John Wyeth Brother, Limited

John Frederick Cavalla

John Leheup Archibald

Alan C White

Robin G Shepherd

Michael G Wyllie

Brian John Bushell

Roger J Stephens

Pharmaceutical compositions containing meptazinol or a pharmaceutically acceptable acid addition salt thereof and ibuprofen or a pharmaceutically acceptable salt thereof are useful in treating pain in mammals.

Pharmaceutical compositions

Treating cerebrovascular disorders characterized by poor oxygenation with 3-[2-C benzamide-1-piperidyl) ethyl] indole.

Method for treatment of cerebrovascular disorders

The invention concerns compounds of formula ##STR1## or salts thereof, wherein R represents an acyl group which possess anti-inflammatory activity and have low toxicity. Methods for preparing the compounds and pharmaceutical compositions are also disclosed.

Thiazoles

2-Oxo-hexahydroazepine, -piperidine or pyrrolidines of formula ##STR1## wherein n is 2,3 or 4, R is hydrogen, lower alkyl, aryl(lower)alkyl, loweralkenylmethyl or cycloalkylmethyl, R.sup.1 is hydrogen or lower alkyl and R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl are prepared by a novel process involving reaction of an anion of a lactam of formula ##STR2## where R.sup.3 is lower alkyl, aryl(lower)alkyl, trialkyl-, triaryl- or triarylalkyl-silyl with a benzyne of formula ##STR3## where R.sup.4 is lower alkyl, aryl(lower)alkyl or trialkyl-, triaryl- or triarylalkyl-silyl. The products are useful as intermediates for preparing pharmacologically active 2-unsubstituted -hexahydroazepine, -piperidine and pyrrolidine derivatives.

Process for preparing hexahydroazepine, piperidine and pyrrolidine

The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine of formula I ##STR1## where n is 2,3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.1 is lower alkyl. The compounds may be aromatized and the aromatized compounds converted to 3,3-disubstituted-hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.

Hexahydroazepine, piperidine and pyrrolidine derivatives

The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine derivatives of formula (I) and their aromatized derivatives of formula (II) ##STR1## where n is 2, 3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl, R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.3 is hydrogen, lower alkyl, aryl(lower)alkyl, lower alkenyl or lower alkynyl. The compounds are useful as intermediates for preparing 3,3-disubstituted -hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.

4-(p-Chlorophenyl)-2-phenyl-5-thiazoleacetic acid and its pharmaceutically acceptable salts are useful as topical anti-inflammatory agents. The compounds can be administered in association with a pharmaceutically acceptable topical carrier.

Thiazole derivatives to treat inflammation

Compounds of the formula ##STR1## in which W is quinolyl or lower alkyl quinolyl;

2-(Benzamido piperidine) quinolyl derivatives

Novel piperidine compounds and their use in treatment of disorders and diseases of the cardiovascular system and/or in the treatment of superficial and deep allergic phenomena is described. These compounds are piperidine compounds linked by the nitrogen atom to cycloalkyl or a substituted or unsubstituted phenyl radical through the intermediary of a lower-alkylene radical. The piperidine ring is further substituted by an acylamino residue.

Piperidino compounds

A group of heterocyclic compounds useful in the treatment of disorders and diseases of the cardiovascular system is described. These compounds are piperidine compounds linked by the nitrogen atom to a methylenedioxyphenyl or an ethylenedioxyphenyl radical through the intermediary of a group selected from a mono-keto lower alkylene radical or a hydroxy-lower-alkylene radical or a bivalent radical of the formula ##STR1## or --O--(lower alkylene). The piperidine rings are further substituted by a benzamido residue.

Benzamido piperidines

Pharmaceutical compositions containing a group of heterocyclic compounds and their use in treatment of disorders and diseases of the cardiovascular system and/or in the treatment of superficial and deep allergic phenomena is described. These compounds used in the composition and/or methods are piperidine compounds linked by the nitrogen atom to a substituted or unsubstituted cycloalkyl, aryl or heterocyclic radical through the intermediary of a group selected from a lower-alkylene radical, a monoketo lower-alkylene radical or a hydroxy-lower-alkylene radical, or a bivalent radical of the formula --NH.CO.(CH.sub.2).sub.n -- where n is 1, 2 or 3, ##STR1## or --0-(lower-alkylene)--. The piperidine ring is further substituted by an acylamino residue.

Pharmaceutical compositions and methods of treating hypertension

A group of benz[g]indolyl compounds useful in the treatment of disorders and diseases of the cardiovascular system is described. These are piperidine compounds linked by the nitrogen atom to a substituted or unsubstituted benz[g]indolyl radical through the intermediary of a lower-alkylene radical. The piperidine rings are further substituted by an acylamino residue.

Benz[g]indolyl compounds

A group of heterocyclic compounds useful in the treatment of disorders and diseases of the cardiovascular system is described. These compounds are piperidine compounds linked by the nitrogen atom to a halogen-substituted or unsubstituted phenyl radical through the intermediary of a ##STR1## GROUP WHEREIN N IS AN INTEGER FROM 1 TO 4, AND Ar represents phenyl or halophenyl. The piperidine rings are further substituted by a benzamido residue.

Benzamidopiperidine derivatives

A group of heterocyclic compounds useful in the treatment of disorders and diseases of the cardiovascular system and/or in the treatment of superficial and deep allergic phenomena is described. These compounds are piperidine compounds linked by the nitrogen atom to a substituted or unsubstituted phenyl radical through the intermediary of a group selected from a lower-alkylene radical, a mono-keto lower alkylene radical or a hydroxy-lower-alkylene radical, or a bivalent radical of the formula ##EQU1## or --O--(lower-alkylene)-. The piperidine rings are further substituted by a benzamido, substituted benzamido or cyclohexylcarboxamido residue.

Growing community of inventors

Isleworth, United Kingdom

John Frederick Cavalla