Acylated 4-amidino-and-4-guanidinobenzylamines for inhibition of plasma kallikrein
申请人:Sturzebecher Jorg
公开号:US20060148901A1
公开(公告)日:2006-07-06
The invention relates to the use of acylated 4-amidino- or 4-guanidinobenzylamine in accordance with the general formula I
P4-P3-P2-P1 (I),
where P4 is a monosubstituted or polysubstituted or unsubstituted benzylsulfonyl group, P3 is a monosubstituted or polysubstituted or unsubstituted, natural or unnatural α-amino acid or α-imino acid in the D configuration, P2 is a monosubstituted or polysubstituted or unsubstituted, natural or unnatural α-amino acid or α-imino acid in the L configuration, and P1 is a monosubstituted or polysubstituted or unsubstituted 4-amidino- or 4-guanidinobenzylamine group, for inhibiting plasma kallikrein (PK), factor XIa and factor XIIa, in particular for preventing the activation of coagulation at synthetic surfaces and for systemic administration as anticoagulants/-antithrombotic agents, in particular for preventing the activation of coagulation at synthetic surfaces for the purpose of averting thromboembolic events.
本发明涉及使用通式IP4-P3-P2-P1的酰化4-氨基酰胺或4-鸟氨酰胺苯甲胺,其中,P4是单取代、多取代或未取代的苯甲磺酰基,P3是单取代、多取代或未取代的天然或非天然的D构型α-氨基酸或α-亚氨酸,P2是单取代、多取代或未取代的天然或非天然的L构型α-氨基酸或α-亚氨酸,P1是单取代、多取代或未取代的4-氨基酰胺或4-鸟氨酰胺苯甲胺基团,用于抑制血浆激酶(PK)、XIa因子和XIIa因子,特别是用于在合成表面上预防凝血的激活和全身给药作为抗凝血剂/-抗血栓剂,特别是用于预防在合成表面上凝血的激活以避免血栓栓塞事件的发生。