Abstract: New thieno [2,3-b] pyrrole compounds of the formula: ##STR1## in which: R is hydrogen, (C.sub.1 -C.sub.5) alkyl, alkali or alkaline earth metals ammnonium or mono- di- or tri-(C.sub.1 -C.sub.5) alkylammnonium;R.sub.1 is hydrogen, or (C.sub.1 -C.sub.5) alkyl;R.sub.2 is hydrogen, (C.sub.1 -C.sub.5) alkyl, phenyl or phenyl-(C.sub.1 -C.sub.5) alkyl;R.sub.3 and R.sub.4, the same or different are each hydrogen, halogen, (C.sub.1 -C.sub.5) alkyl, (C.sub.1 -C.sub.5) alkoxy, orR.sub.3 and R.sub.4 together represent: --CH.dbd.CH--CH.dbd.CH--.These new compounds may be used as medicines especially in the treatment of acute or chronic pain.

Abstract: An 8-substituted pyrrolizidine derivative representable by the formula: ##STR1## (wherein R.sup.1 stands for hydrogen or a lower alkyl group, R.sup.2 stands for hydrogen, a lower alkyl group, a lower alkoxy group or halogen, and R.sup.3 stand for a lower alkyl group, a lower alkoxy group, amino group or halogen), which can be produced by reacting a corresponding substituted anilin with 8-halocarbonylmethyl pyrrolizidine or reacting an alkali metal salt of the corresponding substituted anilin with 8-alcoxycarbonylmethyl pyrrolizidine. The derivative is useful as an antiarrhythmic agent.

Abstract: Heterocyclically substituted nitriles of the formula I ##STR1## where X is SO.sub.2, CO, S, SO or CH.sub.2, A is an alkylene or alkenylene radical of not more than 6 carbon atoms, B is --CH.dbd.CH-- or S, and R.sup.1 and R.sup.2 are each hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, nitro or trifluoromethyl, and their preparation and use.The novel substances are useful for treating disorders.

Abstract: Novel derivatives of N-[2-(tetrahydro-3,5-dioxo-1H-pyrrolizin-7a(5H)-yl)ethyl]amine are effective as cognition activators for reversing the effects of electroshock induced amnesia. A method of preparing the compounds, a useful intermediate in their preparation, pharmaceutical compositions, and a method of treatment are also disclosed.

Abstract: Novel 5-(4-vinyl- or 4-ethynylbenzoyl)-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic alkyl esters and salts thereof, wherein R is vinyl or ethynyl, and Y is hydrogen, a lower alkyl group having from 1 to 6 carbon atoms, chloro or bromo.

Abstract: The instantly claimed invention is a process for preparing a 3-aryl or a 2,3-diaryl-2,5,6,7-tetrahydro-3H-pyrrole[1,2-a]imidazole or a 3-aryl or a 2,3-diaryl-2,3,5,6,7,8-hexa-hydroimidazo[1,2-a]pyridine which comprises (a) contacting the acid addition salt of the corresponding cyclic methylthioimine with a 2-aryl or a 2,3-diarylaziridine and (b) recovering from the resultant reaction mixture the desired compound, useful as immunomodulators.

Abstract: The instantly claimed invention is a process for preparing novel 7-thioether derivatives of 2-aryl, 3 aryl, and 2,3-diary-2,5,7,7-tetra-hydro-3H-pyrrolo [1,2-a] imidazole and 8-thio-ether derivatives of 2-aryl, 3-aryl, and 2,3-diaryl-2,3,5,7,7,8-hexahydro-imidazo [1,2-a]-pyridine which comprises (a) contacting the corresponding amidine with about one molar equivalent of R.sub.1 SSR.sub.1 in the presence of about two molar equivalents of base and at a temperature of -78.degree. C. to about 0.degree. C. (b) contacting the corresponding amidine compound with about two molar equivalents of R,SSR, in the presence of about two molar equivalents of a base and at a temperature of from about -78.degree. C. to about 23.degree. C., said compounds being useful as immunomodulators.

Abstract: Hexahydro-3,5-dioxo-1H-pyrrolizine-2-carboxylic acid, its esters, ammonium, metal, and organic amine salts are useful for the treatment of senility, for enhancing memory, and for reversing electroconvulsive shock induced amnesia in humans. Pharmaceutical compositions including these compounds, and a method of treatment employing these pharmaceutical compositions is disclosed.

Abstract: 1-(Substituted-aryl)-dihydro-1H-pyrrolizine-3,5-[2H,6H]-diones are effective cognition activating agents for the treatment of senility and for reversing amnesia. Pharmaceutical compositions containing these compounds and a method of treating senility or of reversing amnesia are also disclosed.

Abstract: Hydroquinones of the formula ##STR1## wherein X is the residue of a 5- or 6-membered ring, R.sub.1 is hydrogen, alkyl or aryl, R.sub.1,R.sub.3, R.sub.4 and R.sub.5 are hydrogen or alkyl and R.sub.6 is hydrogen or a group of the formula ##STR2## wherein X and R.sub.1 are as defined above, are of use as protected developing agents in photographic silver halide material.

Abstract: The invention provides new derivatives of the formula: ##STR1## in which either (a) Y=COOH or a radical of the formula (II), in which R.sub.2 =alkyl or benzyl, A=a sulphur atom, m=1, n=0, R=pyridin-3-yl and R.sub.1 =H, or (b) Y=CN, COOH or a radical of the formula ##STR2## defined as above, A=S, O or CH.sub.2, m=1 or 2 and n=0, 1 or 2, (m+n) being 1, 2 or 3, R=H, alkyl or phenyl (optionally substituted by halogen, alkyl, alkoxy or CF.sub.3) and R.sub.1 =a radical of the formula ##STR3## in which p=0 or 1, the alkyl radicals and alkyl portions being straight-chain or branched-chain and containing 1 to 4 carbon atoms each. Processes for the production of these compounds are described. They are useful as intermediates for the preparation of new medicaments.

Abstract: New 5-(2,3-dihydro-1H-pyrrolizin-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]thiazol-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]imidazol-5-oyl)-, and 5-(2,3-dihydro-1H-pyrrolo[2,1-b]oxazol-5-oyl)-derivatives of substituted 2,3-dihydro-1H-pyrrolizine-1-alkanoic or carboxylic acids have been prepared. They are found to be effective inhibitors of platelet aggregation and are analgesic/anti-inflammatory agents with low ulcerogenic side effects.

Abstract: Conformationally restricted peptide analogs incorporating a rigid .beta.-bend are formed by replacing a portion of the peptide backbone chain with a bicyclic heterocycle, 5H-6-oxo-2,3,4,4a,7,7a-hexahydropyrano[2,3-b]pyrrole. Properly substituted derivatives of the pyranopyrrole are conformationally rigid and cannot assume non-.beta.-bend conformations in the interior of the peptide chain, while the terminal binding residues are maintained in the proper orientation for receptor interaction. Also described are a novel intermediate for preparation of the peptide analogs and a method for preparation of the intermediate.

Abstract: New 5-(2,3-dihydro-1H-pyrrolizin-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]thiazol-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]imidazol-5-oyl)-, and 5-(2,3-dihydro-1H-pyrrolo[2,1-b]oxazol-5-oyl)-pyrrole-2-alkanoic acid derivatives have been prepared. They are found to be effective inhibitors of platelet aggregation and are analgesic and anti-inflammatory agents with low ulcerogenic side effects.

Abstract: A perfluorobicyclo compound of the general formula: ##STR1## wherein either or both of Ring A and Ring B may optionally be substituted with lower perfluoroalkyl group(s) and m and n each represent 3 or 4.

Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.

Abstract: 5-Aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid derivatives have been prepared from a 5-aroyl-7-hydroxycarbonyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxyli c acid derivative via selective decarboxylation.

Abstract: Compounds of the formula: ##STR1## wherein B is a moiety having the formula: ##STR2## R is mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, cycloalkyl of 4-7 carbon atoms, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, lower alkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro.X is SO.sub.2, SO, S or C.dbd.O; andA is amine selected from the group ##STR3## , wherein R.sup.1 is hydrogen or R.sup.2 CH.sub.2 wherein R.sup.2 is mono- or diloweralkylamino, mono- or di-N-lower alkylaminoloweralkyl, (2-furyl)methylamino, benzylamino, lowercycloalkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-thiazolidinyl, 4-morpholinyl or 4-thiomorpholinyl; R.sup.3 is hydrogen or (1-piperidinyl)methyl with the proviso that when R.sup.

Abstract: A process for dyeing high-molecular organic material in the bulk characterized by the use of a 1,4-diketo-pyrrole[3,4-c]-pyrrol of the formula ##STR1## wherein R.sub.1 and R.sub.2 are isocyclic or heterocyclic aromatic radicals, preferably unsubstituted or substituted phenyl or naphthyl radicals.The dyeings obtained, for example in plastics, fibres, lacquers and printings, are distinguished by very high coloring strength, high saturation, good dispersibility, good fastness to cross-lacquering, migration, heat, light and weather, and also by a high gloss and a good IR-remission behavior.

Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen or lower alkyl; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl;are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.

Abstract: An improved process for recovering Indicine-N-oxide from plant sources which involves water extracting the plant material, preferably by water buffered at pH 7, followed by adsorbing the Indicine-N-oxide from the extract, after which the Indicine-N-oxide is eluted from the adsorbent in alcoholic solution, then concentrated and purified as heretofore.Desirably, the adsorbed Indicine-N-oxide is water washed prior to elution so as to remove any water soluble impurities that had been adsorbed from the extract.A preferred adsorbent is a cross linked polystyrene.

Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.

Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen, lower alkyl, chloro or bromo; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl;are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.

Abstract: Compounds of the formula: ##STR1## wherein A is O or S, halo is chloro, bromo or fluoro; X' is --CH.sub.2 --, O or S; X is hydrogen or halo; R.sup.1 and R.sup.2 are the same or different radicals selected from hydrogen or lower alkyl; and Z can be a variety of substituents and agronomically acceptable salts, esters and amides as well as other heterocyclic benzenes are disclosed as selective herbicides.

Abstract: New organopalladium reactions involving the addition of pi-allylpalladium compounds to strained bicyclic alkenes, and subsequent chain extension reactions employing the chemistry of organopalladium compounds are disclosed. By these techniques a large number of bicyclic prostaglandin analogs are prepared, which are useful as inhibitors of arachidonic acid induced platelet aggregation, and are specific inhibitors of thromboxane synthetase.

Abstract: Compounds of the formula ##STR1## wherein n and m are each 1, 2 or 3, and the sum of n+m is 4;R.sub.1 is alkyl; alkenyl; unsubstituted, mono- or di-substituted aralkyl; unsubstituted, mono- or di-substituted benzoyl; alkoxycarbonyl; aralkoxycarbonyl; or, when m and n are each 2 and/or R.sub.2 and R.sub.3 are other than both hydrogen at the same time, also hydrogen;one of R.sub.2 and R.sub.3 is hydrogen or amino, and the other is carboxyl or alkoxycarbonyl; or, when R.sub.3 is hydrogen,R.sub.2 is hydrogen; amino; alkoxycarbonyl-amino; (unsubstituted or mono-substituted phenyl)-aminocarbonyl-; (unsubstituted or mono-substituted phenyl)ethylaminocarbonyl; azidocarbonyl; or hydrazinocarbonyl;X is oxygen, sulfur or ##STR2## where R.sub.4 is hydrogen; alkyl; phenyl-alkyl; or phenyl; non-toxic, pharmacologically acceptable acid addition salts thereof; and, when R.sub.2 or R.sub.3 is carboxyl, non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases.

Abstract: Compounds of the formula:R'--CH.sub.2 --S--Awherein:R' is hydrogen, alkyl, --COOH or its pharmaceutically acceptable salts, --alkylene--COOH or its pharmaceutically acceptable salts, --alkylene-SO.sub.2 H or its pharmaceutically acceptable salts, --alkylene-SO.sub.3 H or its pharmaceutically acceptable salts, or --alkylene CH.sub.2 OH; andA is the acyl moiety of a pharmaceutically acceptable carboxylic acid, said acid having antiinflammatory properties;are gastrointestinal tract sparing drugs for antiinflammatory pharmaceuticals.

Abstract: Disclosed is a process for preparing (2S)-tetrahydro-2.alpha.-methyl-6-oxo-4.beta.-amino-2H-pyran-3.alpha.-carb oxylic acid (I) which is useful in the synthesis of thienamycin. The process proceeds via a stereospecific reduction of the 2-acetyl-3-(R)-.alpha.-methylbenzylamino-2-pentenedioic acid diester (II). ##STR1## wherein R is, .alpha.-methylbenzyl, and R.sup.1 is lower alkyl having 1-6 carbon atoms or arylalkyl such as benzyl.

Abstract: Substituted benzamides having useful pharmacological properties, pharmaceutical compositions containing the same, pharmaceutically acceptable salts thereof, and procedure for administering said compositions. The active compounds have dopamine antagonist activity which is an effective amount of a compound of formula (I) and the compositions are particularly useful for the treatment of humans suffering from emesis impaired gastro-intestinal motility and disorders of the central nervous system. The administration of the compositions overcomes these disorders of the central nervous system and ordinary additions. The active compounds are characterized by having the formula (I), wherein R.sub.2 and/or R.sub.3 are sulphone groups, preferably either R.sub.2 or R.sub.3 being an aminosulphone or alkylsulphone group, which groups may optionally be substituted by 1 or 2 C.sub.1-6 alkyl groups.

Abstract: The present invention provides novel 8-heteroaryltetrahydrobenzopyrans and analogs thereof. These novel compounds are useful as inhibitors of endoperoxide cyclooxygenase which prevents the conversion of unsaturated fatty acids to endoperoxides. Because of this pharmacological activity, these compounds represent potent platelet aggregation inhibitors.