which may have one or more suitable substituent(s), R3 is lower-alkyl which may have one or more suitable substituent(s), lower alkynyl which may have one or more suitable substituent(s) or cyclo(lower)alkyl which may have one or more suitable substituent(s), R4 is hydrogen, lower alkyl or ar(lower)alkyl, in which R3 and R4 may be linked together to form a heterocyclic group which may have one or more suitable substituent(s), R5 and R6 are each hydrogen or hydroxy, with proviso that (i) R3 is t-butyl, when a group of the formula : Image is cyclopentyl, R1 and R2 are each phenyl which may have chloro, and R5 and R6 are each hydrogen, (ii) R3 is t-butyl, when a group of the formula : Image is cyclohexyl, R1 and R2 are each phenyl, and R5 is hydrogen, (iii) R3 is t-butyl, when a group of the formula : Image is cyclohexenyl, R1 and R2 are each phenyl, and R5 and R6 are each hydrogen, and (iv) R3 is t-butyl, when a group of the formula : Image is cyclopentenyl, and R1, R2, R5 and R6 are each hydrogen, and a pharmaceutically acceptable salt thereof. These compounds have anticholinergic activity and sodium channel blocking activity and are useful for the prevention and/or treatment of dysuria such as pollakiuria, urinary incontinence or the like in case of nervous pollakiuria, neurogenic bladder dysfunction, nocturia, unstable bladder, cystospasm, chronic cystitis, chronic prostatitis or the like; for the prevention and/or treatment of spasm and/or hypanakinesis in case of gastric ulcer, duodenal ulcer, gastroxynsis, esophagospasm, gastritis, enteritis, irritable colon syndrome, enteralgia, cholecystitis, cholangitis, pylorospasm, pancreatitis, pain in case of pancreatitis, biliary dyskinesia, after effect after cholecystectomy, urinary calculus, cystitis, dysmenorrhea, hydrosis, spasm, of urinary tract; and for the prevention and/or treatment of arrhythmia, congestive heart failure, or the like. They are useful as local anesthetic and are expected to be useful for the prevention and/or treatment of asthma, Parkinson disease, angina pectris or the like. The process for the preparation thereof, pharmaceutical compositions comprising the same and a method for the prevention and/or treatment of aforesaid diseases in human being or animals are also disclosed.
Okumura Kazuo
Shiokawa Youichi
Take Kazuhiko
Tsubaki Kazunori
Fujisawa Pharmaceutical Co. Ltd.
Swabey Ogilvy Renault
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