Title:
ANILINE DERIVATIVE HAVING INHIBITING ACTIVITY AGAINST NITROGEN MONOXIDE SYNTHETASE
Document Type and Number:
Japanese Patent JP3655685
Kind Code:
B2
Abstract:
PURPOSE: To obtain a new compound having strong inhibiting activity against a nitrogen monoxide synthetase and useful as a curing agent or an analgesic for cerebrovascular lesion, Alzheimer's disease, a septic shock, etc.
CONSTITUTION: A compound of formula I [R1 is SR6 or NR7R8 (R6 is a straight or a branched chain 1-6C alkyl or a straight or branched chain 2-6C alkyl; R7 is H, nitro, etc.; R8 is a straight or a branched chain 1-6C alkyl); R2 is H, carboxyl, etc.; R3 is H or forms a 3-8 membered ring together with R2, etc.; R4 is H, nitro, etc.; R5 is H, an amino, etc.; Y1 to Y4 are each H, a halogen, etc.; (n) and (m) are each 0,1], a stereo isomer, an optically active compound or a salt of these compounds, e.g. N-{1-[3-(S-methylisothioureido) phenyl]ethyl}amine. The compound of formula I, in which R1 is SR6, is obtained by reacting a compound of formula II with thiophosgene in the presence of a base in an inactive solvent, treating the reaction product with a concentrated aqueous ammonium solution and subsequently converting the product to a quaternary ammonium salt followed by the reaction with a compound of the formula R6X (X is Br or I).
Inventors:
Toshio Honda
Makino Toshihiko
Toshiaki Nagato
Kito Yasushi
Kimura Nobuaki
Makino Toshihiko
Toshiaki Nagato
Kito Yasushi
Kimura Nobuaki
Application Number:
JP35502595A
Publication Date:
June 02, 2005
Filing Date:
December 12, 1995
Export Citation:
Assignee:
Chugai Pharmaceutical Co., Ltd.
International Classes:
A61K31/155; A61K31/195; A61K31/21; A61K31/215; A61K31/27; A61K31/275; A61K31/40; A61P3/00; A61P3/14; A61P9/00; C07D295/12; A61P43/00; C07C57/30; C07C205/11; C07C205/12; C07C205/19; C07C205/37; C07C205/56; C07C211/52; C07C211/53; C07C271/10; C07C279/18; C07C279/30; C07C279/34; C07C279/36; C07C335/16; C07C335/20; C07C335/22; C07C335/32; C07C335/36; C07C381/14; C07D209/48; C07D295/135; (IPC1-7): C07C335/32; A61K31/155; A61K31/215; C07C205/11; C07C211/52; C07C211/53; C07C271/10; C07C279/18; C07C279/34; C07D295/12
Domestic Patent References:
| JP62158249A | ||||
| JP5152152A | ||||
| JP5299227A | ||||
| JP5931757A | ||||
| JP5973574A | ||||
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Foreign References:
| US3641040 |
Attorney, Agent or Firm:
Kazuo Shamoto
Shosuke Imai
Tadashi Masui
Yasushi Kobayashi
Hiroyuki Tomita
Shosuke Imai
Tadashi Masui
Yasushi Kobayashi
Hiroyuki Tomita
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