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19 条记录 (耗时 0.019 秒)

    SELECTIVE ANDROGEN RECEPTOR MODULATORS
    4.
    发明授权
    SELECTIVE ANDROGEN RECEPTOR MODULATORS 有权
    选择性雄激素受体调节剂

    公开(公告)号：EP1991523B1

    公开(公告)日：2012-08-15

    申请号：EP07712597.9

    申请日：2007-03-02

    申请人： Orion Corporation

    发明人： RATILAINEN, Jari ,  TÖRMÄKANGAS, Olli ,  KARJALAINEN, Arja ,  HUHTALA, Paavo

    IPC分类号： C07C255/60 ,  A61K31/277 ,  A61P5/26

    CPC分类号： C07C255/60

    摘要： A compound of formula (I) or an isomer, metabolite, or a pharmaceutically acceptable salt or ester thereof is disclosed. The compound of the invention possesses utility as a tissue-selective androgen receptor modulator (SARM) and is useful in hormonal therapy, e.g. in the treatment or prevention of hypogonadism, muscle wasting, osteoporosis, benign prostate hyperplasia, obesity associated with a metabolic syndrome, male and female sexual dysfunction and reduced libido, and androgen decline in aging male or female.

    IMIDAZOLE DERIVATIVES HAVING AFFINITY FOR ALPHA2 RECEPTORS ACTIVITY
    9.
    发明公开
    IMIDAZOLE DERIVATIVES HAVING AFFINITY FOR ALPHA2 RECEPTORS ACTIVITY 失效
    具有ALPHA2受体活性的咪唑衍生物

    公开(公告)号：EP0888309A1

    公开(公告)日：1999-01-07

    申请号：EP96932609.0

    申请日：1996-10-02

    申请人： ORION CORPORATION (ORION-YHTYMA OY)

    发明人： KARJALAINEN, Arja ,  HUHTALA, Paavo ,  SAVOLA, Juha-Matti ,  WURSTER, Siegfried ,  ELORANTA, Maire ,  HILLILÄ, Maarit ,  SAXLUND, Raimo ,  COCKCROFT, Victor ,  KARJALAINEN, Arja

    IPC分类号： C07D233 ,  A61K31 ,  A61P9 ,  A61P25 ,  A61P27 ,  A61P31

    CPC分类号： C07D233/56 ,  C07D233/64

    摘要： Imidazole derivatives of formula (I), wherein n is 0 or 1, R1 is hydrogen or C1-C4-alkyl, R2 is hydrogen or R2 and R3 together form a double bond, R3 is hydrogen or C1-C4-alkyl or R2 and R3 together form a double bond, R4 is hydrogen, C1-C4-alkyl, hydroxy or C1-C4-alkoxy, R5 is hydrogen or C1-C4-alkyl or R4 and R5 together with the carbon atom to which they are attached form a carbonyl group, R6, R7 and R8 are each the same or different and are independently hydrogen, C1-C4-alkyl or C2-C4-alkenyl, C3-C7-cycloalkyl, hydroxy, C1-C4-alkoxy, C1-C4-hydroxyalkyl, thiol, C1-4-alkylthio, C1-4-alkylthiol, halogen, trifluoromethyl, nitro or optionally substituted amino, X is -CHR9-(CHR10)m-, m is 0 or 1, and R9 and R10 are each the same or different and are independently hydrogen or C1-C4-alkyl; or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described. The compounds have affinity for alpha2 receptors and are useful e.g. in the treatment of hypertension, glaucoma, chronic or acute pain, migraine, diarrhea, common cold, ischemia, addiction to chemical substances, anxiety, especially preoperative anxiety and different neurological, musculoskeletal, psychiatric and cognition disorders or as adjuncts to anesthesia.