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10 条记录 (耗时 0.012 秒)

    N-oxide ergolines as antihypertensive agents
    1.
    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

    申请人： Sergio Mantegani ,  Enzo Brambilla ,  Aldemio Temperilli ,  Daniela Ruggieri ,  Patricia Salvati

    发明人： Sergio Mantegani ,  Enzo Brambilla ,  Aldemio Temperilli ,  Daniela Ruggieri ,  Patricia Salvati

    IPC分类号： A61K31/48 ,  A61P9/12 ,  C07D457/02 ,  C07D457/12

    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.

    Ergoline derivatives
    6.
    发明授权
    Ergoline derivatives 失效
    二元醇衍生物

    公开(公告)号：US4500712A

    公开(公告)日：1985-02-19

    申请号：US438259

    申请日：1982-11-01

    申请人： Luigi Bernardi ,  Aldemio Temperilli ,  Daniela Ruggieri ,  Giuliana Arcari ,  Patricia Salvati

    发明人： Luigi Bernardi ,  Aldemio Temperilli ,  Daniela Ruggieri ,  Giuliana Arcari ,  Patricia Salvati

    IPC分类号： A61K31/48 ,  A61P1/04 ,  A61P9/12 ,  C07D457/02 ,  C07D457/12 ,  C07D457/04

    CPC分类号： C07D457/02 ,  C07D457/12

    摘要： There are provided ergoline derivatives of formula ##STR1## wherein R.sub.1 .dbd.H, CH.sub.3 ; R.sub.2 .dbd.H or halogen atom, or CH.sub.3,CN, alkyl- or phenyl-thio; R.sub.3 .dbd.H, OCH.sub.3 ; R.sub.4 .dbd.C.sub.1 -C.sub.4 hydrocarbon group; X.dbd.O, S, NH; A.dbd.CO, SO.sub.2 ; B.dbd.C.sub.1 -C.sub.4 hydrocarbon group, aryl, aralkyl, heterocyclic ring group, alkoxy, aryloxy; n.dbd.0, 1, 2; and pharmaceutically acceptable salts thereof.A process for preparing said compounds is also provided. The compounds show anti-hypertensive activity and are active on the gastroenteric system.

    摘要翻译： 提供式（Ⅰ）的麦角灵衍生物，其中R1 = H，CH3; R2 = H或卤素原子，或CH3，CN，烷基或苯基 - 硫基; R3 = H，OCH3; R4 = C1-C4烃基; X = O，S，NH; A = CO，SO2; B = C1-C4烃基，芳基，芳烷基，杂环基，烷氧基，芳氧基; n = 0,1,2; 及其药学上可接受的盐。 还提供了制备所述化合物的方法。 这些化合物显示出抗高血压活性，并且对胃肠系统有活性。

    Antitumor glycosides, their preparation and use
    7.
    发明授权
    Antitumor glycosides, their preparation and use 失效
    抗肿瘤糖苷，其制备及用途

    公开(公告)号：US4276289A

    公开(公告)日：1981-06-30

    申请号：US131035

    申请日：1980-03-17

    申请人： Giuseppe Cassinelli ,  Daniela Ruggieri ,  Federico Arcamone ,  Aurelio di Marco

    发明人： Giuseppe Cassinelli ,  Daniela Ruggieri ,  Federico Arcamone ,  Aurelio di Marco

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H15/252 ,  C07H15/24

    CPC分类号： C07H15/252

    摘要： Anthracycline glycosides of the formula I ##STR1## wherein R is hydrogen or hydroxyl and the hydrochlorides thereof, and which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with the novel sugar, 4-O-methyl-2,3,6-trideoxy-3trifluoroacetamidoribohexopyranosyl chloride in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form 3', 4' -diepi-4'-O-methyl-N-trifluoroacetyl daunorubicin, and removing the N-trifluoroacetyl group therefrom. This gives the compound wherein R is hydrogen. The former is converted to the corresponding hydroxyl compound by conventional means.

    摘要翻译： 通过将道诺霉素酮与新的糖4-O-甲基-2,3,3-四氢呋喃缩合来制备其中R为氢或羟基的式I的蒽环酸苷及其盐酸盐，其可用于治疗某些哺乳动物肿瘤 ，6-三脱氧-3-三氟乙酰胺六溴代吡喃葡萄糖氯化物在惰性有机溶剂中，在可溶性银盐和脱水剂存在下反应形成3'，4'-二甲基-4'-O-甲基-N-三氟乙酰柔红霉素，并除去 N-三氟乙酰基。 这得到其中R是氢的化合物。 前者通过常规方法转化成相应的羟基化合物。

    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。