Abstract: Norvaline derivative of the formula [I] or pharmaceutically acceptable salt thereof, method for preparing the same, pharmaceutical composition containing the same, and use of the compound for inhibiting transporting activity of glycine transporter type 2 (GlyT2) wherein X is —CH2—, —O—, —S— or single bond; Ar is optionally substituted aryl or lower cycloalkyl; n is 0 to 2; R1 and R2 are (i) each is hydrogen or lower alkyl; (ii) R1 and R2 are combined to form lower alkylene; or (iii) R1 is hydrogen or lower alkyl and R2 is combined with R4 or R6 to form lower alkylene; R3 and R4 are (i) each is hydrogen or lower alkyl; (ii) R3 and R4 are combined to form lower alkylene; or (iii) R3 is hydrogen or lower alkyl and R4 is combined with R2 or R6 to form lower alkylene; R is ?or —OR7; R5 and R6 are (i) each is optionally substituted lower alkyl, or hydrogen; (ii) R5 and R6 are combined to form aliphatic 5- to 6-membered heterocyclic group; or (iii) R5 is optionally substituted lower alkyl or hydrogen and R

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; A: —CH2— or —S—, B: CH or N, R1: H, a lower alkyl group, etc., X: a single bonding arm, —CO—, -Alk-CO—, —COCH2—, -Alk-O—, —O—CH2—, —SO2—, —S—, —COO—, —CON(R3)—, -Alk-CON(R3)—, —CON(R3)CH2—, —NHCH2—, etc., R3: hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R2: (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is —CO—, then B is N, or a pharmaceutically acceptable salt thereof.

Abstract: Besylate salts of trans-4-({2-[(2S)-2-cyano-pyrrolidinyl]-2-oxoethyl}amino)-N,N-dimethylcyclohexanecarboxamide are described as well as methods of using the same in the treatment of disorders characterized by hyperglycemia.

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; A: —CH2— or —S—, B: CH or N, R1: H, a lower alkyl group, etc., X: a single bonding arm, —CO—, -Alk-CO—, —COCH2—, -Alk-O—, —O—CH2—, —SO2—, —S—, —COO—, —CON(R3)—, -Alk-CON(R3)—, —CON(R3)CH2—, —NHCH2—, etc., R3: hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R2: (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is —CO—, then B is N, or a pharmaceutically acceptable salt thereof.

Abstract: Norvaline derivative of the formula [I] or pharmaceutically acceptable salt thereof, method for preparing the same, pharmaceutical composition containing the same, and use of said compound for inhibiting transporting activity of glycine transporter type 2 (GlyT2).

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; A: —CH2— or —S—, B: CH or N, R1: H, a lower alkyl group, etc., X: a single bonding arm, —CO—, —Alk—CO—, —COCH2—, —Alk—O—, —O—CH2—, —SO2—, —S—, —COO—, —CON(R3)—, —Alk—CON(R3)—, —CON(R3)CH2—, —NHCH2—, etc., R3: hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R2: (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is —CO—, then B is N, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower-alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; A: —CH2— or —S—, B: CH or N, R1: H, a lower alkyl group, etc., X: a single bonding arm, —CO—, -Alk-CO—, —COCH2—, -Alk-O—, —O—CH2—, —SO2—, —S—, —COO—, —CON(R3)—, -Alk-CON(R3)—, —CON(R3)CH2—, —NHCH2—, etc., R3: hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R2: (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is —CO—, then B is N, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; A: —CH2— or —S—, B: CH or N, R1 H, a lower alkyl group, etc., X: a single bonding arm, —CO—, —Alk—CO—, —COCH2—, —Alk—O—, —O—CH2—, —SO2—, —S—, —COO—, —CON(R3)—, —Alk—CON(R3)—, —CON(R3)CH2—, —NHCH2—, etc., R3: hydrogen atom or a lower alkyl group, Alk: a lower alkylene group,,and. R2: (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is —CO—, then B is N, or a pharmaceutically acceptable salt thereof.

Abstract: A pyridopyrimidine or a naphthyridine derivative of the formula (I): wherein R1 is an optionally substituted nitrogen-containing heterocyclic group, etc.; R2 is H or a lower alkyl group; R3 is H or an optionally substituted lower alkyl group, etc.; R4 is H, a lower alkyl group, COOH, etc.; R5 is a lower alkyl group which may optionally be substituted by an optionally substituted aryl etc.; one of X and Y is CH and the other is nitrogen, or both of X and Y are nitrogen; or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent PDE V inhibitory activities, and being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.

Abstract: A pyridopyrimidine or a naphthyridine derivative of the formula (I): wherein R1 is an optionally substituted nitrogen-containing heterocyclic group, etc.; R2 is H or a lower alkyl group; R3 is H or an optionally substituted lower alkyl group, etc.; R4 is H, a lower alkyl group, COOH, etc.; R5 is a lower alkyl group which may optionally be substituted by an optionally substituted aryl etc.; one of X and Y is CH and the other is nitrogen, or both of X and Y are nitrogen; or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent PDE V inhibitory activities, and being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; A: —CH2— or —S—, B: CH or N, R1: H, a lower alkyl group, etc., X: a single bonding arm, —CO—, -Alk-CO—, —COCH2—, -Alk-O—, —O—CH2—, —SO2—, —S—, —COO—, —CON(R3)—, -Alk-CON(R3)—, —CON(R3)CH2—, —NHCH2—, etc., R3: hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R2: (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is —CO—, then B is N, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: 1

Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: 1

Abstract: Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group or lower alkoxy group, R.sup.1 represents a phenyl group which is substituted by a halogen atom, a lower alkyl group or a lower alkoxy group, R.sup.2 represents a naphthyl group, indolyl group, isoquinolyl group, benzimidazolyl group or a group represented by the formula: ##STR2## wherein n represents 1 or 2, R.sup.3 represents a lower alkyl group which is substituted by a carboxyl group, a cyano group or a tetrazolyl group, O represents a single bonding arm, and Y represents a single bonding arm,or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are .beta.-carboline derivatives represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen atom, a lower alkyl group, a lower alkoxy group or hydroxy group; R.sup.5 represents hydrogen atom, or R.sup.1 and R.sup.5 are bonded to represent a lower alkylenedioxy group; R.sup.2 represents hydrogen atom, a halogen atom, a lower alkoxy group or hydroxy group; R.sup.3 represents hydrogen atom, a carbamoyl lower alkyl group, a lower alkyl group, a carboxy lower alkyl group or a lower alkoxycarbonyl lower alkyl group; R.sup.4 represents hydrogen atom, a lower alkyl group, a carboxy lower alkyl group, a lower alkoxycarbonyl lower alkyl group, a lower alkanoyl group, an arylcarbonyl group, a lower alkanesulfonyl group, a lower alkoxycarbonyl group, an aralkyl group, formyl group or a di(lower alkyl)sulfamoyl group; n represents 0, 1 or 2; and the symbol * represents an asymmetric carbon atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.