Azole derivatives in the form of lipase and phospholipase inhibitors

摘要

The invention relates to azole derivatives of the general formula I;
as defined in the present application as well as to their uses in treatment of conditions that would benefit from their inhibitory effect on hormone sensitive lipase, HSL, an allosteric enzyme in adipocytes which is inhibited by insulin and is responsible for the breakdown of fats in fat cells and thus for transferring fat constituents into the blood stream. Inhibition of this enzyme is therefore equivalent to an insulin-like effect of the compounds of the invention.

主权项

1. A compound of the formula I in which: A is S or O; W is —(C═O)—, —(S═O)— and —(SO2)—; X is identically or differently ═C(—R)—; Y is —O— or —NR1-; R is hydrogen, halogen, (C1-C6)-alkyl, (C1-C3)-alkyloxy-(C1-C3)-alkylene, hydroxy, (C1-C6)-alkylmercapto, amino, (C1-C6)-alkylamino, di-(C2-C12)-alkylamino, mono-(C1-C6)-alkylaminocarbonyl, di-(C2-C8)-alkylamino-carbonyl, COOR4, trifluoromethyl, (C1-C6)-alkylsulfonyl, (C1-C6)-alkylsulfinyl, aminosulfonyl, nitro, pentafluorosulfanyl, (C6-C10)-aryl, CO—NR2R3, O—CO—NR2R3, O—CO—(C1-C6)-alkylene —CO—O—(C1-C6)-alkyl, O—CO—(C1-C6)-alkylene-CO—OH, O—CO—(C1-C6)-alkylene-CO—NR2R3 or unsubstituted or mono- or poly-F-substituted (C1-C6)-alkyloxy; R1 is hydrogen, (C1-C6)-alkyl, benzyl; NR2R3 is piperidine which comprises the atomic member CHR5 in position 4; R4 is hydrogen, (C1-C6)-alkyl, benzyl; R5 is (C1-C6)-alkyl, halogen, trifluoromethyl, cyclopropyl, cyclopropylene; The tautomeric forms of the compound and the physiologically tolerated salts thereof.