| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new compound having platelet aggregation inhibiting action. SOLUTION: This compound is represented by formula I [R<1> and R<2> are each H, a lower alkyl, etc.; R<3> is H, a lower alkyl, a lower alkenyl, etc.; R<4> is H, a lower alkyl, etc.; R<5> is H, etc.; P and Q are each a lower alkyl or P and Q form a cycloalkyl together with C; X is N or C; Y1 and Y2 are each H, a lower alkyl, a halogen, etc.; (m) is 0-2] or its salt, e.g. N-(N-4- amidinobenzoyl-α, α-dimethyl-β-alanyl)-4-piperidine acetate. The compound of formula I is obtained by binding an amidinobenzoic part of formula II to a substituted β-amino acid residue part of formula III and a pyridine or piperazine part of formula IV. The compound of formula I is competitive to a fibrinogen receptor and exhibits a high platelet aggregation inhibiting action and is excellent in no influence on the stability of an in vivo proteolytic enzyme and in oral absorbing property. The compound is effective in improvement of platelet thrombosis, thromboembolism and re-occlusion, unstable angina pectoris, cardiac infarction and peripheral circulation blood flow. |
