| 摘要 |
A compound that has formula IV: (see formula IVa) (see formula IVb) (see formula IVc) or (see formula IVd) or pharmaceutically acceptable derivatives thereof, wherein: X is S or -C(R3) =C(R4) -; R1 is halo or lower alkyl; R2 is lower alkyl; R3 and R4 are hydrogen, halo, cyano, etc.; R5 is lower alkyl or -(CH2) x C(O)(CH2)y CH3; R6 is lower alkyl, -(CH2) x C(O)(CH2)y CH3, or heteroaryl; R7 is hydrogen, hydroxy, alkoxy, etc.; x and y are each independently 0 to 14; Y and R8 are: (i) Y is O; and R8 is CONR38R39 (where R38 and R39 are each hydrogen, alkyl, alkenyl, etc.), CN, heteroaryl, etc.; or (ii) Y and R8 form a 3 to 16 membered unsubstituted or substituted cyclic or heterocyclic ring; R9 is H; a is 1 if Y2 is carbon; a is 0 if Y2 is nitrogen; b is 1 if Y1 is carbon; b is 0 if Y1 is nitrogen; and W is NH, and formulations thereof, and methods for modulating or altering the activity of the endothelin family of peptides and methods for treating endothelin-mediated disorders are provided.
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