Abstract: Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: Compounds of structure (I) in which R is C.sub.1-8 alkyl(phenyl)p, C.sub.2-8 alkenyl(phenyl)p, C.sub.2-8 alkenyl(phenyl)p, C.sub.3-8 cycloalkyl or C.sub.1-8 alkylC.sub.3-8 cycloalkyl; p is 0 to 2; n is 0 to 6; A is a bond, oxygen, sulphur or NR.sup.1 ; R.sup.1 is hydrogen, C.sub.1-8 alkylphenylC.sub.1-4 alkyl; m is 0 to 3; and Ar is aryl or heteroaryl, each of which may be optionally substituted, and salts thereof processes for preparing said compounds, pharmaceutical compositions containing them and their use in therapy, in particular as calcium blocking agents.

Abstract: A compound of formula XXII ##STR1## wherein Ar', Q' and Q" are as defined in the specification are useful intermediates for making neurokinin receptor active compounds.

Abstract: The invention relates to triphenylalkyl antibacterial compounds of the general formula: ##STR1## pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are thus useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.

Abstract: The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: ##STR1## wherein: R represents an alkyl or alkynyl group having 1-4 carbon atoms, or a phenyl group optionally substituted by C.sub.1-4 alkyl, alkylthio, alkoxy, halogen, nitro, acylamino, methylsulfonyl or methylenedioxy, or represents tetrahydronaphthyl,R.sup.1 represents hydrogen, trifluoro (C.sub.1-4) alkyl, alkyl or alkynyl,X represents hydrogen, alkyl having 1-4 carbon atoms, alkoxy, trifluoroalkyl, hydroxy, halogen, methylthio or aralkoxy,R.sup.2 represents:a C1-C10 alkyl group,a phenyl group optionally substituted by one or more of the following groups:a C1-C10 alkyl group,a halogen group,a nitro group,hydroxy group,and/or an alkoxy group.

Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.

Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.

Abstract: The invention relates to substituted nitrogenous heterocycles derivatives of general formula (I) ##STR1## in the racemic or optically pure form and/or in the form of cis/trans isomers, their pharmaceutically acceptable salts, and their use for preparing drugs having psychrotropic activity, especially antidepressant activity.

Abstract: Fibrinogen receptor antagonists of the general formula:X-A-Y-Z-B Iand which includes, for example, the compounds of formula ##STR1## are useful for inhibiting the binding of fibrinogen to blood platelets, inhibiting the aggregation of blood platelets, treating thrombus formation or embolus formation, and preventing thrombus or embolus formation.

Abstract: The present invention is directed to certain compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, A.sup.1, A.sup.2, X, m and n are defined herein. The compounds of this invention are tachykinin receptor antagonists and are of particular use in the treatment of pain, inflammation, migraine and emesis.

Abstract: The present invention relates to a process for preparation of substantially pure piperidine derivative compounds of the formulae: ##STR1## wherein R.sub.1 is hydrogen or hydroxy;R.sub.2 is hydrogen;or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;R.sub.3 is --COOH or --COOR.sub.4 ;R.sub.4 has 1 to 6 carbon atoms;A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents.

Abstract: Compounds of formula (I) ##STR1## exemplified by formulae (Ia) and (Ib) ##STR2## are tachykinin receptor antagonists useful in the treatment of disorders associated with the presence of an excess of tachykinins such as pain, inflammation, migraine, emesis and post herpetic neuralgia.

Abstract: Disclosed are the compounds of formula I ##STR1## wherein R represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl or cycloalkyl-lower alkyl;R.sub.1 represents hydrogen, lower alkyl, cycloalkyl, carbocyclic aryl or heterocyclic aryl, or biaryl;R.sub.3 represents hydrogen or acyl;R.sub.4 represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, biaryl or biaryl-lower alkyl;R.sub.5 represents hydrogen or lower alkyl; or R.sub.4 and R.sub.

Abstract: The present invention is directed to compounds of the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.6, R.sup.7, R.sup.8, m, n and X are defined herein, and pharmaceutically acceptable salts thereof, which are useful as tachykinin antagonists.

Abstract: The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.

Abstract: The present invention relates to therapeutically active azaheterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.

Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

Abstract: Piperidinyl-substituted cyclohexanes of Formula I have anti-ischemic properties: ##STR1## wherein R=R.sub.1 and is independently H or halogen; or R and R.sub.1 may be taken together to form an --O(CH.sub.2).sub.m O-- (m=1 or 2);X=a phenyl residue;R.sub.2 =R.sub.3 and is independently H or C.sub.1-4 alkyl; andR.sub.4 =phenyl or substituted phenyl wherein the phenyl group is mono-, or di-substituted with groups selected from: F, Cl, I and C.sub.1-4 alkoxy.

Abstract: Compounds of the following structure, the corresponding N-oxides and agriculturally acceptable salts, are disclosed as effective insecticides: ##STR1## in which U is selected from ##STR2## Q is selected from hydrogen, hydroxy, sulfhydryl, and fluorine; R is selected from a heterocycle having 5 or 6 ring atoms, optionally fused to a benzene ring, and ##STR3## wherein V, W, X, Y, Z are as defined in the specification.

Abstract: The present invention provides a process for preparing an acid addition salt of the Z-isomer of a compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 represent a lower alkyl group, or taken together with the nitrogen atom to which they are attached, form a nitrogen-containing heterocyclic group optionally containing other hetero atom or atoms; R.sup.3 and R.sup.4 represent H, a lower alkyl group, OH, a lower alkoxy group, a lower alkylcarbonyloxy group, an arylcarbonyloxy group optionally substituted with 1-2 substituents selected from lower alkyl, lower alkoxy, halo and CN on the benzene ring, a benzylcarbonyloxy group, a mono- or di(lower alkyl)aminocarbonyloxy group or a mono- or di(aryl)aminocarbonyloxy group; R.sup.

Abstract: Compounds of this formula ##STR1## are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.

Abstract: Compounds of the formula: ##STR1## wherein: m is 0 or 1;R.sup.1 is hydrogen, hydroxy, or lower alkyl;R.sup.2 is hydrogen, or lower alkyl;R.sup.3 is ##STR2## or R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached represent a group of the formula: ##STR3## wherein: n is 0 or 1;p is 0, 1, 2 or 3;q is 0 or 1;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, or optionally substituted phenyl;R.sup.5 is optionally substituted phenyl;X is (CH.sub.2).sub.p, or 4-piperidin-1-yl;Y is CH, CH--O--, CH--S--, or nitrogen;Z is CH.sub.2, NH, sulfur, or oxygen; andA is a substituted furanyl group.

Abstract: The present invention is directed to novel vinyl sulfenic acid derivatives, useful for the synthesis of benzo b!thiophenes, in particular 2-arylbenzo b!thiophenes.

Abstract: The present invention is directed to a new process for the synthesis of vinyl sulfenic acid derivatives. These compounds are useful for the synthesis of benzo b!thiophenes, in particular 2-aryl-benzo b!thiophenes.

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: Bis{[1-(2-A-2-B)ethenyl]} [2-R.sup.2 -4-X-phenyl- or 1-(2-R.sup.2 -4-X-phenyl) ethenyl]methanes useful as color formers, particularly in transfer imaging, pressure sensitive and thermal-responsive carbonless duplicating systems, are prepared by the interaction of two molecular proportions of the corresponding 1-A-1-B-ethene with the appropriate 2-R.sup.2 -4-X-phenyl-(CH.dbd.CH).sub.n --CHO presence of an acidic catalyst.

Abstract: Certain aminoalkyl derivatives of naphthyl-piperidines and tetrahydro-pyridines of Formula (I) are useful antidepressant agents. ##STR1## The symbol (Aryl) denotes phenyl, naphthyl, pyridinyl, pyrimidinyl and pyrazinyl ring systems with n being an integer of 2-4.

Abstract: This invention relates to a process for preparing certain 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates, intermediates, and congeners. Finally, the invention provides new 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates with formulations and methods for using the compounds.

Abstract: This invention provides trans-3,4 1-substituted-3-substituted-4-methyl-4-(3-substituted phenyl)piperidines as opioid antagonists capable of blocking the mu or kappa receptors in the brain.

Abstract: In one aspect, compounds, methods of using them, compositions comprising such compounds, and uses of such compositions.These objects, and others which will become apparent from the following disclosure, are achieved by the present invention which comprises in one aspect compounds of the formula ##STR1## wherein R is alkyl, cycloalkyl, aryl, substituted aryl, alkaryl optionally substituted on the aryl portion or aralkyl optionally substituted on the aryl portion, R having up to 20 carbon atoms and is optionally branched, andA is (CH.sub.2).sub.p, (CH.sub.2).sub.q --O--(CH.sub.2).sub.r, or (CH.sub.2).sub.q --S--(CH.sub.2).sub.r,wherein p=2 to 8, q=1 to 8, and r=1 to 8.R.sub.1 =--(CH.sub.2).sub.m --, --(CH.sub.2 CH.sub.2 --O).sub.n --CH.sub.2 CH.sub.2 --, or --(CH.sub.2 CH.sub.2 CH.sub.2 --O).sub.n --CH.sub.2 CH.sub.2 CH.sub.2 --.

Abstract: 4-Benzylpiperidine derivatives of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein X is hydrogen or fluorine and R is hydrogen, or a group selected from p-fluorobenzoyl, .alpha.-hydroxy-p-fluorobenzyl, p-fluorophenoxy, bis(p-fluorophenyl)methyl and 8-azaspiro[4,5]decane-7,9-dione-8-yl-methyl, with the proviso that X and R may not be simultaneously hydrogen and p-fluorobenzoyl respectively.Such compounds are useful as sigma-receptor ligands.

Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols of the following formula are useful as anxiolytic agents and have other psychotropic properties ##STR1##

Abstract: The ethylamino phenyl ethers of the invention and compositions thereof are endowed with high activities as inhibitors of the growth of several species of pathogen fungi and are applied to plants or to plant parts and are effective in preventing the diseases caused by pathogen fungi, such as, e.g., those belonging to Erysiphe and Helminthosporium genera.

Abstract: An enamine derivative containing a fluoroalkyl group, a fluoroaryl group or a fluoroaralkyl group is effective as a charge transport material in an electrophotographic member excellent in sensitivity, residual potential, durability and the like electrophotographic properties.

Abstract: 4-Phenylpiperidines of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy or lower-alkoxy;R.sub.2 is hydrogen, hydroxy, lower-alkanoyl, aroyl, lower-alkoxycarbonyl, lower-alkanoyloxy, lower-alkoxycarbonyl, or CONR.sub.3 R.sub.4 ; R.sub.3 and R.sub.4 are the same or different lower-alkyl or R.sub.3 and R.sub.4 together represent a lower-alkylene chain;X is methylene or carbonyl;Y is methylene, C.dbd.NOH, hydroxymethylene or carbonyl;or pharmaceutically acceptable acid addition salts thereof, are useful in the treatment of psychoses and other ailments of the central nervous system.

Abstract: Disclosed herein is a specific cinnamic acid derivative such as methyl 4-(4-acetoxy-3-methoxycinnamanide)-1-cyclohexanecarboxylate, or a pharmaceutically acceptable salt thereof. These compounds are useful as IV-type allergic reaction-suppressive drugs.

Abstract: The present invention relates to piperidine derivatives of the formula: ##STR1## wherein, R, R.sup.1, R.sup.3, X, and n are defined in the specification, pharmaceutical compositions thereof and methods of treating anoxia, traumatic injury, ischemia, migraine and epilepsy.

Abstract: Diphenylcyclopropyl analogs in which one or more of the phenyl rings includes substituents comprising a hydroxy group, a hydrogen atom, an acetate group or a substituted or unsubstituted alkoxy group. The compounds are useful as antiestrogens and anti-tumor agents.

Abstract: This invention provides trans-3,4 1-substituted-3-substituted-4-methyl-4-(3-substituted phenyl)piperidines as opioid antagonists capable of blocking the mu or kappa receptors in the brain.

Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.

Abstract: A series of novel N-alkyl or oxyalkyl arylpiperidine derivatives have been prepared, including their pharmaceutically acceptable acid addition salts, wherein the N-alkyl or oxyalkyl side chain is further substituted by certain aryl or heterocyclic ring groups. These particular compounds are useful in therapy as neuroleptic agents for the control of various psychotic disorders. Typical and preferred member compounds include 4-{{4-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}phenyl}}thiazole-2-amine , 4-{{4-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}phenyl}}thiazole-2-a mine, 3-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}-1,8,8-trimethyl-3-azabic yclo[3.2.1]octane-2,4-dione, 5-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}oxindole and 3-{2-[4-(1-naphthyl)-1-piperidinyl]ethyl}-2-methyl-4H-pyrido[1,2-a]pyrimid ine-4-one, respectively. Methods for preparing all these compounds from known starting materials are provided.

Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein: R.sup.1 is hydrogen, lower-alkyl or phenyl-lower-alkyl;R.sup.2 and R.sup.4 are the same or different lower-alkyl;R.sup.3 is hydrogen or lower-alkyl;m is two or three;n is an integer from zero to three; andR.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, allyl, or propargyl;or a pharmaceutically acceptable acid-addition salt thereof.

Abstract: The invention relates to compounds having anti-ischaemic activity, memory enhancing activity and anti-convulsive activity of the formulae 1A and 1B ##STR1## wherein R.sub.1 +R.sub.2 together form an alkylene group having 1-3 C-atoms which may be substituted with one or more alkyl group(s) having 1-3 C-atoms and the remaining R and Z variables are defined as disclosed herein, or a pharmacologically acceptable salt thereof.

Abstract: Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula ##STR1## wherein each of A and B is a group of formula (i) to (iii): ##STR2## wherein Y is --O--, --S-- or --NR-- in which R is hydrogen or C.sub.1 -C.sub.6 alkyl; each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is independently:a) hydrogen, halogen, hydroxy, cyano or nitro;b) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen,c) C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;d) C.sub.1 -C.sub.6 alkyl-sulfonyl;e) a substituted amine group --NR.sub.7 R.sub.8 ;f) a --COR.sub.12 group; org) two adjacent groups of R.sub.3, R.sub.4, R.sub.5 and R.sub.6, taken together, form a C.sub.1 -C.sub.4 alkylenedioxy group;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkenyl or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl; or R.sub.1 and R.sub.

Abstract: There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.

Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.

Abstract: There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.

Abstract: Compounds of the formula I ##STR1## and of the formula II ##STR2## where R.sup.1 is unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, or alkynyl, R.sup.2 is alkyl or alkenyl and X is an acid radical, and the salts of the compounds of the formula I, and fungicides which contain these compounds.