Compounds bearing sulphamoyl and amidino radicals, their prepara

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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549 65, 549 59, 549 60, 549 77, 548527, 548540, 5483111, 5483117, 5483151, 548465, 546213, 5462814, 5462804, 544146, 544379, 544333, 514422, 514256, 514385, 514252, 514336, 514397, 514444, 514445, C07D33322, C07D40912, C07D41312, A61K 3138

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active

056748906

ABSTRACT:
A compound of formula I ##STR1## in which Ar.sub.1 is naphthyl and phenyl, quinolyl or isoquinolyl optionally substituted; Ar.sub.2 is phenyl or thienyl optionally substituted; R.sub.1, R.sub.2 and R'.sub.2 are independently of each other H or (C.sub.1 -C.sub.4)alkyl or R.sub.1 represents a bond and N is covalently bonded to Ar.sub.2, and optionally R.sub.2 and R'.sub.2 form a double bond, or R.sub.1 or R.sub.2 is covalently bonded to Ar.sub.2 and represents a (C.sub.1 -C.sub.3 )alkylene; R.sub.3 and R.sub.4 are independently of each other H or (C.sub.1 -C.sub.4)alkyl or form, with the nitrogen atom to which they are attached pyrrolidine, ppiperidine, or hexahydroazepine; Z.sub.1 represents (C.sub.1 -C.sub.12)alkylene, optionally interrupted by a radical selected from the group consisting of (C.sub.5 -C.sub.7)cycloalkyl and phenyl or substituted with a radical selected from the group consisting of (C.sub.5 -C.sub.7)cycloalkyl and phenyl; Q.sub.1 is selected from the group consisting of methyl, amino, (C.sub.1 -C.sub.4)alkoxycarbonylamino, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1 -C.sub.4)-alkylamino, pyrrolidinyl, piperidino, morpholino, piperazinyl, 4-(C.sub.1 -C.sub.4)alkylpiperazinyl, amidino, (C.sub.1 -C.sub.4)-alkylamidino, guanidino, (C.sub.1 -C.sub.4)alkylguanidino, pyridyl, imidazolyl, pyrimidinyl, indolyl, hydroxy,(C.sub.1 phenyl substituted by a radical selected from the group consisting of Cl, F, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and hydroxyle; Q.sub.2 is selected from the group consisting of H and (C.sub.1 -C.sub.4)alkyl; Q.sub.3 is selected from the group consisting of H and (C.sub.1 -C.sub.4)alkyl or Q.sub.1 and Q.sub.3 are attached to form a heterocycle and together represent (C.sub.2 -C.sub.3)alkylene, whereas Z.sub.1 represents a bond, in the form of pure enantiomer or mixture thereof in any proportions as well as its salt with acid.

REFERENCES:
patent: 4791102 (1988-12-01), Bernat et al.
patent: 5348976 (1994-09-01), Shibata et al.
M.C. Michel et al., "Neuropeptide Y and its antigonists", Drugs of the Future vol. 17, No. 1, 1992, pp. 39-45.

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