ARYL - /HETEROARYL - CYCLOHEXENYL - TETRAAZABENZO [E]AZULENES AS VASOPRESSIN ANTAGONISTS
    12.
    发明公开
    ARYL - /HETEROARYL - CYCLOHEXENYL - TETRAAZABENZO [E]AZULENES AS VASOPRESSIN ANTAGONISTS 有权
    ARYL- /异戊烯 - 环己基 - 四氮杂苯并[E-]亚油酸缓冲肽 - 拮抗剂

    公开(公告)号:EP2558467A1

    公开(公告)日:2013-02-20

    申请号:EP11715194.4

    申请日:2011-04-08

    CPC分类号: C07D487/04

    摘要: The present invention is concerned with aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes of formula I wherein R
    1 , R
    2 and R
    3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

    SPIRO-PIPERIDINE DERIVATIVES
    16.
    发明公开
    SPIRO-PIPERIDINE DERIVATIVES 有权
    SPIRO-PIPERIDINE衍生物

    公开(公告)号:EP2099799A1

    公开(公告)日:2009-09-16

    申请号:EP07847384.0

    申请日:2007-11-27

    CPC分类号: C07D471/10 C07D498/10

    摘要: Present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. The compounds of present invention have the general Formula (I) wherein R1 to R11 and X are as defined in the description.

    摘要翻译: 本发明涉及作为V1a受体拮抗剂的新吲哚-2-基 - 羰基 - 螺 - 哌啶衍生物,它们的制造方法,含有它们的药物组合物以及它们作为药物的用途。 本发明的活性化合物可用于预防和/或治疗焦虑症和抑郁症以及其他疾病。 本发明化合物具有通式(I),其中R 1至R 11和X如说明书中所定义。

    SEROTONIN TRANSPORTER (SERT) INHIBITORS
    17.
    发明授权
    SEROTONIN TRANSPORTER (SERT) INHIBITORS 有权
    羟色胺转运抑制剂(SERT)

    公开(公告)号:EP1957450B1

    公开(公告)日:2009-06-24

    申请号:EP06819656.7

    申请日:2006-11-22

    CPC分类号: C07D207/08 C07D207/09

    摘要: The present invention relates to cis- derivatives of formula (I) wherein R1 is hydrogen, halogen or lower alkyl; R2/R3 are independently from each other hydrogen, halogen, CN, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; X is -O- or -N(R)-; R is hydrogen or lower alkyl; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.

    NK1 ANTAGONISTS
    19.
    发明公开
    NK1 ANTAGONISTS 有权
    NK 1拮抗剂

    公开(公告)号:EP1856052A2

    公开(公告)日:2007-11-21

    申请号:EP06706917.9

    申请日:2006-02-14

    CPC分类号: C07D213/75 C07D213/82

    摘要: The present invention relates to compounds of the formula (I), wherein R1 /R1’ are hydrogen or methyl; X is -C(O)N(CH3)- or -N(CH3)C(O)-; and to pharmaceutically acceptable acid addition salts thereof for the treatment of numerous inflammatory conditions, migraine, rheumatoid arthritis, asthma, inflammatory bowel disease, mediation of the emetic reflex, Parkinson's disease, anxiety, depression, psychosis, motion sickness, induced vomiting, pain, headache, migraine, Alzheimer's disease, multiple sclerosis, attenuation of morphine withdrawal, cardiovascular changes, oedema, such as oedema caused by thermal injury, chronic inflammatory diseases such as rheumatoid arthritis, asthma/bronchial hyperreactivity and other respiratory diseases including allergic rhinitis, inflammatory diseases of the gut including ulcerative colitis and Crohn's disease, ocular injury and ocular inflammatory diseases, traumatic brain injury, motion sickness, emesis and psychoimmunologic or psychosomatic disorders.