| 摘要 |
Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; 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 -CRARB or is absent; Y is =C(R1a)- or -[N<custom-character file="US20020123520A1-20020905-P00900.TIF" wi="20" he="20" id="custom-character-00001"/>(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; -N O2; -(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, e.g., G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturate
|
