Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: Compounds of the formula: ##STR1## which is further defined herein, possess anti-tumor activity.

Abstract: A class of compounds having the structural formula ##STR1## in which R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl or substituted phenyl; N, R.sup.1 and R.sup.2 form a monocyclic or bicyclic nitrogen heterocycle which is at least partially saturated and which may contain oxygen or sulfur or be substituted with lower alkyl; and physiologically acceptable salts thereof is disclosed.A process for forming the thiophene substituted cycloamines of the subject invention is described. A composition comprising the compound of the subject invention and a suitable carrier therefor is taught.A method of controlling phytopathogenetic fungi is disclosed. In this method a fungicidally effective amount of the compound of the present invention is applied to the locus to be protected.

Abstract: A process for the preparation of a substituted acetic acid of the Formula (2): ##STR1## wherein --X--Z is an optionally substituted aromatic or heteroaromatic optionally substituted amino radical; by reacting a compound of the Formula (7):Z--Y--H Formula 7with glyoxylic acid. The compounds of Formula (2) are useful as intermediates in the preparation of polycyclic dyes.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl terahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiphenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: The present invention relates to compounds having anti-ischaemic activity of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and Z are as defined herein. The present invention further relates to a method of preparing such compounds, as well as compositions having anti-ischaemic activity which comprise such compounds and a method of treating ischaemia.

Abstract: 3-Thio or amino substituted benzo[b]thiophene-2-carboxamides and 3-oxygen, thio, or amino substituted benzofuran-2-carboxamides are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases. Certain of these compounds are novel and methods of manufacture are also described.The same benzo[b]thiophene and benzofuran-2-carboxamides also inhibit the activation of human immunodeficiency virus (HIV), latent in infected mammals.

Abstract: Disclosed are benzothiophene and thienothiophene derivatives useful for inhibiting urokinase activity.

Abstract: Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.

Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).

Abstract: The present invention provides novel carbonic anhyrase inhibitors represented by the structural formula: ##STR1## wherein R.sub.1 and R.sub.2 are, for example, independently (a) hydrogen; or(b) OR.sub.4, wherein R.sub.4 is hydrogen or C.sub.1-7 alkyl; or(c) NR.sub.5 R.sub.6, wherein R.sub.5 and R.sub.6 are independently hydrogen, or C.sub.1-7 alkyl, or C.sub.1-7 alkyl substituted with one or more halogen or OR.sub.4 ; or(d) --COR.sub.7, wherein R.sub.7 is hydrogen, C.sub.1-7 alkyl, or NR.sub.5 R.sub.6 ; or(e) --SR.sub.8, wherein R.sub.8 is hydrogen or C.sub.1-7 alkyl, or C.sub.1-7 alkyl substituted with one or more halogen, or OR.sub.4 ; or(f) C.sub.1-7 alkyl, or C.sub.1-7 alkyl substituted with one or more halogen, or OR.sub.4 or NR.sub.5 R.sub.6 ; or(g) R.sub.1 and R.sub.2 are together(i) .dbd.O, or(ii) .dbd.NOR.sub.8 or(iii) .dbd.S;and R.sub.3 is(h) C.sub.1-7 alkyl or C.sub.1-7 substituted with one or more halogen, OR.sub.4 or NR.sub.5 R.sub.6.

Abstract: The compounds of the invention having the formula: ##STR1## in which: A, which is a ring condensed with cyclopentane, represents a substituted or unsubstituted thiophene ring, Q represents an alkylene chain, R.sub.1 and R.sub.2 each represent H or an alkyl, or they form, with the nitrogen atom to which they are linked, a saturated nitrogenous heterocyclic ring containing 5 to 7 atoms, R.sub.3 and R.sub.4 each represent H, alkyl, cycloalkyl, trifluoromethyl or an optionally substituted phenyl, thienyl or furyl group or R.sub.3 and R.sub.4 together form a (C.sub.5 -C.sub.8) cycloalkyl, as well as their addition salts with an acid and their quaternary ammonium derivatives.They can be used as medicines.

Abstract: There is disclosed a benzocycloheptene compound of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, a halogen atom or a lower alkoxy group, R.sup.2 and R.sup.3 are independently selected from hydrogen atom, a lower alkyl group and a lower alkenyl group, or R.sup.2 and R.sup.3 combine together with adjacent nitrogen atom to form a heteromonocyclic group, or a pharmaceutically acceptable salt thereof, which has an excellent inhibitory activity against contraction of urinary bladder.

Abstract: New compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.6 have the meanings given in the description, their preparation and use in plant protection, the protection of materials and in the field of human and veterinary medicine.Formula (I) gives a definition of the compounds which can be prepared by analogous processes, for example from suitable benzothiophene derivatives by oxidation.

Abstract: A taxane derivative of the formula ##STR1## wherein ##STR2## Z is --OT.sub.1, T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2,T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl or monocylic aryl,R.sub.3 is benzoyl, substituted benzoyl or C.sub.1 -C.sub.6 alkoxycarbonyl,Ac is acetyl, andE.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.

Abstract: A process is provided whereby organic carbonyl substrates, including esters, lactones, ketones, amides and imides are reduced in a reaction with a silane reducing reagent and a catalyst. Exemplary catalysts include metal alkoxides and metal aryloxides.

Abstract: Provided is a method of treating inflammatory bowel disease in mammals utilizing certain benzyl-substituted rhodanine derivatives. Also provided are novel benzyl-substituted rhodanine derivatives and pharmaceutical compositions thereof, as well as a novel process for selectively isolating in substantially pure enantiomeric form the enantiomers of certain racemic benzyl-substituted rhodanine derivatives.

Abstract: Compounds of formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or methyl, A is an ethylene or methylene radical which is unsubstituted or substituted by methyl, hydroxyl or oxo,L is a saturated or unsaturated five-membered or six-membered heterocyclic structure which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.6 -alkyl, or C.sub.1 -C.sub.4 -alkanoyl and has from 1 to 3 heteroatoms from the group consisting of N, O and S, the second and third heteroatoms being a nitrogen atom,R.sup.3 is hydrogen, a hydroxy or C.sub.1 -C.sub.6 -alkoxy group,R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen or methoxy,R.sup.5 is hydrogen or methoxy or tert-butyl,R.sup.6 is hydrogen methyl, nitrile or a C.sub.2 -C.sub.10 -ketal group or the radical --CHR.sup.7 OR.sup.8 --CHR.sup.7 --NR.sup.9 R.sup.10, --COR.sup.11, --SR.sup.12, ##STR2## in which R.sup.7 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.8 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.

Abstract: The invention provides furanone derivatives of the general formula ##STR1## in which R.sup.1 represents a halogen atom or an optionally substituted alkyl or alkoxy group, R.sup.2 represents a halogen atom or an optionally substituted alkyl, aryl or heterocyclyl group, R.sup.7 represents a C.sub.1-4 alkyl group and Q represents an optionally substituted morpholino or amino group; processes for their preparation; compositions containing such compounds and their use as fungicides.

Abstract: The present invention provides compounds having the structureY-Het-[Q.sub.1 ]-X-[Q.sub.2 ]-Zwhich inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4.In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl.Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR.The group Q.sub.

Abstract: New thiophene compounds of the formula: ##STR1## in which: X represents hydrogen, halogen, C.sub.1 -C.sub.5 alkyl or alkoxy or dialkylamino;n represents 1 or 2;a represents an integer of from 2 to 6;b represents 2 or 3;c represents 1 or 2, and is such that b+c=4;R.sub.1 and R.sub.2 represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the carbon atom to which they are bonded form a hydrocarbon ring containing from 3 to 6 carbon atoms; andR and R' represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the nitrogen atom to which they are bonded form a pentagonal or hexagonal heterocycle optionally containing an oxygen atom or a second nitrogen atom which may itself be substituted; and their physiologically tolerable salts.The products of the invention can be used therapeutically especially in the treatment of pathologies that are characterized by a loss of bone tissue.

Abstract: The invention relates to new propenone oxime ethers, a method of preparing them and pharmaceutical compositions containing them.Said new propenone oxime ethers have the formula ##STR1## in which--Ar and Ar' each independentlyl denotes a phenyl group non-substituted, mono or polysubstituted, a 9-anthryl group or a naphthyl group, a pyridyl, thienyl or furyl group;R.sub.1 R.sub.2 each independently denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or together with the N-atom to which they are bonded a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl group;M=H, Cl, Br or a C.sub.1 -C.sub.6 alkyl groupn=2 or 3.The invention also deals with the salts of compounds of formula (I). Said compounds have good activity in the anti platelet-clotting tests and are also antagonists of the 5HT.sub.2 receptors.

Abstract: Process for the preparation of thiophene derivatives and also new dihydrothiophene 1-oxides.Thiophene derivatives having an--optionally substituted--amino group on the thiophene ring are prepared by dehydrogenating dihydrothiophenes, substituted in a manner identical to that of the desired thiophene derivatives, by means of H.sub.2 O.sub.2, the dihydrothiophenes being reacted with H.sub.2 O.sub.2 in a first reaction stage in a neutral medium to give the corresponding sulfoxides, which are then rearranged into the thiophene derivatives by means of acid in the second reaction stage.The dihydrothiophene 1-oxides formed as intermediates in this reaction are new compounds. Like the thiophene derivatives formed from them by rearrangement with acid, they are intermediates, mainly in the sector of plant protection agents and pharmaceuticals.

Abstract: The present invention relates to the treatment of diseases caused by invading organisms in a host by first identifying an enzymatic difference between the host and the invading organism and then administering to the host a pharmaceutically effective amount of a subversive substrate for the differing enzyme of the invading organism, whereby the action of the differing enzyme causes a result counter to the intended result and function of the enzyme that results in its debilitation or death. In particular, treatment of parasitic diseases caused by kinetoplastids including trypanosomes and leishmanias, e.g., African sleeping sickness, Chagas' disease, oriental sore and kala-azar is accomplished by administration of a pharmaceutically effective antiparasitic amount of a competitive toxigenic substrate for trypanothione reductase. Methods of treatment and compositions therefor contain a competitive toxigenic substrate for trypanothione reductase. Numerous compounds and corresponding compositions are disclosed.

Abstract: Carbonic anhydrase inhibitors of the thieno[2,3-b]thiopyran-2-sulfonamide type with a substituted-alkyl-amino group in the 4-position are topically effective in lowering intraocular pressure.

Abstract: Renin inhibiting compounds containing a single .alpha.-amino acid of the formula: ##STR1## and analogs thereof which inhibit the substrate-cleaving acting or renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.

Abstract: Diaminothiophenes of the formula ##STR1## or tautomers thereof, where R.sup.1 and R.sup.2 are each hydrogen or together are ##STR2## where T.sup.1 is hydrogen, alkyl or phenyl, T.sup.2 and T.sup.3 are, independently of one another, alkyl or phenyl, or T.sup.2 and T.sup.3 together with the nitrogen linking them are a heterocyclic radical,R.sup.3 is substituted amino andR.sup.4 is alkanoyl, benzoyl, cyano, nitro or ##STR3## where T.sup.4 is hydrogen, alkyl or phenyl and T.sup.5 is the radical of a primary amine or of an active methylene compound,are prepared as described. The present diaminothiophene compound is useful in the synthesis of dyes, crop protection agents and pharmaceuticals.

Abstract: 1. New thiophene compounds of the formula: ##STR1## in which: X represents hydrogen, halogen, C.sub.1 -C.sub.5 alkyl or alkoxy or dialkylamino;n represents 1 or 2;a represents an integer of from 2 to 6;b represents 2 or 3;c represents 1 or 2, and is such that b+c=4;R.sub.1 and R.sub.2 represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the carbon atom to which they are bonded form a hydrocarbon ring containing from 3 to 6 carbon atoms; andR and R' represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the nitrogen atom to which they are bonded form a pentagonal or hexagonal heterocycle optionally containing an oxygen atom or a second nitrogen atom which may itself be substituted; and their physiologically tolerable salts.The products of the invention can be used therapeutically especially in the treatment of pathologies that are characterized by a loss of bone tissue.2.

Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.

Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.

Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.

Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.

Abstract: A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms possible of compounds of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, one of A and B being ##STR2## and the other being ##STR3## R is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2).sub.n -- or branched alkylene of 2 to 8 carbon atoms, n is an integer from 0 to 5, Y is selected from the group consisting of naphthyl, indenyl, heterobicyclics and heteromonocyclic containing 5 to 6 ring members, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.

Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.

Abstract: The invention relates to new compounds corresponding to formula I: ##STR1## in which: W represents C=O, CH.sub.2 or CHOH,Z represents ##STR2## R.sub.1 and R.sub.2 represent especially Cl or F, R, R' and R" represent especially H,X represents especially CH.sub.2,Y represents especially COOH,u and v are two integers ranging from 0 to 10,p and q take the value 0 or 1,n and m are two integers ranging 0 to 10 andt is 0 or 1the total number of carbon atoms in the chain ##STR3## ranging from 2 to 20, and to their physiologically acceptable salts obtained with organic or inorganic acids.These compounds are useful for preparing medicinal products which have, especially, anti-inflammatory properties.

Abstract: Fungicidal substituted 2-phenyl-2,2-difluoroethylthiolcarbonates of the formula ##STR1## in which R.sup.1 represents hydrogen, alkoxycarbonyl, alkoxyalkoxycarbonyl, alkylthioalkoxycarbonyl, halogenoalkoxycarbonyl, cyanoalkoxycarbonyl, alkenoxycarbonyl, alkynoxycarbonyl and cycloalkyloxycarbonyl, or represents cycloalkylalkoxycarbonyl,R.sup.2 represents hydrogen or alkyl, or represents phenyl, orR.sup.1 and R.sup.2 together represent the butadiene-1,4-diyl radical,R.sup.3 represents alkoxy, alkoxyalkoxy, alkylthioalkoxy, fluoroalkoxy, cyanoalkoxy, alkenoxy, alkynoxy, cycloalkyloxy and cycloalkylalkoxy, or represents the group ##STR2## in which R.sup.4 represents alkyl, alkoxyalkyl, alkylthioalkyl, cyanoalkyl, fluoroalkyl, alkenyl, alkinyl or cycloalkyl,R.sup.5 represents hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl, orR.sup.4 and R.sup.

Abstract: Novel fungicidally active acyloxythiophene-carboxamides of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl,R.sup.2 represents alkyl or optionally substituted phenyl,R.sup.

Abstract: The invention relates to pyridazinone compounds of the general formula I: ##STR1## wherein R.sup.1 represents one to four substituents, which may be the same or different and are selected from H, OH, halogen, NO.sub.2, unsubstituted or C1-C4 alkyl substituted amino, C1-C4 alkyl, C1-C4 halogen substituted alkyl, O--ALK--NR.sup.4 R.sup.5, C1-C4 alkoxy, whereby two substituents taken together may also represent a methylenedioxy group;R.sup.2 and R.sup.3 represent independently H or C1-C4 alkyl;R.sup.4 and R.sup.5 represent independently H or C1-C4 alkyl, or form together with the nitrogen a 5- or 6- membered ring;X represents S or O;the dotted line represents an optional bond;and their pharmaceutically acceptable salts.

Abstract: The present invention relates to the treatment of diseases caused by invading organisms in a host by first identifying an enzymatic difference between the host and the invading organism and then administering to the host a pharmaceutically effective amount of a subversive substrate for the differing enzyme of the invading organism, whereby the action of the differing enzyme causes a result counter to the intended result and function of the enzyme that results in its debilitation or death. In particular, treatment of parasitic diseases caused by kinetoplastids including trypanosomes and leishmanias, e.g., African sleeping sickness, Chagas' disease, oriental sore and kala-azar is accomplished by administration of a pharmaceutically effective antiparasitic amount of a competitive toxigenic substrate for trypanothione reductase. Methods of treatment and compositions therefor contain a competitive toxigenic substrate for trypanothione reductase. Numerous compounds and corresponding compositions are disclosed.

Abstract: Benzo-fused cycloalkane and oxa- and thia-cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benezeneacetamide, and the pharmaceutically acceptable salts or N-oxides thereof, are useful as analgesics and/or diuretics.

Abstract: The invention relates to compounds of the formula ##STR1## These compounds may be used in therapeutics for the treatment of acne, psoriasis, disorders of keratinization, in certain forms of cancer and as healing agents, particularly in the ocular field.

Abstract: A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represent a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration.This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.

Abstract: Compounds are described of the formula ##STR1## where: R.sup.1 is --H or --CH.sub.3,n is 1, m is 2-4 and X is --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --;Y is a saturated heterocyclic amino group,R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thineylalkyl or naphthylalkyl or (ii) cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction and may be formualted for use as antithrombotic or antiasthmatic agents.

Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.

Abstract: Compounds of the formula: ##STR1## wherein R is hydrogen, alkoxycarbonyl, benzyloxycarbonyl, heteroarylalkyl, phenylalkenyl, or --T--(Y).sub.p --R.sub.6 (wherein T is single bond or alkylene, Y is oxygen, sulfur or carbonyl, R.sub.6 is phenyl, substituted phenyl, naphthyl, or diphenylmethyl, and p is 0 or 1, provided that when T is single bond, p is 0); R.sub.1 is halogen, hydroxy, alkoxy, cycloalkyloxy, alkenyloxy, alkynyloxy, alkoxy interrupted by oxygen or carbonyl, alkylthio, amino, monosubstituted amino, or a substituted alkoxy; R.sub.2 is hydrogen; R.sub.3 is hydrogen, halogen, amino, alkylamino, dialkylamino, alkanoylamino, or nitro; R.sub.4 is hydrogen, halogen, nitro, sulfamoyl, alkylsulfamoyl, or dialkylsulfamoyl; or any two adjacent groups of the R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may combine to form alkylenedioxy, and the remaining two groups are each hydrogen; R.sub.5 is hydrogen or alkyl; X is alkylene; m and n are each 1 or 2; provided that at least one of the groups R.sub.2, R.sub.3 and R.

Abstract: Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## group, R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.

Abstract: Benzofuran derivatives of the general formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen, alkyl or phenylalkyl, where alkyl in each case is of 1 to 4 carbon atoms, R.sup.3 and R.sup.4 are identical or different and are each hydrogen or C.sub.1 -C.sub.4 -alkyl or together form a 3-membered to 5-membered chain which may be interrupted by an oxygen atom or an NR.sup.1 group, X is --CO--CH.dbd.CH--, --CO--CH.sub.2 --CH.sub.2 --or --CHOH--CH.sub.2 --CH.sub.2 --, n is 2 or 3 and Het is an aromatic 5-membered or 6-membered ring which contains a hetero atom from the group consisting of N, O and S and may additionally contain a (further) N atom, in which the ring may be substituted by C.sub.1 -C.sub.4 -alkyl, fluorine, chlorine, bromine, NH.sub.2 or NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 have the abovementioned meanings, the use of these benzofuran derivatives for the preparation of pharmaceutical, in particular antiulcerogenic, agents, and these agents themselves are described.

Abstract: Benzoin esters of aromatic sulfonic acids can be obtained in high yield from benzoin and the respective sulfonyl halide in molar amounts of a base by carrying out the reaction at low temperature in an organic solvent with the addition of water. Aqueous NaOh or KOH can be used as base in this process.

Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.