N-substituted anilines.

摘要

Compounds of the formula <CHEM> wherein R1 is hydrogen or -(CH2)mCOOR2; R2 is hydrogen, (R6)2N(CH2)2-, R6COOCH2- or -CH2CON(CH2CH2OH)2; R3 is hydrogen, nitro, hydroxy, amino, CH3(CH2) nS(O)0-2-, CH3(CH2)n-, CH3(CH2)nO- ,R5COO-, R5OOC- ,R5HNCOO-, R5NHCO-, R5CONH-, R5NHCONH-, [CH3(CH2)n]2NCO- , CH3(CH2)nCHOHCH2O-, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R8OOC(CH2)tO-, (R6O)2PO(CH2)pO- , (HO) (R6O)PO(CH2)pO-, R6[O(CH2)2]qO- , R7(CH2)pO-, or -O(CH2)p-pyridinium<+>(OH<->); R4 is CH3(CH2) n- , CH3(CH2)nO- , CF3SO2NH-, R5COO-, R5OOC- ,R5HNCOO-, R5NHCO-, R5CONH-R5NHCONH-, [CH3(CH2)n]2NCO-, CH3(CH2)nCHOHCH2O-, carboxy, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R8OOC(CH2)tO-, R6[O(CH2)2]qO- , or R7(CH2)pO-; R5 is CH3(CH2)n-, 1-adamantyl or diphenylmethyl; R6 is lower alkyl; R7 is 1- or 2 -naphthyloxy, 1-, 2- or 3-pyridinyloxy, 2,3- or 3,4-dihydroxyphenyl, 6,7-dihydroxy-2-naphthyl, phenyl, phenoxy or substituted phenyl or phenoxy, wherein the substituent is selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, nitro, amino, halo, R6 S(O)0-2-, carboxy, carboxy-lower alkyl or phenyl; R8 is hydrogen or lower alkyl; n is an integer from 0 to 17; m is an integer from 1 to 3; t is an integer from 1 to 10; p is an integer from 2 to 18, and q is an integer from 1 to 6; and when R2 is hydrogen, a pharmaceutically acceptable salt thereof with a base, are potent inhibitors of phospholipases A2 (PLA2's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.