公开(公告)号：EP1517895A1

公开(公告)日：2005-03-30

申请号：EP03760540.9

申请日：2003-06-23

申请人： MERCK FROSST CANADA INC.

发明人： DESCHENES, Denis ,  DUBE, Daniel ,  DUBE, Laurence ,  GALLANT, Michel ,  GIRARD, Yves ,  LACOMBE, Patrick ,  MACDONALD, Dwight

IPC分类号： C07D215/04 ,  C07D215/12 ,  C07D409/10 ,  C07D407/10 ,  C07D401/10 ,  C07D413/10 ,  C07D413/14 ,  C07D471/04 ,  C07D401/04 ,  C07D403/10 ,  C07D417/10 ,  A61K31/4709 ,  A61K31/47 ,  A61K31/497 ,  A61P29/00

CPC分类号： C07D215/04 ,  C07D215/06 ,  C07D215/12 ,  C07D215/14 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D405/10 ,  C07D407/10 ,  C07D409/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04 ,  C07F7/0812 ,  C07F9/60

摘要： 8-(biaryl) quinolines wherein the bi-aryl group at the 8-position is in a meta relationship to the quinoline group, are PDE4 inhibitors useful in the treatment of asthma, chronic bronchitis, chronic obstructive pulmonary disease, eosinophilic granuloma, psoriasis and other benign or malignant proliferative skin diseases, endotoxic shock, laminitis in horses, colic in horses, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and brain, inflammatory arthritis, chronic glomerulonephritis, atopic dermatitis, urticaria, adult respiratory distress syndrome, chronic obstructive pulmonary disease in animals, diabetes insipidus, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, arterial restenosis, ortherosclerosis, atherosclerosis, neurogenic inflammation, pain, cough, rheumatoid arthritis, ankylosing spondylitis, transplant rejection, graft versus host disease, hypersecretion of gastric acid, bacterial, fungal induced sepsis, viral induced sepsis, fungal induced septic shock, viral induced septic shock, inflammation-mediated chronic tissue degeneration, cytokine-mediated chronic tissue degeneration, osteoarthritis, cancer, cachexia, muscle wasting, depression, memory impairment, tumour growth, or cancerous invasion of normal tissues.In another aspect, the present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and cognition enhancing amount of a phosphodiesterase-4 inhibitor.