Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.

Abstract: A method for treatment of a systemic wasting disease, by administering, to a subject in need thereof, an effective amount of a 3,8-diaminotetrahydroquinoline derivative represented by formula (Ia) (wherein X represents CH2, C?O, CH—OR, CH—SR, or CH—NRR?; m is a number of 1 or 2; Ar represents a phenyl group, a naphthyl group, a 5-membered or 6-membered aromatic heterocyclic group having one or two elements selected from S, N, and O, or a similar group; R1 and R2, which may be identical to or different from each other, each represent a hydrogen atom or a methyl group; R3 represents a C1 to C6 alkyl group or a similar group; n is a number of 0 or 1; R4 and R5, which may be identical to or different from each other, each represent a hydrogen atom, or a C1 to C6 alkyl group, etc.; and R6, R7, R, and R?, which may be identical to or different from one another, each represent a hydrogen atom or a C1 to C6 alkyl group), or a salt thereof.

Abstract: A method for treatment of a systemic wasting disease, by administering, to a subject in need thereof, an effective amount of a 3,8-diaminotetrahydroquinoline derivative represented by formula (Ia) (wherein X represents CH2, C?O, CH—OR, CH—SR, or CH—NRR?; m is a number of 1 or 2; Ar represents a phenyl group, a naphthyl group, a 5-membered or 6-membered aromatic heterocyclic group having one or two elements selected from S, N, and O, or a similar group; R1 and R2, which may be identical to or different from each other, each represent a hydrogen atom or a methyl group; R3 represents a C1 to C6 alkyl group or a similar group; n is a number of 0 or 1; R4 and R5, which may be identical to or different from each other, each represent a hydrogen atom, or a C1 to C6 alkyl group, etc.; and R6, R7, R, and R?, which may be identical to or different from one another, each represent a hydrogen atom or a C1 to C6 alkyl group), or a salt thereof.

Abstract: To provide a compound which has a potent agonistic activity on GHS-R and which is useful as a therapeutic agent for systemic wasting diseases such as cachexia. A 3,8-diaminotetrahydroquinoline derivative represented by formula (1a) (wherein X represents CH2, C?O, CH—OR, CH—SR, or CH—NRR?; m is a number of 1 or 2; Ar represents a phenyl group, a naphthyl group, a 5-membered or 6-membered aromatic heterocyclic group having one or two elements selected from S, N, and O, or a similar group; R1 and R2, which may be identical to or different from each other, each represent a hydrogen atom or a methyl group; R3 represents a C1 to C6 alkyl group or a similar group; n is a number of 0 or 1; R4 and R5, which may be identical to or different from each other, each represent a hydrogen atom, or a C1 to C6 alkyl group, etc.; and R6, R7, R, and R?, which may be identical to or different from one another, each represent a hydrogen atom or a C1 to C6 alkyl group), or a salt thereof.

Abstract: To provide a compound which has a potent agonistic activity on GHS-R and which is useful as a therapeutic agent for systemic wasting diseases such as cachexia. A 3,8-diaminotetrahydroquinoline derivative represented by formula (1a) (wherein X represents CH2, C?O, CH—OR, CH—SR, or CH—NRR?; m is a number of 1 or 2; Ar represents a phenyl group, a naphthyl group, a 5-membered or 6-membered aromatic heterocyclic group having one or two elements selected from S, N, and O, or a similar group; R1 and R2, which may be identical to or different from each other, each represent a hydrogen atom or a methyl group; R3 represents a C1 to C6 alkyl group or a similar group; n is a number of 0 or 1; R4 and R5, which may be identical to or different from each other, each represent a hydrogen atom, or a C1 to C6 alkyl group, etc.; and R6, R7, R, and R?, which may be identical to or different from one another, each represent a hydrogen atom or a C1 to C6 alkyl group), or a salt thereof.

Abstract: Provided is a method for selectively demethylating a 2-methoxy group.

Abstract: The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor.

Abstract: The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof.

Abstract: Provided are 1-N-aminobenzimidazole derivatives represented by the following formula (I): wherein R1 and R2 each represents a substituted or unsubstituted alkyl group or the like, R3, R5 and R6 each represents an alkyl group, alkoxy group, hydrogen atom or the like, R4 represents a substituted or unsubstituted alkyl group or the like, A represents a benzene ring or the like, B represents a hydrogen atom or the like, an n stands for an integer of from 0 to 2, or salts thereof; and medicines containing them. The compounds (I) according to the present invention do not bring about much individual differences in therapeutic effects despite the existence of individual differences in the CYP2C19 activity. At the same dose, they can hence bring about appropriate therapeutic effects for all patients. In addition, they are low in the risk of induction of an interaction or a cancer caused by induction of the CYP1A family.

Abstract: A benzimidazole derivative of formula (1): (wherein R represents a hydrogen atom or a methoxy group, and n is 0 or 1) or a salt thereof; and a medicament containing the same. The compounds of the present invention, due to minimized difference in therapeutic effect between subjects, which difference would otherwise be derived from different CYP2C19 activity from subject to subject, ensure that all patients can enjoy proper therapeutic effects at the same dose of the drug. Also, the compounds of the invention have low risk of drug interaction caused by induction of CYP1A family member enzymes, as well as low risk of development of cancer, and thus is useful as a remedy for peptic ulcer, reliably providing therapeutic effects with safety.

Abstract: Remedies effective for the improvement of colonic motor dysfunction such as irritable bowel syndrome, constipation or intestinal atony without causing side effects on the central nerve system. These colonic motor dysfunction remedies comprise, as active ingredients, aminothiazole derivatives represented by the following formula (I) or a salt or hydrate thereof: wherein R1, R2 and R3 may be the same or different and each independently represent a hydrogen atom or a hydroxyl, lower alkyl, lower alkoxy, amino, nitro or cyano group, R4 and R5 may be the same or different and each independently represent a hydrogen atom or a lower alkyl group, and n stands for an integer of from 2 to 4.

Abstract: A benzimidazole derivative of formula (1): 1

Abstract: Remedies effective for the improvement of colonic motor dysfunction such as irritable bowel syndrome, constipation or intestinal atony without causing side effects on the central nerve system. These colonic motor dysfunction remedies comprise, as active ingredients, aminothiazole derivatives represented by the following formula (I) or a salt or hydrate thereof: wherein R1, R2 and R3 may be the same or different and each independently represent a hydrogen atom or a hydroxyl, lower alkyl, lower alkoxy, amino, nitro or cyano group, R4 and R5 may be the same or different and each independently represent a hydrogen atom or a lower alkyl group, and n stands for an integer of from 2 to 4.

Abstract: Remedies effective for the improvement of colonic motor dysfunction such as irritable bowel syndrome, constipation or intestinal atony without causing side effects on the central nerve system.