Substituted benzoic acids, inhibitors of phospholipases A2

The invention relates to compounds of the formula 1 R is hydrogen, lower alkyl, -(CH2)2N(R3)2 or -CH2OOCR3 wherein R3 is lower alkyl; R1 is CH3(CH2)n-, wherein n is 0-17, or R4(CH2)p-, wherein p is 2-18 and R4 is 1- or 2-naphthyloxy, 2,3- or 3,4-dihydroxyphenyl, phenyl, phenoxy, or substituted phenyl or phenoxy wherein the substituent is selected from the group consisting of hydroxy, benzyloxy, methylsulfinyl, methylsulfonyl or phenyl; R2 is R4(CH2)p-, 1-adamantyl-CO- or diphenylmethyl-CO-, and, when R is hydrogen, pharmaceutically acceptable salts with bases. The compounds of formula I are potent inhibitors of phospholipases A2 (PLA2's) and are therefore useful in the treatment of diseases, such as psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia, and trauma induced inflammation, such as spinal cord injury. The invention relates to compounds of the formula N(R3)2 or -CH2OOCR3 wherein R3 is lower alkyl; R1 is CH3(CH2)n-, wherein n is 0-17, or R4(CH2)p-, wherein p is 2-18 and R4 is 1- or 2-naphthyloxy, 2,3- or 3,4-dihydroxyphenyl, phenyl, phenoxy, or substituted phenyl or phenoxy wherein the substituent is selected from the group consisting of hydroxy, benzyloxy, methylsulfinyl, methylsulfonyl or phenyl; R2 is R4(CH2)p-, 1-adamantyl-CO- or diphenylmethyl-CO-, and, when R is hydrogen, pharmaceutically acceptable salts with bases. The compounds of formula I are potent inhibitors of phospholipases A2 (PLA2's) and are therefore useful in the treatment of diseases, such as psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia, and trauma induced inflammation, such as spinal cord injury.