Benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors

摘要

Compounds of the general formula I;
wherein
each of m and n is independently 0 or 1;R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—;R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3;X is a bond, —CH2—, or —NH—;A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; andR4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy;

or pharmaceutically acceptable salts, hydrates or solvates thereof,

have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.

主权项

1. A method of treating or ameliorating a dermal disease or condition, the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula IIb, optionally together with a pharmaceutically acceptable carrier or one or more excipients, wherein the dermal disease and condition is selected from the group consisting of psoriasis, eczema, dermatitis, urticaria, and alopecia, wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; and
R3 is —OCHF2, or —OCF3;or a pharmaceutically acceptable salt, hydrate or solvate thereof.