Analgetic compounds, compositions and process of treatment

Details Analgetic compounds, compositions and process of treatment Analgetic compounds, compositions and process of treatment

1981-05-15

1984-05-08

Hines, Robert V.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Recombinant or stably-transformed bacterium encoding one or...

424316, 26050118, 564306, A10N 3302, A10N 3730, C07C 8734

Patent

active

044474547

ABSTRACT:
Novel compounds of the formula: ##STR1## wherein R.sub.1 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, CH.sub.2 -alkenyl wherein alkenyl is from 2 to 4 carbon atoms, inclusive, cycloalkyl of from 3 to 6 carbon atoms, inclusive, cycloalkylmethyl of from 3 to 6 carbon atoms, inclusive; R.sub.2 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, inclusive, with the proviso that R.sub.1 and R.sub.2 cannot both be hydrogen at the same time; Y is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, halogen, trifluoromethyl, hydroxy, alkanoyloxy from 2 to 5 carbon atoms, inclusive, alkoxy of from 1 to 4 carbon atoms, inclusive, cycloalkyloxy of from 3 to 6 carbon atoms, inclusive, benzyloxy; m is an integer 0, 1, 2; R.sub.5 is a variable consisting of hydrogen and alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.3 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.4 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, CH.sub.2 -alkenyl wherein alkenyl is of from 2 to 4 carbon atoms, inclusive, and arylalkyl wherein alkyl is from 1 to 4 carbon atoms, inclusive, and aryl is ##STR2## wherein Y' is CF.sub.3, halogen, alkyl of 1 to 4 carbon atoms, inclusive, and alkoxy of from 1 to 4 carbon atoms, inclusive; and R.sub.3 and R.sub.4 when taken together with the nitrogen atom to which they are attached can form saturated heterocycles of from 5 to 7 ring members, a second hetero atom of said ring can be oxygen or nitrogen, e.g., morpholine, piperazine, and said heterocycles can be monosubstituted having a total of up to 9 carbon atoms, with the proviso that when ##STR3## is pyrrolidinyl, then m=1, 2, having analgetic activity in humans and animals are prepared in unit dosage forms. The compositions are useful in relieving pain by administering orally, parenterally, and rectally to humans and animals.

REFERENCES:
patent: 4113866 (1978-09-01), Lednicer

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