US 2004/0106671 A1Published application

Remedies for vesical hyperesthesia

OwnerTsuyoshi Yamagata, Kaoru Atsuki +3inventors

InventorsTsuyoshi Yamagata, Kaoru Atsuki, Tetsuji Ohno, Shiro Shirakura, Akira Karazawa

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Abstract

The present invention provides a therapeutic agent for bladder hypersensitivity comprising, as an active ingredient, a tricyclic compound represented by formula (I): 1 [wherein R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy or halogen; X1—X2—X3 represents CR5═CR6—CR7═CR8, N(O)m═CR6—CR7═CR8, CR5═CR6—N(O)m═CR8, CR5═CR6—CR7═N(O)m, CR5═CR6—O, CR5═CR6—S, O—CR7═CR8, S—CR7═CR8 or O—CR7═N; Y represents —CH2S—, —CH2SO—, —CH2SO2—, —CH2O—, —CH═CH—, —(CH2)p—, —SCH2—, —SOCH2—, —SO2CH2— or —OCH2—; and R2 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkoxy, amino, mono(substituted or unsubstituted lower alkyl)-substituted amino, di(substituted or unsubstituted lower alkyl)-substituted amino, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkylamino, substituted or unsubstituted arylamino or a substituted or unsubstituted heteroalicyclic group] or a pharmaceutically acceptable salt thereof.

Claims27

Dependent claims

A therapeutic agent for bladder hypersensitivity comprising, as an active ingredient, a tricyclic compound represented by formula (I):

10
[wherein R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy or halogen;
X1—X2—X3 represents CR5═CR6—CR7═CR8 (wherein R5, R6, R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, hydroxy, substituted or unsubstituted lower alkoxy, nitro, amino, mono(lower alkyl)-substituted amino, di(lower alkyl)-substituted amino, substituted or unsubstituted lower alkanoylamino or halogen), N(O)m═CR6—CR7═CR8 (wherein R6, R7 and R8 have the same significances as defined above, respectively, and m represents 0 or 1), CR5═CR6—N(O)m═CR8 (wherein R5, R6, R8 and m have the same significances as defined above, respectively), CR5═CR6—CR7═N(O)m (wherein R5, R6, R7 and m have the same significances as defined above, respectively), CR5═CR6—O (wherein R5 and R6 have the same significances as defined above, respectively), CR5═CR6—S (wherein R5 and R6 have the same significances as defined above, respectively), O—CR7═CR8 (wherein R7 and R8 have the same significances as defined above, respectively), SCR7═CR8 (wherein R7 and R8 have the same significances as defined above, respectively) or O—CR7═N (wherein R7 has the same significance as defined above);
Y represents —CH2S—, —CH2SO—, —CH2SO2—, —CH2O—, —CH═CH—, —(CH2)p— (wherein p represents an integer of 0 to 2), —SCH2—, —SOCH2—, —SO2CH2— or —OCH2—;
and
R2 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkoxy, amino, mono(substituted or unsubstituted lower alkyl)substituted amino, di(substituted or unsubstituted lower alkyl)-substituted amino, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkylamino, substituted or unsubstituted arylamino or a substituted or unsubstituted heteroalicyclic group] or a pharmaceutically acceptable salt thereof.

3 more elements

A therapeutic agent for bladder hypersensitivity comprising, as an active ingredient, a tricyclic compound represented by formula (Ia):

11
[wherein R1 and X1—X2—X3 have the same significances as defined above, respectively;
Ya represents —CH2SO2—, —SCH2—, —SOCH2—, —SO2CH2— or —OCH2—;
and
when Ya is —CH2SO2—, —SCH2—, —SOCH2— or —SO2CH2—,
R2a represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, trifluoromethyl, substituted or unsubstituted lower alkoxy, amino, mono(substituted or unsubstituted lower alkyl)-substituted amino, di(substituted or unsubstituted lower alkyl)-substituted amino, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkylamino, substituted or unsubstituted arylamino, a substituted or unsubstituted heteroalicyclic group or formula (II):
12
(wherein n is 0 or 1;
R3 and R4, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl or trifluoromethyl, or R3 and R4 may be combined together with the adjacent carbon atom to form cycloalkyl;
and Q represents hydroxy, substituted or unsubstituted lower alkoxy, amino or halogen), and
when Ya is —OCH2—,
R2a represents a hydrogen atom, substituted or unsubstituted lower alkenyl, trifluoromethyl, substituted or unsubstituted lower alkoxy, amino, mono(substituted or unsubstituted lower alkyl)-substituted amino, di(substituted or unsubstituted lower alkyl)-substituted amino, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkylamino, substituted or unsubstituted arylamino, a substituted or unsubstituted heteroalicyclic group or formula (II):
13
(wherein n, R3, R4 and Q have the same significances as defined above, respectively)] or a pharmaceutically acceptable salt thereof.

11 more elements

Dependencies are inferred from the claim text.