Abstract: The present invention relates to novel substituted quinolines and isoquinolines and derivatives thereof useful in the treatment of neurological disorders. Methods of preparing the compounds, intermediates useful in the preparation and pharmaceutical compositions containing the compounds are also included. The compounds are useful in treating pain, cerebral ischemia, and other cerebrovascular disorders.

Abstract: The present invention provides a cyclohexanediurea derivative, inclusive of its salt, represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and they each represent a straight-chain or branched alkyl group having at least 3 carbons, a cycloalkyl group, a cycloalkyl group having a bridge head, a furyl group, a furyl lower alkyl group or an aralkyl group, A.sub.1 and A.sub.2 are the same or different and they each represent a phenyl, pyridyl, quinolyl, isoquinolyl or indolyl group which may have substituents; a process for production thereof; an intermediate thereof; pharmaceutical use, a method for treatment and use thereof.

Abstract: The invention relates to heteroaroylguanidines of the formula I ##STR1## in which the substituents HA and R(1) to R(5) have the meanings given in the specification. These compounds exhibit very good antiarrhythmic properties and are outstandingly suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventative manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.

Abstract: Novel substituted pyrazolidinones have been found to exhibit significant binding to cholecystokinin (CCK) receptors and gastrin receptors in the brain and/or peripheral sites such as the pancreas, stomach, and ileum. The pyrazolidinones are CCK and gastrin receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders, central nervous system disorders and for appetite regulation in warm-blood vertebrates. Pharmaceutical formulations for such indications are described.

Abstract: Novel benzene derivatives are provided of the general formula (I): ##STR1## [wherein R.sup.1 represents an amino group, a substituted amino group, a protected amino group, or a nitro group; R.sup.2 represents an amino group, a substituted amino group, a protected amino group, a hydroxy group, a substituted hydroxy group, or a protected hydroxy group; R.sup.3 represents an amino group, a substituted amino, a heterocyclyl group having a ring nitrogen atom as the point of binding, or a substituted heterocyclyl group having a ring nitrogen atom as the point of binding; m is 0 to 2; n is 0 to 6; with the proviso that when m is 0, then n represents an integer from 2 to 6] and salts thereof.Compounds of formula (I) except those wherein R.sup.1 is a nitro group have activity in promoting production of nerve growth factor. Compounds of formula (I) wherein R.sup.1 is a nitro group are intermediates for compounds of formula (I) wherein R.sup.1 is an amino group.

Abstract: The invention relates to 6-membered nitrogen-containing heteroaryloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.

Abstract: Polyalkylpiperidine-containing acetic acid and 3-aminoacrylic acid derivatives I ##STR1## where R.sup.1 is hydrogen, C.sub.1 - to C.sub.6 -alkyl, formyl, C.sub.2 - to C.sub.6 -alkanoyl, C.sub.1 - to C.sub.12 -alkoxy, C.sub.5 - to C.sub.6 -cycloalkoxy, cyanomethyl, hydroxymethyl, 2-hydroxyethyl or a radical of the formula --CR.sup.3 =CH--CO--OR.sup.4, whereR.sup.3 is hydrogen, C.sub.1 -to C.sub.6 -alkyl or a radical of the formula --CO--OR.sup.4 andR.sup.4 is C.sub.1 - to C.sub.20 -alkyl, C.sub.5 - to C.sub.8 -cycloalkyl, C.sub.7 - to C.sub.18 -aralkyl, phenyl, tolyl or a radical of the formula --(CH.sub.2 CH.sub.2 O).sub.n H or --[CH(CH.sub.3)CH.sub.2 O].sub.n H, where n is a number from 1 to 30,X is O, NH or NR.sup.6, whereR.sup.6 is C.sub.1 - to C.sub.12 -alkyl, andY is hydrogen or a group of the formula =CH--NHR.sup.7 or =CH--NR.sup.6 R.sup.7, whereR.sup.7 is phenyl which can be substituted by one to three C.sub.1 - to C.sub.12 -alkyl, C.sub.1 - to C.sub.

Abstract: Combatting fungi and bacteria with quinoline derivatives of the formula ##STR1## in which X is a nitrogen atom and Y is a CH-group orY is a nitrogen atom and X is a CH-group,R is hydrogen, halogen, acetyl or alkyl which is optionally substituted by one to three radicals independently selected from the group consisting of alkoxy, phenyl, hydroxy, halogen and cyano, orR is alkenyl which is optionally substituted by one to three radicals independently selected from the group consisting of halogen, cyano, alkoxy, phenyl and hydroxy, orR is alkynyl which is optionally substituted by one to three radicals independently selected from the group consisting of halogen, phenyl, trimethylsilyl, hydroxy, cyano, alkoxy, alkylamino, dialkylamino, alkylcarbonyl, tolyl, alkoxycarbonyl and alkylcarbonyloxy, orR is cycloalkyl which is optionally substituted by one to three radicals independently selected from the group consisting of halogen and cyano,A is hydrogen or halogen andB is halogen or halogenoalkyl,or an acid addition

Abstract: The present invention is directed to a new class of 4-sulfanimide-quinoline derivatives and to their use as NMDA antagonists.

Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Abstract: Thiophenyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, isoxazolyl-thiophenyl-sulfonamides, isoxazolyl-furyl-sulfonamides and isoxazolyl-pyrrolyl-sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Abstract: The present invention is concerned with antiretroviral (e.g. anti-HIV-1)compounds having the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are halo or methyl; R.sup.3 is hydrogen, halo, nitro or trifiuoromethyl; R.sup.4 is trifiuoromethyl or methylcarbonyl; or a radical --C(.dbd.X)--NR.sup.5 R.sup.6 wherein X is O or S, and R.sup.5 and R.sup.6 each independently are hydrogen or C.sub.1-4 alkyl; or a radical -Alk-R.sup.7, wherein Alk is C.sub.1-4 alkanediyl; and R.sup.7 is hydrogen or hydroxy; Het is a heterocyclic radical of formula: ##STR2## Pharmaceutical compositions containing said compounds of formula (I) and processes of preparing said compounds and compositions.

Abstract: Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided. The sulfonamides have formula I: ##STR1## in which Ar.sup.1 is a 3- or 5-isoxazolyl and Ar.sup.2 is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar.sup.2 is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar.sup.

Abstract: Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.

Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.

Abstract: The invention discloses compounds of the formula ##STR1## wherein, Het.sub.1 is chosen from the group consisting of substituted or unsubstituted furyl, oxazolyl, isoxazolyl, oxadiazolyl, tetrazolyl, thiadiazolylY is an alkylene bridge of 3 to 9 carbon atoms.Het.sub.2 is quinolyl quinolyl substituted by R.sub.1 and R.sub.2 ;R.sub.1 and R.sub.2 are each individually chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.

Abstract: N-(4-halo-isoxazolyl)sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(4-halo-3-isoxazolyl)sulfonamides and N-(4-halo-5-isoxazolyl)benzenesulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.

Abstract: The present invention relates to a compounds represented by the following formula or salts thereof. ##STR1## The above compounds have strong angiotensin II antagonistic action, antihypertensive action and action on central nervous system, which are useful for the treatment of circulatory diseases such as hypertension, heart diseases, cerebral apoplexy, nephritis, atherosclerosis or Alzheimer's disease and senile dementia, and for agents of improving cerebral function.

Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties. Therapeutic compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the formula ##STR1## wherein R.sub.4, X, R, Y, R', Q, m and n are herein defined, and pharmaceutically acceptable salts thereof.

Abstract: N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Abstract: Amide tetrazoles of the formula ##STR1## wherein aryl includes phenyl and naphthyl, unsubstituted or substituted, X is .dbd.O, .dbd.N--R.sub.5, or --NR.sub.3 R.sub.4, where R.sub.2, R.sub.4, and R.sub.5 include alkyl and alkoxy and R.sub.3 includes alkyl, are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia or atherosclerosis.

Abstract: Derivatives of 4-anilinoquinoline having the formula: ##STR1## where X is O or H.sub.2 and Z is 1-substituted-4-piperidinylamino or diloweralkylaminoloweralkyl inhibit binding of tritiated bradykinin to guinea pig ileum and inhibit bradykinin-induced writhing in mice. Bradykinin is a nonapeptide formed in plasma as a result of inflammation or injury and produces pain when it binds with pain receptors. A drug which inhibits the binding of bradykinin therefore has analgetic properties.

Abstract: An aromatic amino-substituted compound represented by formula: ##STR1## wherein A represents CH, N, or N.fwdarw.O; R.sub.1 represents a nitro group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, or an acyl group; and R.sub.3 represents a group: ##STR2## wherein m represents 0 or 1; n represents an integer of from 0 to 3; R.sub.4 and R.sub.5 each represents a hydrogen atom or a lower alkyl group; R.sub.6 and R.sub.7 each represents a hydrogen atom or a straight chain or branched lower alkyl group; R.sub.4 and R.sub.6 may be joined together to form an alkylene chain forming a heterocyclic ring; R.sub.5 and R.sub.7 may be joined together to form an alkylene chain forming a heterocyclic ring and R.sub.6 and R.sub.

Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.

Abstract: Compounds of formula ##STR1## wherein; R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 X where X is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro;Z is NR.sub.5 or CR.sub.6 R.sub.7 ;R.sub.5 is hydrogen, aryl, arylthio, arylsulfonyl, lower-alkyl, cycloalkyl, heterocycloalkyl, amino-lower-alkyl, lower-alkylamino-lower-alkyl, dilower-alkylamino-lower-alkyl, lower-alkoxy, hydroxy or NR.sub.8 R.sub.9 ;R.sub.6 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro or lower-alkylsulfonyl;R.sub.7 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro, aryl, or lower-alkylsulfonyl;R.sub.8 is hydrogen, lower-alkyl, aryl, heterocycloalkyl, carbamyl, alkanoyl, aroyl, hydroxy-lower-alkyl; andR.sub.9 is hydrogen, lower-alkyl or lower-alkanoyl or pharmaceutically acceptable acid addition salts thereof are useful as anticancer agents.

Abstract: Pyridone transfer dyes have the formula ##STR1## where Q.sup.1 is hydrogen, fluorine, chlorine, methyl or a substituted amino radical,Q.sup.2 is hydrogen, fluorine or chlorine or Q.sup.1 and Q.sup.2 together with the carbon atoms to which they are attached form an aromatic carbocyclic or heterocyclic ring,x is a heterocyclic radical, a carboxylic or carboxamide radical or substituted amino radical andK is an aromatic radical.

Abstract: The compounds of the formula: ##STR1## wherein the substituents are herein below defined; are plant fungicides, insecticides, and miticides.

Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.

Abstract: The compounds of the formula: ##STR1## where the substituents are herein below defined, are fungicides, insecticides, and miticides.

Abstract: Phenyl substituted 2-thiazolyl tetrazolium salt compounds characterized by a reflectance spectrum exhibiting an extended plateau above about 600-650 nm. Such compounds are useful as chromogenic indicators for reducing substances such as NADH. The reflectance plateau confers improved accuracy to analytical assays, particularly for the determination of analytes of medical diagnostic significance, in which a colorimetric response on a reagent carrier matrix is measured by reflectance.

Abstract: (1H-azol-1-ylmethyl)substituted quinoline derivatives, compositions containing the same, and methods of treating mammals suffering from disorders which are characterized by an increased proliferation and/or abnormal differentiation of epithelial tissues.

Abstract: Quinoline derivatives of the formula: ##STR1## , wherein R is hydrogen, alkyl or aralkyl; m and n are 0 or 1, and each of rings A, B and C can have substituents, which are useful as inhibitors for acyl-CoA:Cholesterolacyltransferase.

Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.

Abstract: Compounds and compositions containing alkylphosphonothioates, for insecticidal control, particularly for use as soil and/or foliar insecticides, having the formula. ##STR1## in which R is C.sub.1 -C.sub.3 alkyl;R.sub.1 is C.sub.4 -C.sub.6 branched alkyl;R.sub.2 is hydrogen, methyl, ethyl, cyano or C.sub.2 -C.sub.4 alkynyl; ##STR2## R.sub.4 is halo, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 thioalkyl or mono-or di-C.sub.1 -C.sub.2 alkylamino;n is 1-3; andX is O or S.

Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.

Abstract: (Quinolin-2-ylmethoxy)Heterotetrahydrocarbazoles as inhibitors of the biosynthesis of leukotrienes useful in the treatment of asthma and eye inflamation.

Abstract: There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl or --(CH.sub.2).sub.m R.sub.7 wherein m is 1, 2 or 3 and R.sub.7 is cyano or amino; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl, or R.sub.5 +R.sub.6 taken together with the carbon atom to which they are attached constitute a cyclobutane, cyclopentane, cyclohexane, cycloheptane, pyrrolidine, piperidine, morpholine or thiomorpholine ring, or R.sub.5 is hydrogen and R.sub.6 is aryl or --CH.sub.2 OR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or loweralkylcarbonyl, which are useful for enhancing memory.

Abstract: Compounds of the formula (1) ##STR1## the substituents are described in the specification. The compouns of formula (I) are plant fungicides.

Abstract: Substituted 4-aminoquinazoline derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy C.sub.1-6 alkyl,C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl C.sub.1-6 alkyl, phenyl C.sub.1-6 alkyl, the phenyl group being optionally substituted;R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, C.sub.1-6 alkanoyl or trifuromethyl;m is 1 to 3;R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkanoyl, amino, C.sub.1-6 alkylamino, ci-C.sub.1-6 alkylamino, halogen, trifluoromethyl or cyano;n is 1 or 2; andR.sup.4 is hydrogen; or a salt thereof are useful as inhibitors of gastric acid secretion.

Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.

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 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: The invention relates to the compounds of the formula ##STR1## wherein each R independently represents hydrogen, lower alkyl, halogen, trifluoromethyl, lower alkoxy, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryloxy, carbocyclic or heterocyclic aryl-lower alkyloxy, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyloxy, or C.sub.3 -C.sub.7 -cycloalkyloxy; n represents 1, 2, 3 or 4; m represents 0, 1 or 2; A represents a direct bond or lower alkylene; X represents oxygen or sulfur; R.sub.1 represents hydrogen, acyl, lower alkoxycarbonyl, aminocarbonyl, mono- or di-lower alkylaminocarbonyl, lower alkenylaminocarbonyl, lower alkynylaminocarbonyl, carbocyclic or heterocyclic aryl-lower alkylaminocarbonyl, carbocyclic or heterocyclic arylaminocarbonyl, C.sub.3 -C.sub.7 -cycloalkylaminocarbonyl or C.sub.3 -C.sub.7 -cycloalkyl-lower alkylaminocarbonyl; R.sub.2 represents lower alkyl, lower alkoxycarbonyl-lower alkyl, C.sub.3 -C.sub.

Abstract: This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compound, a process for the preparation thereof and an anti-ulcer agent containing the same.

Abstract: A fungicidal method which comprises applying to the locus of a plant pathogen a fungicidally effective but non-phytotoxic amount of a compound of the formula (1) ##STR1## wherein: R.sup.1 to R.sup.4 are independentlyH, halo, (C.sub.1 -C.sub.4) alkyl, branched (C.sub.3 -C.sub.4) alkyl, halo (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, NO.sub.2, or HN.sub.2, at least two of R.sup.1 to R.sup.4 being H,or one of R.sup.2 to R.sup.4 is --NR.sup.7 --Y--Ar or O--Y--Ar and the rest of R.sup.1 to R.sup.4 are H;W is N, or CR.sup.5 ;R.sup.5 is H, CH.sub.3, Cl, O--Y--Ar, or --NR.sup.7 --Y--Ar;R.sup.6 is H, CH.sub.3, Cl, or Br;A is --O--Alk or --X--Y--Ar;Alk is a C.sub.2 -C.sub.18 saturated or unsaturated hydrocarbon chain, straight chain or branched, optionally substituted with halo, halo (C.sub.1 -C.sub.4) alkoxy, (C.sub.3 -C.sub.8) cycloalkyl, hydroxy, or acetyl;X is O, NR.sup.7, or CR.sup.8 R.sup.9, provided that if one of R.sup.2 to R.sup.5 is NR.sup.

Abstract: The invention relates to a quinoline of the formula: ##STR1## wherein each of R.sup.1 and R.sup.2, which may be the same or different, is hydrogen, halogeno, hydroxy, cyano, carbamoyl, nitro or amino, alkyl, alkoxy, alkylthio, alkylamino, dialkylamino or alkanoylamino each of up to 4 carbon atoms, or substituted alkyl or alkoxy each of up to 3 carbon atoms, provided that both R.sup.1 and R.sup.2 are not hydrogen; the quinoline ring may bear further substituents; R.sup.3 is hydrogen or alkyl of up to 4 carbon atoms; R.sup.4 is hydrogen, alkyl, alkenyl or alkynyl each of up to 4 carbon atoms or substituted alkyl of up to 3 carbon atoms; Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or which bears one or more substituents; R.sup.5 is such that R.sup.5 --NH.sub.2 is an amino acid; or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumor activity.

Abstract: The invention relates to new triazolyl quinoline derivatives and acid addition salts thereof whereinR.sup.1 stands for hydrogen, methyl, trihalogenomethyl or carboxy;R.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, phenoxy, amino, acetamino, C.sub.1-4 dialkylamino, acetyl, benzoyl, methylthio, carboxy, cyano, ethoxycarbonyl, nitro or trihalogenomethyl;R.sup.3 represents hydrogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;R.sup.4 stands for hydrogen, methyl or ethyl andX stands for a valency bond or --S--.The new compounds of the general Formula (I) ##STR1## possess valuable analgesic, antiphlogistic and fungicidal effect and can be used both in therapy and agriculture.

Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.

Abstract: A novel prolinal derivatives of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms,R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.