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1. 发明授权

US4252948A Ergoline derivatives 失效
标题翻译：二元醇衍生物
公开(公告)号：US4252948A
公开(公告)日：1981-02-24
申请号：US21671
申请日：1979-03-19
申请人： Luigi Bernardi , Carlo Elli , Giovanni Falconi , Alberto Bonsignori
发明人： Luigi Bernardi , Carlo Elli , Giovanni Falconi , Alberto Bonsignori
IPC分类号： C07D457/02
CPC分类号： C07D457/02 , Y10S514/823
摘要： Pyridazinyl-ergoline compounds having neuroleptic activity are obtained by reacting an 8.beta.-tosylmethyl ergoline with the sodium derivative of an aminopyridazine or a mercaptopyridazine in a dipolar aprotic solvent.
摘要翻译：通过使8β-甲苯基甲基麦角灵与氨基哒嗪或巯基哒嗪的钠衍生物在偶极非质子溶剂中反应，得到具有精神抑制活性的哒嗪基 - 麦角灵化合物。

2. 发明授权

US4166911A Pyridazinyl-ergoline compounds having neuroleptic activity 失效
标题翻译：具有精神抑制活性的哒嗪基 - 麦角灵化合物
公开(公告)号：US4166911A
公开(公告)日：1979-09-04
申请号：US870095
申请日：1978-01-17
申请人： Luigi Bernardi , Carlo Elli , Giovanni Falconi , Alberto Bonsignori
发明人： Luigi Bernardi , Carlo Elli , Giovanni Falconi , Alberto Bonsignori
IPC分类号： C07D457/02 , A61K31/50
CPC分类号： C07D457/02 , Y10S514/823
摘要： Pyridazinyl-ergoline compounds having neuroleptic activity are obtained by reacting an 8.beta.-tosylmethyl ergoline with the sodium derivative of an amino-pyridazine or a mercaptopyridazine in a dipolar aprotic solvent.
摘要翻译：通过使8β-甲苯基甲基麦角灵与氨基哒嗪或巯基哒嗪的钠衍生物在偶极非质子溶剂中反应，得到具有精神抑制活性的哒嗪基 - 麦角灵化合物。

3. 发明授权

US4089862A Pyridyl substituted ergoline derivatives 失效
标题翻译：吡啶基取代麦角灵衍生物
公开(公告)号：US4089862A
公开(公告)日：1978-05-16
申请号：US756725
申请日：1977-01-04
申请人： Luigi Bernardi , Carlo Elli , Giovanni Falconi , Rosella Ferrari
发明人： Luigi Bernardi , Carlo Elli , Giovanni Falconi , Rosella Ferrari
IPC分类号： A61K31/48 , A61P7/02 , C07D457/02
CPC分类号： C07D457/02 , Y10S514/822
摘要： A process is disclosed for the preparation of a compound of the formula I ##STR1## where R is hydrogen or methyl, X is sulphur or the NH group, Y is selected from the class consisting of methyl, methoxy, chlorine, bromine, iodine, nitro or cyano, m is 0, 1 or 2, and n is 1 or 2, characterized in that a compound of the formula II: ##STR2## where R and n have the above-mentioned meanings, is reacted in a suitable polar aprotic solvent, such as dimethylforamide or dimethylsulphoxide, under a nitrogen atmosphere and at a temperature between 50.degree. and 100.degree. C, with the sodium salt of an appropriate 2-aminopyridine or 2-mercaptopyridine to give, after evaporation of the solvent in vacuo, the desired compound of formula I which is then purified by methods known "per se".The invention also includes the compounds of general formula I, where R, X, Y, m and n have the same meanings, and their pharmaceutically acceptable salts. These compounds have good alpha-adrenoyltic activity, and especially a very high and unexpected platelets aggregating inhibiting activity compared to e.g. nicergoline.
摘要翻译：公开了制备式I的化合物的方法，其中R是氢或甲基，X是硫或NH基，Y选自甲基，甲氧基，氯，溴，碘硝基或氰基，m为0,1或2，n为1或2，其特征在于其中R和n具有上述含义的式II化合物以适合的方式反应极性非质子溶剂如二甲基甲酰胺或二甲基亚砜，在氮气氛下，在50至100℃的温度下，加入适当的2-氨基吡啶或2-巯基吡啶的钠盐，在真空下蒸发溶剂后得到，所需的式I化合物，然后通过本身已知的方法纯化。

4. 发明授权

US4123613A Substituted pyrazines as inhibitors of platelet aggregation 失效
标题翻译：取代的吡嗪作为血小板聚集的抑制剂
公开(公告)号：US4123613A
公开(公告)日：1978-10-31
申请号：US799167
申请日：1977-05-23
申请人： Luigi Bernardi , Carlo Elli , Giovanni B. Falconi , Rosella Ferrari
发明人： Luigi Bernardi , Carlo Elli , Giovanni B. Falconi , Rosella Ferrari
IPC分类号： A61K31/48 , A61P7/02 , C07D457/02 , C07D241/18
CPC分类号： C07D457/02 , Y10S514/822
摘要： Novel substituted pyrazine derivatives are disclosed having the general formula (I): ##STR1## where R.sub.1 and R.sub.2 may be methyl, methoxy, halogen (particularly chlorine, bromine or fluorine), or hydrogen, with the proviso that R.sub.1 and R.sub.2 cannot both be hydrogen, and X may be S or NH.These novel substituted pyrazine derivatives show a remarkable activity as inhibitors of platelet aggregation at very low dosages.
摘要翻译：公开了具有通式（I）的新型取代的吡嗪衍生物：其中R 1和R 2可以是甲基，甲氧基，卤素（特别是氯，溴或氟）或氢，但条件是R 1和R 2 不能都是氢，X可以是S或NH。

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