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156 条记录 (耗时 0.027 秒)

    Novel ergol-8-ene and ergolin compounds and process for preparing same
    41.
    发明授权
    Novel ergol-8-ene and ergolin compounds and process for preparing same 失效
    新型麦角苷8-烯和麦角蛋白化合物及其制备方法

    公开(公告)号：US4299836A

    公开(公告)日：1981-11-10

    申请号：US167341

    申请日：1980-07-10

    申请人： Erzsebet Mago nee Karacsony ,  Lajos Toldy ,  Jozsef Borsy ,  Laszlo Tardos ,  Ildiko Kiraly ,  Andras Ronay

    发明人： Erzsebet Mago nee Karacsony ,  Lajos Toldy ,  Jozsef Borsy ,  Laszlo Tardos ,  Ildiko Kiraly ,  Andras Ronay

    IPC分类号： A61K31/48 ,  A61P9/12 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D457/02

    CPC分类号： C07D457/02

    摘要： The invention relates to new ergol-8-ene and ergoline derivatives of the general formula /I/ ##STR1## wherein x y stands for --CH.dbd.C.dbd. or --CH.sub.2 --CH.dbd. group,R stands for hydrogen atom or methyl group,R.sub.1 stands for hydrogen or halogen atom,R.sub.2 stands for lower alkylsulfonyloxy group, phenylsulfonyloxy group optionally substituted with a lower alkyl group, or azido group,R.sub.3 stands for lower alkylsulfonyloxy group or phenylsulfonyloxy group optionally substituted with a lower alkyl group, and acid addition salts thereof. These compounds can be prepared from compounds of the general formula II ##STR2## wherein x y and R are as defined above, by reacting at least two equivalents of a lower alkylsulfonic acid chloride or phenylsulfonic acid chloride substituted with lower alkyl group. The resulting compound can be reacted with an alkali metal azide, and, if desired, the compound obtained is treated with a halogenating agent to form the 2-halogenide derivative, and, if desired, any resulting compound of general formula I is treated with an acid to form a therapeutically acceptable acid addition salt, or the free base is liberated from a salt.The compounds of general formula I possess valuable antiserotonine, antidepressant, dopamine receptor stimulant and hypotensive effects.

    摘要翻译： 本发明涉及通用化合物/ I / IMAGE> / I /的新的麦角8-ene和麦角灵衍生物，其中xy代表-CH = C =或-CH 2 -CH =基团，R代表氢原子或甲基 基团，R1代表氢或卤素原子，R2代表低级烷基磺酰氧基，任选被低级烷基取代的苯基磺酰氧基或叠氮基，R3代表低级烷基磺酰氧基或任选被低级烷基取代的苯基磺酰氧基， 其加成盐。 这些化合物可以通过使至少两当量的低级烷基磺酰氯或被低级烷基取代的苯基磺酰氯反应，由通式II＆lt; IMAGE＆gt; / II /的化合物制备，其中x y和R如上定义。 所得化合物可以与碱金属叠氮化物反应，如果需要，用卤化剂处理所得化合物以形成2-卤化物衍生物，如果需要，将所得到的通式I化合物用 酸形成治疗上可接受的酸加成盐，或游离碱从盐中释放出来。 通式I的化合物具有有价值的抗塞冬糖，抗抑郁药，多巴胺受体兴奋剂和降血压作用。

    Biologically active new 8.beta.-hydrazinomethyl-ergoline derivatives and a process for the preparation thereof
    43.
    发明授权
    Biologically active new 8.beta.-hydrazinomethyl-ergoline derivatives and a process for the preparation thereof 失效
    生物活性的新的8β-肼基甲基 - 麦角灵衍生物及其制备方法

    公开(公告)号：US4235912A

    公开(公告)日：1980-11-25

    申请号：US21947

    申请日：1979-03-19

    申请人： Tivadar Rettegi ,  Erzsebet Mago nee Karacsony ,  Lajos Toldy ,  Jozsef Borsi ,  Laszlo Tardos

    发明人： Tivadar Rettegi ,  Erzsebet Mago nee Karacsony ,  Lajos Toldy ,  Jozsef Borsi ,  Laszlo Tardos

    IPC分类号： A61K31/48 ,  A61P9/12 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D457/02

    CPC分类号： C07D457/02

    摘要： The invention relates to new 8.beta.-hydrazinomethyl-ergoline derivatives of the general formula (I), ##STR1## wherein x y stands for a ##STR2## or ##STR3## group, R stands for hydrogen or methyl group, andR.sub.1 stands for hydrogen, a lower acyl group, a di-(lower-alkylaminocarbonyl group, a group of the general formula (VI), ##STR4## wherein Z.sub.1, Z.sub.2 and Z.sub.3 each represent hydrogen, halogen or a trifluoromethyl group, or a group of the general formula (VII), ##STR5## wherein Y represents a lower alkyl group, allyl group or phenyl group, and acid addition salts thereof. These compounds possess valuable antiserotonine, antidepressant and hypotensive effects, furthermore they can be applied as starting substances in the preparation of other biologically active ergoline derivatives.The new compounds of the general formula (I) are prepared according to the invention by reacting the respective 6-methyl-8.beta.-mesyloxymethyl or -tosyloxymethyl-ergoline derivatives with dry hydrazine. In order to obtain the N-substituted hydrazinomethyl compounds, the N-unsubstituted derivatives are reacted with an acylating agent or with an isothiocyanate.

    摘要翻译： 本发明涉及通式（I）的新的8β-肼基甲基 - 麦角灵衍生物，其中xy代表或基团，R代表氢或甲基，R1表示 代表氢，低级酰基，二 - （低级烷基氨基羰基，通式（VI）的基团，其中Z 1，Z 2和Z 3各自表示氢，卤素或三氟甲基， 或者通式（VII）的基团，其中Y代表低级烷基，烯丙基或苯基，及其酸加成盐，这些化合物具有有价值的抗塞冬糖，抗抑郁药和降压作用，而且它们 可以将其用作制备其它生物活性麦角灵衍生物的起始物质，通式（I）的新化合物根据本发明通过使各自的6-甲基-8β-甲氧基甲基或 - 苯甲氧基甲基 - 麦角灵衍生物 用干肼。 为了得到N-取代的肼基甲基化合物，N-未取代的衍生物与酰化剂或异硫氰酸酯反应。

    6-Methyl-and 1,6-dimethyl-8.beta.-carbobenzyloxy-aminomethyl-10.alpha.-ergoline as inhibitors of prolactin secretion
    45.
    发明授权
    6-Methyl-and 1,6-dimethyl-8.beta.-carbobenzyloxy-aminomethyl-10.alpha.-ergoline as inhibitors of prolactin secretion 失效
    6-甲基 - 和1,6-二甲基-8（62-羰基苄氧基 - 氨基甲基-10（60-麦角灵）作为催乳素分泌的抑制剂

    公开(公告)号：US4151283A

    公开(公告)日：1979-04-24

    申请号：US810872

    申请日：1977-06-28

    申请人： Enrico DI Salle ,  Claudio Praga ,  Erminia Castegnaro

    发明人： Enrico DI Salle ,  Claudio Praga ,  Erminia Castegnaro

    IPC分类号： C07D457/02

    CPC分类号： C07D457/02

    摘要： A method is disclosed for inhibiting prolactin secretion in a female mammal which comprises administering to the mammal an effective dose of 6-methyl-8.beta.-carbobenzyloxy-aminomethyl-10.alpha.-ergoline, or 1,6-dimethyl-8.beta.-carbobenzyloxy-aminomethyl-10.alpha.-ergoline, or a pharmaceutically acceptable acid addition salt thereof.

    摘要翻译： 公开了一种用于抑制雌性哺乳动物中的催乳素分泌的方法，其包括向哺乳动物施用有效剂量的6-甲基-8β-羰基苄氧基 - 氨基甲基-10α-麦角蛋白或1,6-二甲基-8β-苄氧羰基 - 氨基甲基-10α-麦角林，或其药学上可接受的酸加成盐。

    Pyrrole-carboxylic acids lumilysergol esters
    47.
    发明授权
    Pyrrole-carboxylic acids lumilysergol esters 失效
    吡咯羧酸lumilysergol酯

    公开(公告)号：US3966739A

    公开(公告)日：1976-06-29

    申请号：US232605

    申请日：1972-03-07

    申请人： Luigi Bernardi ,  Germano Bosisio ,  Gian Carlo Fregnan

    发明人： Luigi Bernardi ,  Germano Bosisio ,  Gian Carlo Fregnan

    IPC分类号： C07D457/02

    CPC分类号： C07D457/02

    摘要： Esters of 1-methyl-lumilysergol-10-methylether having the formula: ##SPC1##Wherein R is selected from the group consisting of 2-furanoyl and the pyrrole group of the formula: ##SPC2##Wherein Y is selected from the group consisting of hydrogen, lower alkyl having from 1 to 6 carbon atoms and phenyl; R.sub.1 is selected from the group consisting of hydrogen, methyl and carbonyl; R.sub.2 is selected from the group consisting of hydrogen, methyl, halogen and carbonyl, provided that only one of R.sub.1 and R.sub.2 can be carbonyl; R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen, halogen, alkyl, alkoxy having from 1 to 6 carbon atoms and carboethoxy; the pharmaceutically acceptable addition salts thereof with an organic acid and a process for the preparation thereof. The compounds possess adrenolytic, hypotensive, sedative and antiserotoninic activities.

    摘要翻译： 具有下式的1-甲基 - 亮片葡聚糖-10-甲醚的酯：

    Synthesis of elymoclavine
    49.
    发明授权
    Synthesis of elymoclavine 失效
    合成丝裂霉素

    公开(公告)号：US3923812A

    公开(公告)日：1975-12-02

    申请号：US49414974

    申请日：1974-08-02

    申请人： LILLY CO ELI

    发明人： BACH NICHOLAS J ,  KORNFELD EDMUND C

    IPC分类号： C07D457/02

    CPC分类号： C07D457/02

    摘要： Elymoclavine is prepared by oxidation of D-6-methyl-8hydroxymethyl-10 Alpha -methoxy-8-ergolene to the corresponding D-8-aldehyde followed by reduction with an active metal in acid medium.

    摘要翻译： 通过将D-6-甲基-8-羟甲基-10α-甲氧基-8-己烯醇氧化成相应的D-8-醛，然后用酸性介质中的活性金属还原来制备丝裂霉素。