4-Amino-2-ureido (or -thioureido)-pyrimidine-5-carboxylic acid anilides
AssigneeHoechst Aktiengesellschaft
InventorsKlaus-Dieter Kampe, Ernold Granzer
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Abstract
What is disclosed are 4-amino-2-ureido (or -thioureido)-pyrimidine-5-carboxylic acid anilides of the formula ##STR1## further defined in the specification, and physiologically acceptable acid addition salts thereof, methods for treating adiposity and disturbances of the lipometabolism with these compounds or salts, and pharmaceutical compositions containing these compounds or salts and useful for inducing anorexia or affecting the lipometabolism.
Claims9
A 4-amino-2-ureido (or -thioureido)-pyrimidine-5-carboxylic acid anilide of the formula ##STR79## or a physiologically acceptable acid addition salt thereof, wherein X is oxygen or sulfur,
- R.sup.1 is hydrogen, (C.sub.1 -C.sub.3)-alkyl, or phenyl;
- R.sup.2 taken alone is hydrogen, (C.sub.1 -C.sub.10)-alkyl, (C.sub.3 -C.sub.4)-alkenyl, (C.sub.4 -C.sub.8)-cycloalkyl, phenyl, phenylalkyl having 1 or 2 carbon atoms in the alkyl portion, or is phenyl or such phenylalkyl mono- or di-substituted in the benzene ring by (C.sub.1 -C.sub.3)-alkyl, halogen, or (C.sub.1 -C.sub.4)-alkoxy, or substituted by trifluoromethyl, methoxycarbonyl, ethoxycarbonyl, or methylenedioxy;
- R.sup.3 taken alone is hydrogen, (C.sub.1 -C.sub.3)-alkyl, or phenyl;
- R.sup.2 and R.sup.3 taken together are --(CH.dbd.CH)--, linear or branched (C.sub.2 -C.sub.8)-alkylene, or such alkylene substituted by (C.sub.2 -C.sub.4)-alkenyl, by phenyl, or by phenyl substituted by chlorine, bromine, methyl, ethyl, methoxy, or ethoxy;
- R.sup.4 is hydrogen or (C.sub.1 -C.sub.8)-acyl;
- R.sup.6 is hydrogen, (C.sub.1 -C.sub.3)-alkyl, (C.sub.3 -C.sub.4)-alkenyl, benzyl, phenyl, benzyl mono- or di-substituted in the benzene ring by chlorine or methoxy, or phenyl substituted by methyl, chlorine, or by methyl and chlorine;
- R.sup.7 taken alone is hydrogen, (C.sub.1 -C.sub.3)-alkyl, (C.sub.3 -C.sub.4)-alkenyl, (C.sub.5 -C.sub.6)-cycloalkyl, phenyl, halogen, trifluoromethyl, (C.sub.1 -C.sub.4)-alkylthio, (C.sub.1 -C.sub.2)-alkoxycarbonyl, cyano, acetamino, amino, nitro, carboxyl, (C.sub.1 -C.sub.4)-alkoxy or ##STR80## wherein Z is oxygen, sulfur, ##STR81## --CH.sub.2 --, or --CH.sub.2 CH.sub.2 --, and R.sup.9 and R.sup.10, which are the same or different, are hydrogen, fluorine, chlorine, bromine, (C.sub.1 -C.sub.3)-alkyl, (C.sub.1 -C.sub.2)-alkoxy, acetamino, (C.sub.1 -C.sub.2)-alkoxycarbonyl, or carbonyl;
- R.sup.8 is fluorine, chlorine, bromine, methyl, (C.sub.1 -C.sub.2)-alkoxy, or trifluoromethyl;
- n is 0, 1, 2, or 3;
- and if n is 1, then
- R.sup.7 and R.sup.8, taken together, may be methylenedioxy or ethylenedioxy.
Dependencies are inferred from the claim text.