CAS: 170569-99-0; Celecoxib 2-Methyl Analog

1-甲基苯基乙酮置于sodium Methylate体系中,用 甲醇,乙醇 用作溶剂,化学反应 44.0H,反应生成塞来昔布杂质
参考文献:Synthesis And Biological Evaluation Of The 1,5-Diarylpyrazole Class Of Cyclooxygenase-2 Inhibitors: Identification Of 4-[5-(4-Methylphenyl)-3-(Trifluoromethyl)-1H-Pyrazol-1-Yl]Benzenesulfonamide (Sc-58635,Celecoxib)
标题:Synthesis And Biological Evaluation Of The 1,5-Diarylpyrazole Class Of Cyclooxygenase-2 Inhibitors: Identification Of 4-[5-(4-Methylphenyl)-3-(Trifluoromethyl)-1H-Pyrazol-1-Yl]Benzenesulfonamide (Sc-58635,Celecoxib)
摘要:A Series Of Sulfonamide-Containing 1,5-Diarylpyrazole Derivatives Were Prepared And Evaluated For Their Ability To Block Cyclooxygenase-2 (Cox-2) In Vitro And In Vivo. Extensive Structure-Activity Relationship (Sar) Work Was Carried Out Within This Series,And A Number Of Potent And Selective Inhibitors Of Cox-2 Were Identified. Since An Early Structural Lead (1F,Sc-236) Exhibited An Unacceptably Long Plasma Half-Life,A Number Of Pyrazole Analogs Containing Potential Metabolic Sites Were Evaluated Further In Vivo In An Effort To Identify Compounds With Acceptable Pharmacokinetic Profiles. This Work Led To The Identification Of Ii (4-[5-(4-Methylphenyl)-3-(Trifluoromethyl)-1H-Pyrazol-1-Yl]Benzenesulfonamide,Sc-58635,Celecoxib),Which Is Currently In Phase Iii Clinical Trials For The Treatment Of Rheumatoid Arthritis And Osteoarthritis.
Doi:10.1021/jm960803Q

专利信息

专利号:US-7041694-B1
优先权日:1997-12-17
标 题 :Cyclooxygenase-2 inhibition
发明人：DANNENBERG ANDREW J
权利人:CORNELL RES FOUNDATION INC
摘要:Selective inhibitors of cyclooxygenase-2 are used to treat liver disease and in combination with anti-viral drugs to treat virus-caused liver disorders. Selective inhibitors of cyclooxygenase-2 which also inhibit the synthesis of cyclooxygenase-2 improve over the efficacy of conventional selective inhibitors of cyclooxygenase-2 in the treatment of inflammatory conditions, Alzheimer's disease and cancer.