| abstract |
Non-peptide-containing acetamide derivatives of formula I (such as: 2 - [(benzofuran-2-ylmethyl) -amino] -3- (1H-indole-3-yl) -2-methyl-N- ( 1-phenyl-ethyl) propionamide) are specific NK antagonists where R is pyridyl, thienyl, furyl, pyrrolyl, pyrazoyl, quinolyl, isoquinolyl, maphthyl, etc; R1 and R2 are H or alkyl, m is an integer from 0 to 3; n is integers from 1 to 2, X is NR8 or NHCONH, R3 and R9 are H or alkyl, R4 is naphthyl or indolyl, q is an integer from 1 to 3; R5 and R7 are H or alkyl, and R6 is phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyrazolyl, indoline, etc. A pharmaceutical formulation characterized by comprising a compound of formula I mixed with a pharmaceutically acceptable diluent, carrier or excipient. The compounds are useful agents for the treatment of inflammatory and allergic disorders, pain, anxiety, depression, schizophrenia, and emesis. |