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    8-pyridazinylcarbamoyl ergolines
    3.
    发明授权
    8-pyridazinylcarbamoyl ergolines 失效
    8-哒嗪基氨基甲酰基麦角碱

    公开(公告)号：US4675404A

    公开(公告)日：1987-06-23

    申请号：US885315

    申请日：1986-07-14

    申请人： Luigi Bernardi ,  Aldemio Temperilli ,  Germano Bosisio ,  Gabriella Traquandi ,  Rosanna Eccel ,  Alessandro Rossi ,  Patricia Salvati

    发明人： Luigi Bernardi ,  Aldemio Temperilli ,  Germano Bosisio ,  Gabriella Traquandi ,  Rosanna Eccel ,  Alessandro Rossi ,  Patricia Salvati

    IPC分类号： C07D457/02 ,  C07D457/06 ,  A61K31/48

    CPC分类号： C07D457/06 ,  C07D457/02

    摘要： Ergoline derivatives of formula: ##STR1## wherein n=0,1,2; R.sub.1 =H, CH.sub.3 ; R.sub.2 =H, CH.sub.3, halogen; R.sub.3 =H, OCH.sub.3 ; R.sub.4 =hydrocarbon group and R.sub.5 is a residue of general formula II, III, IV, V, VI, VII: ##STR2## wherein R.sub.6 =H, Cl, OCH.sub.3, NR.sub.11 R.sub.12, wherein R.sub.11 and R.sub.12 =H, lower alkyl; phenyl or are bonded together to form a heterocyclic ring, R.sub.7, R.sub.8 and R.sub.9 and R.sub.10 =H or C.sub.1 -C.sub.3 alkyl, with the proviso that if R.sub.5 is of formula II and R.sub.2 =R.sub.7 =R.sub.8 =H, then R.sub.4 is not methyl or n is not 0.Pharmaceutically acceptable acid addition salts are also provided. A method for their preparation is also provided.The compounds have anti-depressive, anti-hypertensive and antiprolactin activity.

    摘要翻译： 式：其中n = 0,1,2; R1 = H，CH3; R2 = H，CH3，卤素; R3 = H，OCH3; R4 =烃基，R5是通式Ⅱ，Ⅲ，Ⅳ，Ⅴ，Ⅵ，Ⅶ的残基：其中R6 = H，Cl，OCH3，NR11R12，其中R11和R12 = H，低级烷基; 苯基或键合在一起形成杂环，R 7，R 8和R 9和R 10 = H或C 1 -C 3烷基，条件是如果R 5为式II且R 2 = R 7 = R 8 = H，则R 4不是甲基 或n不为0.还提供药学上可接受的酸加成盐。 还提供了它们的制备方法。 该化合物具有抗抑郁，抗高血压和抗催乳素活性。

    Ergoline derivatives and a process for their preparation
    6.
    发明授权
    Ergoline derivatives and a process for their preparation 失效
    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。

    Process for the production of substituted 4-thia-2,6-diaza[3.2.0]-2-heptene-7-one
    9.
    发明授权
    Process for the production of substituted 4-thia-2,6-diaza[3.2.0]-2-heptene-7-one 失效
    制备取代的4-硫杂-2,6-二氮杂{8 3.2.0 {9,2-庚烯-7-酮

    公开(公告)号：US4155911A

    公开(公告)日：1979-05-22

    申请号：US820895

    申请日：1977-08-01

    申请人： Maurizio Foglio ,  Antonino Suarato ,  Paolo Masi ,  Giovanni Franceschi ,  Giorgio Palamidessi ,  Luigi Bernardi

    发明人： Maurizio Foglio ,  Antonino Suarato ,  Paolo Masi ,  Giovanni Franceschi ,  Giorgio Palamidessi ,  Luigi Bernardi

    IPC分类号： C07D205/08 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D205/08

    摘要： A new process is disclosed for the preparation of compounds of structure: ##STR1## and are as defined herein characterized in that a compound of structure ##STR2## where R and R.sup.1 have the meanings given herein, is reacted in a suitable solvent with a haloamide in the presence of a metal oxide or a haloamide in the presence of a free radical initiator under the influence of light or heat or alternatively with a halogen in the presence of a metal oxide, to give a compound of structure: ##STR3## where R and R.sup.1 have the meanings given herein, Hal is a halogen atom; THE INTERMEDIATE COMPOUND (III) in a suitable solvent is then reacted with an appropriate nucleophilic reagent to obtain the compound IV where Z replaces Hal, where Z is defined herein;The compound (IV) is then subjected to an allylic halogenation in a suitable solvent by reacting it with a haloamide either under the influence of light alone or by heating it in the presence of a free radical initiator, to give a compound of structure: ##STR4## where R, R.sup.1 and Hal and Z have the above meanings; THE INTERMEDIATE COMPOUND (V) is then reacted with a reducing agent to give finally the desired compound (I).

    摘要翻译： 公开了用于制备结构式（I）的化合物的新方法，其定义如下，其特征在于其中R和R 1具有本文给出的含义的结构式（II）的化合物在 在金属氧化物或卤代酰胺的存在下，在自由基引发剂的存在下，在光或热的作用下，或者在卤素存在下，在金属氧化物的存在下，与卤代酰胺合适的溶剂，得到结构化合物 （III）其中R和R1具有本文给出的含义，Hal是卤素原子; 然后将合适的溶剂中的中间体化合物（III）与合适的亲核试剂反应，得到Z代替Hal的化合物IV，其中Z在本文中定义; 然后使化合物（IV）在合适的溶剂中通过与单独的光的影响下的卤代酰胺反应或通过在自由基引发剂的存在下加热使其与卤代酰胺反应，得到结构式 （V）其中R，R1，Hal和Z具有上述含义; 然后将中间体化合物（V）与还原剂反应，最终得到所需化合物（I）。

    Process for preparing azetidinone thiazolidine derivatives
    10.
    发明授权
    Process for preparing azetidinone thiazolidine derivatives 失效
    制备氮杂环丁酮噻唑烷衍生物的方法

    公开(公告)号：US4077969A

    公开(公告)日：1978-03-07

    申请号：US587090

    申请日：1975-06-16

    申请人： Luigi Bernardi ,  Maurizio Foglio ,  Giovanni Francheschi

    发明人： Luigi Bernardi ,  Maurizio Foglio ,  Giovanni Francheschi

    IPC分类号： C07D513/04

    CPC分类号： C07D513/04

    摘要： A process is disclosed for preparing azetidonethiazolidines of the formula ##STR1## where R and V are defined herein below, wherein a compound of the structure ##STR2## dissolved in a suitable solvent, is treated at about 0.degree. C with a solution of preferably anhydrous hydrochloric acid in a lower aliphatic alcohol with a slight excess of sodium cyanoborohydride.

    摘要翻译： 公开了一种制备下式定义的式“IMAGE”的氮杂环丁烷的方法，其中R和V如下文定义，其中溶解在合适溶剂中的结构式“IMAGE”的化合物在约0℃下用优选无水溶液 在低级脂族醇中加入盐酸，稍加过量氰基硼氢化钠。