Patent number: 6960575
Abstract: A compound having 3-oxo-3, 4-dihydro-2H-1, 4-thiazine 4-tetrahydropyrazine as a main skeleton. The compound is a chymase inhibitor and is represented by the following formula [I] and salts thereof: In the formula [I], X is S; R1 and R2 are H, alkyl, cycloalkyl or aryl; R3 and R4 are H, alkyl, cycloalkyl, aryl or an aromatic heterocycle; R5 is H, alkyl, cycloalkyl, aryl or -A3-A4-R7; R6 is H, alkyl, cycloalkyl, hydroxy, alkoxy, aryl, aryloxy or an aromatic heterocycle; R7 is H, alkyl, hydroxy, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle; A1 is alkylene; A2 is carbonyl or sulfonyl; A3 is alkylene; A4 is carbonyl or oxalyl; and n is 0 or 1.
Type:
Grant
Filed:
November 13, 2003
Date of Patent:
November 1, 2005
Assignee:
Santen Pharmaceutical Co., Ltd.
Inventors:
Kazuo Nishimura, Masakazu Ban, Ken-ichi Fujimura, Naoyuki Kobayashi, Masanori Hori, Takahiro Honda, Eiko Matsumoto, Junzo Matsumoto
Patent number: 6713472
Abstract: A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R6—(A2)n—N, R1 and R2 are H, alkyl, cycloalkyl or aryl, R3 and R4 are H, alkyl, cycloalkyl, aryl or aromatic heterocycle, R5 is H, alkyl, cycloalkyl, aryl or —A3—A4—R7, R6 is H, alkyl, cycloalkyl, OH, alkoxy, aryl, aryloxy or an aromatic heterocycle, R7 is H, alkyl, OH, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle, A1 is alkylene, A2 is carbonyl or sulfonyl, A3 is alkylene, A4 is carbonyl or oxalyl and n is o or 1.
Type:
Grant
Filed:
January 18, 2002
Date of Patent:
March 30, 2004
Assignee:
Santen Pharmaceutical Co., Ltd.
Inventors:
Kazuo Nishimura, Masakazu Ban, Ken-ichi Fujimura, Naoyuki Kobayashi, Masanori Hori, Eiko Matsumoto
