Abstract: Invented are sulfonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.

Abstract: Disclosed herein are novel benzisothiazole derivatives having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of a variety of central nervous system disorders.

Abstract: Pyrrole derivatives of the general formula I ##STR1## wherein R denotes alkyl which is substituted by --NH.sub.2 or acylamino, R.sup.1 and R.sup.2 independently of one another denote hydrogen or alkyl having 1 to 4 carbon atoms, R.sup.3 denotes hydrogen, alkyl having 1 to 4 carbon atoms or a carboxylic acid grouping, R.sup.

Abstract: A thienotriazolodiazepine compound of the formula: ##STR1## wherein each symbol is as defined in the specification or a pharmaceutically acceptable salt thereof, and pharmaceutical uses thereof.Said compounds exhibit PAF-antagonistic activity and are useful for the prevention or treatment of various PAF-induced diseases.

Abstract: Disclosed herein are novel benzopyrans having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of hypertension.

Abstract: The present invention provides ketones of the general formula (I): ##STR1## and physiologically acceptable salts and solvates thereof, wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a C.sub.1-6 alkyl group; Im represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.3, R.sup.4 and R.sup.5 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and an aromatic or heteroaromatic group as defined in the specification.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety and nausea and vomiting.

Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## B is ##STR3## R.sup.1 is hydrogen; halogen, cyano or optionally substituted C.sub.1-4 alkyl; andQ is NR.sup.8 R.sup.9 or ##STR4## where R.sup.2 to R.sup.11 are substituents of various types. The compounds are useful as fungicides.

Abstract: A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## in which R.sub.1 denotes hydrogen; linear or branched C.sub.1 -C.sub.4 alkyl; or benzyl:R.sub.2 denotes linear or branched C.sub.1 -C.sub.6 alkyl; cyclohexyl; trichloromethyl; 1-propenyl; allyl; phenyl; 4-chlorophenyl; or benzyl; or R.sub.1 and R.sub.2 together denote a C.sub.3 -C.sub.5 aliphatic chain:X denotes halogen; C.sub.1 -C.sub.3 alkyl; methylthio; trifluoromethyl; optionally esterified carboxy of formula --COOR in which R denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH--or --N(C.sub.1 -C.sub.4 alkyl)--; alkylamino of formula NHR.sub.5 in which R.sub.

Abstract: Substituted allylmercaptoacetylsydnonimines of the general formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which R.sub.1 represents a secondary amino group of the formula ##STR2## and X denotes ##STR3## R.sub.2 denotes one of the radicals R.sub.3 OOC--, R.sub.4 SO.sub.2 -- or alkyl having1-4 C atoms,n denotes one of the values 1, 1 or 2,and R.sub.3 denotes alkyl having 1-4 C atoms,and R.sub.4 represents R.sub.3 or (R.sub.3).sub.2 N--, have valuable pharmacological properties.

Abstract: This invention relates to quaternary compounds having the formula ##STR1## wherein W.sup.- is an anion; m and n are integers having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms; R.sub.1 is a radical having from 8 to 25 carbon atoms and is selected from the group of alkyl, alkenyl and alkoxy alkylene and each of R.sub.2, R.sub.3 and R.sub.4 is a radical having from 1 to 25 carbon atoms and is alkyl, alkoxy or ##STR2## where p has a value of from 1 to 4 and X is hydrogen or methyl. The invention also relates to the preparation and use of said diquaternized compounds.

Abstract: N-monosubstituted and N,N-disubstituted amides of the 1-methyl-5-p-toluoylpyrrole-2-acetic acid, which are active as antiinflammatory, analgesic, antipyretic, antisecretive and antitussive agents, are disclosed.These amides are prepared by reacting an amine with an activated derivative of the 1-methyl-5-p-toluoylpyrrole-2-acetic-acid of formula ##STR1## where X is an activating group suitable for promoting the formation of an amide bond.

Abstract: A continuous method for the high-yield, one-step, solvent-free manufacture of blocked polyisocyanurate compounds useful as curing agents in powder coating compositions. The preferred method of manufacture is to pre-mix a blocking agent and a polymerization catalyst (BAC mix) prior to injection with an organic isocyanate monomer having two or more isocyanate groups (herein termed a polyisocyanate) into a preheated reaction zone wherein the BAC mix and the polyisocyanate react to form the blocked polyisocyanurate compound that is obtained after discharge from the reaction zone and cooling.

Abstract: 1-Hydroxy-2,2,6,6,-tetraalkylpiperidine derivatives are effective as light stabilizers in a variety of substrate systems.

Abstract: Novel .delta.-caprolactam derivatives of formula I have anti-tumor, antibiotic and anthelmintic activity: ##STR1## wherein: R is H, lower alkyl, or lower acyl;R.sub.1, R.sub.2, and R.sub.3 are each independently H or lower acyl;R.sub.4 is H or acyl of 1 to 22 carbon atoms;R.sub.5 is H or lower acyl;R.sub.6 and R.sub.7 are each H or OH, or R.sub.6 and R.sub.7 together form an epoxide or a double bond;and the pharmaceutically acceptable salts thereof.

Abstract: A compound of the formula (1) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 are both hydrogen; orR.sub.1 is hydrogen, C.sub.1-6 alkyl; and R.sub.2 is CN; CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or together are C.sub.4-6 polymethylene; or COR.sub.10 is OH or C.sub.1-4 alkyl, or COR.sub.10 is a pharmaceutically acceptable ester or amide; orR.sub.2 is hydrogen, C.sub.1-6 alkyl, or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; orR.sub.1 and R.sub.2 together form C.sub.3 -C.sub.

Abstract: Herbicidal and plant growth-regulating novel 5-acylamino-pyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,Ar represents in each case optionally substituted phenyl or pyridyl,X represents oxygen or sulphur,A represents a straight-chain or branched optionally substituted alkylene bridge,n represents the numbers 0 or 1 andY represents cyano or the grouping ##STR2## wherein X.sup.1 represents oxygen or sulphur andR.sup.3 represents hydroxyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, amino, alkylamino, dialkylamino, alkenylamino, dialkenylamino, alkyl-alkenylamino or a --OM radical,whereinM represents one equivalent of the cation of an inorganic or organic base.Intermediates therefor of the formula ##STR3## are also new.

Abstract: An imide derivative of the formula: ##STR1## or a pharmaceutically acceptable salt, which is useful as an antipsychotic drug.

Abstract: Furopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.

Abstract: Certain .alpha.-[(2-nitro-1H-imidazol-1-yl)methyl]-aziridinylethanols and the corresponding aziridine-ring opened analogs are useful as radiation sensitizers for X-irradiation therapy of tumors.

Abstract: Compounds of formula (I): ##STR1## (wherein A is an alkylene group substituted by an optionally substituted amino or heterocyclic group and optionally interrupted by an oxygen or sulfur atom, R.sup.2 is various organic groups, B is C.sub.1 -C.sub.2 alkylene and Y is sulfur or methylene) and pharmaceutically acceptable salts and esters thereof are valuable hypotensive agents which may be prepared by a condensation reaction of the corresponding compound having an amino group in place of the group A--CH(COOH)--NH--.

Abstract: Compounds of formula I ##STR1## in which R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, a C.sub.1 to C.sub.3 alkyl group or R.sub.1 and R.sub.2 together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring; R.sub.3 and R.sub.4, which may be the same or different are hydrogen, a C.sub.1 to C.sub.3 alkyl or an optionally substituted C.sub.3 to C.sub.6 cycloalkyl group, or R.sub.3 and R.sub.4 together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring; m is 0, 1 or 2; p is 0, 1 or 2; E is an alkylene group connected to or interrupted by an oxygen or a sulphur atom; J is hydrogen or a substituent group; and their pharmaceutically acceptable salts have utility as histamine H.sub.2 -receptor antagonists.

Abstract: A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## or a pharmacologically acceptable acid addition salt is useful in therapy.

Abstract: This invention relates to substituted benzodiazinone-pyridone compounds and their use as cardiotonic agents including methods for increasing cardiac contractility, pharmaceutical compositions including the same and methods for the preparation thereof.

Abstract: This invention provides compositions comprising a physiologically-active agent and an azacycloalkene having at least one double bond in the ring and of the general formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a straight or branched chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3; and R is --CH.sub.3, ##STR2## wherein R" is H or halogen in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.

Abstract: Certain substituted 1,2,3,6-tetrahydro- and 1,2,5,6-tetrahydropyridine-3-carboxylic acids, esters, and amides possessing muscarinic binding activity, having utility for the treatment of the symptoms of senile cognitive decline disclosed. Pharmaceutical compositions and a pharmaceutical method of treatment are also disclosed.

Abstract: Compounds of formula (I): ##STR1## (wherein R.sup.1 and R.sup.3 are organic groups, A is a direct bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CO--CH.sub.2, --O--CH.sub.2 -- or --S--CH.sub.2 --, B is lower alkylene and n is 1-3) are valuable hypotensive agents which may be prepared by a condensation reaction of the corresponding compound having an amino group at the 3-position.

Abstract: The single stage process of reacting a lactam with an epihalohydrin in the presence of alkali metal hydroxide and between about 10.sup.-1 and about 10.sup.-4 molar concentration based on lactam of a phase transfer catalyst selected from the group of tetraalkyl ammonium hydrogen sulfate and tetraalkyl ammonium halide.

Abstract: Disclosed herein are 3,5-pyridinedicarboxylic acid derivatives having heteroatom substitution at the 4 position which are useful as herbicides and herbicide precursors.

Abstract: This invention relates to 5-oxypyrimidinone compounds having H.sub.2 -antagonist activity. A particular compound of the invention is 2-[3-(3-piperidinomethyl)phenoxy)propyl]-5-benzyloxypyrimidin-4-one.

Abstract: This invention relates to aminoalkylphenoxyalkyl substituted heterocycles. These compounds antagonize the action of histamine on histamine H.sub.2 -receptors in the brain. A compound of the invention is 2-[3-[3-(piperidinomethyl)phenoxy]propylamino]benzthiazole.

Abstract: The invention in its broad aspects relates to caprolactam derivatives which are useful as angiotensin converting enxyme inhibitors and as antihypertensives.

Abstract: Tetrahydropyridazinones of the formula I ##STR1## wherein R denotes an optionally substituted carbocyclic or heterocyclic radical, R.sup.1 denotes hydrogen; alkyl; aralkyl, which is optionally substituted in the aryl part; or acyl, and R.sup.2 denotes hydrogen; alkyl, which can optionally be substituted; or optionally substituted phenyl; and their acid addition compounds, if these can be prepared.The tetrahydropyridazinone derivatives of the formula I according to the invention and their physiologically acceptable salts exhibit useful pharmacological actions.

Abstract: Novel thioketene derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, an alkyl group, a lower alkenyl group, a phenyl group or a group of the formula: --B--Y;Y is a nitrogen-containing monocyclic heterocyclic group or a substituted or unsubstituted phenyl group;B is a straight or branched lower alkylene group;R.sup.2 and R.sup.3 are both a lower alkyl group or are combined together to form a group of the formula: --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;R.sup.4 is hydrogen atom, a lower alkyl group or a (lower alkoxy)carbonyl group;A is a group of the formula: --(CH.sub.2).sub.n -- or --CH(COOR.sup.5)--;n is an integer of 0, 1 or 2 andR.sup.5 is a lower alkyl group,are disclosed. The compound (I) is useful as an agent for treating and protecting various liver diseases.

Abstract: A novel process for the preparation of 4,5-dihydrodithieno[3,4-b:3',4'-e]azepine-5,9-dione is described.

Abstract: Compounds which are imidazo[1,2-a]pyridine derivatives of general formula (I) ##STR1## in which each of X.sub.1, X.sub.2, X.sub.3, independently of each other, is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, methoxy, methylthio, ethylthio, methylsulphonyl, nitro, amino, methylamino, dimethylamino, acetylamino or diacethylamino, Y is hydrogen, chlorine or methyl, R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or benzyl, R.sub.2 is C.sub.1 -C.sub.6 alkyl, cyclohexyl, trichloromethyl, 1-propenyl, allyl, phenyl, 4-chlorophenyl or benzyl, or R.sub.1 and R.sub.2 together represent a divalent C.sub.3 -C.sub.5 alipathic group and their pharmaceutically acceptable acid salts have anxiolytic, sleep-inducing, hypnotic, anticonvulsant, analgesic and anti-ulcer properties.

Abstract: 1-phenoxy-3-(4-phenylpiperazino)-2-propanol derivatives of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 is hydrogen, halo or lower alkyl; R.sup.2 is pyrrolidino, piperidino, morpholino or perhydroazepino unsubstituted or substituted by carbonyl at the alpha-position; R.sup.3 is hydrogen, lower alkyl or lower alkoxycarbonyl; and R.sup.4 is hydrogen, lower alkyl unsubstituted or alpha-substituted by lower alkoxy, lower alkoxy, halo or lower alkanoyl are useful for their alpha and beta-adrenergic blocking action and their hypotensive activity in humans and animals.

Abstract: N-Phenylsulfonyl-N'-triazinylureas of the general formula I ##STR1## and the salts of these compounds with amines, alkali metal bases or alkaline earth metal bases or with quaternary ammonium bases, have good selective herbicidal and growth regulating properties when applied pre- and postemergence. The symbols in formula I have the following meanings:R.sub.1 is hydrogen, halogen, nitro, cyano, or an alkyl, alkoxy, alkylthio, alkylsulfonyl, alkylcarbonyl, alkylcarbamoyl or alkoxycarbonyl group, each unsubstituted or substituted by halogen or alkoxy,R.sub.2 is hydrogen, halogen, alkyl, or an alkyl, alkoxy or alkylthio group, each unsubstituted or substituted by halogen or alkoxy,R.sub.3 is alkyl, haloalkyl, alkoxy or haloalkoxy,R.sub.4 is hydrogen, halogen, R.sub.3, alkylamino or dialkylamino,R.sub.

Abstract: The invention in its broad aspects relates to caprolactam derivatives which are useful as angiotensin converting enxyme inhibitors and as antihypertensives.