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Title:
VAP-1阻害活性を有するチアゾール誘導体
Document Type and Number:
Japanese Patent JP2008512346
Kind Code:
A
Abstract:
A compound of the formula (I): U-V-W-X-Y-Z (I) wherein U is lower alkyl; V is -CONH- or -NR1CO- wherein R1 is a hydrogen or lower alkyl; W is a bond or lower alkylene; X is a bivalent residue derived from optionally substituted thiazole; Y is a bond or lower alkylene; and Z is a group of the formula: wherein R2 is a group of the formula: -A-B-D-E-F-G wherein A is a bond or lower alkylene; B is a bond, -NH- or D is a bond, -CS- or -CO-; E is a bond or -NH-; F is a bond, -CO-, -O- or -SO2-; and G is lower alkyl, optionally protected amino, -OH, phenyl, R3 is lower alkyl, provided that when Z is a group of the formula: then G should not be amino, when Z is a group of the formula: then G should not be when Z is a group of the formula: and G is optionally protected amino, then D should be -CS-, or then A should be lower alkylene, B or E should be -NH- and F should be -CO-; or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor as well as a pharmaceutical composition and a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a subject, and the like.

Inventors:
Takayuki Inoue
Takashi Tojo
Morita Masashi
Application Number:
JP2007511147A
Publication Date:
April 24, 2008
Filing Date:
September 08, 2005
Export Citation:
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Assignee:
Astellas Pharma Inc.
International Classes:
A61K31/427; C07D277/20; A61K31/433; A61K31/495; A61K31/496; A61P1/02; A61P1/04; A61P1/16; A61P3/04; A61P3/10; A61P7/10; A61P9/00; A61P9/10; A61P9/12; A61P11/00; A61P11/06; A61P13/12; A61P17/00; A61P17/06; A61P19/02; A61P21/00; A61P25/00; A61P25/04; A61P25/28; A61P27/02; A61P29/00; A61P37/02; A61P43/00; C07D277/44; C07D417/06; C07D417/10; C07D417/12; C07D417/14
Attorney, Agent or Firm:
Takashima Ichi