| abstract |
PCT No. PCT/US97/15443 Sec. 371 Date Jan. 22, 1998 Sec. 102(e) Date Jan. 22, 1998 PCT Filed Sep. 2, 1997 PCT Pub. No. WO98/11090 PCT Pub. Date Mar. 19, 1998The small nonpeptides of the instant invention are tachykinin antagonists of formula or a pharmaceutically acceptable salt thereof wherein: R1 is straight or branched alkyl of from 5 to 15 carbon atoms, aryl, or heteroaryl; R2 is hydrogen, hydroxy, amino, or thiol; R3 is aryl, arylsulfonylmethyl, or saturated or unsaturated heterocycle; R4 is from 1 to 4 groups each independently selected from halogen, alkyl, hydroxy, and alkoxy; n is an integer of from 2 to 6; and the carbon atom of (CH2)n group can be replaced by oxygen, nitrogen, or sulphur. The compounds are highly selective and functional NK3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders. |