- Peroxides as "switches" of dialkyl H-phosphonate: Two mild and metal-free methods for preparation of 2-acylbenzothiazoles and dialkyl benzothiazol-2-ylphosphonates
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Two mild and metal-free methods for the preparation of two kinds of important benzothiazole derivatives, 2-acylbenzothiazoles and dialkyl benzothiazol-2-ylphosphonates, respectively, were developed. The dialkyl H-phosphonate (RO)2P(O)H exists i
- Chen, Xiao-Lan,Li, Xu,Qu, Ling-Bo,Tang, Yu-Chun,Mai, Wen-Peng,Wei, Dong-Hui,Bi, Wen-Zhu,Duan, Li-Kun,Sun, Kai,Chen, Jian-Yu,Ke, Dian-Dian,Zhao, Yu-Fen
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p. 8407 - 8416
(2015/03/18)
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- Pyrazole derivatives and COX inhibitors containing them
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PCT No. PCT/JP98/01664 Sec. 371 Date Oct. 7, 1999 Sec. 102(e) Date Oct. 7, 1999 PCT Filed Apr. 10, 1998 PCT Pub. No. WO98/46594 PCT Pub. Date Oct. 22, 1998The purpose is to provide anti-inflammatory agents which have potent pharmacological actions and exert a selective inhibitory activity on COX-2, thereby being expected to reduce adverse effects such as disorders in gastric mucosa. The present invention encompasses a compound of the formula (1): wherein R1 is hydrogen or halogen, R2 and R3 are each independently hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy or lower alkanoyloxy, R4 is lower haloalkyl or lower alkyl, X is sulfur, oxygen or NH, and Y is lower alkylthio, lower alkylsulfonyl or sulfamoyl, which exerts superior anti-inflammatory activity, and highly inhibits COX-2 induced in inflamed sites, with less inhibitory action on COX-1 present in stomach, kidney, etc. Pharmaceutical agents comprising the compound of the present invention are provided as selective COX-2 inhibitors, and anti-inflammatory agents rarely accompanying adverse actions including attacks on gastric mucosa.
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