申请人:Albert Scott Jeffrey
公开号:US20070021406A1
公开(公告)日:2007-01-25
The present application relates to internally cyclized naphthamide compounds of the formula Ia (wherein R
1a
, R
1b
, R
1c
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
, R
8
, X
1
, X
2
, Y, Z, and n are as defined herein), which are useful, for example, for antagonizing the pharmacological actions of the neurokinin 1 (NK
1
) receptor. In particular, these compounds are useful in the treatment of diseases in which Substance P is involved such as, for example, major depressive disorder, severe anxiety disorders, stress disorders, major depressive disorder with anxiety, eating disorders, bipolar disorder, substance use disorder, schizophrenic disorders, psychotic disorders, movement disorders, cognitive disorders, depression and/or anxiety, mania or hypomania, aggressive behaviour, obesity, rheumatoid arthritis, Alzheimer's disease, cancer, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, Huntington's disease, chronic obstructive pulmonary disorder (COPD), hypertension, migraine, bladder hypermotility, and urticaria.
本申请涉及公式Ia的内环化萘酰胺化合物(其中R1a,R1b,R1c,R2,R3,R4,R5,R6,R7,R8,X1,X2,Y,Z和n的定义如本文所述),这些化合物可用于拮抗神经激肽1(NK1)受体的药理作用。特别地,这些化合物可用于治疗与物质P有关的疾病,例如重度抑郁障碍、严重焦虑障碍、应激障碍、伴有焦虑的重度抑郁障碍、进食障碍、躁狂障碍、物质使用障碍、精神分裂障碍、精神病性障碍、运动障碍、认知障碍、抑郁和/或焦虑、狂躁或亢进行为、肥胖症、类风湿性关节炎、阿尔茨海默病、癌症、水肿、过敏性鼻炎、炎症、疼痛、胃肠道高动力性、亨廷顿病、慢性阻塞性肺疾病(COPD)、高血压、偏头痛、膀胱高动力性和荨麻疹。