Abstract: A process for the asymmetric hydrogenation of a compound of the formula ##STR1## wherein each R, independently, is alkyl, arylmethyl, aryl, alkoxy, arylmethoxy or aryloxy or both R's, taken together, are methylene, ethylene or 1,2-phenylene and n is 1,2 or 3,or of a salt thereof to a compound of the formula ##STR2## in the form of an (S) or (R) enantiomer, wherein R and n have the significances given above, using an optically active ruthenium-diphosphine complex as catalyst, is described. The preparation of the compounds of formula II, as well as the compounds of formula II, which form a further object of the invention, are also described.

Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed. These compounds possess inhibitory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and are thus useful as cardiovascular agents.

Abstract: Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.

Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents.

Abstract: Compounds of the formula ##STR1## wherein: ##STR2## A is are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.

Abstract: Fibrinogen receptor antagonists of the ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets, for example ##STR2##

Abstract: The present invention relates to certain novel mercaptoacetylamido pyridazo[1,2]pyridazine, pyrazolo[1,2]pyridazine, pyridazo[1,2- a] [1,2]diazepine and pyrazolo[1,2- a ][1,2]diazepine derivatives useful as inhibitors of enkephalinase and of ACE.

Abstract: Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula ##STR1## wherein one or two carbon atoms of the ##STR2## moiety may be substituted with C.sub.1-4 alkyl, C.sub.1-4 alkyloxy or two carbon atoms of the CH.sub.2 groups of said moiety may be bridged with a C.sub.2-4 alkanediyl radical;X represents CH or N; R.sup.1 represents hydrogen, C.sub.1-4 alkyl, halo, hydroxy, trifluoromethyl, cyano, C.sub.1-4 alkyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkylcarbonyl or aryl; R.sup.2 and R.sup.3 each independently represent hydrogen or C.sub.1-4 alkyl; Alk represents C.sub.1-4 alkanediyl; R.sup.4 and R.sup.5 each independently represent hydrogen, C.sub.1-4 alkyl or halo; andHet represents ##STR3## the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity.

Abstract: A novel class of sulfonamoyl-substituted 1,6-diaza[4.4]spirodilactams, having a sulfonamoyl substituent on the hydrocarbyl group attached to each spiro ring nitrogen atom, is useful for the preparation of polymers, including polyamides and as latent curing agents for epoxy resins.

Abstract: The present invention pertains to boron containing thiouracil derivatives, their method of preparations, and their use in the therapy of malignant melanoma using boron neutron capture therapy.

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 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: Diazabicycloalkane derivatives of the formula ##STR1## where R is alkyl, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are identical or different and independently of one another are each hydrogen or methyl, X is chlorine or bromine, m is 0 or 1, n is 1 or 2, and p and q are each 0, 1 or 2, the carbon atom functioning as bridgehead having an R configuration, and herbicidal agents containing acetanilides as herbididally active compounds and diazabicycloalkane derivatives as antagonistic agents.

Abstract: There are disclosed new naphthyridine- and quinoline-carboxylic acids having a 1-tertiary-alkyl substituent, compositions containing them, and their use in treating bacterial infections in warm-blooded animals. Also disclosed are novel amines and intermediates used in the preparation of the naphthyridine- and quinoline-carboxylic acids.

Abstract: Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof posses, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.

Abstract: Novel 1-azaspiro[4.4] lactams are produced by reaction of at least one hydroxy-containing primary amino compound with a 4-ketodiacid compound or a 1,6-dioxaspiro[4.4]lactone. Molar excesses of amion compound result in production of spirodilactams, while limited molar quantities of amino compound results in production of a spirolactam-lactone which reacts further with hydroxy-containing primary amino compound or with hydroxy-free primary amino compound to produce a spirodilactam. Certain of the spirolactams are useful as precursors for glycidyloxy derivatives which react with epoxy curing agents to form insoluble thermoset resins while others are useful as curing agents and yet others are converted to glycidyloxy derivatives useful as reactive diluents in epoxy resin applications.

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: This invention relates to 1-aminoalkyl-3-oxysubstituted-4-aryl-1,3,4,5-tetrahydro-2H-1,3-benzodiazep ine-2-ones having the formula ##STR1## where R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl, aryl, arylloweralkyl, and acyl; R.sub.3 is hydrogen, loweralkyl, arylloweralkyl aryl and acyl; X is hydrogen, halogen, hydroxy loweralkyl, loweralkoxy, NO.sub.2, NH.sub.2 and CF.sub.3 ; m is an integer of 1 to 3, n is an integer of 1 to 3; the pharmaceutically acceptable acid addition salts thereof and where appropriate the geometric and optical isomers thereof. The compounds of this invention display utility as analgesics, calcium ion antagonists and antihypertensives.

Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of benzodiazinone-pyridazinone and hydroxy-pyrazolyl compounds and pharmaceutical compositions including the same.

Abstract: Novel epoxyalkoxy-containing [4.4] spirodilactams having ring nitrogen atoms in the 1- and the 6- ring positions and having a substituent on each ring nitrogen atom, at least one of which substituents contains an epoxyalkyl moiety. Such epoxy compounds are produced by reaction of a 1-halo-2,3-epoxyalkane and the corresponding hydroxy-containing spirodilactam followed by treatment with strong base.

Abstract: Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## (wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof possess, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.

Abstract: Compounds of the formula ##STR1## wherein: z is O or I;X is ##STR2## a and b are 0, 1, or 2 and a+b=0, 1 or 2; R, R.sup.1, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, alkyl or aralkyl;R.sub.n is hydrogen, alkyl, aralkyl, acyl, carbalkoxy, carbamyl, carbalkoxyalkyl, hydroxyalkyl, alkoxyalkyl or amidino;R.sup.5 groups on vicinal carbon atoms may together form a carbon-carbon double bond when a or b=2;R groups on vicinal carbon atoms may together form a carbon-carbon double bond when R.sub.n is hydrogen and z=1;R.sup.4 and R.sup.5 geminal groups may together form a spiro substituent, --(CH.sub.2).sub.d --, where d is 2 to 5;R.sup.5 and R.sup.6 groups may together form a carbon-nitrogen double bond when R.sub.3 is hydrogen and a+b=1;R.sup.2 is hydrogen or --(CH.sub.2).sub.y --Y where y is 1-3;Y is hydrogen, --O--R.alpha., --S-R.alpha. or ##STR3## R.alpha. is hydrogen, alkyl, cycloalkyl or acyl; R.beta. is hydrogen or alkyl; andR.alpha. and R.beta.

Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## , R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --or--N(R.sup.6)--in which R.sup.6 is hydrogen, alkyl or aralkyl, as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently represent hydrogen, C.sub.1 -C.sub.10 -alkyl, adamantyl-(C.sub.1 -C.sub.4 -alkyl) or (C.sub.2 -C.sub.6 -alkanoyloxy)-(C.sub.1 -C.sub.4 -alkyl), and pharmaceutically acceptable salts thereof possess antihypertensive activity and can be used as theraputic or prophylactic agents in pharmaceutical preparations. Intermediates for the production of such compounds are also provided.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl,as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently represent hydrogen, C.sub.1 -C.sub.10 -alkyl, adamantyl-(C.sub.1 -C.sub.4 -alkyl) or (C.sub.2 -C.sub.6 -alkanoyloxy)-(C.sub.1 -C.sub.4 -alkyl), and pharmaceutically acceptable salts thereof possess antihypertensive activity and can be used as theraputic or prophylactic agents in pharmaceutical preparations. Intermediates for the production of such compounds are also provided.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 represents hydroxy, alkyl, aralkyl, aralkoxy-alkyl, hydroxy-alkyl, amino-alkyl, acylamino-alkyl, monoalkylamino-alkyl, dialkylamino-alkyl, alkoxycarbonylamino-alkyl, halo-alkyl, carboxy-alkyl, alkoxycarbonyl-alkyl, alkoxy or aralkoxy; R.sup.2 and R.sup.3 each represent hydrogen, alkyl or aralkyl; R.sup.4 and R.sup.5 each represent hydrogen or R.sup.4 and R.sup.5 together represent oxo; and X represents an oxygen atom or the group --NR.sup.6 -- in which R.sup.6 represents hydrogen, alkyl or aralkyl or --(CH.sub.2).sub.n -- in which n stands for zero, 1 or 2,and racemates, enantiomers, diastereoisomers or pharmaceutically acceptable salts thereof have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations. They can be prepared according to known methods.Compounds useful as starting materials for producing the compounds of formula I are also provided.

Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of benzodiazinonepryidazinone and hydroxy-pyrazolyl compounds and pharmaceutical compositions including the same.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl,as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.

Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of hydroxy and aminothiazolyl-benzodiazinone compounds and pharmaceutical compositions including the same.

Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.

Abstract: This invention relates to novel indole derivatives of the formula ##STR1## wherein A represents a --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## group and B represents a methylene, carbonyl, or thiocarbonyl group or A represents a --CO--CO-- or ##STR3## group and B represents a methylene group, E represents an alkylene group or a 2-hydroxy-n-propylene, 2-hydroxy-n-butylene, or 3-hydroxy-n-butylene group,G represents an alkylene group,R.sub.1 represents a hydrogen, chlorine, or bromine atom or a trifluoromethyl, nitro, amino, alkylamino, dialkylamino, alkyl, hydroxyl, alkoxy, or phenylalkoxy group,R.sub.2 represents a hydrogen, chlorine, or bromine atom or a hydroxyl, alkoxy, phenylalkoxy, or alkyl group orR.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen, chlorine, or bromine atom or an alkyl group,R.sub.4 represents a hydrogen atom or an alkyl or phenylalkyl group,R.sub.

Abstract: This invention relates to benzazepine derivatives of formula I ##STR1## wherein A is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;R.sub.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.3 alkyl, amino, C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3 dialkylamino, acylamino, hydroxy, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy;R.sub.2 is hydrogen, chlorine, bromine, hydroxy, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy or phenyl C.sub.1 -C.sub.3 alkoxy or, together with R.sub.1, can be C.sub.1 -C.sub.3 alkylenedioxy;R.sub.3 is hydrogen, chlorine, bromine or C.sub.1 -C.sub.3 alkoxy;R.sub.4 is hydrogen, benzyl, C.sub.1 -C.sub.3 alkyl or C.sub.3 -C.sub.5 alkenyl;R.sub.5 is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy;R.sub.6 is hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy or, together with R.sub.5, can be a C.sub.1 -C.sub.2 alkylenedioxy;X is an imino, optionally substituted by a benzyl or C.sub.1 -C.sub.