Abstract: A method of treating pain or pruritis comprising administering to a patient in need thereof a pharmaceutically effective amount of a ? opioid receptor agonist of the formula wherein R is an alkyl having an amino group as a substituent; and R1 is acyl.

Abstract: A compound or a salt thereof having the following formula wherein R1 is acyl, R2 is hydrogen, halogen, unsubstituted alkyl or alkyl substituted by halogen; R3 is halogen or alkoxy; R4 is cycloalkyl, unsubstituted alkyl or alkyl substituted by cycloalkyl, aryl or hydroxyl or an ester thereof or alkoxy; R5 is hydroxyl or an ester thereof, alkoxy or alkoxyalkyl; or R4 and R5 are bonded with each other to form a pyrrolidine ring substituted by hydroxyl or an ester thereof, alkoxy or alkoxyalkyl; R6 is hydroxyl or an ester thereof, alkoxy, alkoxyalkoxy, alkoxyalkoxyalkoxy, mercapto or alkylthio; and A1 and A2, are the same or different, and are alkylene, provided that (i) when R4 and R5 are bonded to each other to form the pyrrolidine ring substituted by hydroxyl or an ester thereof, R2 is halogen; (ii) when R4 and R5 are bonded to each other to form the pyrrolidine ring substituted by alkoxyalkyl, R2 is hydrogen; (iii) when R6 is hydroxyl or an ester thereof, R4 is isopropyl.

Abstract: A method of treating pain or pruritis comprising administering to a patient in need thereof a pharmaceutically effective amount of a ? opioid receptor agonist of the formula wherein R is an alkyl having an amino group as a substituent; and R1 is acyl.

Abstract: A compound having 3-oxo-3, 4-dihydro-2H-1, 4-thiazine 4-tetrahydropyrazine as a main skeleton. The compound is a chymase inhibitor and is represented by the following formula [I] and salts thereof: In the formula [I], X is S; R1 and R2 are H, alkyl, cycloalkyl or aryl; R3 and R4 are H, alkyl, cycloalkyl, aryl or an aromatic heterocycle; R5 is H, alkyl, cycloalkyl, aryl or -A3-A4-R7; R6 is H, alkyl, cycloalkyl, hydroxy, alkoxy, aryl, aryloxy or an aromatic heterocycle; R7 is H, alkyl, hydroxy, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle; A1 is alkylene; A2 is carbonyl or sulfonyl; A3 is alkylene; A4 is carbonyl or oxalyl; and n is 0 or 1.

Abstract: The present invention provides ? opioid receptor agonists comprising 2-phenylbenzothiazoline derivatives. The present invention relates to ? opioid receptor agonists comprising compounds or salts thereof having the chemical structure represented by the general formula [I]. Namely, it is important for exhibition of the ? opioid receptor agonist actions to have an alkyl group having an amino group at a phenyl group of 2-phenylbenzothiazoline as a substituent and to have an acyl group at a nitrogen atom of 2-phenylbenzothiazoline, wherein R is alkyl having the amino group as the substituent; and R1 is acyl.

Abstract: A compound having 3-oxo-3,4-dihydro-2H-1,4-thiazine 4-tetrahydropyrazine as a main skeleton.

Abstract: A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R6—(A2)n—N, R1 and R2 are H, alkyl, cycloalkyl or aryl, R3 and R4 are H, alkyl, cycloalkyl, aryl or aromatic heterocycle, R5 is H, alkyl, cycloalkyl, aryl or —A3—A4—R7, R6 is H, alkyl, cycloalkyl, OH, alkoxy, aryl, aryloxy or an aromatic heterocycle, R7 is H, alkyl, OH, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle, A1 is alkylene, A2 is carbonyl or sulfonyl, A3 is alkylene, A4 is carbonyl or oxalyl and n is o or 1.

Abstract: An object of the present invention is to provide novel thiazolidine derivatives which are useful as drugs. The thiazolidine derivatives according to the present invention are compounds represented by the following general formula [I] and salts thereof, wherein R1 is alkyl, hydroxy, alkoxy, alkoxyalkyl, phenyl, phenylalkyl, phenylalkoxy, phenoxy, phenoxyalkyl, amino, alkylamino or a nonaromatic heterocycle; R2 is H or alkyl; R3 is H, alkyl or phenyl; R4 is H or alkyl; R5 is alkyl, halogenoalkyl, hydroxy, alkoxy, phenyl, phenylalkoxy, phenoxy, carboxyl, alkoxycarbonyl, phenylalkoxycarbonyl or an aromatic heterocycle; A1 is alkylene; and A2 is alkylene.

Abstract: The present invention relates to leukotriene A4 hydrolase inhibitors containing compounds represented by the formula [I] or salts thereof as active ingredients, wherein R1 represents hydrogen, alkyl, phenylalkyl, alkanoyl or benzoyl; R2 and R3 each represent hydrogen or alkyl; R4 represents hydroxyl, alkoxy, phenylalkoxy, amino, alkylamino or phenylalkylamino; R5 represents phenylalkyl or naphthylalkyl; “Z” represents sulfur or oxygen; “A” represents alkylene; and “n” represents 0, 1 or 2; providing that the phenyl ring in R1 can be substituted by alkyl, alkoxy or halogen, and that the phenyl ring or the naphthyl ring in R5 can be substituted by alkyl, cycloalkyl, alkoxy, alkylthio or halogen.

Abstract: The present invention relates to compounds represented by the formula [I] and salts thereof, wherein R.sup.1 and R.sup.5 each represents carboxyl, phosphonic or a derivative thereof; R.sup.2 represents hydrogen, lower alkyl, (substituted) phenyl lower alkyl, lower alkoxy or (substituted) phenyl lower alkoxy; R.sup.3 represents lower alkyl or (substituted) phenyl lower alkyl; and R.sup.4 represents a group represented by the formula [XI], [XII] or [XIII]. The compounds of the present invention have endopeptidase 24.11 inhibitory activity and are useful for treating cardiovascular diseases such as heart failure and hypertension, renal diseases such as renal failure, gastroenteric disorders such as diarrhea and hyperchlorhydria, endocrine and metabolic diseases such as obesity, and autoimmune diseases such as rheumatic disease, and for mitigating myosalgia, migraine, etc.

Abstract: The present invention related to compounds represented by the following formula (I) and salts thereof, ##STR1## wherein R.sup.1 and R.sup.4 each represents a carboxyl or a carboxyl which is converted into an ester, an amide or hydroxamic acid; R.sup.2 represents a lower alkyl or a phenyl-lower alkyl; R.sup.3 represents a hydrogen atom, a lower alkyl, an amino-lower alkyl, a lower alkylamino-lower alkyl, a hydroxy-lower alkyl, a mercapto-lower alkyl, a carboxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an imidazolyl-lower alkyl, an indolyl-lower alkyl, a (substituted) phenyl group, a (substituted) phenyl-lower alkyl group, a (substituted) naphthyl group, or a (substituted) naphtyl-lower group. The compounds of the present invention have inhibitory effects on endopeptidase 24.

Abstract: A compound of the formula [I]. ##STR1## The compounds of this invention has excellent thymulin-line activities and expected to be useful for treatment of various diseases such as immunodeficiency and autoimmune diseases.