Aryl-substituted piperazinyl-alkylamino-uracils, -uracil ethers and -uracil thioethers as therapeutics
AssigneeByk Gulden
InventorsKurt Klemm, Wolfgang Schoetensack, Wolfgang Prusse
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Abstract
Aryl-substituted piperazinyl-alkylamino-uracils, the corresponding uracil ethers and uracil-thioethers and their pharmaceutically acceptable salts such as the hydrochloride, and method for the preparation of these compounds. The novel compounds are useful for lowering the blood pressure, causing an analgesic, a sedative or antihistiminic effect in mammalians.
Claims20
The method of causing a lowering of the blood pressure, causing an analgesic effect, antihistiminic effect or a sedative effect in a warm-blooded animal which comprises administering in a therapeutically effective dose, a pharmaceutical composition comprising a compound of the formula:
- ##STR26## wherein R.sup.1 and R.sup.2 each is hydrogen, alkyl or alkenyl of 1 to 6 carbon atoms, cycloalkyl of 5 to 6 carbon atoms, or phenyl;
- R.sup.3 is hydrogen, alkyl or alkenyl of 1 to 6 carbon atoms, cycloalkyl of 5 to 6 carbon atoms, chlorine or bromine, phenyl, aralkyl, wherein the alkyl is of 1 to 3 carbon atoms, nitro, nitroso, amino, alkylamino of 1 to 3 carbon atoms, dialkylamino wherein each of the alkyl groups contain 1 to 3 carbon atoms, alkanoylamino of 1 to 4 carbon atoms, formyl, ethoxycarbonylamino, thiocyanato, COCH.sub.3 or CONHC.sub.6 H.sub.5 ;
- X is --NH--, --NC.sub.2 H.sub.5 --, --O-- or --S--;
- A is --CH.sub.2 --CH.sub.2 CH.sub.2 --, --CH(CH.sub.3)--CH.sub.2 -- or --CH.sub.2 -- CH(CH.sub.3);
- Z is hydrogen, a methyl group, one or two methoxy groups or an ethoxy group, a chlorine atom and
- Y is hydrogen, and the pharmaceutically acceptable salts of these compounds, in mixture with a pharmaceutically acceptable carrier.
A pharmaceutical composition for use in mammals to cause:
- a lowering of blood pressure, an analgesic, a sedative, or an histiminic effect, comprising, in a therapeutically effective amount to cause such effect, a compound of the general formula ##STR27## wherein R.sup.1 and R.sub.2 each is hydrogen, alkyl or alkenyl of 1 to 6 atoms, cycloalkyl of 5 to 6 carbon atoms, or phenyl;
- R.sup.3 is hydrogen, alkyl or alkenyl of 1 to 6 carbon atoms, cycloalkyl of 5 to 6 carbon atoms, chlorine or bromine, phenyl, benzylalkyl wherein the alkyl is of 1 to 3 carbon atoms, nitro, nitroso, amino, alkylamino of 1 to 3 carbon atoms, dialkylamino wherein each of the alkyl groups contain 1 to 3 carbon atoms, alkanoylamino of 1 to 4 carbon atoms, formyl, ethoxycarbonylamino, thiocyanato, COCH.sub.3 or CONHC.sub.6 H.sub.5 ;
- X is --NH--, --NC.sub.2 H.sub.5 --, --O-- or --S--;
- A is --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH(CH.sub.3)--CH.sub.2 -- or --CH.sub.2 -- CH(CH.sub.3);
- Z is hydrogen, a methyl group, one or two methoxy groups or an ethoxy group, a chlorine atom and
- Y is hydrogen, and the pharmacetucally acceptable salts of these compounds in mixture with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.