Abstract: The present invention is directed to (S)-(?)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate, to a method producing the dihydrate, and to a drug composition containing the dihydrate. The compound of the present invention has less hygroscopicity as compared with (S)-(?)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride anhydrous crystals and thus, exhibits excellent chemical stability.

Abstract: The present invention is directed to (S)-(?)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate, to a method producing the dihydrate, and to a drug composition containing the dihydrate. The compound of the present invention has less hygroscopicity as compared with (S)-(?)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride anhydrous crystals and thus, exhibits excellent chemical stability.

Abstract: The present invention relates to diamide derivatives represented by the following general formula (1): wherein A is a phenyl group or the like, which may be substituted, B is —CH═CH—, —C≡C—, —(CH═CH)2—, —C≡C—CH═CH—, —CH═CH—C≡C—, phenylene or the like, and W is and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.

Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: wherein Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or an oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NR6—; R4 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.

Abstract: Compounds having the formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyindeny, pyridyl, indolyl,isoindolyl, quinolyl or isoquinolyl group which are optionally substituted; X is optionally substituted alicyclic, aromatic, imino or heterocyclic groups or —S— or —O—; Y is a single bond or an alkylene group; Z is an unsubstituted aliphatic group or divalent residue of benzene or pyridine, which is optionally substituted; anis hydrogen, lower alkyl, cycloalkyl, aryl or aralkyl; with certain provisos. These compounds exhibit an inhibitory effect on the production of IgE antibodies and are, hence, useful as antiallergic agents.

Abstract: The present invention relates to diamide derivatives represented by the following general formula (1): 1

Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them.

Abstract: The present invention provides diamide derivatives represented by the following general formula (1): wherein A is a phenyl group or the like, which may be substituted, B is —CH═CH—, —C═C—, —(CH═CH)2—, —C≡C—CH═CH—, —CH═CH—C≡C—, phenylene or the like, and W is or and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.

Abstract: The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: [wherein R1 represents a lower alkyl group; each of R2 and R3 represents H, alkyl, or alkoxy; each of R4 and R5 represents H or alkyl; R6 represents alkyl, —OR7, or —NR8R9; and n is a number between 0 and 3 inclusive (wherein each of R7, R8, and R9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.

Abstract: The present invention relates to compounds represented by the following general formula (1): 1

Abstract: The present invention relates to compounds represented by the following general formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyl, indenyl, pyridyl, indolyl, isoindolyl, quinolyl or isoquinolyl group which may be substituted; X is a lower alkylene group which may be substituted, or the like; Y is a single bond or an alkylene group; Z is a group of —CH═CH—, —C≡C—, —(CH═CH)2—, —C≡C—CH═CH— or —CH═CH—C≡C—, or the like; and R is a hydrogen atom, a lower alkyl group or the like, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.

Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: where Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NH6—; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.

Abstract: The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## [wherein R.sup.1 represents a lower alkyl group; each of R.sup.2 and R.sup.3 represents H, alkyl, or alkoxy; each of R.sup.4 and R.sup.5 represents H or alkyl; R.sup.6 represents alkyl, --OR.sup.7, or --NR.sup.8 R.sup.9 ; and n is a number between 0 and 3 inclusive (wherein each of R.sup.7, R.sup.8, and R.sup.9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.

Abstract: The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## ?wherein R.sup.1 represents a hydroxyl group, a lower alkoxy group, a phenyloxy group which may have a substituent, an aralkyloxy group which may have a substituent, or --NR.sup.2 R.sup.3 ; X represents an oxygen atom or N--R.sup.4 ; m is 2 or 3; and n is 1 or 2 (wherein each of R.sup.2 and R.sup.3, which are identical to or different from each other, represents a hydrogen atom, a hydroxyl group, a lower alkyl group which may have a substituent, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, or a heterocyclic group which may have a substituent; R.sup.4 represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)!, as well as to a medicine containing the derivative or salt as the active ingredient.

Abstract: An azoxy compound represented by the following general formula ##STR1## wherein R.sub.1 denotes a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkoxy group, a lower alkoxy-lower alkoxy group or a group of the formula X.sub.1 --C.tbd.C--CH.sub.2 O-- wherein X.sub.1 is a hydrogen atom or a halogen atom;R.sub.2 denotes a hydrogen atom or a lower alkyl group;R.sub.3 denotes a hydrogen atom or a lower alkyl group;R.sub.4 denotes a hydrogen atom or a group of the formula X.sub.2 --C.tbd.C--CH.sub.2 -- wherein X.sub.2 is a hydrogen atom or a halogen atom;R.sub.5 denotes a hydrogen atom or a lower alkyl group;andn is 0 or 1.This compound has an excellent antifungal activity against fungi infectious to warm-blooded animals and fungi infectious to agrohorticultural crops or fruit trees, and is useful as a medicine, a veterinary drug and an agrohorticultural antifungal agent.

Abstract: A compound expressed by the formula: ##STR1## in which R.sub.11, R.sub.21 and R.sub.31 are identical with or different from each other and each denotes a hydrogen atom, a halogen atom, an alkyl group, an alkenyl group, a haloalkyl group, an alkoxy group, an alkylthio group, an aryl or an aralkyl group which aromatic ring is optionally substituted appropriately by one to three substituents or a heterocyclic group optionally substituted appropriately by one to three substituents, or R.sub.11 and R.sub.21 may together form an alkylene group, Y denotes O or NOH, with a proviso that where R.sub.21 (or R.sub.11) and R.sub.31 denote a hydrogen atom at the same time, R.sub.11 (or R.sub.21) cannot represent an n-butyl group. This compound is useful as an antifungal agent.

Abstract: A novel 2-imino derivative of an antifungal product KA-7367A represented by formula, ##STR1## which has high antifungal activity and excellent stability and is useful as an antifungal agent for warm-blooded animals including humans and for agricultural and horticultural usages.

Abstract: Thrombin-binding substances are obtained by fractionating human urine by ion-exchange chromatography, affinity chromatography using a thrombin-bound carrier, immune adsorption column chromatography, gel filtration, and/or molecular-weight fractionation. One of the substances has a molecular weight of 46,500.+-.6,000 in reduced condition and 39,000.+-.10,000 in unreduced condition by SDS PAGE and an isoelectric point at pH 5.0-5.3, while the other has a molecular weight of 40,000.+-.8,000 in reduced condition and 31,000.+-.10,000 in unreduced condition by SDS PAGE and an isoelectric point at pH 4.9-5.7. They have strong affinity to thrombin. They are capable of promoting the thrombin catalyzed activation of protein C and prolong clotting time. They are stable to denaturing agents (urea and sodium dodecylsulfate).

Abstract: Novel thrombin-binding substances (A) and (B) are disclosed. The thrombin-binding substances have the following characteristics:(a) molecular weight:Thrombin-binding substance (A):90,000-92,000 under reduced conditions55,000-58,000 under unreduced conditionsThrombin-binding substance (B):98,000-105,000 under reduced conditions60,000-65,000 under unreduced conditions(b) isoelectric point:Thrombin-binding substance (A): pH 6.0-6.8Thrombin-binding substance (B): pH 5.8-6.5(c) affinity: strong affinity to thrombin(d) activity:(1) capable of promoting the thrombin catalyzed activation of protein C(2) prolongs clotting time; and(e) stability: stable to denaturing agents (sodium dodecylsulfate and urea).The thrombin-binding substances are useful as a medicine for curing thrombosis.

Abstract: Novel azoxy compounds having antifungal activity and being useful for the treatment of mycoses, represented by the following formula ##STR1## are prepared by culturing a microorganism of Streptomyces sp. (KC-7367, FERM BP-1277) and separating the compounds from the culture broth.