Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-04-15
1993-06-15
Tsang, Cecilia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5142332, A61K 31495, A61K 31535
Patent
active
052198570
ABSTRACT:
Novel compounds of the formula ##STR1## wherein n is an integer from 1 to 4 inclusive; R.sub.1 represents a mono-or disubstituent of hydrogen, lower alkyl(C.sub.1 -C.sub.3), lower alkoxy(C.sub.1 -C.sub.3), halogen, nitro or trifluoromethyl; R.sub.2 is cyano, carboxamido, ethyl carboxylate or halogen; R.sub.3 is hydrogen, straight or branched chain lower alkyl(C.sub.1 -C.sub.3), alkenyl(C.sub.2 -C.sub.3), alkynyl(C.sub.2 -C.sub.3), cycloalkyl(C.sub.3 -C.sub.6), hydroxyalkyl(C.sub.1 -C.sub.3), dimethylaminoalkyl(C.sub.1 -C.sub.3), ethylcarboxylate, alkyl(C.sub.1 -C.sub.13)carbonyl, 1-(methylethyl)acetamide, cyclohexylethyl, phenyl, mono-or disubstituted phenyl (wherein the phenyl substituent is halogen, trifluoromethyl, lower alkyl(C.sub.1 -C.sub.3) or lower alkoxy(C.sub.1 -C.sub.3)), benzyl, mono-or disubstituted benzyl (wherein the benzyl substituent is halogen, lower alkyl(C.sub.1 -C.sub.3), lower alkoxy(C.sub.1 -C.sub.3) or trifluoromethyl), benzoyl, 4-methoxybenzoyl, straight or branched chain alkyl(C.sub.2 -C.sub.3)phenyl, 4-chlorophenylphenylmethyl, 1,3-benzodioxol-5-ylmethyl, 1,3-benzodioxol-5-yl, 2-furanylcarbonyl, 2-pyrimidinyl, 2-pyridinyl, 4-morpholinyl-2-oxoethyl, 1-pyrrolidinyl-2-oxoethyl, bis(4-fluorophenyl)methyl, phenylcarboxamido, mono- and disubstituted phenylcarboximido (wherein the phenyl substituents is halogen, trifluoromethyl or lower alkyl(C.sub.1 -C.sub.3)), adamantanoyl, 3-phenoxypropyl,5-chloro-2-methoxyphenylacetamide, (2-oxo-1-pyrrolidinyl)-2-butynyl, phenylmethylcarboxylate, or (2-phenyl-2H-1,2,3-triazol-4-yl)methyl; R.sub.4 and R.sub.5 are independently hydrogen or lower alkyl(C.sub.1 -C.sub.3); the dotted line between positions 6 and 7 of the pyrimidine ring represents the presence or absence of a double bond; and the pharmacologically acceptable salts thereof: methods of producing them; therapeutic compositions containing them: and methods of using them to treat anxiety, hypertension, depression, senile dementia, cognitive defects and other neural behavior problems in warm-blooded animals.
REFERENCES:
patent: 4963553 (1990-10-01), Tseng et al.
patent: 5126340 (1992-06-01), Tseng et al.
Brabander Herbert J.
Epstein Joseph W.
Tseng Shin S.
American Cyanamid Company
Bernhardt E.
Jackson H. G.
Tsang Cecilia
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