Abstract: 4-[aryl(piperidin-4-yl)]aminobenzamides are delta-opioid receptor agonists/antagonists. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their agonist/antagonist effect, such compounds may also be useful immunosuppressants, antiinflammatory agents, agents for the treatment of mental illness, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents, and agents for the treatment of respiratory diseases.

Abstract: This invention relates to a series of compounds of Formula I ##STR1## pharmaceutical compositions containing them and intermediates used in their manufacture. Compounds of the invention alleviate pain in animal models at levels comparable to known analgesic agents. As such the compounds are useful in the treatment of pain.

Abstract: The 4-arylcyclopenta[c]pyrroles of the following formula are effective analgesics: ##STR1## including stereoisomers and pharmaceutically acceptable salts thereof, wherein ##STR2## with the proviso that where there is a 4-position hydroxy then such is trans to the 3a and 6a hydrogens.

Abstract: Aroyl(piperidinyl and piperazinyl)acyl pyrroles of the following formula have anxiolytic activity: ##STR1## wherein, Y is selected from the group consisting of N, CH or COH;A.sup.1 is selected from the group consisting of ##STR2## n is an integer from 1 to 5; R1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 and R.sup.3 are selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.4 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; andR.sup.5 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; and acid addition salts thereof.

Abstract: The 4-arylisoindoles of the following formula are effective analgesics: ##STR1## including the purified stereoisomers and pharmaceutically acceptable salts thereof,wherein ##STR2## R.sup.b is hydroxy or C.sub.1-5 alkylcarbonyloxy.

Abstract: The 4-arylcyclopenta[c]pyrroles of the following formula are effective analgesics: ##STR1## including stereoisomers and pharmaceutically acceptable salts thereof, wherein ##STR2## with the proviso that the 3a and 6a hydrogens are cis and where there is a 4-position hydroxy then such is trans to the 3a and 6a hydrogens, andwith the proviso that R.sup.b is not hydrogen when the 4-position aryl is cis to the 3a and 6a hydrogens and there is no hydroxy at the 4-position.

Abstract: The 4-arylcyclopenta[c]pyrroles of the following formula are effective analgesics: ##STR1## including stereoisomers and pharmaceutically acceptable salts thereof, wherein ##STR2## with the proviso that where there is a 4-position hydroxy then such is trans to the 3a and 6a hydrogens.

Abstract: The 4-arylisoindoles of the following formula are effective analgesics: ##STR1## including stereoisomers and pharmaceutically acceptable salts thereof, wherein ##STR2## with the proviso that there is 0 or 1 unsaturated bond in the isoindole ring and with the proviso that where the stereoisomer is:a) the 3a.beta., 4.beta., 7a.alpha. diastereomer, then a double bond joins the 5- and 6-position carbons or the 6- and 7-position carbons;b) the 3a.beta., 4.alpha., 7a.alpha. or the 3a.beta., 4.alpha., 7a.beta. diastereomers, then the double bond joins the 5- and 6-position carbons; andc) the 3a.beta., 4.beta., 7a.beta. diastereomer, then the double bond joins the 6- and 7-position carbons.

Abstract: Aroyl(piperidinyl and piperazinyl)acyl pyrroles of the following formula have anxiolytic activity: ##STR1## wherein, Y is selected from the group consisting of N, CH or COH;A.sup.1 is selected from the group consisting of ##STR2## n is an integer from 1 to 5;R.sup.1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 and R.sup.3 are selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.4 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; andR.sup.5 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; and acid addition salts thereof.

Abstract: This invention relates to substituted thiazole derivatives of the following general formula, the substituent groups of which are as defined herein: ##STR1## These compounds are useful as inhibitors of platelet aggregation and inhibitors of adhesion molecules and may be provided in pharmaceutical compositions and in methods of treating reperfusion thrombosis injury in patients.

Abstract: Aroyl aminoacyl pyrroles are pharmaceutically useful as anti-convulsants, which includes utility for the treatment of epilepsy.

Abstract: Hexahydropyrrolizines of the formula (I): ##STR1## wherein A is a 3-7 carbon or hetero-containing ring,R.sup.1 is a substituent, andx is 0-3.Also, pharmaceutical compositions for treating pain and methods for synthesis and use as well as novel intermediates in the synthesis.

Abstract: Octahydroquinolizine and corresponding octahydroquinolizinium compounds of formulae (I) and (Va): ##STR1## where A is a 3 to 7 membered carbocyclic ring, R.sup.1 is a substituent, n is 0-2, x is 0-3, and Y is an anion. Also, pharmaceutical compositions for treating pain containing (I) and methods for synthesis and use as well as novel intermediates in the synthesis.

Abstract: Octahydroindolizidines and corresponding ketones of the formulae (I) and (II): ##STR1## where A is a 3-7 carbon or hetero-containing ring, R.sup.1 is a substituent, n is 0-6 and x is 0-3. Also, pharmaceutical compositions for treating pain containing (I) or (II) and methods for synthesis and use as well as novel intermediates in the synthesis.

Abstract: Octahydroindolizine compounds of formula (I): ##STR1## wherein Q is --NR--, --(CH.sub.2).sub.z --, --CH.dbd.CH--, --C.tbd.C--, --OCH.sub.2 --, --SCH.sub.2 --, --SO.sub.2 --, --SO--, --CO--, or an oxygen or a sulfur atom and where R, R.sup.1 and R.sup.2 are substituents such as alkyl and x, y and z are independently the integers 0-3. Also, pharmaceutical compositions containing (I), intermediates and methods for treating pain.

Abstract: Octahydroindolizidines of the formula (I): ##STR1## where A is a 3-7 carbon or hetero-containing ring, R.sup.1 is a substituent and x is 0-3. Also, pharmaceutical composition for treating pain and methods for synthesis and use as well as novel intermediates in the synthesis.

Abstract: Loweralkyl 1-methylpyrrole-2-acetates are prepared by the recuction of loweralkyl .alpha.-imino-1-methylpyrrole-2-acetates using a divalent sulfur reducing agent.

Abstract: Loweralkyl 1-methylpyrrole-2-acetates are prepared by the reduction of loweralkyl .alpha.-imino-1-methylpyrrole-2-acetates using sodium dithionite as the reducing agent.

Abstract: Loweralkyl 1-loweralkyl-pyrrole-2-glyoxylates are reduced by the base-catalyzed action of hydrogen sulfide under pressure of at least 30 p.s.i. to loweralkyl 1-loweralkyl-pyrrole-2-acetates.

Abstract: 1-Methylpyrrole-2-acetonitrile is prepared by the reduction of .alpha.-imino-1-loweralkylpyrrole-2-acetonitrile using hydrogen sulfide as the reducing agent.