1,6-Dimethyl-8.beta.-[2' or 3'-pyrroyloxyethyl or substituted
pyrroyloxyethyl]-10.alpha.-methoxyergolene compounds
    73.
    发明授权
    1,6-Dimethyl-8.beta.-[2' or 3'-pyrroyloxyethyl or substituted pyrroyloxyethyl]-10.alpha.-methoxyergolene compounds 失效
    1,6-二甲基-8- {62 - {8 2 {40 {0或3 {40-吡咯氧基乙基或取代的吡咯氧基乙基{9-10 {60-甲氧基己烯基化合物

    公开(公告)号:US3972883A

    公开(公告)日:1976-08-03

    申请号:US436927

    申请日:1974-01-28

    IPC分类号: A61K31/48 C07D457/02

    CPC分类号: C07D457/02

    摘要: Ergoline derivatives are disclosed having the general formula ##SPC1##Wherein R is selected from the group consisting of a lower alkyl radical having from 1 to 4 carbon atoms; an --NH-lower alkyl radical having from 1 to 4 carbon atoms; a free or substituted phenyl- or 2-furanoyl radical; the --O--CH.sub.2 --C.sub.6 H.sub.5 radical; a (3)- or (4)-pyridine radical free or substituted by a methyl radical or a chlorine or bromine atom; a pyrrole radical of formula ##SPC2##WhereinY is hydrogen, a lower alkyl radical having from 1 to 4 carbon atoms or phenyl;R.sub.1 is hydrogen or methyl;R.sub.2 is hydrogen, methyl or halogen; andR.sub.3 and R.sub.4 are the same or different and are hydrogen, halogen, a lower alkyl radical having from 1 to 4 carbon atoms, carbethoxy, or a lower alkyloxy radical having from 1 to 4 carbon atoms.Novel processes for the preparation of these compounds are also disclosed.

    摘要翻译: 公开了具有通式为WHEREIN R选自具有1至4个碳原子的低级烷基的衍生物, 具有1至4个碳原子的-NH-低级烷基; 游离或取代的苯基或2-呋喃酰基; -O-CH 2 -C 6 H 5基团; (3) - 或(4) - 吡啶基自由或被甲基或氯或溴原子取代; 式WHEREIN Y的吡咯基是氢,具有1至4个碳原子的低级烷基或苯基; R1是氢或甲基; R2是氢,甲基或卤素; 并且R 3和R 4相同或不同,为氢,卤素,具有1至4个碳原子的低级烷基,乙氧羰基或具有1至4个碳原子的低级烷氧基。

    Composition for preventing lactation or pregnancy in mammals and the
method for using the same
    74.
    发明授权
    Composition for preventing lactation or pregnancy in mammals and the method for using the same 失效
    用于预防哺乳动物哺乳期或哺乳期怀孕的组合物及其使用方法

    公开(公告)号:US3966941A

    公开(公告)日:1976-06-29

    申请号:US315838

    申请日:1972-12-18

    IPC分类号: C07D457/02 A61K31/48

    CPC分类号: C07D457/02

    摘要: .alpha.-D-6-methylergolinyl-8-acetamides of the formula: ##SPC1##Are readily prepared from .alpha.-D-6-methylergolinyl-8-acetic acid azide hydrochloride and amines of the formula R.sub.1 -NH-R.sub.2 and may be converted to their salts with inorganic and organic acids by neutralization. In these formulas, R.sub.1 may be hydrogen or lower alkyl, R.sub.2 may be hydrogen, lower alkyl, cycloalkyl having 5 or 6 carbon atoms, hydroxyalkyl having 3 or 4 carbon atoms, or lower alkoxycarbonylmethyl or R.sub.1 and R.sub.2 jointly may be divalent alkylene having 4 or 5 C atoms. The salts of most of these bases with physiologically tolerated acids are nontoxic in doses which suppress lactatical and prevent pregnancy in rats when applied orally after copulation. The others, equally non-toxic, extend the effective period of thiopental.

    摘要翻译: 具有下式的α-D-6-甲基麦角酰基-8-乙酰胺:

    8-Oxymethylergolines and process therefor
    75.
    发明授权
    8-Oxymethylergolines and process therefor 失效
    8-氧甲基麦角碱及其制备方法

    公开(公告)号:US3959288A

    公开(公告)日:1976-05-25

    申请号:US532333

    申请日:1974-12-13

    IPC分类号: C07D457/02

    CPC分类号: C07D457/02

    摘要: 6-methyl-8-alkoxymethylergolines are prepared by reaction of a 6-methyl-8-(substituted)methylergoline with a benzyl quaternary ammonium alkoxide. 6-Methyl-8-phenoxymethylergolines are prepared by reaction of an 8-(substituted)-methylergoline with phenol in the presence of strong base. The new 8-oxymethylergolines of this invention are useful as prolactin inhibitors.

    摘要翻译: 通过6-甲基-8-(取代的)甲基麦角灵与苄基季铵盐醇盐的反应来制备6-甲基-8-烷氧基甲基麦角碱。 6-甲基-8-苯氧基甲基麦角碱通过在强碱存在下8-(取代的) - 甲基麦角灵与苯酚的反应来制备。 本发明的新的8-氧甲基麦角苷可用作催乳激素抑制剂。

    D-6-methyl-8-cyano methylergoline (i) and method of making the same
    80.
    发明授权
    D-6-methyl-8-cyano methylergoline (i) and method of making the same 失效
    D-6-甲基-8-氰基甲基吗啉(I)及其制备方法

    公开(公告)号:US3732231A

    公开(公告)日:1973-05-08

    申请号:US3732231D

    申请日:1971-06-18

    IPC分类号: C07D457/02 C07D43/20

    CPC分类号: C07D457/02

    摘要: D-6-METHYL-8-CYANO METHYLERGOLINE HAVING THE FORMULA

    7-CH3-5A,6,6A,7,8,9,10,10A-OCTAHYDROINDOLO(4,3-FG)-

    QUINOLINE

    PREPARED BY REACTING D-6-METHYL-8-HYDROXYMETHYLERGOLINE (I) WITH PHOSPHORYL CHLORIDE AND THEREAFTER REACTING THE D-6-METHYL-8-CHLOROMETHYLERGOLINE FORMED WITH AN ALKALI METAL CYANIDE. THE COMPOUNDS OF THE INVENTION CONSTITUTE ANTIFERTILITY AND LACTATION INHIBITING AGENTS.