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公开(公告)号:US4859682A
公开(公告)日:1989-08-22
申请号:US40938
申请日:1987-04-21
申请人: Tibor Keve , Gabor Megyeri , Bela Stefko , Lajos Kovacs, Jr. , Anna Kassai nee Zieger , Bela Kiss , Istvan Laszlovszky , Erzsebet Lapis , Eva Palosi , Dora Groo , Laszlo Szporny
发明人: Tibor Keve , Gabor Megyeri , Bela Stefko , Lajos Kovacs, Jr. , Anna Kassai nee Zieger , Bela Kiss , Istvan Laszlovszky , Erzsebet Lapis , Eva Palosi , Dora Groo , Laszlo Szporny
IPC分类号: A61K31/48 , A61P9/00 , A61P25/18 , C07D457/02
CPC分类号: C07D457/02
摘要: The invention relates to novel 2-halogenated 8- and 1,8-substituted ergolene derivatives of the formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## wherein X stands for a halogen;R stands for a C.sub.1-4 alkyl group andR" means a hydroxyl group; orR stands for an acyl or substituted acyl group andR" represents a halogen or an --OR' group, whereinR' stands for an acyl or substituted acyl group; orR stands for hydrogen andR" means a halogen or an --OR' group, wherein R' stands for an acyl or substituted acyl group; and the dotted line means a double bond between the 8-9 or 9-10 positions.The compounds of the formula (I) possess an antipsychotic and antihypoxic action and a negligable extrapyramidal side-effect.
摘要翻译: 本发明涉及式(I)的新型2-卤代8-和1,8-取代的麦角烯衍生物及其酸加成盐,含有它们的药物组合物及其制备方法。 在式(I)中,其中X代表卤素; R代表C 1-4烷基,R“表示羟基; 或R表示酰基或取代的酰基,R“表示卤素或-OR'基团,其中R'表示酰基或取代的酰基; 或R表示氢,R“表示卤素或-OR'基团,其中R'表示酰基或取代的酰基; 虚线表示8-9或9-10位之间的双键。 式(I)的化合物具有抗精神病和抗低氧作用和可忽略的锥体束外副作用。
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公开(公告)号:US4816587A
公开(公告)日:1989-03-28
申请号:US58576
申请日:1987-06-05
申请人: Gabor Megyeri , Tibor Keve , Lajos Kovacs, Jr. , Bela Stefko , Erik Bogsch , Anna Kassia nee Zieger , Ferenc Trischler , Gabor Szepesi , Maria Gazdag
发明人: Gabor Megyeri , Tibor Keve , Lajos Kovacs, Jr. , Bela Stefko , Erik Bogsch , Anna Kassia nee Zieger , Ferenc Trischler , Gabor Szepesi , Maria Gazdag
IPC分类号: C07B39/00 , C07B31/00 , C07C67/00 , C07D457/00 , C07D457/02 , C07D457/04 , C07D519/00 , C07D519/02
CPC分类号: C07D457/04 , C07D457/00 , C07D457/02 , C07D519/02
摘要: The invention relates to a novel process for the halogenation in 2-position of ergot alkaloids. The process is characterized by that as a halogenating agent a system consisting of dimethylsulfoxide, a trialkylhalosilane or triarylhalosilane and optionally a hydrogen halide is used.
摘要翻译: 本发明涉及麦角生物碱2-位卤化的新方法。 该方法的特征在于,作为卤化剂,使用由二甲基亚砜,三烷基卤硅烷或三芳基卤代硅烷和任选的卤化氢组成的体系。
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公开(公告)号:US4697017A
公开(公告)日:1987-09-29
申请号:US869203
申请日:1986-05-30
申请人: Gabor Megyeri , Tibor Keve , Janos Galambos , Lajos Kovacs, Jr. , Bela Stefko , Erik Bogsch , Ferenc Trischler
发明人: Gabor Megyeri , Tibor Keve , Janos Galambos , Lajos Kovacs, Jr. , Bela Stefko , Erik Bogsch , Ferenc Trischler
IPC分类号: A61K31/48 , A61P25/00 , C07D519/02
CPC分类号: C07D519/02
摘要: The invention relates to a novel process for the preparation of 2-bromo-.alpha.-ergocryptine and its acid addition salt by brominating .alpha.-ergocryptine in such a way that the bromination is carried out at room temperature by using a dimethylsulphoxide-hydrogen bromide mixture containing no more 0.02% of water and, if desired, converting the thus-obtained 2-bromo-.alpha.-ergocryptine to an acid addition salt in a known manner.
摘要翻译: 本发明涉及通过溴化α-麦角灵素的方法制备2-溴-α-麦角灵及其酸加成盐的新方法,使得溴化在室温下通过使用二甲基亚砜 - 溴化氢混合物进行,该混合物含有 不再需要0.02%的水,如果需要,以已知的方式将由此得到的2-溴-α-麦角灵转化为酸加成盐。
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