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公开(公告)号:US6093720A
公开(公告)日:2000-07-25
申请号:US91260
申请日:1998-06-09
申请人: Csaba Szantay , Istvan Moldvai , Andras Vedres , Maria Incze , Janos Kreidl , Laszlo Czibula , Maria Farkas Nee Kiriak , Ida Deutsch Nee Juhasz , Aniko Gere , Margit Pellionisz Nee Paroczai , Erzsebet Lapis , Andras Szekeres , Maria Zajer Nee Balazs , Adam Sarkadi , Ferenc Auth , Bela Kiss , Egon Karpati , Sandor Farkas
发明人: Csaba Szantay , Istvan Moldvai , Andras Vedres , Maria Incze , Janos Kreidl , Laszlo Czibula , Maria Farkas Nee Kiriak , Ida Deutsch Nee Juhasz , Aniko Gere , Margit Pellionisz Nee Paroczai , Erzsebet Lapis , Andras Szekeres , Maria Zajer Nee Balazs , Adam Sarkadi , Ferenc Auth , Bela Kiss , Egon Karpati , Sandor Farkas
IPC分类号: A61K31/00 , A61K31/395 , A61K31/435 , A61K31/4353 , A61K31/4375 , A61P9/00 , A61P9/10 , A61P25/28 , C07D461/00 , C07D471/22
CPC分类号: C07D461/00
摘要: The invention relates to novel racemic and optically active trans apovincaminic acid ester derivatives of formula (I), ##STR1## wherein R means hydrogen or a group (a), wherein Z stands for C.sub.1-4 alkyl, optionally substituted aryl, aralkyl, heteroaryl or 14-eburnameninyl group; and n is an integer of 2, 3 or 4, as well as therapeutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions, and in addition, to a method of treatment. The novel compounds of Formula (I) exhibit particularly antioxidant, antiischemic as well as antiamnesic effects and are useful for inhibiting lipid peroxidation and for protection from or treatment of ischemia and amnesia as well as for treating various degenerative neurological diseases, e.g. Alzheimer's disease.
摘要翻译: PCT No.PCT / HU96 / 00075 Sec。 371日期1998年6月9日第 102(e)1998年6月9日PCT 1996年12月13日PCT PCT。 公开号WO97 / 23481 日期1997年7月3日本发明涉及式(I)的新型外消旋和光学活性反氨基丁酸酯衍生物,其中R表示氢或基团(a),其中Z表示C1-4烷基,任选取代的芳基,芳烷基 ,杂芳基或14-桦烷亚胺基; 和n为2,3或4的整数,以及其可治疗的盐。 本发明还涉及含有这些化合物的药物组合物以及制备上述化合物和组合物的方法,此外还涉及治疗方法。 式(I)的新化合物显示出特别的抗氧化,抗缺血和抗病毒作用,并且可用于抑制脂质过氧化和保护或治疗缺血和遗忘以及用于治疗各种退行性神经系统疾病,例如, 阿尔茨海默氏病。