Fluorosteroids VII. Synthesis and biological activity of derivatives of 6α-fluoro-16α,17α-isopropylidenedihydroxypregna-1,4-diene-11β, 21-diol--3,20-dione
Chemical compounds having a substituted oxepane ring and methods of preparing such compounds are described. The compounds are active as utero-evacuant agents.
描述了具有取代氧杆环的化合物以及制备这种化合物的方法。这些化合物作为子宫清除剂具有活性。
Pharmaceutically active bicyclic-heterocyclic amines
申请人:The Upjohn Company
公开号:US05502187A1
公开(公告)日:1996-03-26
The pharmaceutically active bicyclic heterocyclic amines (XXX) ##STR1## where W.sub.1 is --N.dbd. or --CH.dbd.; W.sub.3 is --N.dbd. or --CH.dbd.; W.sub.5 is --N.dbd. or --CR.sub.5 -- with the proviso that W.sub.5 is --CR.sub.5 -- when both W.sub.1 and W.sub.3 are --N.dbd. which are useful as pharmaceuticals in treating mild and/or moderate to severe head injury, subarachnoid hemorrhage and subsequent ischemic stroke, asthma and reduction of mucous formation/secretion in the lung and other diseases and injuries.
Nucleoside compounds of the formula ##STR1## wherein: B is a purine or a pyrimidine; X and X' are H, OH or F, provided that at least one is H; Y and Y' are H, OH, OCH.sub.3 or F, provided that at least one is H; Y' and Z together form a cyclic phosphate ester, provided that Y is H; or Z is ##STR2## where n is zero, one, two or three; and Z' is N.sub.3 or OCH.sub.3 ; provided that when X' and Y' are OH and Z' is N.sub.3, B is not cytosine, and when X' and Y' are OH and Z' is OCH.sub.3, B is not uracil, adenine or cytosine; and the pharmaceutically acceptable esters, ethers and salts thereof, have been found to have potent antiviral activity with a high therapeutic ratio.
17.alpha.-Acyloxy-5.alpha.-pregnanes (I) and 17.alpha.-acyloxy-5.alpha.-pregnanes (IV) have an excellent activity split providing high topical anti-inflammatory activity with very low systemic side effects.
17.alpha.-Acyloxy-5.beta.-pregnanes (I) and 17.alpha.-acyloxy-5.alpha.-pregnanes (IV) have an excellent activity split providing high topical antiinflammatory activity with very low systemic side effects.