Thiazole Derivatives Having Vap-1 Inhibitory Activity

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United States of America Patent

APP PUB NO 20080015202A1
SERIAL NO

11574946

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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A compound of the formula (I): U-V-W-X-Y-Z (I) wherein U is lower alkyl; V is --CONH-- or --NR.sup.1CO-- wherein R.sup.1 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 R.sup.2 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 --SO.sub.2--; and G is lower alkyl, optionally protected amino, --OH, phenyl, R.sup.3 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.

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Patent Owner(s)

Patent OwnerAddress
ASTELLAS PHARMA INC5-1 NIHONBASHI-HONCHO 2-CHOME CHUO-KU 103-8411

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Inoue, Takayuki Tokyo, JP 184 2170
Morita, Masataka Tokyo, JP 24 355
Tojo, Takashi Tokyo, JP 15 161

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