| 摘要 |
<p>Compounds useful as inhibitors of PFE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of the formula, given in the description, where j is 0 or 1, k is 0 or 1; m is 0, 1, 2 or 3, n is 1 or 2; W1 is -O-; or -S(=O)t-, where t is 0, 1 or 2 or -N(R3)-; W2 is -O-CRARB- or is absent; Y is =C(R1a)-or -[N(r)(O)k]- where k is 0 or 1; RA and RB are -H; -F, -CF3; -(C1-C4) alkyl; -(C3-C7) cycloalkyl; phenyl; or benzyl substituted with 0 to 3 substituents R10; or RA and RB are taken together, but only in the case where m is 1, to form a spiro moiety; RC and RD have the same meaning as RA and RB except that one of them must be -H, R1 and R2 are -H; -F; -Cl; -CN;-NO2;-(C1-C4) alkyl; -(C2-C4) alkynyl; fluorinated -(C1-C3) alkyl; -OR16; and -C(=O)NR22aR22b; R3 is H; -(C1-C3) alkyl; phenyl; benzyl; or -OR16; R4, R5 and R6 in addition to other meanings may be taken together to form formula (II) given in the description; G is a saturated or unsaturated carbon ring system; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; -G2 is a saturated or unsaturated carbon ring system, wherein one carbon atom may be replaced by a heteroatom selected from N, O and S; and E is selected from formula (III) given in the description. 10 claims</p> |
