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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。

    Tetracyclic indole derivatives
    4.
    发明授权
    Tetracyclic indole derivatives 失效
    四环吲哚衍生物

    公开(公告)号：US4317912A

    公开(公告)日：1982-03-02

    申请号：US129333

    申请日：1980-03-11

    申请人： Aldemio Temperilli ,  Sergio Mantegani ,  Giuliana Arcari ,  Anna M. Caravaggi

    发明人： Aldemio Temperilli ,  Sergio Mantegani ,  Giuliana Arcari ,  Anna M. Caravaggi

    IPC分类号： C07D457/02 ,  A61K31/40 ,  A61K31/48 ,  A61P9/12 ,  C07D487/06 ,  A61K31/445 ,  A61K31/535 ,  C07D487/00

    CPC分类号： C07D487/06

    摘要： A compound is disclosed of the formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, or a carboxy, alkoxycarbonyl, piperidinocarbonyl, 1-pyrrolidinylcarbonyl, morpholinocarbonyl, carbamoyl or benzylcarbamoyl group, or an alkylcarbamoyl or dialkylcarbamoyl group in which the, or each, alkyl group has from 1 to 4 carbon atoms;R.sub.2 represents a hydrogen or fluorine atom, or a cyano, acetyl or carbamoyl group; andR.sub.3 represents a hydrogen atom or a methyl group; and represents a single or a double bond, with the proviso that R.sub.1 and R.sub.2 do not simultaneously represent hydrogen atoms;or a pharmaceutically acceptable salt thereof.

    摘要翻译： 公开了式（I）的化合物：其中R 1表示氢原子，或羧基，烷氧基羰基，哌啶子基羰基，1-吡咯烷基羰基，吗啉代羰基，氨基甲酰基或苄基氨基甲酰基，或烷基氨基甲酰基或二烷基氨基甲酰基 其中或每个烷基具有1至4个碳原子; R2表示氢或氟原子，或氰基，乙酰基或氨基甲酰基; 并且R 3表示氢原子或甲基; 并且表示单键或双键，条件是R1和R2不同时表示氢原子; 或其药学上可接受的盐。

    Ercoline derivatives and therapeutic compositions having CNS affecting activity
    5.
    发明授权
    Ercoline derivatives and therapeutic compositions having CNS affecting activity 失效
    具有CNS影响活性的Ercoline衍生物和治疗组合物

    公开(公告)号：US4382940A

    公开(公告)日：1983-05-10

    申请号：US211920

    申请日：1980-12-01

    申请人： Luigi Bernardi ,  Germano Bosisio ,  Sergio Mantegani ,  Alessandro Rossi ,  Aldemio Temperilli

    发明人： Luigi Bernardi ,  Germano Bosisio ,  Sergio Mantegani ,  Alessandro Rossi ,  Aldemio Temperilli

    IPC分类号： A61K31/48 ,  A61P9/12 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D457/02 ,  A61K31/55

    CPC分类号： C07D457/02

    摘要： Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen atom or a methoxy group;X represents an oxygen or sulphur atom or an NH or NCH.sub.3 group;R.sub.3 represents a hydrogen atom, a trifluoromethyl or phenyl group or a hydrocarbon group having from 1 to 4 carbon atoms;R.sub.4 represents a hydrogen atom, a methyl or acetyl group or a hydrocarbon having from 1 to 4 carbon atoms, or R.sub.3 and R.sub.4 together represent a 3- or 4-membered carbon atom chain;Y represents an electron-withdrawing group such as a cyano, nitro, alkylsulphonyl or alkylsulprinyl group or a group of the formula COR.sub.5 wherein R.sub.5 represents an alkyl group having from 1 to 4 carbon atoms or a phenyl, alkoxy, amino or N-substituted amino group or R.sub.5 and R.sub.3 together represent a 2- or 3-membered carbon atom chain;R.sub.6 represents a hydrocarbon group having from 1 to 4 carbon atoms or a benzyl or phenethyl group; andR.sub.7 represents a hydrogen or halogen atom or a methyl or formyl group or a group of the formula SR.sub.8 wherein R.sub.8 represents a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group;and the pharmaceutically acceptable addition salts with organic or inorganic acids thereof. A process for producing these compounds is also disclosed.These compounds are useful antidepressant, anxiolytic and neuroleptic agents. They also display from moderate to good antiprolactinic and antihypertensive activity.

    摘要翻译： 公开了式（I）的化合物：其中R 1表示氢原子或甲基; R2表示氢原子或甲氧基; X表示氧或硫原子或NH或NCH 3基团; R3表示氢原子，三氟甲基或苯基或具有1至4个碳原子的烃基; R4表示氢原子，甲基或乙酰基或具有1至4个碳原子的烃，或R3和R4一起表示3-或4-元碳原子链; Y表示吸电子基团，例如氰基，硝基，烷基磺酰基或烷基磺基，或式COR5的基团，其中R5表示具有1至4个碳原子的烷基或苯基，烷氧基，氨基或N-取代的氨基 基团或R 5和R 3一起表示2-或3-元碳原子链; R6表示具有1至4个碳原子的烃基或苄基或苯乙基; 并且R 7表示氢或卤素原子或甲基或甲酰基或式SR 8的基团，其中R 8表示具有1至4个碳原子的烃基或苯基; 和其药学上可接受的加成盐与其有机酸或无机酸。 还公开了制备这些化合物的方法。 这些化合物是有用的抗抑郁药，抗焦虑剂和抗精神病药。 它们还显示从中度到良好的促乳素和抗高血压活性。

    Pyrimidinoaminoethyl ergoline derivatives
    6.
    发明授权
    Pyrimidinoaminoethyl ergoline derivatives 失效
    嘧啶氨基乙基麦角灵衍生物

    公开(公告)号：US3996228A

    公开(公告)日：1976-12-07

    申请号：US530617

    申请日：1974-12-09

    申请人： Giuliana Arcari ,  Luigi Bernardi ,  Germano Bosisio ,  Alfredo Glasser ,  Aldemio Temperilli

    发明人： Giuliana Arcari ,  Luigi Bernardi ,  Germano Bosisio ,  Alfredo Glasser ,  Aldemio Temperilli

    IPC分类号： C07D457/02

    CPC分类号： C07D457/02

    摘要： Pyrimidinoaminoethyl ergoline derivatives of the formula: ##STR1## wherein R is hydrogen or methyl; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkyl having 1 to 3 carbon atoms, methoxy and phenyl;R.sub.3 is hydrogen, halogen, alkyl and alkoxy each having 1 to 3 carbon atoms, phenyl, nitro, amino, cyano, acylamino, carboxamido and carbalkoxy each having 1 to 3 carbon atoms, trifluoromethyl or --SO.sub.2 --Y wherein Y is hydroxyl, amino or methyl and R.sub.4 is hydrogen or methoxy are prepared by reacting an ergoline derivative of formula III and a 2-aminopyrimidine anion of formula II ##STR2##

    摘要翻译： 具有下式的嘧啶基氨基乙基麦角灵衍生物：其中R是氢或甲基; R 1和R 2独立地选自氢，具有1至3个碳原子的烷基，甲氧基和苯基; R3是氢，卤素，烷基和烷氧基，各自具有1至3个碳原子，苯基，硝基，氨基，氰基，酰氨基，甲酰胺基和碳烷氧基，各自具有1至3个碳原子，三氟甲基或-SO2-Y，其中Y是羟基， 或甲基和R 4是氢或甲氧基通过使式III的麦角灵衍生物与式II的2-氨基嘧啶阴离子反应来制备。

    N-oxide ergolines as antihypertensive agents
    8.
    发明授权
    N-oxide ergolines as antihypertensive agents 失效
    N-氧化物麦角醇作为抗高血压药

    公开(公告)号：US4859678A

    公开(公告)日：1989-08-22

    申请号：US210420

    申请日：1988-06-21

    申请人： Sergio Mantegani ,  Enzo Brambilla ,  Aldemio Temperilli ,  Daniela Ruggieri ,  Patricia Salvati

    发明人： Sergio Mantegani ,  Enzo Brambilla ,  Aldemio Temperilli ,  Daniela Ruggieri ,  Patricia Salvati

    IPC分类号： A61K31/48 ,  A61P9/12 ,  C07D457/02 ,  C07D457/12

    CPC分类号： C07D457/12 ,  C07D457/02

    摘要： An ergoline derivative of the formula I: ##STR1## wherein R.sub.1 represents hydrogen or a methyl group; R.sub.2 represents hydrogen or a halogen atom, a methyl, cyano or phenyl group or an alkylthio group having from 1 to about 4 carbon atoms; R.sub.3 represents a hydrocarbon group having from 1 to about 4 carbon atoms; R.sub.4 represents hydrogen, a phenyl group or a hydrocarbon group having from 1 to about 4 carbon atoms; wherein either (a) R.sub.6 and R.sub.7 represent a valence bond or hydrogen atoms and R.sub.8 represents a hydrogen atom or a methoxy group, or (b) R.sub.6 represents a hydrogen atom and R.sub.7 and R.sub.8 taken together represent a valence bond; W represents an oxygen atom or an imino group; A represents a group of the formula CHR.sub.5, CH.dbd.CR.sub.5 or CH.sub.2 CHR.sub.5 wherein R.sub.5 represents a hydrogen atom or an alkyl group having from 1 to about 4 carbon atoms; X represents an oxygen or sulphur atom or an imino group; and n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

    Ergoline derivatives
    9.
    发明授权
    Ergoline derivatives 失效
    二元醇衍生物

    公开(公告)号：US4657914A

    公开(公告)日：1987-04-14

    申请号：US488168

    申请日：1983-04-25

    申请人： Luigi Bernardi ,  Aldemio Temperilli ,  Sergio Mantegani ,  Gabriella Traquandi ,  Patricia Salvati

    发明人： Luigi Bernardi ,  Aldemio Temperilli ,  Sergio Mantegani ,  Gabriella Traquandi ,  Patricia Salvati

    IPC分类号： A61K31/48 ,  A61P9/12 ,  C07D457/02

    CPC分类号： C07D457/02

    摘要： There are provided ergoline compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a methyl group; R.sub.2 is a hydrogen or halogen atom, a methyl or thiomethyl group; R.sub.3 is a hydrogen atom or a methoxy group; R.sub.4 is a hydrocarbon group having from 1 to 4 carbon atoms; n is 1 or 2; each of R.sub.5 and R.sub.6 independently is a hydrogen atom, an alkyl group having from 1 to 3 carbon atoms, or a phenyl or hydroxy or alkoxy group having from 1 to 4 carbon atoms, and X is an oxygen atom or a group of the formula NR.sub.7 wherein R.sub.7 is selected from the group consisting of a hydrogen atom, an alkyl having from 1 to 4 carbon atoms and a phenyl group, or a group of the formula N.dbd.C--R.sub.8 wherein the carbon atom is positioned between the nitrogen atoms in the ring and R.sub.8 is an amino, substituted amino, methyl, phenyl, thiomethyl or mercapto group. The compounds have antihypertensive and antiprolactin activity.

    摘要翻译： 提供下式的麦角灵化合物：其中R 1是氢原子或甲基; R2是氢或卤素原子，甲基或硫代甲基; R3是氢原子或甲氧基; R4是具有1至4个碳原子的烃基; n为1或2; R 5和R 6各自独立地为氢原子，具有1至3个碳原子的烷基或具有1至4个碳原子的苯基或羟基或烷氧基，X为氧原子或式 NR7，其中R7选自氢原子，具有1至4个碳原子的烷基和苯基，或式N = C-R8的基团，其中碳原子位于氮原子之间 环和R8是氨基，取代的氨基，甲基，苯基，硫代甲基或巯基。 该化合物具有抗高血压和抗催乳素活性。