Abstract: A method for preserving mammalian hearts while under ischemic conditions is accomplished by exposing the heart to a preservation solution containing a pharmacologically effective concentration of a Na.sup.+ /K.sup.+ /Cl.sup.- co-transporter blocker agent, such as Furosemide, Bumetanide or Piretanide, thereby extending survival of the heart.

Abstract: The instant invention is a method of using known compounds, such as (-)-5.alpha.,7.alpha.,-8.beta.-N-methyl-N-[7-(1-pyrrolidinyl)-1-oxaspiro[4 .5]dec-8-yl]-4-benzofuranacetamide, as agents for treating benign prostatic hyperplasia.

Abstract: Invented is a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans which comprises administering to such human an effective therefor amount of a substituted azaspirane.

Abstract: A method for combatting anxiety in a subject in need of such treatment is provided. The method comprises administering to the subject a 2-aminocycloaliphatic amide kappa opioid agonist in an effective anxiety-combatting amount.

Abstract: The invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded represent a substituted cycle,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents 0, 1, 2 or 3,G represents hydrogen (a) or the groups ##STR2## represents a metal ion equivalent or an ammonium ion, L and M represents oxygen and/or sulphur,R.sup.1 represents in each case optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, alkylthioalkyl, polyalkoxyalkyl or cycloalkyl, which can be interrupted by hetero atoms, optionally substituted phenyl, optionally substituted phenylalkyl, substituted hetaryl, substituted phenoxyalkyl or substituted hetaryloxyalkyl,R.sup.2 represents in each case optionally halogen-substituted alkyl, alkenyl, alkoxyalkyl, polyalkoxyalkyl or in each case optionally substituted phenyl or benzyl,R.sup.3, R.sup.

Abstract: Invented is a method of treatment of hyperlipidemia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective therefor amount of a substituted azaspirane.

Abstract: Fungicidally active compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents cycloalkyl, or represents optionally substituted aryl, or represents the radical ##STR2## R.sup.1 and R.sup.2 each independently is hydrogen or an organic radical, or together with the nitrogen atom form a heterocyclic radical,R.sup.3 represents hydrogen, alkyl or optionally substituted aryl, andR.sup.4 represents alkyl or cycloalkyl, or represents optionally substituted aryl,but wherein R.sup.3 and R.sup.4 may not simultaneously represent methyl,and acid addition salts thereof, as well as intermediates therefor.

Abstract: 3,9-disubstituted-spiro[5.5]undecanes and ##STR1## wherein, R, Y, A, B and n are defined in the specification, pharmaceutical compositions containing same for the treatment of cardiovascular disorders, such as heart failure and hypertension, are disclosed.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, A and m are as defined in the description.Medicinal product which is useful for treating depression and anxiety.

Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.

Abstract: This invention relates to compounds of the formula: ##STR1## which are useful as 5-HT.sub.4 agonists or antagonists and 5-HT.sub.3 antagonists.

Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.

Abstract: This invention discloses a method of treating hyperlipidemia in a mammal by administering an effective amount of a substituted azaspirane.

Abstract: Fungicidally active compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents cycloalkyl, or represents optionally substituted aryl, or represents the radical ##STR2## R.sup.1 and R.sup.2 each independently is hydrogen or an organic radical, or together with the nitrogen atom form a heterocyclic radical,R.sup.3 represents hydrogen, alkyl or optionally substituted aryl, andR.sup.4 represents alkyl or cycloalkyl, or represents optionally substituted aryl,but wherein and R.sup.3 and R.sup.4 may not simultaneously represent methyl,and acid addition salts thereof, as well as intermediates therefore.

Abstract: Methods for using substituted phenoxy-, 1-, and 2-naphthalenyloxy-, indenyl-, indolyl-, benzo[b]furanyl-, and benzo[b]thienylcarboxamides of 7,8-(substituted-diamino)-1-oxaspiro[4.5]decanes as agents for alleviating the symptoms of Parkinson's disease, dystonia, and other movement disorders are disclosed. Pharmaceutical compositions employing the compounds are also disclosed.

Abstract: A synergistic pharmaceutical composition of substituted phenoxy-, 1-, and 2-naphthalenyloxy-, indenyl-, indolyl-, benzo[b]furanyl-, and benzo[b]thienylcarboxamides of 7,8-(substituted-diamino)-1-oxaspiro[4.5]decanes and L-DOPA as a composition alleviating the symptoms of Parkinson's disease and/or dystonia. A method of using the pharmaceutical composition is also disclosed.

Abstract: Methods for using substituted phenoxy-, 1-, and 2-naphthalenyloxy-, indenyl-, indolyl-, benzo[b] furanyl-, and benzo[b]thienylcarboxamides of 7,8-(substituted-diamino)-1-oxaspiro[4.5]decanes as agents for alleviating the symptoms of Parkinson's disease, dystonia, and other movement disorders are disclosed. Pharmaceutical compositions employing the compounds are also disclosed.

Abstract: Certain spirocyclic heterocyclic compounds, and their pharmaceutically-acceptable salts, are inhibitors of the aldose reductase enzyme, and so are useful for the control of diabetic complications.

Abstract: O-substituted fumagillol derivatives and its salts have an angiogenesis regressing activity are useful for treatment of diseases induced by abnormally stimulated neovascularization.

Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is 2-methyl-1-propenyl group or isobutyl group; R.sup.2 and R.sup.3 are each hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group or R.sup.2 and R.sup.3 may form a ring together with the adjacent nitrogen atom; and the bonding mark .about. represents an .alpha.-linkage or .beta.-linkage, or a salt thereof. The compound (I) of the present invention has, among others, angiogenesis inhibiting activity, cell-growth inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.

Abstract: N-succinimidyl and N-phthalimidyl esters of phenylalkanoic acid derivatives which are useful as inhibitors of HLE or HNE.

Abstract: The invention relates to a method for the treatment of cardiac and of vascular hypertrophy and hyperplasia by administration of angiotensin converting enzyme inhibitors. Administration of compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each is hydrogen or an organic radical, and R.sup.4 and R.sup.5 form, together with the atoms carrying them, a mono-, bi- or tricyclic heterocyclic ring system, is preferred. The invention additionally relates to angiotensin converting enzyme inhibitors and to agents containing these for administration for the treatment of the abovementioned diseases.

Abstract: Substituted 4,5-dihydrothieno[2,3-b]thiophene-2-sulfonamides and 6,6-dioxides thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.

Abstract: This invention relates to 1,3-dihydro-1-(pyridinylamino)-2H-indol-2-ones of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl cycloalkane or heterocycloalkyl selected from the group consisting of piperidine and tetrahydropyran; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and, where applicable the optical, geometrical and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics, anticonvulsants, for enhancing memory and for the treatment of Alzheimer's disease.

Abstract: Avermectin analogs are disclosed wherein the 6,6-spiroketal ring system has been reduced in size to a 6,5-spiroketal ring system by the deletion of the 25-position carbon atom and the 25-alkyl substituent and which has a 23-acyl cycloalkyl, phenyl or substituted hydroxymethyl substituent. This is accomplished by opening the outer spiroketal ring with the elimination of ring carbon atoms 23, 24 and 25 and the alkyl substituent at the 25-position and incorporation a new component, reclosing the spiroketal to a 5-membered ring with a 23-acyl substituent and new substituents at the 24-position. The compounds are used as anti-parasitic insecticidal and anti-helmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome. A particularly preferred class of compounds comprise difluoro-dialkoxy substituted spiro-(9H-fluorene-9,4'-imidazolidine)-2',5-diones.

Abstract: A method is provided for preventing or reducing the risk of restenosis following angioplasty by administering pravastatin alone or in combination with an ACE inhibitor such as captopril or ceranapril, prior to, during and/or after angioplasty.

Abstract: Fungicidal and microbicidal substituted 1-aminomethyl-3-aryl-4-cyano-pyrroles of the formula ##STR1## in which Ar represents optionally substituted phenyl,R.sup.1 represents optionally substituted alkyl, alkenyl, alkynyl or cycloalkyl or in each case optionally substituted aralkyl or aryl andR.sup.2 represents alkyl or in each case optionally substituted cycloalkylalkyl, aralkyl, cycloalkyl or aryl,and their acid addition salts.

Abstract: Compound of the general formula (I), which is useful as an agricultural and horticultural fungicide, an agricultural and horticultural fungicidal composition containing said compound, use of said composition for controlling plant disease, and process for the production of said compound: ##STR1## wherein ##STR2## shows a case in which R.sup.3 and R.sup.4 together form a cyclic substituent, and R.sup.1 and R.sup.4 are substituents disclosed in the specification.

Abstract: A method is provided for imhibiting loss of cognitive functon, including memory, which may or may not be associated with Alzheimer's disease, by administering an ACE inhibitor, such as captopril, fosinopril, zofenopril or ceranapril in combination with a drug that acts as serotonin receptors such as zacopride, over a prolonged period of treatment.

Abstract: The present invention relates to spiroisoindolines that are antagonists at the phencyclidine receptor of the N-methyl-D-aspartate receptor complex and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides processes for preparing the spiroisoindolines, intermediates useful for their synthesis, pharmaceutical compositions containing them, and methods for their use.

Abstract: By incorporating a liquid or solid silicone or paraffin into 1,3,5-trioxane, agglomeration of trioxane particles and adhesion of the trioxane to a machine wall or the like can be prevented. The silicone or paraffin is used in an amount of 0.003 to 1% by weight.

Abstract: Disclosed are spirocyclic compounds of the formula: ##STR1## The compounds of formula I are oxytocin antagonists useful in the treatment of preterm labor and dysmenorrhea, and for the stoppage of labor preporatory to Caesarian delivery. Also disclosed are pharmaceutical compositions containing these compounds as well as methods for preparing the compounds.

Abstract: 3-Alkyl-4-arylpyrrolidine derivatives of the formula ##STR1## where R.sup.1 is alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkyl-cycloalkyl, cycloalkyl-alkyl, alkyl-cycloalkyl-alkyl, cycloalkenyl-alkyl, alkyl-cycloalkenyl, bicycloalkyl, bicycloalkylalkyl, alkyl-bicycloalkyl, heterocycloalkyl, heterocycloalkylmethyl, aryl, arylalkyl, alkylary, alkyl-aryl-alkyl,R.sup.2 is alkyl, alkoxy,R.sup.3 is alkylR.sup.4 is alkyl, alkenyl, alkynyl and phenylalkyl,X.sup.- is a plant-tolerated anion, andn is 0 or 1,their plant-tolerated salts, and fungicides containing these compounds.

Abstract: N-Substituted 3-arylpyrrolidine derivatives of the formula ##STR1## where R.sup.1 is 2,2-dimethylpropyl, 3,3-dimethylbutyl, 4,4-dimethylpentyl, 2,4,4-trimethylpentyl, 6-methylhept-2-yl, 3,5,5-trimethylhexyl, 6,10-dimethylundec-2-yl, 3-methylcyclohexyl, 3,3-dimethylcyclohexyl, 3,3,5-trimethylcyclohexyl, 3,3,5,5-tetramethylcyclohexyl, 4-methylcyclohexyl, 4-ethylcyclohexyl, 4-propylcyclohexyl, 4-isopropylcyclohexyl, 4-tert.-butylcyclohexyl, trans-4-tert.-butylcyclohexyl, 4(2-methylbut-2-yl)cyclohexyl, 4(2,4,4-trimethylpent-2-yl)-cyclohexyl, cyclododecanyl, C.sub.3 -C.sub.9 -trialkylsilyl-substituted C.sub.4 -C.sub.12 -cycloalkyl, 4-hydroxycyclohexyl, 4-hydroxy-3-methylcyclohexyl, 4-hydroxy-3,5-dimethylcyclohexyl, 4-hydroxy-3,3-dimethylcyclohexyl, 4-hydroxy-3,3,5-trimethylcyclohexyl, unsubstituted or hydroxy-, C.sub.1 -C.sub.9 -alkyl-, C.sub.1 -C.sub.5 -alkoxy- or C.sub.3 -C.sub.9 -trialkylsilyl-substituted C.sub.5 -C.sub.12 -cycloalkenyl,R.sup.1 is further bicycloalkyl,R.sup.1 is further 4-tert.

Abstract: A series of novel 3-mono(substituted methyl)- and 3,3-di(substituted methyl)-2-oxo-indoline-1-alkanoic acid compounds have been prepared, including their lower alkyl esters and unsubstituted amide derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Typical members include those compounds derived from 2-oxo-indoline-1-acetic acid wherein a 3,4-dichlorobenzyl or 3,4-dichloro-.alpha.-methylbenzyl moiety is substituted at 3-position of the molecule. Preferred member compounds include 3-(3,4-dichlorobenzyl)-2-oxo-indoline-1-acetic acid, 5-chloro-3-(3,4-dichlorobenzyl)-2-oxo-indoline-1-acetic acid, 3-(3,4-dichlorobenzyl)-6-methoxy-2-oxo-indoline-1-acetic acid, 3-(3,4-dichlorobenzyl)-6-hydroxy-2-oxo-indoline-1-acetic acid and 3-(3,4-dichloro-.alpha.-methylbenzyl)-2-oxo-indoline-1-acetic acid.

Abstract: Antihypercholesterolemic activity has been discovered in compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein: Z is ##STR2## X is lower alkyl, lower alkenyl, or lower alkenyl; R.sup.1 is hydrogen, alkyl, alkenyl, aryl, alkylaryl, or substituted aryl having one or more substituents; andone of R.sup.2 and R.sup.3 is hydrogen and the other is hydrogen, alkyl, alkenyl, aryl, alkylaryl or alkenyl aryl; or R.sup.2 and R.sup.3 are both lower alkyl; or R.sup.2 and R.sup.3 together complete a substituted or unsubstituted hydrocarbon ring that is cycloalkyl or cycloalkenyl with substituents as defined in the specification.

Abstract: Antihypercholesterolemic activity is exhibited by novel compounds of the formula ##STR1## wherein: Z is ##STR2## X is lower alkyl or lower alenyl; R.sup.1 is aryl or alkyl;R.sup.2 and R.sup.3 are the same or different and are hydrogen, or lower alkyl or aryl, or R.sup.2 and R.sup.3 taken together to form a cycloalkyl group; andR.sup.4 is hydrogen, lower alkyl, or alkali metal (such as sodium, lithium, or potassium) or a radical such as ammonium.Methods of use and novel intermediates of these compounds are also provided.

Abstract: A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula ##STR1##

Abstract: The invention relates to amino acid esters of the formula I ##STR1## in which n is 2 and R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meaning indicated in the description, to a process and intermediates for the preparation thereof, to agents containing them, and the use thereof.

Abstract: A method is provided for inhibiting onset of or treating depression by administering an ACE inhibitor, such as captopril, fosinopril, zofenopril or ceranapril in combination with a drug that acts at serotonin receptors such as zacopride, over a prolonged period of treatment.

Abstract: Novel 1,2-cyclohexylaminoaryl amides useful as analgesic agents having very high kappa-opioid affinity and selectivity and potency and useful as analgesics, diuretics, antiinflammatory and psychotherapeutic agents are disclosed. Methods for making the compounds and pharmaceutical compositions containing them are also disclosed.

Abstract: The present invention provides compounds of the general formula (I) which inhibit the aggregation of erythrocytes or thrombocytes ##STR1## wherein A is hydrogen or C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, benzyl or C.sub.3 -C.sub.7 -cycloalkyl radical, B is hydrogen, R.sub.1 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.3 -C.sub.7 -cycloalkyl radical, R.sub.2 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, aminocarbonyl or hydrazinocarbonyl radical, or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a C.sub.3 -C.sub.7 -cycloalkyl ring, n is 0, X is a valency bond or a C.sub.1 -C.sub.6 -alkylene radical, R.sub.3 is a carbocyclic aromatic ring, which may be substituted; and the tautomers, optically-active forms and physiologically acceptable salts thereof with organic and inorganic acids.

Abstract: A method is provided for inhibiting loss of cognitive function, including memory, which may or may not be associated with Alzhemier's disease, in a mammalian species by administering an ACE inhibitor, which is a phosphonate substituted amino or imino acid or salt, such as SQ 29,852 over a prolonged period of treatment.

Abstract: Compounds are described of formula (1) ##STR1## and salts thereof wherein R.sup.1 is a methyl, ethyl or isopropyl group;R.sup.2 represents a hydrogen atom or a group OR.sup.4 (where OR.sup.4 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.CH.sub.2, >C.dbd.O or >C.dbd.NOR.sup.5 (where R.sup.5 is a hydrogen atom or a C.sub.1-8 alkyl group and the group >C.dbd.NOR.sup.5 is in the E configuration).These compounds may be used for controlling insect, acarine, nematode or other pests.

Abstract: Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids and esters derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl(NOH) or --C(C.sub.1-6 alkyl)NNH.

Abstract: Lactam compounds of the formula ##STR1## in which: R is hydrogen, alkyl or cycloalkyl;R.sup.1 is hydrogen, alkyl, alkenyl or cycloalkyl;R.sup.2 is alkyl, alkenyl, cyano or a carbonyl substituted hydroxyl, alkyl, alkoxy, amino, alkylamino or hydrazino; orR.sup.1 and R.sup.2 together represent alkylidene cycloalkylidene; orR.sup.1, R.sup.2 and the adjacent carbon atom form a spirocyclic ring;n is 0 or 1;A is a --Co--NH--, --NH--CO--NH-- or --O--CO--NH--;X is a valency bond, alkylene or alkenylene; andR.sup.3 is optionally substituted phenyl, pyridyl, methylenedioxyphenyl or a five-membered heterocycle; or when X is a valency bond, R.sup.3 can also be an optionally substituted alkyl or alkino group, or cycloalkyl. The compounds are useful for the inhibition of erythrocyte and thrombocyte aggregation.

Abstract: Compounds of the formulae: ##STR1## are useful as anti-hypertensives.