abstract |
A compound of the formula: wherein y is 1 to 3; each Ra, Rb and Rm is independently selected from the group consisting of H, C1-C6alkyl, or when Ra and Rb are attached to the same nitrogen, then Ra and Rb, together with the nitrogen to which they are attached, can form a 4 to 7 member ring; each R1 and R2 is independently selected from the group consisting of H, C1-C6alkyl, -CF3, -C2F5, Cl, Br, I, F, -NO2, -ORa, -CN, -NRaRb; provided Ra is not H; in each R3 is independently selected from the group consisting of H, C1-C6alkyl, -CF3, -C2F5, Cl, Br, I, F, -ORa, -OCF3, phenyl, -ORb; Rn is CN and n11 is 1-4; m1 and m2 are both 0, or one of m1 and m2 is 0 and the other is 1; m3 is 3; n6 is 0 to 2; X4 and X4a are -O- or n3 is 0 to 4; X8 is -ORm or -O-(CH2)n11-Rn; Rg is H, C1-C6alkoxy, C1-C6alkyl, Rn is H, C1-C6alkyl, -C(O)Ra, -C(O)NRaRb, -C(O)ORa, -SO2Rm, -(CH2)n11-Rn, provided that when Rh is -C(O)ORa, Ra is not H; RI is -CH or -Ra; each Re and Rf is independently selected from the group consisting of H, C1-C6alkyl, each R5 is independently H or C1-C6alkyl; R6 is H, C1-C6alkyl, thienyl, pyridyl, imidazolyl, indolyl, oxazolyl provided that when the sum of m1 plus m2 is 1, provided that when R3 is H, C1-C6alkyl, -CF3, -C2F5, Cl, Br, I, F, -ORa, -OCF3, phenyl, and provided that when G is not or any enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma. |