Method of using certain tetralin derivatives to produce analgesic relief
AssigneeMerrell Dow Pharmaceuticals Inc.
InventorsHugues d'Orchymont, Celine Tarnus
Life of this patent
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Abstract
This invention relates to novel derivatives of tetralin, to the processes for their preparation, to their use as amino-peptidase inhibitors and to their end-use application as immunomodulators and as analgesic agents.
Claims8
A method of treating a patient in need of analgesic relief which comprises administering to said patient an effective analgesic amount of a compound having the formula;
- ##STR10## the enantiomeric forms and mixtures thereof, and the pharmaceutically acceptable salts thereof wherein the dotted lines represent facultative double bonds, R.sub.1 is H, F, Cl, C.sub.1-6 alkyl, OH, C.sub.1-6 alkoxy, C.sub.1-6 alkyl thio, C.sub.1-6 acylamino, or C.sub.1-6 acyloxy;
- R.sub.2 is H, Cl, F or C.sub.1-6 alkyl;
- each of R.sub.6, R.sub.7, R.sub.8 and R.sub.9 is H, Cl, F, C.sub.1-6 alkyl, C.sub.1-6 alkylamino, C.sub.1-6 alkoxy, aryl or aralkyl;
- and when R.sub.6 and R.sub.7, R.sub.7 and R.sub.8, and R.sub.8 and R.sub.9 are taken together with the carbon atoms to which they are attached form a 5-6 membered carbocyclic moiety, with the proviso that the number of so-formed carbocyclic moieties is limited to less than 3, and with the further proviso that when the depicted ring moiety having the facultative double bonds is saturated then any 5-6 membered carbocyclic moiety formed therewith is also saturated.
A pharmaceutical composition comprising having a therapeutically effective amount of a compound having the formula ##STR11## The enantiomeric forms and mixtures thereof, and the pharmaceutically acceptable salts thereof wherein the dotted lines represent facultative double bonds, R.sub.1 is H, F, Cl, C.sub.1-6 alkyl, OH, C.sub.1-6 alkyl thio, C.sub.1-6 acylamino, or C.sub.1-6 acyloxy;
- R.sub.2 is H, Cl, F or C.sub.1-6 alkyl;
- each of R.sub.6, R.sub.7, R.sub.8 and R.sub.9 is H, Cl, F, C.sub.1-6 alkyl, C.sub.1-6 alkylamino, C.sub.1-6 alkoxy, aryl or aralkyl;
- and when R.sub.6 and R.sub.7, R.sub.7 and R.sub.8, and R.sub.8 and R.sub.9 are taken together with the carbon atoms to which they are attached form a 5-6 membered carbocyclic moiety, with the proviso that the number of so-formed carbocyclic moieties is limited to less than 3, and with the further proviso that when the depicted ring moiety having the facultative double bonds is saturated then any 5-6 membered carbocyclic moiety formed therewith is also saturated in combination with a pharmaceutically acceptable carrier.
A pharmaceutical composition comprising having a therapeutically effective amount of a compound having the formula R.sub.1 is H, F, Cl, C.sub.1-6 alkyl, OH or C.sub.1-6 alkoxy, R.sub.2 is H, Cl, F or C.sub.1-6 alkyl, each of R.sub.6, R.sub.7, R.sub.8 and R.sub.9 is H, Cl, F or C.sub.1-6 alkyl, and when R.sub.6 and R.sub.7, R.sub.7 and R.sub.8, and R.sub.8 and R.sub.9 are taken together with the carbon atoms to which they are attached, they form a 6-membered carbocyclic moiety with the proviso that when the depicted ring moiety having the facultative double bonds is saturated R.sub.1, R.sub.2, R.sub.6, R.sub.7, R.sub.8, and R.sub.9 cannot all be hydrogen, and with the further proviso that when the depicted ring moiety having the facultative double bonds is saturated then the 6-membered carbocyclic moiety formed is also saturated in combination with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.