Thiazole derivatives
AssigneeAstellas Pharma Inc.
InventorsAkira Nagashima, Takayuki Inoue, Mitsuru Ohkubo, Kousei Yoshihara, Takashi Tojo, Masataka Morita
Life of this patent
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Abstract
A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, 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 mammal, and the like.
Claims19
A method for treating retinopathy comprising:
- administering to a subject in need thereof in an amount effective to treat retinopathy a compound of formula (I):
- wherein the 1,3-thiazole ring is optionally substituted at the 5-position;
- Y is lower alkylene, lower alkenylene, or —CONH—;
- and
- Z is a group of the formula:
- wherein R2 is a group of the formula:
- -A-B-D-E,
- wherein
- A is a bond, lower alkylene, —NH— or —SO2—;
- B is a bond, lower alkylene, —CO— or —O—;
- D is a bond, lower alkylene, —NH— or —CH2NH—;
- provided that B and D are not both simultaneously bonds, and
- E is amino, which may be optionally protected, —N═CH2,
- wherein
- Q is —S— or —NH—;
- and
- R3 is hydrogen, lower alkyl, lower alkylthio, or —NH—R4, wherein R4 is hydrogen, —NH2, or lower alkyl;
- or a pharmaceutically acceptable salt thereof.
A method for treating retinopathy comprising:
- administering to a subject in need thereof in an amount effective to treat retinopathy a compound of formula (I):
- wherein the 1,3-thiazole ring is optionally substituted at the 5-position;
- Y is lower alkylene, lower alkenylene or —CONH—;
- and
- Z is a group of the formula:
- wherein R2 is a group of the formula:
- (wherein G is a bond, —NHCOCH2— or lower alkylene and R4 is hydrogen, —NH2 or lower alkyl);
- —NH2;
- —CH2NH2;
- —CH2ONH2;
- —CH2ON═CH2;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.