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1. 发明授权

US4141899A 4,5,6,7-Tetrahydroimidazo-[4,5-c]-pyridine derivatives 失效
标题翻译： 4,5,6,7-四氢咪唑并 - {8 4,5-c {9-吡啶衍生物
公开(公告)号：US4141899A
公开(公告)日：1979-02-27
申请号：US838844
申请日：1977-10-03
申请人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Fulvio Luini , Giorgio Palamidessi , Ugo Scarponi
发明人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Fulvio Luini , Giorgio Palamidessi , Ugo Scarponi
IPC分类号： C07D471/04
CPC分类号： Y10S514/926 , Y10S514/927
摘要： New 4,5,6,7-tetrahydroimidazo-[4,5-c]-pyridine derivatives are disclosed, and more particularly derivatives of Formula I ##STR1## where R.sub.1 is hydrogen or an alkyl having from 1 to 4 carbon atoms;R.sub.2 is hydrogen, an alkyl having from 1 to 4 carbon atoms, a cycloalkyl having from 3 to 6 carbon atoms, phenyl or a heterocycle;R.sub.3 is hydrogen, a saturated or unsaturated straight or branched alkyl having from 1 to 6 carbon atoms, a cycloalkyl having from 3 to 6 carbon atoms, benzoyl or phenyl; andX is O, S or NR.sub.4 where R.sub.4 is hydrogen, an alkyl having from 1 to 4 carbon atoms, cyano, amino, nitro or acylamino;Or pharmaceutically acceptable acid addition salts thereof. Also disclosed is a process of preparing these compounds which comprises condensing an appropriate 4,5,6,7-tetrahydroimidazo-[4,5-c]-pyridine with an appropriate alkyl isocyanate, alkyl isothiocyanate or substituted S-methyl thiourea, preferably in a solvent such as ethanol, acetonitrile or dioxane, usually under reflux for from 4 to 12 hours. The products can be isolated by crystallization as free bases or as salts of pharmaceutically acceptable acids. The new compounds have proved to be well tolerated and to inhibit both the number of experimental ulcers and the gastric secretion in experimental animals. Thus, they should prove useful in the therapy of gastric and duodenal ulcers in man.
摘要翻译：公开了新的4,5,6,7-四氢咪唑并[4,5-c] - 吡啶衍生物，更具体地，其中R 1是氢或具有1至4个碳原子的烷基的式I的衍生物; R 2是氢，具有1至4个碳原子的烷基，具有3至6个碳原子的环烷基，苯基或杂环; R3是氢，具有1至6个碳原子的饱和或不饱和直链或支链烷基，具有3至6个碳原子的环烷基，苯甲酰基或苯基; 且X为O，S或NR 4，其中R 4为氢，具有1至4个碳原子的烷基，氰基，氨基，硝基或酰氨基; 或其药学上可接受的酸添加剂。还公开了制备这些化合物的方法，其包括将合适的4,5,6,7-四氢咪唑并[4,5-c] - 吡啶与适当的烷基异氰酸酯，异硫氰酸烷基酯或取代的S-甲基硫脲缩合，优选在溶剂如乙醇，乙腈或二恶烷，通常在回流下4至12小时。可以通过结晶作为游离碱或药学上可接受的酸的盐分离产物。这些新化合物已被证明是良好的耐受性，并且在实验动物中抑制实验性溃疡的数量和胃分泌。因此，它们应该证明在治疗人和十二指肠溃疡方面是有用的。

2. 发明授权

US4223146A 4,5,6,7-Tetrahydroimidazo-[4,5-c]-pyridine derivatives 失效
标题翻译： 4,5,6,7-四氢咪唑并[4,5-c] - 吡啶衍生物
公开(公告)号：US4223146A
公开(公告)日：1980-09-16
申请号：US959506
申请日：1978-11-13
申请人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Ugo Scarponi
发明人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Ugo Scarponi
IPC分类号： A61K31/4188 , A61K31/435 , A61K31/437 , A61P1/04 , A61P25/02 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/925
摘要： Compounds are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms; R.sub.2 is hydrogen or a lower alkyl having from 1 to 4 carbon atoms; and R.sub.3 is a saturated or unsaturated straight or branched alkyl having from 1 to 4 carbon atoms. A process for making such compounds is also disclosed. These compounds are useful as antiulcer agents and as inhibitors of gastric secretion.
摘要翻译：公开了通式（I）的化合物：其中R 1是具有1至4个碳原子的低级烷基; R2是氢或具有1至4个碳原子的低级烷基; 并且R 3是具有1至4个碳原子的饱和或不饱和的直链或支链烷基。还公开了制备这些化合物的方法。这些化合物可用作抗溃疡剂和胃分泌抑制剂。

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

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。

5. 发明授权

US4196288A Ergoline derivatives and a process for their preparation 失效
标题翻译：艾尔莫林衍生物及其制备方法
公开(公告)号：US4196288A
公开(公告)日：1980-04-01
申请号：US856536
申请日：1977-12-01
申请人： Enzo Beacco , Luigi Bernardi , Enrico Di Salle , Giovanni Falconi , Bianca Patelli
发明人： Enzo Beacco , Luigi Bernardi , Enrico Di Salle , Giovanni Falconi , Bianca Patelli
IPC分类号： A61K31/48 , A61K31/495 , A61K31/505 , C07D457/02
CPC分类号： C07D457/02
摘要： New ergoline derivatives are disclosed which are compounds of formula (I) having the structure: ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or methyl; andX is hydroxy, R.sub.3 COO, S--R.sub.4 or NR.sub.5 R.sub.6 in which R.sub.3 is a straight or branched alkyl having from 1 to 6 carbon atoms, unsubstituted- or substituted-phenyl, the substituents being selected from the class consisting of chlorine, bromine, alkyl or alkoxy having from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, or a heterocycle;R.sub.4 is phenyl or a heterocycle, andR.sub.5 and R.sub.6 are alkyl having from 1 to 4 carbon atoms, or together with the N atom to which they are attached, forming a heterocycle. The heterocycle may be a 5- or 6-membered ring which contains from 1 to 3 hetero atoms selected from the class consisting of nitrogen, oxygen and sulphur, and may be saturated or unsaturated, and unsubstituted or substituted by halogen, alkyl having from 1 to 3 carbon atoms, hydroxy, nitro, amino, CONHNH.sub.2 and COOH.
摘要翻译：公开了新的麦角灵衍生物，其是具有以下结构的式（I）的化合物：其中R 1是氢或甲氧基; R2是氢或甲基; 并且X是羟基，R 3 COO，S-R 4或NR 5 R 6，其中R 3是具有1至6个碳原子的直链或支链烷基，未取代或取代的苯基，所述取代基选自氯，溴，烷基或具有1至4个碳原子的烷氧基，含3至6个碳原子的环烷基或杂环; R 4是苯基或杂环，R 5和R 6是具有1至4个碳原子的烷基，或与它们相连的N原子一起形成杂环。杂环可以是含有1至3个选自氮，氧和硫的杂原子的5或6元环，并且可以是饱和或不饱和的，未取代的或被卤素取代的烷基，具有1个至3个碳原子，羟基，硝基，氨基，CONHNH 2和COOH。

6. 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。

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