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    • 4. 发明授权
    • 2-substituted ergolines
    • 2-取代的麦角碱
    • US5158957A
    • 1992-10-27
    • US720996
    • 1991-06-26
    • Thomas BrumbyGerhard SauerJosef HeindlJonathan TurnerGerhard KuhneHelmut Wachtel
    • Thomas BrumbyGerhard SauerJosef HeindlJonathan TurnerGerhard KuhneHelmut Wachtel
    • A61K31/48A61P25/00A61P43/00C07D457/12
    • C07D457/12
    • 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.
    • 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。
    • 5. 发明授权
    • 2-substituted ergolines
    • 2-取代的麦角碱
    • US5037832A
    • 1991-08-06
    • US380352
    • 1989-07-17
    • Thomas BrumbyGerhard SauerJosef HeindlJonathan TurnerGerhard KuhneHelmut Wachtel
    • Thomas BrumbyGerhard SauerJosef HeindlJonathan TurnerGerhard KuhneHelmut Wachtel
    • A61K31/48A61P25/00A61P43/00C07D457/12
    • C07D457/12
    • 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.
    • 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。