Abstract: The invention relates to compounds of formula ##STR1## in which R.sub.1 is selected from the groups R.sub.3 and OR.sub.3, R is selected from H and a group CHR.sub.2 R', in which R.sub.2 is selected from H, alkyl, carboxy and carboxamido and R', is H, alkyl or phenyl, Z represents S or O; and m and n, which may be identical or different, equal 1 or 2, and their N-oxides, salts and quaternary ammonium derivatives.The invention also relates to the process for preparing these compounds, as well as to pharmaceutical compositions containing them.

Abstract: (-)-Swainsonine is prepared by the steps of first reacting a compound having the formula: ##STR1## wherein each R.sub.2 is lower alkyl, with (4-carbalkoxybutyl) triphenylphosphonium bromide in a strong base to obtain an alcohol having the formula: ##STR2## wherein R.sub.2 is as defined above and R is C.sub.1 -C.sub.8 alkyl; the alcohol is then reacted with methanesulfonyl chloride or p-toluenesulfonyl chloride or benzenesulfonyl chloride in the presence of a tertiary amine to obtain the corresponding sulfonate. Heating the sulfonate with an azide in an organic solvent yields an imine having the formula: ##STR3## wherein R.sub.2 and R are ad defined above. Treating the imine with an inorganic base, in aqueous alcohol provides upon acidification, the corresponding acid. Heating the acid at reflux temperature in organic solvent, yields an enamide having the formula: ##STR4## wherein R.sub.2 is as defined above.

Abstract: Heterobicyclic and heterocyclic intermediate compounds and their use in treating inflammation, hyperproliferative skin conditions such as psoriasis and allergy are disclosed.

Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl);R.sub.1 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, C.sub.2 -C.sub.6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH.sub.2 -aryl, --CH.sub.2 -substituted aryl, --CH.sub.2 -heteroaryl, or --CH.sub.2 -substituted heteroaryl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or aryl; ##STR2## is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl)are described. These compounds are useful as agents for treating viruses.

Abstract: 2,7-Diazabicyclo[3.3.0]octanes, suitable for 7-position substituents or antibacterially active quinolone carboxylic acids, of the formula ##STR1## in which R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 may be identical or different and in each case denote H, C.sub.1 -C.sub.5 -alkyl (optionally substituted by halogen, hydroxyl or C.sub.1 -C.sub.3 -alkoxy), C.sub.1 -C.sub.3 -alkoxycarbonyl or C.sub.6 -C.sub.12 -aryl,R.sup.4 additionally denotes halogen,R.sup.2 and R.sup.6 may be identical or different, denote H, C.sub.1 -C.sub.6 -alkyl, benzyl, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.3 -alkanoyl, benzoyl or C.sub.1 -C.sub.5 -alkoxycarbonyl, orR.sup.2 and R.sup.3 together denote a bridge of the structure (CH.sub.2).sub.n, n=2-4, CH.sub.2 --CHOH--CH.sub.2, CH.sub.2 --S--CH.sub.2 or C(CH.sub.3).sub.2 --S--CH.sub.2,excluding 2,7-diazabicyclo[3.3.0]octane.Also their preparation by the reaction ##STR2## Intermediates II are also new.

Abstract: There are given disclosures on a polyisoprene compound of the formula ##STR1## wherein Y is S, O, NH or ##STR2## .sub.l is an integer of 2-10, Z is a group of ##STR3## R.sup.1 and R.sup.2 are same or different and each means a hydrogen atom or an alkyl group having C.sub.1-4, m is an integer of 0 or 1, and .sub.n is an integer of 0, 1 or 2,a salt thereof, a process for the preparation of same, and use thereof.

Abstract: The invention relates to a process for resolving racemic mixtures of bicyclic imino-.alpha.-carboxylic esters into the components by crystallization of diastereomeric salts, which comprises preparing the salts of the racemic esters with optionally active N-acylated R- or S-aminocarboxylic acids which contain a phenyl nucleus, recrystallizing them from an organic solvent, decomposing the precipitated, optically homogeneous diastereomeric salts in a manner known per se, and isolating the enantiomers and, where appropriate, converting the latter into the free acids by hydrolysis in a manner known per se. The invention also relates to optically pure compounds of the formula ##STR1## and to diastereomeric salts of these compounds, in which two of the radicals A, B.sup.1, B.sup.2 and C form a carbon chain and the other denote hydrogen, and R is an esterifying group.

Abstract: Compositions containing(a) at least one 1,4-diketopyrrolo[3,4-c]pyrrole of the formula I, II, IIa, III or IV ##STR1## and (b) an auxiliary redox system from the ferrocyanide, ferrocene or ammonium iron (II) sulfate series in combination with at least one conductive salt (c), where, in the formula I,R and R.sub.2 are, for example, --H and R.sub.1 is --SO.sub.3 Na,in the formulae II and IIa, R and R.sub.3 are, for example, --H, R.sub.1 is --SO.sub.3 H and p is 3,in the formula III, R.sub.4 and R.sub.5 are, for example, phenyl and R.sub.6 and R.sub.7 are, for example, methyl, andin the formula IV R.sub.8 and R.sub.9 are, for example, phenyl,are suitable as electrochromic materials in display systems.

Abstract: Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 -alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which X represents R.sub.1 OOC-- in which R.sub.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl; R.sub.2 O-- in which R.sub.2 is C.sub.1-2 alkyl, C.sub.1 -2 alkylcarbonyl or aminocarbonyl optionally substituted by one or two methyl groups;a group ##STR2## in which Y represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, any amino nitrogen optionally substituted by a C.sub.1-2 alkyl group, Y being optionally C-substituted by a methyl group; ora group ##STR3## in which A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.3 and the other is nitrogen or CR.sub.4 where R.sub.3 and R.sub.4 are independently selected from hydrogen and methyl; and each of p and q independently represents an integer of 2 to 4.

Abstract: Novel compounds of formula (I), a process for their preparation, and their use as pharmaceutical agents are described: ##STR1## wherein R.sub.1 represents ##STR2## in which each of p and q independently represents an integer of 2 to 4, r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1;R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4, or a group NHR.sub.6 or NR.sub.7 R.sub.8 where R.sub.6, R.sub.7 and R.sub.8 are independently C.sub.1-2 alkyl; andR.sub.3 is hydrogen or C.sub.1-4 alkyl, subject to the proviso that when R.sub.2 is a group OCOR.sub.5 or a group NHR.sub.6, R.sub.3 is C.sub.1-4 alkyl.

Abstract: There are described 1-azoniabicyclo[3.3.0]oct-1(5)-ene salt derivatives inclusive of 1-azonia-4,6-dimethylbicyclo[3.3.0]oct-1(5)-ene perchlorate, and a process for the preparation of the same. The derivatives can be prepared by heating dicyclopropylmethanimine salt derivative in a solvent, in the presence or absence of an ammonium salt. Each of the derivatives is employed as an intermediate for preparing various medicines and agricultural chemicals.

Abstract: The invention concerns heterocyclic nitromethane derivatives of the formula 1 as defined hereinafter (and their non-toxic salts) wherein the heterocyclic moiety Q is thienyl, benzothienyl or dibenzothienyl and may bear a wide variety of optional substituents, together with pharmaceutical compositions containing them. The nitromethane derivatives are inhibitors of the enzyme aldose reductase and are of value in the treatment of certain complications of diabetes and galactosemia.

Abstract: Organic pigments selected from the diketopyrrolopyrrole, azo, isoindolinone and isoindoline series, which pigments consist of 50% by weight of platelets which are from 5 to 50 .mu.m long, 2 to 50 .mu.m wide and 0.01 to 5 .mu.m thick, with the proviso that the ratios of length:thickness and width:thickness must be at least 3.The pigments in platelet form are excellently suited to producing effect colorations in high molecular weight organic material and in cosmetic products.

Abstract: 1S,4S and 1R,4R-2-Alkyl-2,5-diazabicyclo[2.2.1]heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.

Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## in which X is .dbd.CH-- or .dbd.N--; R.sup.2 is hydrogen, alkyl, phenyl, benzyl or phenethyl; Y is --CH.sub.2--, --NH-- or --O--; and Z is --H.sub.2 or .dbd.O; B is His, Leu, Ile, Nva, Nle, Ala or Val; and R.sup.1 is hydrogen, alkyl, phenyl or phenylalkyl; or a pharmaceutically acceptable salt thereof are renin inhibitors.

Abstract: Processes for the preparation of compounds of the formula ##STR1## in which R and R.sup.1 are identical or different and represent hydrogen or halogen, in the racemic form or in the form of its pure enantiomers by cyclicizing compounds of the formula ##STR2## with 2,6-lutidine or by cyclicizing compounds of the formula ##STR3## with diethyl azodicarboxylate. Compounds where R is halogen are new and are useful as cerebral therapeutics, nootropics or in the reduction of increased glutamine pyruvate transaminase in serum.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which one of X and Y represents hydrogen and the other represents --CH.sub.2 --Z where Z is a group ##STR2## in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, or three nitrogen atoms, any amino nitrogen being optionally substituted by a C.sub.1-2 alkyl, cyclopropyl or propargyl group, and any ring carbon atom being optionally substituted by a group R.sub.1 ; or a group ##STR3## in which A.sub.1, A.sub.2 and A.sub.3 complete a 5-membered aromtic ring and A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.2 and the other is nitrogen or CR.sub.3, or A.sub.2 is oxygen or sulphur, one of A.sub.1 and A.sub.3 is CR.sub.2 and the other is CR.sub.3 ; and R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen, halogen, CN, OR.sub.4, SR.sub.4, N(R.sub.4).sub.2, NHCOR.sub.4, NHCOOCH.sub.

Abstract: Diazabicycloamine compounds of the general formula I and their acid salts ##STR1## wherein m represents an integer of 1 to 3,n represents 1 or 2, andR.sub.1 or R.sub.2 represents hydrogen or lower alkyl group, a process for their manufacture and their use for the preparation of novel quinolone compounds having excellent antibacterial activity.

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl and hydroxyalkyl of 1 to 5 carbon atoms and amino, n is an integer from 1 to 3, X and X.sub.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms or taken together with the carbon atom to which they are attached are ##STR2## Y is --O-- or --S--, R.sub.3 is alkyl of 1 to 3 carbon atoms or aryl of 6 to 8 carbon atoms, ##STR3## is selected from the group consisting of ##STR4## R.sub.4 and R.sub.5 are individually aryl unsubstituted or substituted with at least one member of the group consisting of halogen, --NO.sub.2 and alkyl and alkoxy of 1 to 3 carbon atoms and non-toxic, pharmaceutically acceptable salts thereof with acids and bases having cyclooxygenase inhibiting and antibiotic acitvity.

Abstract: 5-Aroyl-2,3-dihydro-1H-pyrrolizine-1,1-dicarboxylates of the formula ##STR1## are prepared from 2-aroylpyrroles. Hydrolysis and mono-decarboxylation of these compounds affords ketorolac and related compounds.

Abstract: 5-Aroyl-2,3-dihydro-1H-pyrrolizine-1,1-dicarboxylates of the formula ##STR1## are prepared from 2-aroylpyrroles. Hydrolysis and mono-decarboxylation of these compounds affords ketorolac and related compounds.

Abstract: Swainsonine and analogs, namely, 1,4-dideoxy-1,4-imino-D-mannitol and the novel ring contracted swainsonines, (1S,2R,7R,7aR)-1,2-trihydroxypyrrolizidine and (1S,2R,7S,7aR)-1,2,7-trihydroxypyrrolizidine, are synthesized from the divergent intermediate, 4,5-anhydro-1-azido-1-deoxy-2,3-O-isopropylidene-D-talitol. These novel compounds are glycosidase inhibitors.

Abstract: Swainsonine and analogs, namely 1,4-dideoxy-1,4-imino-D-mannitol and the novel ring contracted swainsonines, .DELTA.(1S,2R,7R,7aR)-1,2-trihydroxypyrrolizidine and (1S,2R,7S,7aR)-1,2,7-trihydroxypyrrolizidine, are synthesized from the divergent intermediate, 4,5-anhydro-1-azido-1-deoxy-2,3-O-isopropylidene-D-talitol. These novel compounds are glycosidase inhibitors.

Abstract: 2,7-Diazabicyclo[3.3.0]octanes, suitable for 7-position substituents or antibacterially active quinolone carboxylic acids, of the formula ##STR1## in which R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 may be identical or different and in each case denote H, C.sub.1 -C.sub.5 -alkyl (optionally substituted by halogen, hydroxyl or C.sub.1 -C.sub.3 -alkoxy), C.sub.1 -C.sub.3 -alkoxycarbonyl or C.sub.6 -C.sub.12 -aryl,R.sup.4 additionally denotes halogen,R.sup.2 and R.sup.6 may be identical or different, denote H, C.sub.1 -C.sub.6 -alkyl, benzyl, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.3 -alkanoyl, benzoyl or C.sub.1 -C.sub.5 -alkoxycarbonyl, orR.sup.2 and R.sup.3 together denote a bridge of the structure (CH.sub.2).sub.n, n=2-4, CH.sub.2 --CHOH--CH.sub.2, CH.sub.2 --S--CH.sub.2 or C(CH.sub.3).sub.2 --S--CH.sub.2,excluding 2,7-diazabicyclo[3.3.0]octane.Also their preparation by the reaction ##STR2## Intermediates II are also new.

Abstract: Novel bicyclic tetrahydroxylated pyrrolizidines are disclosed which are inhibitors of glycosidase enzymes. A preferred inhibitor is (1S,2R,6R,7S)-1,2,6,7-tetrahydroxypyrrolizidine.

Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which R represents a group of formula (II) ##STR2## in which R.sub.x is the remainder of a heterocyclic group, or an optionally substituted phenyl group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 and R.sub.5, which may be located on the same or different carbon atoms, are independently hydrogen, C.sub.1-6 alkyl, or phenyl;m is 1, 2 or 3;R.sub.7 is hydrogen or C.sub.1-6 alkyl;n is 0, 1 or 2;X is direct bond, or O, S or NR.sub.6 in which R.sub.6 is hydrogen or C.sub.1-6 alkyl;Y is >C.dbd.O, >CHOH, >S.dbd.O or >SO.sub.2 ;each is R.sub.8 and R.sub.9 is C.

Abstract: Novel derivatives of 1,4-dideoxy-1,4-imino-D-mannitol and method for their synthesis from 4,5-anhydro-1-azido-1-deoxy-2,3-O-isopropylidene-D-talitol or its triflate derivative are disclosed. The novel derivatives, 6-fluoro-1,4-imino-1,4,6-trideoxy-D-mannitol and the N-butyl and N-benzyl derivatives of 1,4-dideoxy-1,4-imino-D-mannitol, have useful mannosidase inhibitory activity.

Abstract: (R,R)-2,5-Diazabicyclo[ 2.2.1]heptanes are prepared from a compound of the formula ##STR1## wherein X and R.sub.2 are as defined herein, by heating with tosylchloride in pyridine, reacting the formed compound of the formula ##STR2## with a C.sub.1 -C.sub.6 alkylamine or ammonia, and reducing or hydrolyzing the formed compound of the formula ##STR3## wherein R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl.

Abstract: Novel bicyclic tetrahydroxylated pyrrolizidines are disclosed which are inhibitors of glycosidase enzymes. A preferred inhibitor is 1.alpha.,2.alpha.,6.alpha.,7.alpha.,7.alpha..beta.-1,2,6-7-tetrahydroxypyr rolizidine. It is synthesized from D-glycero-D-gulo-heptono-1,4-lactone.

Abstract: Novel bicyclic tetrahydroxylated pyrrolizidines are disclosed which are inhibitors of glycosidase enzymes. A preferred inhibitor is 1.alpha.,2.alpha.,6.alpha.,7.alpha.,7.alpha..beta.-1,2,6-7-tetrahydroxypyr rolizidine. It is synthesized from D-glycero-D-gulo-heptono-1,4-lactone.

Abstract: Swainsonine and analogs, namely, 1,4-dideoxy-1,4-imino-D-mannitol and the novel ring contacted swainsonines, (1S,2R,7R,7aR)-1,2-trihydroxypyrrolizidine and (1S,2R,7S,7aR)-1,2,7-trihydroxypyrrolizidine, are synthesized from the divergent intermediate, 4,5-anhydro-1-azido-1-deoxy-2,3-O-isopropylidene-D-talitol. These novel compounds are glycosidase inhibitors.

Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## in which X is .dbd.CH-- or .dbd.N--; R.sup.2 is hydrogen, alky, phenyl, benzyl or phenethyl; Y is --CH.sub.2 --, --NH-- or --O--; and Z is --H.sub.2 or .dbd.O; B is His, Leu, Ile, Nva, Nle, Ala or Val; and R.sup.1 is hydrogen, alkyl, phenyl or phenylalkyl; or a pharmaceutically acceptable salt thereof are renin inhibitors.

Abstract: Pyrrolopyrroles of this type are suitable for coloring high-molecular organic material to give intensely colored, brilliant and transparent colorations with good general fastness properties, and for use in photoelectric recording materials as photoconductive substances.

Abstract: A compound, or a solvate or salt thereof, of formula I: ##STR1## in which: R.CO-- is an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 is C.sub.1-6 alkyl, or phenyl;R.sub.5 is hydrogen or together with R.sub.4 forms a --(CH.sub.2).sub.n -- group in which n=1, 2 or 3; and `Het` is an optionally substituted single or fused ring heterocyclic group, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from oxygen, nitrogen and sulphur, with the proviso that when, simultaneously, R.sub.

Abstract: Novel derivatives of 1,4-dideoxy-1,4-imino-D-mannitol and method for their synthesis from 4,5-anhydro-1-azido-1-deoxy-2,3-O-isopropylidene-D-talitol or its triflate derivative are disclosed. The novel derivatives, 6-fluoro-1,4-imino-1,4,6-trideoxy-D-mannitol and the N-butyl and N-benzyl derivatives of 1,4-dideoxy-1,4-amino-D-mannitol, have useful mannosidase inhibitory activity.

Abstract: Novel bicyclic tetrahydroxylated pyrrolizidines are disclosed which are inhibitors of glycosidase enzymes. A preferred inhibitor is 1.alpha., 2.alpha., 6.alpha., 7.alpha., 7.alpha..beta.-1,2,6,7-tetrahydroxypyrrolizidine. It is synthesized from D-glycero-D-gulo-heptono-1,4-lactone.Novel Intermediate compounds prepared during this synthesis are 7-O-tert-butyldiphenylsilyl-2,3:5,6-di-O-isopropylidene-D-glycero-D-gulo-h ept ono-1,4-lactone and 1.alpha., 2.alpha., 6.alpha., 7.alpha., 7.alpha..beta.-1,2:6,7-di-O-isopropylidene-1,2,6,7-tetrahydroxypyrrolizidi ne.

Abstract: A compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 0 or 1; andAr is an aromatic amide moiety, which compound exhibits prokinetic activity and is a 5-HT3 antagonist.

Abstract: Unsymmetric biaryl compounds are prepared by coupling two different halogenoaromatics by reaction with a metal and carrying out the reaction in the presence of catalytic amounts of a nickel compound, a promoter and a phosphorus-containing ligand.

Abstract: Inhibiting HMG-CoA reductase, as in treating hyperlipopproteinaemia, lipoproteinaemia and arteriosclerosis, with the new N-substituted N-amino-pyrroles of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2 is an aryl or heteroaryl radical,R.sup.3 is a hydrogen or an organic radical,R.sup.4 and R.sup.5 each independently is hydrogen or an organic radical or, together, they complete a heterocylic ring,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.10 is hydrogen or alkyl, and R.sup.11 is hydrogen, an organic radical or a cation.

Abstract: 5-Aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1,1-dicarboxylates of the formula ##STR1## are prepared from 2-halopyrroles. Hydrolysis and .beta.-decarboxylation of these compounds affords ketorolac and related compounds.

Abstract: A 3-aryl-pyrrolidine-2,4-dione (e) derivative of the formula (I) ##STR1## in which X represents alkyl, halogen and alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy and halogenoalkyl,Z represents alkyl, halogen and alkoxy,m represents a number from 1-4,n represents a number from 0-3, R represents hydrogen, ##STR2## or A where A represents a metal cation equivalent or represents an ammonium ion,R.sup.1 represents optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, polyalkoxyalkyl and optionally substituted cycloalkyl which can be interrupted by hetero atoms, or represents optionally substituted phenyl, optionally substituted phenylalkyl, substituted hetaryl, substituted phenoxyalkyl and substituted hetaryloxyalkyl andR.sup.2 represents optionally halogen-substituted alkyl, cycloalkyl, alkenyl, alkoxyalkyl, polyalkoxyalkyl and optionally substituted phenyl,as well as the pure enantiomeric forms of compounds of the formula (I).

Abstract: 7a-Nitromethyl-2,3,5,6,7,7a-hexahydro-1H-pyrrolizine of the formula ##STR1## and salts thereof, as well as processes for the preparation of the compound and 7a-aminomethyl-2,3,5,6,7,7a-hexahydro-1H-pyrrolizine and salts thereof.

Abstract: New derivatives of penem and pharmaceutically acceptable salt thereof are herein disclosed; these compounds being useful as an antibacterial agent which has an extremely wide antibacterial spectrum, exhibits a high sensitivity to bacteria resistant to conventional penicillins and cephalosporing antibiotics and is excellent in its physico-chemical stability, solubility to water and biological stability, in particular, stability to decomposition by enzyme such as dehydropeptidase I in kidney, .beta.-lactamase; these derivatives of penem being able to be prepared by reacting 2-substituted sulfinyl derivative of penem with a thiol compound and then optionally removing protective group(s) and further alkylating the reaction product or vice versa.

Abstract: Novel 1-azabicycloalkane- and alkene-oximes (Ia) and 8-azabicyclo[3.2.1]octane- and octene-oximes (Ib) are provided, these compounds being useful as agents for treating pain or for treating the symptoms of senile cognitive decline. Also provided are pharmaceutical compositions containing the compounds and methods of treatment using the compounds in dosage form.

Abstract: Process for the preparation of 1,4-diketopyrrolo[3,4-c]pyrroles of the formula I ##STR1## in which R.sub.1 and R.sub.2 independently of one another are phenyl, biphenyl or naphthyl radicals or aromatic O-heterocyclic, S-heterocyclic or N-heterocyclic radicals, by reacting 1 mole of a dicyclohexyl succinate, dialkyl succinate, monoalkylmonophenyl or diphenyl succinate, alkyl in the succinic acid ester radical being C.sub.1 -C.sub.18 alkyl and phenyl being phenyl which is unsubstituted or substituted by one or two halogen atoms or one or two C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy groups, with 2 moles of a nitrile of the formula II or III or with 1 mole of a nitrile of the formula II and 1 mole of a nitrile of the formula III ##STR2## in which R.sub.1 and R.sub.

Abstract: The present invention relates to a compound of the formula: ##STR1## wherein X is sulfur or optionally substituted imino group; Y is a bond, oxygen, phenylene, phenyleneoxy, or oxyphenyleneoxy; R.sup.1 is hydrogen or optionally substituted hydrocarbon residue; R.sup.2 is optionally substituted hydrocarbon residue; and R.sup.1 may form, together with the imino-nitrogen atom as X, a nitrogen-containing 5- to 7-membered ring, production and use thereof.The compound (I) of the present invention has an anti-oxidation activity and activities of preventing or improving functional disorders due to biologically active oxygen species, thus being useful as a pharmaceutical agent for prophylaxis and therapy of disorders in the circulatory system.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein R.sub.c is carboxy, esterified carboxy or amidated carboxy; R.sub.2 is hydrogen or lower alkyl or joins with R.sub.a and R.sub.b and the atoms therebetween to form a fused ring ##STR2## and either R.sub.a is methyl and R.sub.b is ##STR3## or R.sub.2 and R.sub.b and the atoms therebetween form a group ##STR4## wherein R.sub.3 and R.sub.4 are either both hydrogen, or together are propylene, butylene, or with the two atoms to which they are attached form a benzene ring. Methods of manufacture and use thereof in the production of angiotensin converting enzyme inhibitors are disclosed.

Abstract: Compositions comprising(a) a pyrrolopyrrole of formula I ##STR1## wherein A and B are identical or different alkyl, arlkyl, aryl or heterocyclic aromatic radicals, R.sub.1 and R.sub.2 are hydrogen atoms, unsubstituted or substituted alkyl radicals, and also alkenyl, alkynyl, aralkyl, cycloalkyl, carbamoyl, alkylcarbamoyl, arylcarbamoyl, alkoxycarbonyl, aryl, alkanoyl or aroyl groups, and X is an --O-- or --S-- atom, and(b) a pyrrolopyrrole of the above formula I that contains at least one group of formula --SO.sub.3 L, --CO.sub.2 L, --PO.sub.3 (L).sub.2, --N(R.sub.4)(R.sub.5), ##STR2## or --NHCOR wherein L is --H, a group of formula ##EQU1## or N.sup.+ H(R.sub.3)(R.sub.4)(R.sub.5), M is monovalent, divalent or trivalent metal cation, n is 1, 2 or 3, R.sub.3, R.sub.4 and R.sub.5 are each independently --H or alkyl, aralkyl, C.sub.5 -C.sub.6 cycloalkyl or aryl radicals, or R.sub.4 and R.sub.

Abstract: A process for the preparation of pyrrolizine derivatives of the formula ##STR1## wherein R is --CN or --CH.sub.2 NH.sub.2, and salts thereof.