Abstract: This invention is directed to aroyl aminoacyl pyrroles pharmaceutically useful as agents and modulators for the treatment of central nervous system disorders and a method for the treatment of central nervous system disorders including, but not limited to, use of the compounds of the present invention as anticonvulsant agents and modulators, antiepileptic agents and modulators, neuroprotective agents and modulators, muscle relaxant agents and modulators and as agents and modulators for the treatment of neuropathic pain.

Abstract: Aroyl aminoacyl pyrroles are pharmaceutically useful in treating neuropathic pain, which includes utility for the treatment of neuropathic pain.

Abstract: 4-[aryl(8-azabicyclo[3.2.1]octan-3yl)]aminobenzoic acid derivatives are delta-opioid receptor modulators. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their antagonist effect, such compounds may also be useful immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.

Abstract: &bgr;-Aminotetralin derivatives of the formula: which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a &bgr;-aminotetralin derivative as the active ingredient are described. The 62 -aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.

Abstract: Aroyl aminoacyl pyrroles are pharmaceutically useful in treating neuropathic pain, which includes utility for the treatment of neuropathic pain.

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: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2 R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess anti-hypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.

Abstract: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess antihypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.

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: Acetylenes of the formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, q, Alk, R.sup.3 n and R.sup.4 are as defined herein and Ar.sup.1 and Ar.sup.2 are aromatic, including the salts and ammonium derivatives of formula (I), in treating angina, hypertension and cardiac arrhythmias. Pharmaceutical compositions, methods of use and synthesis and novel intermediates are also part of the invention.

Abstract: N-Aminoalkyl 1,5-benzothiazepines of the following formula (I): ##STR1## for the treatment of angina or hypertension or the prevention of heart attacks in mammals, in particular their use as coronary vasodilators.