Abstract: The invention is to compounds exhibiting neurokinin inhibitory properties, pharmaceutical compositions comprising same and methods of treatment for neurokinin-mediated conditions.

Abstract: Compounds of the formula (1) where R1 is of formula (II), (III), or (IV), or (V); R2 is —R4, —O—R4, —O—S(O)2—R4, —NR4R5, R4—(CH2)b—NH(C?X)—(CH2)C—, R4—(CH2)b—O(C—O)NH—(CH2)c—(C?O)NH—, R4—(C?O)NH—(C?O)NH—, —CH2)b—NH(C?X)—(CH2)c—R4, R4—(CH2)b—O(C?O)CH2)c—, —(CH2)b—O(C?O)—(CH2)c—R4, —NH(C?X)NH—R4, R4—O(C?O)O—, —O(C?O)NH—R4, R4—O(C?O)NH—, —(CH2)b—(C?O—(CH2)c—R4, —NH—S(O)2—R4, —C(OH)R4R5, —CH(OH)—R4, —(C?O)—NR4, —CN, —NO2, substituted C1 to C6 alkyl, substituted or unsubstituted C1 to C6 alkenyl, or substituted or unsubstituted C1 to C6 alkynyl, said substituted moieties substituted with a moiety of the formula —R4, —R4R5, —O—R4, or —S(O)d—R4; R3 is hydrogen, C1 to C6 alkyl, C1 to C6 alkylaryl, or aryl; R4 and R5 are each independently (XV), (XVI), (XVII), (XVII) hydrogen, —CF3, C1 to C6 alkyl, C1 to C6 alkylaryl, with the proviso that when R2 is —R4 or —OR4, R4 is not hydrogen or C1 to C6 alkyl these compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists and may be used