Abstract: Heterocyclic compounds represented by the general formula (I) and having elastase inhibiting activity; and intermediates for the synthesis thereof: (I) wherein R1 is a heterocyclic group represented by the general formula (II): (II) [wherein A represents the presence or absence of a benzene ring; X is oxygen, sulfur or NH; and Y is nitrogen or CH], and the heterocyclic group may be substituted with one to three substituents which may be the same or different and are selected from the group consisting of lower alkyl, lower alkoxy, and phenyl which may be substituted with optionally halogenated lower alkyl, lower alkoxy or halogeno; and R2 and R3 are each hydrogen or hydroxyl, or R2 and R3 may be united to form an oxo group, with the proviso that both are not hydrogen.

Abstract: Heterocyclic compounds represented by the general formula (I) and having elastase inhibiting activity; and intermediates for the synthesis thereof: (I) wherein R1 is a heterocyclic group represented by the general formula (II): (II) [wherein A represents the presence or absence of a benzene ring; X is oxygen, sulfur or NH; and Y is nitrogen or CH], and the heterocyclic group may be substituted with one to three substituents which may be the same or different and are selected from the group consisting of lower alkyl, lower alkoxy, and phenyl which may be substituted with optionally halogenated lower alkyl, lower alkoxy or halogeno; and R2 and R3 are each hydrogen or hydroxyl, or R2 and R3 may be united to form an oxo group, with the proviso that both are not hydrogen.

Abstract: Novel pyrrolidine derivatives, being useful as chymase inhibitor or intermediate for synthesis of the active compounds, which has the formula (I): wherein R1 is cycloalkyl, substituted or unsubstituted phenyl or naphthyl, indanyl, thienyl, furyl, substituted or unsubstituted indolyl, benzofuryl, substituted or unsubstituted benzothienyl, etc.; R2 is H, alkyl, phenyl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; R3 is (i) substituted or unsubstituted monocyclic heterocyclic group, (ii) substituted or unsubstituted benzene- or pyridine-fused heterocyclic group, or (iii) a group (a): R4 and R5 are independently H or OH, but R4 and R5 are not simultaneously H, or both form oxo; n is 0, 1, 2 or 3; or a salt thereof.

Abstract: The present invention relates to a heterocyclic compound of the following formula (I-a), its ester, or a salt thereof, and a human neutrophilic elastase inhibitor containing the same as the active ingredient, etc. wherein A and B are the same or different and each is a lower alkylene group being optionally substituted by an oxo group, D is a heteromonocyclic or heterobicyclic group being optionally substituted by an oxo group, R1 and R2 are the same or different and each is a lower alkyl group, R3 and R4 are different from each other, and each is a hydrogen atom or a hydroxy group, or both combine together to form an oxo group, and R5 is 2-benzoxazolyl, trifluoromethyl, benzylamino-carbonyl, etc.

Abstract: Novel pyrrolidine derivatives, being useful as chymase inhibitor or intermediate for synthesis of the active compounds, which has the formula (I): wherein R1 is cycloalkyl, substituted or unsubstituted phenyl or naphthyl, indanyl, thienyl, furyl, substituted or unsubstituted indolyl, benzofuryl, substituted or unsubstituted benzothienyl, etc.; R2 is H, alkyl, phenyl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; R3 is (i) substituted or unsubstituted monocyclic heterocyclic group, (ii) substituted or unsubstituted, benzene- or pyridine-fused heterocyclic group, or (iii) a group (a): R4 and R5 are independently H or OH, but R4 and R5 are not simultaneously H, or both form oxo; n is 0, 1, 2 or 3; or a salt thereof.

Abstract: The present invention provides a process for industrially producing (aminomethyl)trifluoromethylcarbinol derivatives, in particularly, optically active compounds thereof, which are useful as starting compounds for drugs such as protease inhibitors, etc.