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156 条记录 (耗时 0.057 秒)

    Ergoline amine derivatives with blood pressure lowering effect
    3.
    发明授权
    Ergoline amine derivatives with blood pressure lowering effect 失效
    艾曲林胺衍生物具有降血压作用

    公开(公告)号：US06358967B1

    公开(公告)日：2002-03-19

    申请号：US09743869

    申请日：2001-04-19

    申请人： Ralf Wyrwa ,  Albert Haertl ,  Erika Glusa ,  Susanne Grabley ,  Ralf Thiericke

    发明人： Ralf Wyrwa ,  Albert Haertl ,  Erika Glusa ,  Susanne Grabley ,  Ralf Thiericke

    IPC分类号： A61K3148

    CPC分类号： C07F15/025 ,  C07D457/02 ,  C07F17/02

    摘要： The invention relates to novel derivatives of ergoline of the general formula 1 in which R1 together with the two adjacent N atoms is the residue of a diamine and R4 together with the two adjacent carbonyl groups is the residue of a dicarboxylic acid. R2, R3, R6, R7, R8 can be H or an organic radical. R7 and R8 are H or together are a bond. The compounds show a strong antihypertensive effect. These effects moreover occur after intravenous and enteral administration even at dosages in the region of a few &mgr;g/kg (body weight). The compounds can accordingly be used as pharmaceuticals for hypertensive diseases in human medicine.

    摘要翻译： 本发明涉及通用1的麦角灵素的新衍生物，其中R1与两个相邻的N原子一起是二胺的残基，R4与两个相邻的羰基一起是二羧酸的残基。 R2，R3，R6，R7，R8可以是H或有机基团。 R7和R8是H或一起是一个键。化合物显示出强烈的抗高血压作用。 即使在几公斤/公斤（体重）的剂量下，静脉内和肠内给药也会发生这些影响。 因此，这些化合物可以用作人类医学中的高血压疾病的药物。

    3-oxo-piperazin-1-yl-ergolines exhibiting antidopaminergic activity
    9.
    发明授权
    3-oxo-piperazin-1-yl-ergolines exhibiting antidopaminergic activity 失效
    具有抗癌剂活性的3-氧代 - 哌嗪-1-基 - 麦角酰胺

    公开(公告)号：US4728649A

    公开(公告)日：1988-03-01

    申请号：US817135

    申请日：1986-01-08

    申请人： Sergio Mantegani ,  Aldemio Temperilli ,  Gabriella Traquandi ,  Alessandro Rossi ,  Lorenzo Pegrassi

    发明人： Sergio Mantegani ,  Aldemio Temperilli ,  Gabriella Traquandi ,  Alessandro Rossi ,  Lorenzo Pegrassi

    IPC分类号： A61K31/48 ,  A61P9/12 ,  A61P25/00 ,  A61P25/20 ,  C07D457/02 ,  C07D457/12 ,  A61K31/445

    CPC分类号： C07D457/02

    摘要： The invention relates to ergoline derivatives having the general formula (I): ##STR1## where R=H, CH.sub.3 ; R.sub.1 =H, halogen, CH.sub.3, phenylthio, C.sub.1 -C.sub.4 alkylthio; R.sub.2 =H, CH.sub.3 O, and R.sub.3 =H or R.sub.2 +R.sub.3 =chemical bond; R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.5, R.sub.6, R.sub.8, R.sub.9 independently=H, C.sub.1 -C.sub.4 alkyl, or R.sub.5, R.sub.8 independently=H, C.sub.1 -C.sub.4 alkyl and R.sub.6 +R.sub.9 =CH.sub.2 CH.sub.2, CH.sub.2 CH.sub.2 CH.sub.2 ; R.sub.7 =H, C.sub.1 -C.sub.4 alkyl, phenyl, NR'R"; R',R" independently=H, C.sub.1 -C.sub.4 alkyl, acyl or NR'R"=heterocyclic ring; W=0, H.sub.2 ; n=0, 1, 2, and their pharmaceutically acceptable salts, these compounds exhibiting antihypertensive activity making them useful anxiolytic and antipsychotic agents. A process for their preparation and pharmaceutical compositions containing them are also described.

    摘要翻译： 本发明涉及具有通式（I）的麦角灵衍生物：其中R = H，CH 3; R1 = H，卤素，CH3，苯硫基，C1-C4烷硫基; R2 = H，CH3O，R3 = H或R2 + R3 =化学键; R4 = C1-C4烃; R5，R6，R8，R9独立地为H，C1-C4烷基或R5，R8独立地为H，C1-C4烷基和R6 + R9 = CH2CH2，CH2CH2CH2; R7 = H，C1-C4烷基，苯基，NR'R“ R'，R“独立地为H，C 1 -C 4烷基，酰基或NR'R”=杂环; W = 0，H2; n = 0,1,2及其药学上可接受的盐，这些具有抗高血压活性的化合物使它们成为抗焦虑药和抗精神病药。 还描述了其制备方法和含有它们的药物组合物。

    Ergolines exhibiting protactin secretion inhibition activity
    10.
    发明授权
    Ergolines exhibiting protactin secretion inhibition activity 失效
    Ergolines表现出protactin分泌抑制活性

    公开(公告)号：US4690929A

    公开(公告)日：1987-09-01

    申请号：US604041

    申请日：1984-04-26

    申请人： Luigi Bernardi ,  Laura Chiodini ,  Sergio Mantegani ,  Daniela Ruggieri ,  Aldemio Temperilli ,  Patricia Salvati

    发明人： Luigi Bernardi ,  Laura Chiodini ,  Sergio Mantegani ,  Daniela Ruggieri ,  Aldemio Temperilli ,  Patricia Salvati

    IPC分类号： C07D457/02 ,  C07D457/12 ,  A61K31/48 ,  C07D457/04

    CPC分类号： C07D457/02 ,  C07D457/12

    摘要： Compounds of formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen or halogen atom or a methyl, cyano, C.sub.1 -C.sub.4 alkylthio or phenylthio group; R.sub.7 and R.sub.8 represent hydrogen atoms and R.sub.3 represents a hydrogen atom or a methoxy group, or R.sub.7 represents a hydrogen atom and R.sub.3 and R.sub.8 taken together represent a bond, or R.sub.3 represents a hydrogen atom or a methoxy group and R.sub.7 and R.sub.8 taken together represent a bond; R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; R.sub.5 represents a hydrogen atom or a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group; X represents an oxygen or sulphur atom or an imino group, R.sub.9 represents a hydrogen atom and B represents a cyano, a C.sub.2 -C.sub.5 alkoxycarbonyl or carbamoyl group, or R.sub.9 and B taken together represent a ##STR2## group wherein W represents an oxygen atom or an imino group; A represents a group of the formula CHR.sub.6, CH.sub.2 --CHR.sub.6 or CH.dbd.CR.sub.6 group wherein R.sub.6 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and n is 0, 1 or 2; and their pharmaceutically acceptable salts are disclosed, along with the use of these compounds as antiprolactinic and antihypertensive agents. The preparation of these compounds and pharmaceutical compositions containing them are also described.

    摘要翻译： 式I的化合物：其中R 1表示氢原子或甲基; R 2表示氢或卤素原子或甲基，氰基，C 1 -C 4烷硫基或苯硫基; R7和R8表示氢原子，R3表示氢原子或甲氧基，或R7表示氢原子，R3和R8表示一个键，或R3表示氢原子或甲氧基，R7和R8表示 一个债券 R4表示具有1至4个碳原子的烃基; R5表示氢原子或碳原子数1〜4的烃基或苯基; X表示氧或硫原子或亚氨基，R9表示氢原子，B表示氰基，C2-C5烷氧基羰基或氨基甲酰基，或R9和B表示“IMA”基团，其中W表示氧原子 或亚氨基; A表示式CHR 6，CH 2 -CHR 6或CH = CR 6基团的基团，其中R 6表示氢原子或C 1 -C 4烷基; 且n为0,1或2; 以及它们的药学上可接受的盐以及这些化合物作为抗孕激素和抗高血压药的用途。 还描述了这些化合物的制备和含有它们的药物组合物。