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1. 发明申请

WO1998015541A1 NOVEL ISOXAZOL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND A PROCESS FOR THE PREPARATION OF THE NOVEL COMPOUNDS 审中-公开
标题翻译：新型的ISOXAZOL衍生物，含有它们的药物组合物，以及制备新型化合物的方法
公开(公告)号：WO1998015541A1
公开(公告)日：1998-04-16
申请号：PCT/HU1997000059
申请日：1997-10-08
申请人： EGIS GYOGYSZERGYAR RT. , NYITRAI, József , NAGY, József , SIMIG, Gyula , GREFF, Zoltán , BLASKO, Gábor , WELLMANN, János , SZÉNASI, Gábor , GACSALYI, István , SZABADOS, Tamás , GYERTYAN, István , SCHMIDT, Éva , PALLAGI, Katalin , BILKEI-GORZO, András , TIHANYI, Károly , EGYED, András
发明人： EGIS GYOGYSZERGYAR RT.
IPC分类号： C07D261/04
CPC分类号： C07D413/12 , C07D261/04 , C07D261/08
摘要： The invention refers to novel isoxazole and 4,5-dihydroisoxazole derivatives of formula (I) being suitable for the treatment of especially a pathological alteration of the central nervous system and/or a cardiovascular and/or gastrointestinal disease, furthermore pharmaceutical compositions containing the above derivatives, and a process for the preparation of the novel compounds. Specifically, the invention refers to isoxazole derivatives of formula (I). In formula (I), A and B represent, independently, a hydrogen atom, or A forms, together with B, a valence bond; Z stands for a hydrogen atom, a halo atom, a C1-4 alkyl group, a trifluoromethyl group or one or two C1-4 alkoxy group(s); R and R mean, independently, a C1-6 alkyl group or a C3-7 cycloalkyl group; or R and R form, together with the nitrogen atom they are attached to and optionally with one or more further nitrogen and/or oxygen atom(s), a 5 to 8-membered heterocyclic ring that can be substituted by a C1-4 alkyl group, a (C1-4 alkyl) phenyl group, a (C1-4 alkoxy) phenyl group, a di(C1-4 alkoxy) phenyl group, a halophenyl group, a trifluoromethylphenyl group or a furoyl group; m has a value of 0 or 1; n has a value of 0 or 1.
摘要翻译：本发明涉及式（I）的新型异恶唑和4,5-二氢异恶唑衍生物，其特别适用于治疗中枢神经系统和/或心血管和/或胃肠道疾病的病理改变，此外，含有上述衍生物，以及制备新化合物的方法。具体地说，本发明涉及式（I）的异恶唑衍生物。在式（I）中，A和B独立地表示氢原子，或A与B键合，形成价键; Z表示氢原子，卤素原子，C1-4烷基，三氟甲基或一个或两个C1-4烷氧基; R 1和R 2独立地表示C 1-6烷基或C 3-7环烷基; 或R 1和R 2与它们连接的氮原子一起形成，并且任选地与一个或多个另外的氮原子和/或氧原子一起形成可被取代的5至8元杂环通过C 1-4烷基，（C 1-4烷基）苯基，（C 1-4烷氧基）苯基，二（C 1-4烷氧基）苯基，卤代苯基，三氟甲基苯基或糠基 ; m的值为0或1; n的值为0或1。

2. 发明申请

WO1997016429A1 NOVEL PIPERAZINYLALKYLTHIOPYRIMIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND A PROCESS FOR THE PREPARATION OF THE NOVEL COMPOUNDS 审中-公开
标题翻译：新型哌嗪二甲基乙二胺衍生物，含有它们的药物组合物和制备新型化合物的方法
公开(公告)号：WO1997016429A1
公开(公告)日：1997-05-09
申请号：PCT/HU1996000061
申请日：1996-10-25
申请人： EGIS GYOGYSZERGYAR RT. , JAKOCZI, Iván , BOZSING, Dániel , RATZNÉ SIMONEK, Ildikó , GACSALYI, István , SZÉNASI, Gábor , SCHMIDT, Éva , MIKLOSNÉ KOVACS, Anikó , BILKEI GORZO, András , BLASKO, Gábor , GYERTYAN, István , NÉMETH, Gábor , SIMIG, Gyula , TIHANYI, Károly , EGYED, András
发明人： EGIS GYOGYSZERGYAR RT.
IPC分类号： C07D239/38
CPC分类号： C07D239/22 , C07D239/38 , C07D239/47 , C07D239/48
摘要： The invention refers to novel piperazinylalkylthiopyrimidine derivatives of formula (I) being suitable for the treatment of diseases due to pathological alterations of the central nervous system, pharmaceutical compositions containing the above derivatives, and a process for the preparation of the novel compounds.
摘要翻译：本发明涉及适用于治疗由于中枢神经系统的病理改变引起的疾病的式（I）的新型哌嗪基烷基硫代嘧啶衍生物，含有上述衍生物的药物组合物及其制备方法。

3. 发明申请

WO1998017230A2 NEW 1,7,7-TRIMETHYL-BICYCLO[2.2.1]HEPTANE DERIVATIVES 审中-公开
标题翻译：新的1,7,7-三甲基双环[2.2.1] HEPTANE衍生物
公开(公告)号：WO1998017230A2
公开(公告)日：1998-04-30
申请号：PCT/HU1997000064
申请日：1997-10-16
申请人： EGIS GYOGYSZERGYAR RT. , GACSALYI, István , KLEBOVICH, Imre , BUDAI, Zoltán , LUKACS, Gyula , KAUFMANNÉ BOJTI, Erzsébet , SCHMIDT, Éva , GYERTYAN, István , BILKEI GORZO, András , BLASKO, Gábor , ABERMANN, Miklós , BALOGHNÉ NEMES, Katalin , GRÉZAL, Gyula , EGYED, András
发明人： EGIS GYOGYSZERGYAR RT.
IPC分类号： A61K00/00
CPC分类号： C07C217/12 , C07C2602/42 , Y02P20/55
摘要： The new compound of Formula (I) and salts thereof possess valuable anxiolytic properties.
摘要翻译：新的式（I）化合物及其盐具有有价值的抗焦虑性质。

4. 发明申请

WO1995023137A1 ACETIC ACID AMIDE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：乙酸酰胺衍生物及其制备方法
公开(公告)号：WO1995023137A1
公开(公告)日：1995-08-31
申请号：PCT/HU1995000003
申请日：1995-02-22
申请人： EGIS GYOGYSZERGYAR RT. , REITER, Józsefné , BUDAI, Zoltán , TAKATS, Gáborné , MEZEI, Tibor , BLASKO, Gábor , SIMIG, Gyula , EGYED, András , VIZI, E. Szilveszter , FEKETE, Márton , SZEMERÉDI, Katalin , GYERTYAN, István , GACSALYI, István
发明人： EGIS GYOGYSZERGYAR RT.
IPC分类号： C07D219/10
CPC分类号： C07D401/12 , C07D219/10 , C07D471/04
摘要： The invention relates to new acetic acid derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said acetic acid amide derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases. The new compounds according to the invention can be characterized by general formula (I), wherein R stands for hydrogen and B represents piperazino, 8-azaspiro[4,5]decane-7,9-dion-8-yl or 2-(1,2,4-triazolo[4,3-a]pyridyl-3(2H)-on-2-yl) optionally carrying an aryl, aralkyl or heteroaryl substituent, and possess valuable pharmaceutical properties, they are suitable for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及新的乙酸衍生物，其制备方法，包含其的药物组合物，使用所述乙酸酰胺衍生物用于治疗疾病和制备适用于治疗疾病的药物组合物。根据本发明的新化合物可以由通式（I）表征，其中R代表氢，B代表哌嗪子基，8-氮杂螺[4,5]癸烷-7,9-二酮-8-基或2-（任选带有芳基，芳烷基或杂芳基取代基的1,2,4-三唑并[4,3-a]吡啶基-3（2H） - 酮-2-基），并且具有有价值的药物性质，它们适用于阿尔茨海默氏病。

5. 发明申请

WO1997044334A2 NOVEL PIPERAZINE OR HOMOPIPERAZINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND A PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：新型哌嗪或异丙嗪衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：WO1997044334A2
公开(公告)日：1997-11-27
申请号：PCT/HU1997000020
申请日：1997-05-15
申请人： EGIS GYOGYSZERGYAR RT. , RATZNÉ SIMONEK, Ildikó , BOZSING, Dániel , JAKOCZI, Iván , KOVANYINÉ LAX, Györgyi , BLASKO, Gábor , SIMIG, Gyula , GACSALYI, István , SCHMIDT, Éva , MIKLOSNÉ KOVACS, Anikó , SZIRTNÉ KISZELLY, Eniko"e; , SZÉNASI, Gábor , GYERTYAN, István , EGYED, András , TIHANYI, Károly
发明人： EGIS GYOGYSZERGYAR RT.
IPC分类号： C07D295/02
CPC分类号： C07D295/185 , C07D243/08 , C07D295/096 , C07D295/135 , C07D295/155
摘要： The invention refers to novel piperazine and homopiperazine derivatives of formula (I) being suitable for the treatment of dieseases due to pathological alterations of the central nervous system, pharmaceutical compositions containing the above derivatives, and a process for the preparation of the novel compounds. In formula (I) R stands for a halo, a C1-4 alkyl group, a C1-4 alkoxy group, a trihalomethyl group, a nitro group or an amino group which latter can be substituted by a C1-4 alkyl group, and n has a value of 1 or 2, or R represents a cyano group, and n has a value of 2, m is 0, 1, 2 or 3, R , R and R mean, independently, a hydrogen, a halo, a trihalomethyl group, a C1-4 alkyl group, a C1-4 alkoxy group, a nitro group, a carboxy group, a formyl group, a hydroxy group or an amino group which latter can be substituted by a C1-4 alkyl group.
摘要翻译：本发明涉及式（I）的新型哌嗪和高哌嗪衍生物，其适用于治疗由于中枢神经系统病理改变引起的疾病，含有上述衍生物的药物组合物，以及制备新化合物的方法。在式（I）中，R 1代表卤素，C 1-4烷基，C 1-4烷氧基，三卤甲基，硝基或氨基，后者可被C 1-4烷基取代基团，n为1或2，R 1表示氰基，n为2，m为0,1,2或3，R 2，R 3和 R 4独立地表示氢，卤素，三卤代甲基，C 1-4烷基，C 1-4烷氧基，硝基，羧基，甲酰基，羟基或氨基后者可以被C 1-4烷基取代的基团。

6. 发明申请

WO1995019173A1 PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：药物组合物
公开(公告)号：WO1995019173A1
公开(公告)日：1995-07-20
申请号：PCT/HU1995000001
申请日：1995-01-13
申请人： EGIS GYOGYSZERGYAR RT. , EGYED, András , GAAL, László , GIGLER, Gábor , GROO, Dóra , GYERTYAN, István , SIMO, Annamária , SZEMERÉDI, Katalin , MANDI, Attila
发明人： EGIS GYOGYSZERGYAR RT.
IPC分类号： A61K31/485
CPC分类号： A61K31/485
摘要： The invention relates to pharmaceutical compositions containing papaverine or pharmaceutically acceptable acid addition salts thereof, which are useful for the treatment or prevention of diseases associated with the glutamatergic neurotransmission. Such diseases are e.g. the transitional ischaemic attack, cerebral or spinal embolism, thrombosis, brain infarction, anoplexy, arteriosclerosis; various degenerative disorders of the central nervous system, such as sclerosis multiplex, Parkinson's disease, Huntington's disease or dementiae of Alzheimer or other origin. Papaverine is effective also against the sequels of metabolic origin, particularly diabetes mellitus or Wilson's syndrome. The invention furthermore relates to the preparation of the above compositions as well as the use of papaverine or pharmaceutically acceptable acid addition salts thereof for the treatment and prevention of the above diseases.
摘要翻译：本发明涉及含有罂粟碱或其药学上可接受的酸加成盐的药物组合物，其可用于治疗或预防与谷氨酸能神经传递相关的疾病。这些疾病是例如过渡性缺血发作，脑或脊柱栓塞，血栓形成，脑梗死，中风，动脉硬化; 中枢神经系统的各种退行性疾病，例如硬化症多发性，帕金森病，亨廷顿氏病或阿尔茨海默氏痴呆症或其他来源的痴呆症。罂粟碱对抗代谢起源的后遗症，特别是糖尿病或威尔逊综合征也是有效的。本发明还涉及上述组合物的制备以及罂粟碱或其药学上可接受的酸加成盐在治疗和预防上述疾病中的用途。

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