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    Ergoline derivatives, processes for their preparation and pharmaceutical compositions containing same
    15.
    发明公开
    Ergoline derivatives, processes for their preparation and pharmaceutical compositions containing same 失效
    麦角灵衍生物，其制备方法和含有它们的药物组合物。

    公开(公告)号：EP0126968A1

    公开(公告)日：1984-12-05

    申请号：EP84104568.5

    申请日：1984-04-24

    申请人： FARMITALIA CARLO ERBA S.r.l.

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

    IPC分类号： C07D457/00 ,  C07D457/12 ,  C07D457/02 ,  A61K31/48

    CPC分类号： C07D457/02 ,  C07D457/12

    摘要： R 1 =H, CH 3
    R 2 =H, halogen, CH 3 , CN, lower alkylthio, phenylthio
    R 7 and R 8 =H; R 3 =H, OCH 3
    R 7 =H, R 3 and R s = bond
    R 7 and R 8 =bond, R 3 =H, OCH 3
    R 4 =C 1 -C 4 hydrocarbon
    R s =H, C 1 -C 4 hydrocarbon, phenyl
    A=CHR 6 , CH 2 CHR 6 , CH=CR 6
    R 6 =H, lower alkyl
    n=O, 1, 2
    X=O,S,NH B=CN, COOalK. CONH 2
    R 9 =H or B and R 9 =-C=W
    W=O,NH

    and their pharmaceutically acceptable salts are antiprolacti- nic and antihypertensive agents. Their preparation and pharmaceutical compositions containing them are also described.

    摘要翻译： ... ... R1 = H，CH3 ... R2 = H，卤素，CH 3，CN，低级烷硫基，苯硫基... ... R4 = C1-C4烃... R5 = H，C1-C4烃，苯基... A = CHR6，CH2CHR6，CH = CR 6 ... R6 = H，=低级烷基，...，N 0，1，2 ... X = O，S，NH B = CN，COOalk，CONH 2 ... R9 = H或B和R9 = -C = W ... W = O，NH ...和它们的药学上可接受的盐是抗催乳素和抗高血压剂。 含有这些制剂和药物组合物如此描述。

    NOVEL FLUOROERGOLINE ANALOGS
    18.
    发明公开
    NOVEL FLUOROERGOLINE ANALOGS 审中-公开
    新FLUORERGOLIN类似物

    公开(公告)号：EP2723735A1

    公开(公告)日：2014-04-30

    申请号：EP12803230.7

    申请日：2012-06-22

    申请人： MAP Pharmaceuticals Inc

    发明人： COOK, Robert, O. ,  ZHANG, Jian ,  ARMER, Thomas, A.

    IPC分类号： C07D457/00

    CPC分类号： C07D519/02 ,  A61K9/0075 ,  A61K9/0078 ,  A61K31/495 ,  A61K31/4985 ,  C07D457/04 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00

    摘要： Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HTiD and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and composittons disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.

    TRANSDERMALES THERAPEUTISCHES SYSTEM MIT ZWEIPHASIGEM FREISETZUNGSPROFIL
    19.
    发明公开
    TRANSDERMALES THERAPEUTISCHES SYSTEM MIT ZWEIPHASIGEM FREISETZUNGSPROFIL 审中-公开
    透皮治疗系统两相释放曲线

    公开(公告)号：EP2079458A2

    公开(公告)日：2009-07-22

    申请号：EP07802907.1

    申请日：2007-08-27

    申请人： Axxonis Pharma AG

    发明人： TACK, Johannes ,  SCHURAD, Björn ,  MÜLLER-SCHUBERT, Antje ,  HOROWSKI, Reinhard

    IPC分类号： A61K9/70 ,  A61K47/06 ,  A61K47/10 ,  A61K47/32 ,  A61K47/44 ,  C07D457/00 ,  A61K47/16

    CPC分类号： A61K9/7061 ,  A61K31/48

    摘要： The present invention relates to a transdermal therapeutic system (TTS) comprising an impermeable covering layer, a matrix containing an ergolin compound of formula (I) or the physiologically compatible salt or derivative thereof, wherein R1 represents an H atom or a halogen atom and R2 an alkyl group with 1 to 4 carbon atoms and ------ a single or double bond, and a removable protective layer, the ergolin compound or the physiologically compatible salt or derivative thereof being stabilized by an antioxidant and a basic polymer. The TTS is characterized in that the matrix contains at least one hydrocarbon having 8 to 18 carbon atoms in a linear or branched chain and carrying a functional group at the end of the alkyl chain, and/or aloe vera oil so that, in a first phase (0-5 hours after application), only 0 to 20 % of the therapeutically desired steady state plasma concentration of the ergolin compound is achieved and, in a second phase (5-20 hours after application), the therapeutically desired steady state plasma concentration of the ergolin compound is achieved.

    4-Piperidinyl-ergoline derivatives
    20.
    发明公开
    4-Piperidinyl-ergoline derivatives 失效
    4-哌啶基 - 麦角灵衍生物

    公开(公告)号：EP0449346A3

    公开(公告)日：1992-03-25

    申请号：EP91200446.2

    申请日：1991-03-01

    申请人： PHARMACIA S.p.A.

    发明人： Mantegani, Sergio ,  Bandiera, Tiziano ,  Brambilla, Enzo ,  Buonamici, Metilde

    IPC分类号： C07D457/02 ,  C07D457/00 ,  A61K31/48

    CPC分类号： C07D457/02

    摘要： A compound of the formula I

    wherein R represents a hydrogen atom or a C₁ -C₄ alkyl group; R₁ represents a hydrogen, a halogen atom, a methyl group, a phenylthio group or an alkylthio group having from 1 to 4 carbon atoms; R₂ represents a hydrogen atom or a methoxy group; R₃ represents a hydrogen atom or R₂ and R₃ together represent a chemical bond; R₄ represents a hydrocarbon group having from 1 to 4 carbon atoms; R₅ represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms or a phenyl group and n is 0, 1 or 2 or a pharmaceutically acceptable salt thereof. Such compounds are useful as dopaminergic agents. A method of preparation and pharmaceutical compositions comprising them are also provided.

    摘要翻译： 式I化合物，其中R代表氢原子或C 1 -C 4烷基; R 1表示氢，卤素原子，甲基，苯硫基或具有1至4个碳原子的烷硫基; R 2代表氢原子或甲氧基; R 3代表氢原子或R 2和R 3一起代表化学键; R 4代表具有1至4个碳原子的烃基; R 5代表氢原子，具有1至4个碳原子的烷基或苯基，并且n是0,1或2或其药学上可接受的盐。 这类化合物可用作多巴胺能药物。 还提供了一种制备方法和包含它们的药物组合物。