PYRAZOLOPYRIMIDINES AS CRF ANTAGONISTS
    5.
    发明授权
    PYRAZOLOPYRIMIDINES AS CRF ANTAGONISTS 失效
    吡唑并嘧啶AS CRF拮抗剂

    公开(公告)号:EP0674642B1

    公开(公告)日:2000-08-23

    申请号:EP94903283.3

    申请日:1993-11-26

    申请人: PFIZER INC.

    IPC分类号: C07D487/04 A61K31/505

    CPC分类号: C07D487/04

    摘要: Corticotropin-releasing factor (CRF) antagonists have formula (I), wherein A, R3, R4 and R5 are as defined herein. They are useful in the treatment of illnesses induced or facilitated by CRF, such as inflammatory disorders, and depression and anxiety related disorders.

    Novel compositions containing sertraline and a 5-HT1D receptor agonist or antagonist
    8.
    发明公开
    Novel compositions containing sertraline and a 5-HT1D receptor agonist or antagonist 失效
    含有舍曲林的新组合物和5-HT 1D受体的激动剂或拮抗剂

    公开(公告)号:EP0701819A3

    公开(公告)日:1999-06-23

    申请号:EP95306249.4

    申请日:1995-09-07

    申请人: PFIZER INC.

    IPC分类号: A61K45/06 A61K31/135

    CPC分类号: A61K45/06 Y10S514/811

    摘要: The present invention relates to novel compositions containing the serotonin selective re-uptake inhibitor (SSRI), preferably (1S-cis)4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine, and an agonist or antagonist of the serotonin 1 (5-HT₁) receptor and to the use of such compositions for treating or preventing a condition selected from mood disorders, including depression, seasonal affective disorders and dysthmia, anxiety disorders including generalized anxiety disorder and panic disorder; agoraphobia, avoidant personality disorder; social phobia; obsessive compulsive disorder; post-traumatic stress disorder; memory disorders including dementia, amnestic disorders and age-associated memory impairment; disorders of eating behavior, including anorexia nervosa and bulimia nervosa; obesity; cluster headache; migraine; pain; Alzheimer's disease; chronic paroxysmal hemicrania; headache associated with vascular disorders; Parkinson's disease, including dementia in Parkinson's disease, neuroleptic-induced parkinsonism and tardive dyskinesias; endocrine disorders such as hyperprolactinaemia; vasospasm (particularly in the cerebral vasculature); hypertension; disorders in the gastrointestinal tract where changes in motility and secretion are involved; sexual dysfunction, including premature ejaculation; and chemical dependencies.

    4-Phenyl-3-(heteroarylureido)-1,2-dihydro-2-oxoquinoline derivatives as antihypercholesterolemic and antiatherosclerotic agents
    10.
    发明授权
    4-Phenyl-3-(heteroarylureido)-1,2-dihydro-2-oxoquinoline derivatives as antihypercholesterolemic and antiatherosclerotic agents 失效
    4-苯基-3-(heteroarylureido)-1,2-二氢-2-氧代喹啉衍生物作为antihypercholesterolemische和动脉粥样硬化剂

    公开(公告)号:EP0623112B1

    公开(公告)日:1998-12-30

    申请号:EP93901257.1

    申请日:1992-12-21

    申请人: PFIZER INC.

    CPC分类号: C07D215/38 C07D401/12

    摘要: Compounds of formula (I) wherein each m is independently selected from 0 to 4; R2 is selected from hydrogen and (C¿1?-C6) alkyl; each R?3 and R4¿ is independently selected from halogen, (C¿1?-C6) alkyl optionally substituted with one or more halogen atoms, (C1-C6) alkoxy optionally substituted with one or more halogen atoms, (C1-C6) alkylthio optionally substituted with one or more halogen atoms; nitro, carboxyl optionally esterified with a (C1-C6) alkyl group; hydroxyl, (C1-C4) acyloxy and (C1-C3) acyl; X is sulfur or oxygen; and Q is a group of formula (XIV), (XV) or (XVI) wherein m is as defined above; n is 0 or 1. Each 1 is independently selected from 0 to 3; each R?6 and R7¿ is defined in the description; B, D, E and G are selected from the group consisting of nitrogen and carbon, with the proviso that one or more of B, D and E is nitrogen, and with the proviso that when G is nitrogen, the group XVI is attached to the nitrogen of formula (I) at the 4 or 5 position of the pyrimidine ring (designated by a and b) wherein any of said nitrogens may be oxidized, or the pharmaceutically acceptable salts thereof, and intermediates having formula (IV) used in the synthesis of such compounds. The compounds of formula (I) are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.