C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 403/00 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01) C07D 209/08 (2006.01) C07D 215/08 (2006.01) C07D 223/14 (2006.01) C07D 223/16 (2006.01) C07D 223/20 (2006.01) C07D 241/44 (2006.01) C07D 243/04 (2006.01) C07D 243/12 (2006.01) C07D 401/00 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 403/06 (2006.01) C07D 405/14 (2006.01) C07D 413/12 (2006.01) C07D 453/02 (2006.01) C07D 471/04 (2006.01)
Patent
CA 2121112
ABSTRACT OF THE DISCLOSURE Compounds of the formula: Image (I) wherein R1 is hydrogen or lower alkyl, R2 is hydrogen, lower alkyl, halo(lower)alkyl, halogen or lower alkoxy, R3 and R4 are each hydrogen, lower alkyl or taken together to form oxo, R5 is hydrogen, halogen, nitro, hydroxy, protected hydroxy, lower alkyl or lower alkoxy optionally substituted with lower alkylamino, R6 is hydrogen, lower alkyl or acyl, A is Image , Image , Image , Image or Image in which R7 is hydrogen; lower alkyl optionally substituted with halogen, amino, lower alkylamino, protected amino, acyl, a heterocyclic group, hydroxy or protected hydroxy; or acyl; and R8 and R9 are each hydrogen, or taken together to form oxo or thioxo; or R7 and R8 are taken together to form a bond; and R9 is lower alkylamino, N-lower alkylpiperazinyl or lower alkylthio optionally substituted with lower alkylamino; R10 is hydrogen; R11 is hydrogen, hydroxy, lower alkylamino or lower alkyl optionally substituted with acyl; or R10 and R11 are taken together to form oxo or lower alkoxyimino optionally substituted with acyl; R12 is lower alkyl optionally substituted with acyl; and R13 is lower alkyl; X1 is CH or N, X2 is CH or N, Y is Image or Image in which R14 is hydrogen, halogen, hydroxy or lower alkoxy, R15 is aryloxy, naphthyl, phenyl substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, halogen, halo(lower)alkyl, hydroxy, amino(lower)alkyl, azido(lower)alkyl, lower alkylamino(lower)alkyl, acylamino(lower)alkyl, hydroxy(lower)alkyl, cyano and acyl, or a heterocyclic group, and R16 is aryl, and n is 0, 1 2 or. 3, and pharmaceutically acceptable salts thereof. These derivatives possess vasopressin antagonistic activity, vasodilating activity, hypotensive activity, activity for inhibiting saccharide release in liver, activity for inhibiting growth of masegium cells, water diuretic activity, platelet agglutination inhibitory activity, oxytocin antagonistic activity and the like. Pharmaceutical compositions containing same methods of preparation thereof and methods for the treatment and/or prevention of hypertension, heart failure, renal insufficiency, edema, ascites, vasopressin parasecretion syndrome, hepatocirrhosis, hyponatremia, hypokalemia, diabetic, circulation disorder, oxytocin related diseases (e.g. premature delivery, dysmenorrhea, endometritis, etc) and the like, are also disclosed.
Hemmi Keiji
Ohkawa Takehiko
Setoi Hiroyuki
Tanaka Hirokazu
Zenkoh Tatsuya
Fujisawa Pharmaceutical Co. Ltd.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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