Title:
N-(CARBAMIMIDOYLPHENYL)GLYCINAMTDE DERIVATIVE, ITS PRODUCTION AND MEDICINE PREPARATION CONTAINING THE SAME
Document Type and Number:
Japanese Patent JP3236267
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To obtain the subject new compound useful as an inhibitor for blood coagulation factors and thrombin formation, or an antitumor agent.
SOLUTION: This compound is shown by formula I [E is H or OH; Q is H or an alkyl; R is a substituted aryl, a cycloalkyl or an alkyl; N(Q, R) is COOH or the like; three of X1 to X4 are each C(Ra), C(Rb) or C(Rc) and the fourth group is C(Rd) or N; Ra to Rd are each H, OH, NO2 or the like; G is an amino protecting group, one of G1 and G2 groups is H and the other is H, an alkyl or the like] such as (R,S)-N-benzyl-2-(4-benzyloxy-3- methoxyphenyl)-2-(4-carbamimidoylphenylamino)acetamide hydrochloride. The compound of the formula I is obtained by reacting an aldehyde of formula II with an isonitrile of the formula RNC and a 4-aminobenzamidine of formula III.
Inventors:
Katrin Grapeke
Yu-Foo Ji
Sabine Valbaum
Roots Weber
Jean Ackerman
Yu-Foo Ji
Sabine Valbaum
Roots Weber
Jean Ackerman
Application Number:
JP34587598A
Publication Date:
December 10, 2001
Filing Date:
December 04, 1998
Export Citation:
Assignee:
F. HOFFMANN-LA ROCHE AKTIENGESELLSCHAFT
International Classes:
A61K31/00; A61K31/155; A61K31/16; A61K31/395; A61K31/40; A61K31/403; A61K31/404; A61K31/4045; A61K31/415; A61K31/4164; A61K31/44; A61K31/4402; A61K31/4409; A61K31/47; A61K31/472; A61P35/00; A61P43/00; C07C255/59; C07C257/18; C07C259/18; C07C271/64; C07C311/08; C07D295/08; C07C311/21; C07C311/46; C07D207/16; C07D209/08; C07D209/14; C07D209/16; C07D213/30; C07D213/36; C07D213/40; C07D213/69; C07D215/14; C07D217/02; C07D217/04; C07D217/18; C07D217/26; C07D233/24; C07D233/54; C07D233/64; C07D295/092; C07D317/60; A61K31/00; (IPC1-7): C07C257/18; A61K31/155; A61K31/404; A61K31/4045; A61K31/4164; A61K31/4402; A61K31/4409; A61K31/47; A61K31/472; A61P35/00; A61P43/00; C07C255/59; C07C271/64; C07D207/16; C07D209/08; C07D209/16; C07D213/30; C07D213/69; C07D215/14; C07D217/04; C07D217/26; C07D233/64; C07D295/08
Other References:
【文献】国際公開97/30971(WO,A1)
Attorney, Agent or Firm:
Hajime Tsukuni (3 outside)