| abstract |
The invention relates to tachykinin receptor antagonists, the tachykinin family of receptors comprising the neurokinins substance P (SP), neurokinin A, and neurokinin B and related neuropeptides that are widely distributed in the peripheral and central nervous system. The present invention discloses novel neurokinin antagonists represented by formulas I-IV, and synthesis and uses thereof for treating diseases mediated directly or indirectly by the tachykinin receptors. Such conditions include central nervous system disorders such as anxiety, pain, depression, emesis, e.g., cancer chemotherapy-induced emesis, respiratory and inflammatory to bowel disease and other gastric disorders, asthma, schizophrenia, ophthalmic diseases such as glaucoma, ocular hypotension, neural injury, stroke, cardiac disorders, psoriasis, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included. |