首页> 外国专利> Ethyl-3-(2-{4-(hexyloxycarbonylamino-imino-methyl)-phenylamino-methyl}-1- methyl-1h-benzimidazol-5-carbonyl)-pyridine-2-yl-amino-propionic acid ethyl ester methane sulphonate in crystalline form ii, pharmaceutical composition comprising it and uses thereof for preparing pharmaceutical compositions which are suitable for the post-operative prophylaxis of deep vein thrombosis and the prevention of stroke and process for the preparation thereof

Ethyl-3-(2-{4-(hexyloxycarbonylamino-imino-methyl)-phenylamino-methyl}-1- methyl-1h-benzimidazol-5-carbonyl)-pyridine-2-yl-amino-propionic acid ethyl ester methane sulphonate in crystalline form ii, pharmaceutical composition comprising it and uses thereof for preparing pharmaceutical compositions which are suitable for the post-operative prophylaxis of deep vein thrombosis and the prevention of stroke and process for the preparation thereof

机译:乙基-3-[(2-{[4-(己氧基羰基氨基-亚氨基甲基)-苯基氨基]-甲基} -1-甲基-1h-苯并咪唑-5-羰基)吡啶-2-基-氨基]-丙酸结晶形式的乙酯甲烷磺酸甲酯ii,包含它的药物组合物及其在制备适合于术后预防深静脉血栓形成和预防中风的药物组合物中的用途及其制备方法

摘要

Ethyl 3-(N-(2-(4-(hexyloxycarbonylamidino)phenylaminomethyl)-1-methyl-1H-benzimidazole-5-carbonyl)-N-(2-pyridyl)amino)propionate methanesulfonate polymorph I (Ia), polymorph II (Ib) and hemihydrate (Ic), with melting points of 180+-3[deg]C, 190+-3[deg]C and 120+-5[deg]C respectively, are new. Independent claims are also included for the preparation of (Ia)-(Ic). ACTIVITY : Anticoagulant; Cerebroprotective; Vasotropic. No biological data is given. MECHANISM OF ACTION : Thrombin inhibitor.
机译:3-(N-(2-(4-(己氧基氧羰基ami基)苯基氨基甲基)-1-甲基-1H-苯并咪唑-5-羰基)-N-(2-吡啶基)氨基)丙酸酯甲磺酸盐多晶型物I(Ia),多晶型物II (Ib)和半水合物(Ic)的熔点分别为180 + -3℃,190 + -3℃和120 + -5℃。独立的权利要求也包括用于制备(Ia)-(Ic)。活性:抗凝剂;脑保护趋溶性没有给出生物学数据。作用机理:凝血酶抑制剂。

著录项

  • 公开/公告号IL173885A

    专利类型

  • 公开/公告日2015-04-30

    原文格式PDF

  • 申请/专利权人 BOEHRINGER INGELHEIM INTERNATIONAL GMBH;

    申请/专利号IL20060173885

  • 发明设计人

    申请日2006-02-23

  • 分类号A61K;A61K31/4439;A61P;A61P7/02;C07D;C07D401/12;

  • 国家 IL

  • 入库时间 2022-08-21 15:15:23

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