Abstract: The present invention relates to a compound represented by the general formula [I]: ##STR1## wherein Ar.sup.1 represents an aryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl and lower haloalkyl groups; Ar.sup.2 represents an aryl or heteroaryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino and aryl groups; R.sup.1 and R.sup.2 may be the same or different and each represents a hydrogen atom or a lower alkyl group; R.sup.3 and R.sup.4 may be the same or different and each represents a hydrogen atom or a lower alkyl group, or R.sup.3 and R.sup.4 are linked to each other to form an alkylene group containing 2 to 4 carbon atoms which may have a lower alkyl group; and R.sup.

Abstract: The present invention relates to a compound of the general formula: ##STR1## wherein each of R.sup.1 and R.sup.2 which may be the same or different, is e.g. a hydrogen atom, a halogen atom or a lower alkyl group, X is an oxygen atom, a sulfur atom or CH, Y is CH or a nitrogen atom, and A is e.g. a 1-substituted-4-piperidinyl group, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable anion-exchange product thereof or a hydrate thereof. The compounds of the present invention have chemokine receptor antagonism, and thus they are useful as treating agents for various diseases relating to chemokine, such as acute inflammatory diseases, chronic inflammatory diseases, acquired immune deficiency syndrome, cancer, ischemic reflow disorder and/or arteriosclerosis.

Abstract: The invention relates to compounds represented by the general formula [I] ##STR1## [wherein Ar means an aryl group or a heteroaryl group which may have a substitutive group selected from a group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; R.sup.1 means a C.sub.3 -C.sub.6 cycloalkyl group which is substitutable with a fluorine atom; R.sup.2 and R.sup.4 mean hydrogen atoms, groups represented by --(A.sup.1).sub.m --NH--B or the like; R.sup.3 and R.sup.5 mean hydrogen atoms, C.sub.1 -C.sub.6 aliphatic hydrocarbon groups or the like which are substitutable with a lower alkyl group(s); n means 0 or 1; and X means an oxygen atom or a sulfur atom].Compounds according to the invention, since they not only have potent selective antagonistic activity against muscarinic M.sub.

Abstract: The present invention relates to a process for producing a compound represented by the formula (II): ##STR1## wherein X is a halogen atom, each of A.sup.1, A.sup.2 and A.sup.3 are the same or different and are selected from a carbon atom or a nitrogen atom, provided that at least A.sup.1, A.sup.2, or A.sup.3 is a nitrogen atom. Each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a halogen atom, and a nitro group. It is also provided that where R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, and an amino-(lower alkyl) group.

Abstract: The present invention relates to a compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently a hydrogen atom, a C.sub.1 -C.sub.16 alkyl group, a C.sub.2 -C.sub.10 alkenyl group, a C.sub.3 -C.sub.6 alkynyl group, a C.sub.6 -C.sub.12 aryl group, a C.sub.7 -C.sub.15 aralkyl group or a heterocyclic group which is not substituted, a C.sub.1 -C.sub.16 alkyl group, a C.sub.2 -C.sub.10 alkenyl group, a C.sub.3 -C.sub.6 alkynyl group, a C.sub.6 -C.sub.12 aryl group, a C.sub.7 -C.sub.15 aralkyl group or a heterocyclic group which has substituent(s), or a group represented by --Y--R.sup.3 (provided that when R.sup.2 is a hydrogen atom, R.sup.1 is not a methyl group or an acetyl group; when R.sup.2 is an acetyl group, R.sup.1 is not a methyl group), an antifungal agent containing it as an active ingredient and an antifungal composition containing it and an azole type antifungal agent.

Abstract: A method for preventing and/or treating heart failure and ventricular dysfunction in a warm blooded animal comprising administering to the warm blooded animal a therapeutically effective amount of an endothelin antagonist of the formula: as defined herein.

Abstract: The present invention relates to an antitumor or anti-AIDS composition containing a protein-farnesyltransferase inhibitor and an agent which decreases farnesyl pyrophosphate in vivo as active ingredients.

Abstract: The present invention relates to a compound represented by the general formula [I]: ##STR1## wherein A and B rings are ortho-condensed to each other, A ring represents an aromatic carbocyclic or heterocyclic ring and B ring represents an aliphatic four- to seven-membered carbocyclic or nitrogen-containing heterocyclic ring, said nitrogen atom being possible to present at only the position where the A ring is condensed; Ar represents an aromatic carbocyclic or heterocyclic ring group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino and aromatic carbocyclic ring groups; and R represents a substituent selected from the group consisting of a halogen atom and nitro, lower alkyl, lower alkoxy, aromatic carbocyclic ring groups and a carbonyl group having an aromatic carbocyclic ring group, or a hydrogen atom, provided that when the group represented by ##STR2## is the

Abstract: The present invention relates to a compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: ##STR1## [wherein each of ##STR2## is an aryl group or an aromatic heterocyclic group; A.sup.1 is a C.sub.1-6 chain hydrocarbon group or a group represented by --A.sup.1a --W.sup.1 --A.sup.1b -- (wherein W.sup.1 is an oxygen atom, a sulfur atom, an ethynylene group, a cyclopropylene group or a group represented by --NR.sup.W --); A.sup.2 is a C.sub.1-8 chain hydrocarbon group; R.sup.1 is a lower alkyl group, a lower alkenyl group, a lower alkoxy group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a group represented by R.sup.a COO-- (wherein R.sup.a is a hydrogen atom, an amino group, a lower alkyl group, a lower alkoxy group or a lower alkylamino group) or by R.sup.b CONR.sup.c -- (wherein R.sup.

Abstract: The present invention relates to a compound represented by the general formula [I]: ##STR1## wherein A represents a nitrogen atom or a group represented by C--R.sup.5 ; Ar.sup.1 represents an aryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl and lower haloalkyl groups; Ar.sup.2 represents an aryl or heteroaryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino and aryl groups; R.sup.1 represents a hydrogen atom, a lower alkyl group or a bond formed by linking to R.sup.5 ; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 and R.sup.4 may be the same or different and each represents a hydrogen atom or a lower alkyl group, or R.sup.3 and R.sup.4 are linked to each other to form an alkylene group containing 2 to 4 carbon atoms which may have a lower alkyl group; and R.sup.

Abstract: In the production of fluorine-containing 1,4-disubstituted piperidine derivatives by the reaction of a carboxylic acid of formula where Ar represents aryl or heteroaryl and R.sup.10 represents C.sub.3 -C.sub.6 cycloalkyl in which up to 4 hydrogen atoms are substituted with fluorine or C.sub.3 -C.sub.6 cycloalkyl having 1 to 2 protected or unprotected hydroxyl or oxo groups, or a reactive derivative thereof, with a piperidine derivative of formula [IV] as defined in the specification, especially useful results are obtained using 4-amino-1-(6-aminopyridin-2-ylmethyl)piperidine or a salt thereof, e.g., trihydrochloride, as the piperidine derivative.

Abstract: The present invention relates to an oxidation using sodium chlorite in the presence of a catalytic amount of TEMPO and sodium hypochlorite which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid ##STR1##

Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.

Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for hyperphagia, obesity or diabetes, which comprises such a compound or salt as an active ingredient: ##STR1## wherein Ar.sup.1, Ar.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and W are as defined.

Abstract: The present invention relates to a compound of the formula (I), or its pharmaceutically acceptable salt or ester: ##STR1## wherein Ar.sup.1 is an aryl group or a heteroaromatic ring group; Ar is a group of the formula ##STR2## each of Ar.sup.2 and Ar.sup.3 is an aryl group or a heteroaromatic ring group; Cy is an aryl group, a heteroaromatic ring group or an aliphatic ring group which may contain one or two oxygen atoms; A.sup.1 is a C.sub.1-4 chain hydrocarbon group; m is an integer of from 1 to 6; each of n and p is an integer of from 0 to 3; Q.sup.1 is a single bond, a group of the formula --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S-- or --SCH.sub.2 --, or a C.sub.1-6 chain hydrocarbon group; Q.sup.2 is a single bond or a group of the formula --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p --; Q.sup.3 is a single bond, an oxygen atom, a sulfur atom, a methylene group, a vinylene group or a group of the formula --CO--, --NH--, --COO--, --OCO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.

Abstract: A compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: [wherein each of Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 is an aryl group or an aromatic heterocyclic group; A.sup.1 is a C.sub.2-6 chain hydrocarbon group or a group represented by --A.sup.1a --W.sup.1 --A.sup.1b -- (wherein W.sup.1 is an oxygen atom, a sulfur atom, an ethynylene group, a cyclopropylene group or a group represented by --NR.sup.W --; A.sup.2 is a C.sub.2-8 chain hydrocarbon group; each of X and Y is an oxygen atom, a sulfur atom, a carbonyl group or a group represented by --CHR.sup.a -- or by --NR.sup.b --, or X and Y together represent a vinylene group or an ethynylene group; each of R.sup.1, R.sup.2, R.sup.3, R.sup.7 and R.sup.8 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkenyl group or a lower alkoxy group; each of R.sup.4 and R.sup.

Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist, the synthesis of this key intermediate and the synthesis of an endothelin antagonist using this intermediate in a stereoselective deoxygenation reaction.

Abstract: Novel fluorine-containing 1,4-disubstituted piperidine derivatives, represented by general formula ?I! ##STR1## such as, for example, (2R)-N-?1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl!-2-?(1R)-3,3-difluoroc yclopentyl!-2-hydroxy-2-phenylacetamide or pharmaceutically acceptable salt thereof, are potent and selective antagonists for muscarinic M.sub.3 receptors with little side effects. The compounds of formula ?I! exhibit excellent oral activity, duration of activity and pharmacolkinetics. They are useful for treatment and prophylaxis of respiratory diseases, such as chronic obstructive pulmonary diseases; urinary diseases, such as urinary incontinence; and digestive diseases, such as irritable bowel syndrome, and motion sickness.

Abstract: The present invention relates to a compound represented by the general formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom, or ##STR2## and R.sub.2 is a hydrogen atom or OH and R.sub.2 is a hydrogen atom or a lower alkanoyl group, and an antifungal agent containing it as an active ingredient.

Abstract: An antifungal composition, containing a synergistic mixture, containing the compound of the formula (I): ##STR1## wherein R is acetyl or lower alkyl; or a pharmaceutically acceptable salt thereof; and an azole antifungal agent selected from the group consisting of an imidazole compound and a triazole compound, as an active ingredient.