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67 条记录 (耗时 0.024 秒)

    2-substituted ergolines
    3.
    发明授权
    2-substituted ergolines 失效
    2-取代的麦角碱

    公开(公告)号：US5158957A

    公开(公告)日：1992-10-27

    申请号：US720996

    申请日：1991-06-26

    申请人： Thomas Brumby ,  Gerhard Sauer ,  Josef Heindl ,  Jonathan Turner ,  Gerhard Kuhne ,  Helmut Wachtel

    发明人： Thomas Brumby ,  Gerhard Sauer ,  Josef Heindl ,  Jonathan Turner ,  Gerhard Kuhne ,  Helmut Wachtel

    IPC分类号： A61K31/48 ,  A61P25/00 ,  A61P43/00 ,  C07D457/12

    CPC分类号： C07D457/12

    摘要： 2-Substituted ergolines ##STR1## wherein C.sub.2 C.sub.3 and C.sub.9 C.sub.10 represent a single of double bond;X is oxygen or sulfur;R.sup.2 is C.sub.1-10 alkyl, optionally halogen-substituted C.sub.2-10 alkenyl, CH.sub.2 YR.sup.3, CR.sup.12 (OR.sup.4)R.sup.5, CH.sub.2 --CHR.sup.9 --COR.sup.10 or COR.sup.12, whereinY is oxygen or sulfur,R.sup.3 is hydrogen, C.sub.1-4 alkyl, phenyl, C.sub.2-5 acyl or phenyl C.sub.1-4 alkyl,R.sup.4 is hydrogen or C.sub.2-5 acyl,R.sup.5 is C.sub.1-9 alkyl,R.sup.9 is COCH.sub.3 or COO-C.sub.1-4 alkyl,R.sup.10 is C.sub.1-4 alkyl or O-C.sub.1-4 alkyl,R.sup.12 is hydrogen or C.sub.1-9 alkyl; andR.sup.6 is C.sub.2-10 alkyl, C.sub.3-10 alkenyl or C.sub.4-10 cycloalkyl-C.sub.1-3 -alkyl,and acid addition salts, isomers and isomeric mixtures thereof are dopaminergic agonists and useful for treating Parkinson's Disease.

    摘要翻译： 2-取代的ergolines 其中C2 C3和C9 C10表示单键的双键; X是氧或硫; R 2是C 1-10烷基，任选被卤素取代的C 2-10烯基，CH 2 YR 3，CR 12（OR 4）R 5，CH 2 -CHR 9 -CON 10或COR 12，其中Y是氧或硫，R 3是氢，C 1-4烷基，苯基， C2-5酰基或苯基C1-4烷基，R4是氢或C2-5酰基，R5是C1-9烷基，R9是COCH3或COO-C1-4烷基，R10是C1-4烷基或O-C1-4 烷基，R 12是氢或C 1-19烷基; 并且R 6是C 2-10烷基，C 3-10烯基或C 4-10环烷基-C 1-3烷基，其酸加成盐，异构体和异构体混合物是多巴胺能激动剂，可用于治疗帕金森病。

    2-substituted ergolines
    4.
    发明授权
    2-substituted ergolines 失效
    2-取代的麦角碱

    公开(公告)号：US5037832A

    公开(公告)日：1991-08-06

    申请号：US380352

    申请日：1989-07-17

    申请人： Thomas Brumby ,  Gerhard Sauer ,  Josef Heindl ,  Jonathan Turner ,  Gerhard Kuhne ,  Helmut Wachtel

    发明人： Thomas Brumby ,  Gerhard Sauer ,  Josef Heindl ,  Jonathan Turner ,  Gerhard Kuhne ,  Helmut Wachtel

    IPC分类号： A61K31/48 ,  A61P25/00 ,  A61P43/00 ,  C07D457/12

    CPC分类号： C07D457/12

    摘要： 2-Substituted ergolines ##STR1## wherein C.sub.2 C.sub.3 and C.sub.9 C.sub.10 represent a single or double bond;X is oxygen or sulfur;R.sup.2 is C.sub.1-10 alkyl, optionally halogen-substituted C.sub.2-10 alkenyl, CH.sub.2 YR.sup.3, CR.sup.12 (OR.sup.4)R.sup.5, CH.sub.2 -CHR.sup.9 -COR.sup.10 or COR.sup.12, whereinY is oxygen or sulfur,R.sup.3 is hydrogen, C.sub.1-4 alkyl, phenyl, C.sub.2-5 acyl or phenyl C.sub.1-4 alkyl,R.sup.4 is hydrogen or C.sub.2-5 acyl,R.sup.5 is C.sub.1-9 alkyl,R.sup.9 is COCH.sub.3 or COO-C.sub.1-4 alkyl,R.sup.10 is C.sub.1-4 alkyl or O-C.sub.1-4 alkyl,R.sup.12 is hydrogen or C.sub.1-9 alkyl; andR.sup.6 is C.sub.2-10 alkyl, C.sub.3-10 alkenyl or C.sub.4-10 cycloalkyl-C.sub.1-3 -alkyl,and acid addition salts, isomers and isomeric mixtures thereof are dopaminergic agonists and useful for treating Parkinson's Disease.

    摘要翻译： 2-取代的麦角糖苷其中C2 C3和C9 C10表示单键或双键; X是氧或硫; R 2是C 1-10烷基，任选被卤素取代的C 2-10烯基，CH 2 YR 3，CR 12（OR 4）R 5，CH 2 -CHR 9 -CON 10或COR 12，其中Y是氧或硫，R 3是氢，C 1-4烷基，苯基， C2-5酰基或苯基C1-4烷基，R4是氢或C2-5酰基，R5是C1-9烷基，R9是COCH3或COO-C1-4烷基，R10是C1-4烷基或O-C1-4 烷基，R 12是氢或C 1-19烷基; 并且R 6是C 2-10烷基，C 3-10烯基或C 4-10环烷基-C 1-3烷基，其酸加成盐，异构体和异构体混合物是多巴胺能激动剂，可用于治疗帕金森病。

    8 beta-substituted ergolines, process for their production and their use
    7.
    发明授权
    8 beta-substituted ergolines, process for their production and their use 失效
    8替代白蛋白，其生产过程及其使用

    公开(公告)号：US5219862A

    公开(公告)日：1993-06-15

    申请号：US623933

    申请日：1990-12-21

    申请人： Gerhard Sauer ,  Thomas Brumby ,  Helmut Wachtel ,  Jonathan Turner ,  Peter A. Loschmann

    发明人： Gerhard Sauer ,  Thomas Brumby ,  Helmut Wachtel ,  Jonathan Turner ,  Peter A. Loschmann

    IPC分类号： A61K31/48 ,  A61P43/00 ,  C07D457/02 ,  C07D457/04 ,  C07D457/06

    CPC分类号： C07D457/06 ,  C07D457/02

    摘要： Compounds of formula I ##STR1## in which R.sup.2 means optionally substituted C.sub.1-7 alkyl, C.sub.2-7 alkenyl, CH.sub.2 --O--C.sub.1-4 alkyl or CH.sub.2 --S--C.sub.1-4 alkylR.sup.6 means C.sub.2-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-5 -cycloalkyl-C.sub.1-2 alkyl andR.sup.8 means CH.sub.2 --X, ##STR2## in which X stands for CN, OCH.sub.3, SCH.sub.3 or CONH.sub.2 and R.sup.1 stands for hydrogen, halogen, methyl or methoxy, and R.sup.3 and R.sup.4 each mean C.sub.1-4 alkyl or (CH.sub.2).sub.n --N(CH.sub.3).sub.2, in which n=1-4, and their acid addition salts, the process for their production, their use as pharmaceutical agents as well as intermediate compounds are described.

    摘要翻译： PCT No.PCT / DE90 / 00282 Sec。 371 1990年12月21日第 102（e）1990年12月21日日期PCT提交1990年4月6日PCT公布。 WO90 / 12796 PCT公开号 日期：1990年11月1日。其中R 2表示任选取代的C 1-7烷基，C 2-7烯基，CH 2 -O-C 1-4烷基或CH 2 -S-C 1-4烷基R 6的式I化合物I表示 C2-6烷基，C3-6烯基或C3-5-环烷基-C1-2烷基，R8表示CH2-X，其中X代表CN，OCH3，SCH3或CONH2，R1代表氢，卤素， 甲基或甲氧基，R3和R4各自表示C 1-4烷基或（CH 2）n N（CH 3）2，其中n = 1-4及其酸加成盐，其生产方法，其作为药剂用作 以及中间体化合物。

    Novel ergolinyl compounds nitrogen-substituted in the 8-position, useful for treating dopamine deficiency
    8.
    发明授权
    Novel ergolinyl compounds nitrogen-substituted in the 8-position, useful for treating dopamine deficiency 失效
    在8-位氮取代的新型麦角酰基化合物，可用于治疗多巴胺缺乏症

    公开(公告)号：US4826852A

    公开(公告)日：1989-05-02

    申请号：US878762

    申请日：1986-06-26

    申请人： Gregor Haffer ,  Gerhard Sauer ,  Helmut Wachtel ,  Herbert Schneider ,  Ulrich Eder

    发明人： Gregor Haffer ,  Gerhard Sauer ,  Helmut Wachtel ,  Herbert Schneider ,  Ulrich Eder

    IPC分类号： A61K31/48 ,  A61P9/12 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00 ,  C07D457/04 ,  C07D457/06 ,  C07D457/12 ,  A61K31/44 ,  A61K31/54 ,  C07D417/14

    CPC分类号： C07D457/04 ,  C07D457/06 ,  C07D457/12

    摘要： Ergolinyl compounds which are nitrogen-substituted in the 8-position and have Formula (I) ##STR1## and physiologically compatible salts thereof, wherein (a) R.sup.1 is hydrogen, the 8-substituent can be in the .alpha.- or .beta.-position and ##STR2## represents a single or a double bond, R.sup.2 is hydrogen, C.sub.1-4 -alkyl or C.sub.1-7 -acyl,R.sup.3 is hydrogen, chlorine or bromine, andR.sup.4 is C.sub.1-6 -alkyl, C.sub.3-6 -cycloalkyl-C.sub.1-3 -alkyl, C.sub.3-6 -alkenyl, or C.sub.3-6 -alkynyl; or(b) R.sup.1 is ##STR3## and the 8-substituent can be in the .alpha.- or .beta.-position, ##STR4## represents a single or double bond, R.sup.2, R.sup.3 are as defined above,R.sup.4, is C.sub.1.varies.6 -alkyl, C.sub.3-6 -cycloalkyl-C.sub.1-3 -alkyl, C.sub.3-6 -alkenyl, or C.sub.3-6 -alkynyl; andR.sup.5 is hydrogen, C.sub.-10 -alkyl, C.sub.3-10 -alkenyl, or C.sub.3-10 -alkynyl, andR.sup.6 is C.sub.1-10 -alkyl, C.sub.3-10 -alkenyl, C.sub.3-10 -alkynyl, or aryl, orR.sup.5 and R.sup.6 together with the connecting N-atom form a 5- to 10-membered heterocyclic ring, preferably 5- or 6-membered, which optionally can contain further heteroatoms.

    摘要翻译： 在8-位上被氮取代且具有式（I）的化合物和其生理上相容的盐，其中（a）R 1是氢，所述8-取代基可以是α-或β- - 位和表示单键或双键，R 2为氢，C 1-4 - 烷基或C 1-7 - 酰基，R 3为氢，氯或溴，且R 4为C 1-6 - 烷基，C 3-6 环烷基-C 1-3 - 烷基，C 3-6 - 烯基或C 3-6 - 炔基; 或（b）R 1是，并且8-取代基可以是α-或β-位，表示单键或双键，R2，R3如上所定义，R4是C1， 烷基，C 3-6 - 环烷基-C 1-3 - 烷基，C 3-6 - 烯基或C 3-6 - 炔基; 和R 5是氢，C 1-10烷基，C 3-10 - 烯基或C 3-10 - 炔基，R 6是C 1-10烷基，C 3-10 - 烯基，C 3-10 - 炔基或芳基或R 5 和R6连同连接的N-原子形成5-至10-元杂环，优选5-或6-元，其任选地可含有其它杂原子。

    1-alkyl ergolinylthiourea derivatives and their use as antidepressant agents
    9.
    发明授权
    1-alkyl ergolinylthiourea derivatives and their use as antidepressant agents 失效
    1-烷基麦角酰硫基脲衍生物及其作为抗抑郁药的用途

    公开(公告)号：US4772610A

    公开(公告)日：1988-09-20

    申请号：US893727

    申请日：1986-08-06

    申请人： Helmut Biere ,  Gerhard Sauer ,  Helmut Wachtel

    发明人： Helmut Biere ,  Gerhard Sauer ,  Helmut Wachtel

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

    CPC分类号： C07D457/12

    摘要： Novel 1-alkyl ergolinylthiourea derivatives of the general formula ##STR1## wherein R.sup.1 is C.sub.1-6 alkyl,R.sup.2 and R.sup.3 are C.sub.1-4 alkyl,R.sup.4 is hydrogen or C.sub.1-4 alkyl andC.sub.9---- C.sub.10 is a single bond or a double bond,and the acid addition salts thereof, with the provision that when R.sup.3 and R.sup.4 are both ethyl, R.sup.1 and R.sup.2 are not methyl and acid addition salts thereof are provided; as well as a process for the preparation of these compounds. The compounds are useful as medicinal agents, e.g., for the treatment of mental depression.

    摘要翻译： 新颖的通式为：其中R 1为C 1-6烷基，R 2和R 3为C 1-4烷基，R 4为氢或C 1-4烷基，C 9 -C 10为单键或双键的1-烷基麦角酰硫基脲衍生物 键和其酸加成盐，条件是当R 3和R 4都是乙基时，R 1和R 2不是甲基，并且提供其酸加成盐; 以及制备这些化合物的方法。 这些化合物可用作药物，例如用于治疗精神抑郁症。