| 摘要 |
A compound having the formula (I) and its pharmaceutically-acceptable salt is disclosed, wherein: R1 is H or CH3; R2 is H, halogen,-OR7 or C1-4alkyl; R3 is H, halogen, -OR7 or-CN; R4 is H, halogen, -OR7 or C1-4alkyl; R5 is H, C1-8alkyl, -C(=O)R9, -C(=O)OR8, -C(=O) N (R6) R8, -S(=O)nR9, cyanoguanidino or C1-4acylguanidino; R6 is, independently at each instance, H or C1-6alkyl; R7 is, independently at each instance, C1-6alkyl; R8 is H, C1-6alkyl substituted by 0,1 or 2 substituents selected from-OH and-NHR6 or C1-3alkyl substituted by 1,2,3 or 4 halogen atoms; R9 is, independently at each instance, C1-6alkyl substituted by 0,1 or 2 substituents selected from-OH and-NHR6 or C1-3alkyl substituted by 1,2,3 or 4 halogen atoms; n is 0,1 or 2; and X1 and X2 are independently H,-CH3 or halogen. These compounds antagonize the pharmacological actions of the neurokinin 1 (NK1) receptor and are useful for the treatment 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, emesis, 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, or urticaria.
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