Thienotriazolodiazepine compound and pharmaceutical use thereof
AssigneeYoshitomi Pharmaceutical Industries, Ltd.
InventorsMinoru Moriwaki, Hiroyuki Kitani, Syuji Ehara, Hirotsugu Komatsu, Mariko Amano
Life of this patent
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Abstract
N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno 3,2-f!1,2,4!triazolo4,3-a!1,4!diazepin-6-yl )-N'- (2-methoxyphenyl)urea, optical isomers thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention strongly and selectively inhibit the expression of VCAM-1 and have an inhibitory effect on leukocyte adhesion to vascular endothelial cells. Accordingly, the compounds of the present invention can be used as cell adhesion inhibitors for prophylaxis or treatment of various diseases in which cell adhesion is involved in the onset and progress thereof.
Claims12
N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno 3,2- f!1,2,4!triazolo4,3-a!1,4!diazepin-6-yl)-N'-(2- methoxyphenyl)urea, an optical isomer thereof or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising N-(4-(4-chloro- phenyl)-2,3,9-trimethyl-6H-thieno3,2-f!1,2,4!triazolo4,3-a!- 1,4!diazepin-6-yl)-N'-(2-methoxyphenyl)urea, an optical isomer thereof or a pharmaceutically acceptable salt thereof, and an additive for pharmaceuticals.
A method for inhibiting VCAM-1 expression in a human, comprising administering N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H- thieno3,2-f!1,2,4!triazolo4,3-a!1,4!diazepin-6-yl)-N'-(2- methoxyphenyl)urea, an optical isomer thereof or a pharmaceutically acceptable salt thereof.
A method for the prophylaxis or treatment of rhinitis in a human, comprising administering N-(4-(4-chlorophenyl)-2,3,9- trimethyl-6H-thieno3,2-f!1,2,4!triazolo4,3-a!1,4!diazepin-6- yl)-N'-(2-methoxyphenyl)urea, an optical isomer thereof or a pharmaceutically acceptable salt thereof.
A method for the prophylaxis or treatment of dermatitis in a human, comprising administering N-(4-(4-chlorophenyl)-2,3,9- trimethyl-6H-thieno3,2-f!1,2,4!triazolo4,3-a!1,4!diazepin-6- yl)-N'-(2-methoxyphenyl)urea, an optical isomer thereof or a pharmaceutically acceptable salt thereof.
A method for the prophylaxis or treatment of asthma in a human, comprising administering N-(4-(4-chlorophenyl)-2,3,9- trimethyl-6H-thieno3,2-f!1,2,4!triazolo4,3-a!1,4!diazepin-6- yl)-N'-(2-methoxyphenyl)urea, an optical isomer thereof or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.