公开(公告)号：US09249115B2

公开(公告)日：2016-02-02

申请号：US13976544

申请日：2011-11-08

申请人： Olga Sergejevna Veselkina ,  Nikolay Borisovich Viktorov ,  Nikolay Nikolaevich Petrishchev ,  Yuliya Vyacheslavovna Poplavskaya

发明人： Olga Sergejevna Veselkina ,  Nikolay Borisovich Viktorov ,  Nikolay Nikolaevich Petrishchev ,  Yuliya Vyacheslavovna Poplavskaya

IPC分类号： C07D295/195 ,  C07D295/096 ,  A61K31/495 ,  C07D295/08 ,  C07D295/14 ,  C07D295/18 ,  C07D295/22 ,  C07D295/26

CPC分类号： C07D295/096 ,  A61K31/495 ,  C07D295/08 ,  C07D295/14 ,  C07D295/18 ,  C07D295/195 ,  C07D295/22 ,  C07D295/26

摘要： The invention relates to derivatives of N,N′-substituted piperazines of the general formula (I): where R1 and R2 denote linear or branched (C1-C4)alkyl, linear or branched (C1-C4)alkoxy, CH3C(═O)O or halogen; n=1-5; m=0-3; Z denotes CH2, C═O or SO2; X denotes C(═NH)NH2, C(═NH)NHC(═NH)NH2 or CH2(CHR3)pCH2SO3H, where R3 denotes H, OH, CH3C(═O)O or HOSO2O and p=0-1; and G denotes low-molecular-weight organic or mineral acid, sodium, potassium or ammonium cations, or water. Said derivatives have antiaggregant, anticoagulant and vasodilatory properties. The invention further relates to a method for producing said derivatives by reacting N-substituted piperazines either with carboxamide amidating agents or salts thereof, or with haloalkyl sulfonic acids or salts thereof in organic solvents or in water in the presence of bases. The compounds may be used for the prophylaxis and treatment of disorders of the hemostatic system.

摘要翻译： 本发明涉及通式（I）的N，N'-取代哌嗪衍生物：其中R1和R2表示直链或支链（C1-C4）烷基，直链或支链（C1-C4）烷氧基，CH3C（= O） ）O或卤素; n = 1-5; m = 0-3; Z表示CH 2，C = O或SO 2; X表示C（= NH）NH 2，C（= NH）NHC（= NH）NH 2或CH 2（CHR 3）p CH 2 SO 3 H，其中R 3表示H，OH，CH 3 C（= O）O或HOSO 2 O，p = G表示低分子量有机或无机酸，钠，钾或铵阳离子或水。 所述衍生物具有抗凝血，抗凝血和血管扩张性质。 本发明还涉及通过使N-取代的哌嗪与羧酰胺酰胺化剂或其盐，或其卤代烷基磺酸或其盐在有机溶剂中或在碱存在下反应生成所述衍生物的方法。 该化合物可用于预防和治疗止血系统疾病。

公开(公告)号：US20130267707A1

公开(公告)日：2013-10-10

申请号：US13976544

申请日：2011-11-08

申请人： Olga Sergejevna Veselkina ,  Nikolay Borisovich Viktorov ,  Nikolay Nikolaevich Petrishchev ,  Yuliya Vyacheslavovna Poplavskaya

发明人： Olga Sergejevna Veselkina ,  Nikolay Borisovich Viktorov ,  Nikolay Nikolaevich Petrishchev ,  Yuliya Vyacheslavovna Poplavskaya

IPC分类号： C07D295/096 ,  C07D295/14 ,  C07D295/26 ,  C07D295/195

CPC分类号： C07D295/096 ,  A61K31/495 ,  C07D295/08 ,  C07D295/14 ,  C07D295/18 ,  C07D295/195 ,  C07D295/22 ,  C07D295/26

摘要： The invention relates to derivatives of N,N′-substituted piperazines of the general formula (I): where R1 and R2 denote linear or branched (C1-C4)alkyl, linear or branched (C1-C4)alkoxy, CH3C(═O)O or halogen; n=1-5; m=0-3; Z denotes CH2, C═O or SO2; X denotes C(═NH)NH2, C(═NH)NHC(═NH)NH2 or CH2(CHR3)pCH2SO3H, where R3 denotes H, OH, CH3C(═O)O or HOSO2O and p=0-1; and G denotes low-molecular-weight organic or mineral acid, sodium, potassium or ammonium cations, or water. Said derivatives have antiaggregant, anticoagulant and vasodilatory properties. The invention further relates to a method for producing said derivatives by reacting N-substituted piperazines either with carboxamide amidating agents or salts thereof, or with haloalkyl sulfonic acids or salts thereof in organic solvents or in water in the presence of bases. The compounds may be used for the prophylaxis and treatment of disorders of the hemostatic system.

摘要翻译： 本发明涉及通式（I）的N，N'-取代哌嗪衍生物：其中R 1和R 2表示直链或支链（C 1 -C 4）烷基，直链或支链（C 1 -C 4）烷氧基，CH 3 C（= O ）O或卤素; n = 1-5; m = 0-3; Z表示CH 2，C = O或SO 2; X表示C（= NH）NH 2，C（= NH）NHC（= NH）NH 2或CH 2（CHR 3）pCH 2 SO 3 H，其中R 3表示H，OH，CH 3 C（= O）O或HOSO 2 O，p = G表示低分子量有机或无机酸，钠，钾或铵阳离子或水。 所述衍生物具有抗凝血，抗凝血和血管扩张性质。 本发明还涉及通过使N-取代的哌嗪与羧酰胺酰胺化剂或其盐，或其卤代烷基磺酸或其盐在有机溶剂中或在碱存在下反应生成所述衍生物的方法。 该化合物可用于预防和治疗止血系统疾病。