N-oxide ergolines as antihypertensive agents
    3.
    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

    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.

    Abeo-ergoline derivatives as 5HT1A ligands
    9.
    发明授权
    Abeo-ergoline derivatives as 5HT1A ligands 失效
    二氢麦角灵衍生物作为5HT1A配体

    公开(公告)号:US06284896B1

    公开(公告)日:2001-09-04

    申请号:US08998867

    申请日:1997-12-29

    IPC分类号: C07D48706

    CPC分类号: C07D487/06

    摘要: There are provided compounds of formula (I), wherein R1 is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R2 is C1-C3 alkyl or an alkyl group; R3 and R4 are independently a hydrogen atom, a C1-C5 alkyl group, a C3-C5 alkenyl group, a C5-C6 cycloalkyl C1-C3 alkyl group, a phenyl-C3-C5 alkenyl or phenyl group: which groups are optionally substituted by C1-C3 alkyl, C1-C3 alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R6 is hydrogen atom or a C1-C3 alkyl group and R7 is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R5 is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.

    摘要翻译: 提供式(I)化合物,其中R 1是氢,氯或溴原子或甲基,甲硫基,羟基,氰基或甲酰氨基; R2是C1-C3烷基或烷基; R3和R4独立地是氢原子,C1-C5烷基,C3-C5烯基,C5-C6环烷基C1-C3烷基,苯基-C3-C5链烯基或苯基:这些基团是任选取代的 C 1 -C 3烷基,C 1 -C 3烷氧基,三氟甲基,羟基或氨基; 或式(a)的基团,其中R6是氢原子或C1-C3烷基,R7是苯基,如上所述的取代苯基或杂环,R5是氢或溴原子或有机 残基,R为H或有机残基,或其药学上可接受的盐。 还提供了其制备方法和包含它们的药物组合物。

    Antineurodegenerative ergoline derivatives
    10.
    发明授权
    Antineurodegenerative ergoline derivatives 失效
    抗神经变性麦角灵衍生物

    公开(公告)号:US6060483A

    公开(公告)日:2000-05-09

    申请号:US147448

    申请日:1998-12-28

    摘要: The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or C.sub.2 -C.sub.5 alkenyl group optionally substituted with a C.sub.3 -C.sub.7 cycloalkyl, a hydroxy group or a R.sub.3 -substituted phenyl group wherein R.sub.3 is a hydroxy or a hydroxymethyl group; R.sub.2 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or a C.sub.2 -C.sub.5 alkenyl group optionally substituted with a hydroxy group, or a R.sub.3 -substituted phenyl group wherein R.sub.3 is as above defined, or with a C.sub.1 -C.sub.5 alkoxy group; the symbols--at positions 2,3 and 8, 9 independently denote a single or double chemical bond and Z represents a group (CH.sub.2).sub.n OH, wherein n is 0 or an integer from 1 to 3, or a group C(R.sub.4).sub.2 OH wherein R.sub.4 is a C.sub.1 -C.sub.5 alkyl or a phenyl group, or a pharmaceutically acceptable salt thereof. Some compounds of formula (I) are novel. Processes for their preparation and pharmaceutical compositions containing them are also described.

    摘要翻译: PCT No.PCT / EP97 / 02955 Sec。 371日期1998年12月28日第 102(e)日期1998年12月28日PCT提交1987年5月29日PCT公布。 第WO98 / 00424号公报 日本1998年1月8日本发明提供了用于治疗神经变性疾病的新用途,其中式(I)的麦角灵衍生物其中R 1表示氢原子或直链或支链C 1 -C 5烷基或C 2 -C 5烯基,任选被 C3-C7环烷基,羟基或R3-取代的苯基,其中R3是羟基或羟甲基; R2表示氢原子或任选被羟基取代的直链或支链C 1 -C 5烷基或C 2 -C 5烯基,或其中R 3如上所定义的R 3取代苯基,或与C 1 -C 5烷氧基 ; 位置2,3和8,9独立地表示单一或双重化学键,Z表示基团(CH 2)n OH,其中n为0或1至3的整数,或基团C(R 4)2 OH 其中R4是C1-C5烷基或苯基,或其药学上可接受的盐。 一些式(I)化合物是新的。 还描述了其制备方法和含有它们的药物组合物。