C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 65/24 (2006.01) A61K 31/19 (2006.01) A61K 31/235 (2006.01) C07C 43/225 (2006.01) C07C 69/92 (2006.01) C07C 69/94 (2006.01) C07C 219/14 (2006.01) C07C 317/22 (2006.01)
Patent
CA 2110116
ABSTRACT The invention relates to compounds of the formula Image I wherein R is hydrogen, lower alkyl, -(CH2)2N(R3)2 or -CH2OOCR3 wherein R3 is lower alkyl; R1 is CH3(CH2)n-, wherein n is 9-17, or R4(CH2)p-, wherein p is 3-10 and R4 is 1- or 2-naphthyloxy, 2,3- or 3,4-dihydroxyphenyl, 2,3- or 3,4-dibenzyloxyphenyl, 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, a pharmaceutically acceptable salt with a base. 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.
Carson Mathew
Han Ru-Jen L.
Lemahieu Ronald A.
Madison Vincent S.
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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