PHENYL HETEROCYCLIC RING AS CYCLOOXYGENASE-2 INHIBITOR

摘要

PROBLEM TO BE SOLVED: To obtain a new compound useful in pharmaceutical compositions for treating inflammatory diseases sensitive to the therapies using nonsteroidal anti-inflammatory agents. SOLUTION: This new compound is shown by formula I [X-Y-Z is such as to be CH2CH2CH2, C(O)CH2CH2, S-N=CH, or the like when side (b) is a double bond and side (a) and side (c) are each a single bond, =N-S-CH=, =N-O-CH=, =N-S-N=, or the like when side (a) and side (c) are each a double bond and side (b) is a single bond; R1 is S(O)2CH3, S(O)2NHC(O)CF3, P(O)(CH3)OH, or the like; R2 is a 1-6C alkyl, 3-7C cycloalkyl, trisubstituted phenyl or the like], e.g. 3-[4-(aminosulfonyl)phenyl]-2-(4-fluorophenyl)-5-(2- hydroxy-2-propyl)thiophene. The compound of formula I is obtained, for example, by using a ketone of formula II (Ra is SMe or the like) as starting material to form a compound of formula III (R4 is H or the like).