| 摘要 |
The present invention relates to new phosphodiesterase inhibitors, more specifically soft PDE4 inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new soft PDE4 inhibitors compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including inflammatory diseases.; |
| 主权项 |
1. A compound of Formula I or a stereoisomer, tautomer, racemic, salt, hydrate, or solvate thereof, Wherein W is N, N═O, or N+—O−; A is selected from the group consisting of a direct bond, —Z—Y, —C(═O)—NH—R21, —C(═O)—NH—R21—Z—Y—, —N(R22)—R23—, and —Z-Cy-(CH2)m—: wherein
Z is selected from a direct bond, O, NH, and S;R21 is a direct bond or an optionally substituted C1-8alkylene;R22 is selected from hydrogen and C1-8 alkyl;R23 is an optionally substituted C1-8alkylene;Cy is an optionally substituted cyclic structure selected from cycloalkyl, aryl, or heteroaryl; andm is selected from 0 and 1; R1 is selected from cycloalkyl or optionally substituted alkyl; R2 is an optionally substituted group selected from C1-8alkyl, C3-8cycloalkyl, heterocyclyl, aryl, and heteroaryl; with the proviso that if Y is part of A then R2 together with Y forms a cyclic ester (lactone) structure selected from R3 and R4 are independently selected from hydrogen, C1-8alkyl, or halo; n is an integer from 0 to 9. |
