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NOVEL GLUCOCORTICOID RECEPTOR AGONISTS
专利权人:
PFIZER LIMITED
发明人:
MILLAN, DAVID SIMON,GLOSSOP, PAUL ALAN,PRICE, DAVID ANTHONY
申请号:
NZ58543408
公开号:
NZ585434A
申请日:
2008.11.17
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are 16a,17a-benzylidenedioxy-11b,21-dihydroxypregna-1,4-diene-3,20-dione derivatives as represented by the general formula (I), wherein: R1 is a benzyl, phenylthio or phenylthiomethyl moiety as defined herein. Of particular importance is the compound (4aS,4bR,5S,6aS,6bS,8R,9aR,10aS,10bS,12S)-8-(4-{ [(3-chloro-4-hydroxyphenyl)thio]methyl} phenyl)-4b,12-difluoro-6b-glycoloyl-5-hydroxy-4a,6a-dimethyl-4a,4b,5,6,6a,6b,9a,10,10a,10b,11,12-dodecahydro-2H-naphtho[2,1:4,5]indeno[1,2-d][1,3]dioxol-2-one. Further disclosed is a pharmaceutical composition which comprises an effective amount of a compound as defined above, or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate of said compound or salt, and one or more pharmaceutically acceptable excipients, for the treatment of one or more diseases, disorders and conditions selected from skin diseases inflammatory conditions of the nose, throat and lungs (such as rhinitis, sinusitis, asthma, nasal polyps, chronic obstructive pulmonary disease (COPD) and fibrosis) inflammatory diseases of the intestine auto-immune diseases and ocular conditions.
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