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1.发明授权Aromatic heterocyclic esters of steroids, their preparation and pharmaceutical compositions containing them 失效异烟肼的芳香杂环化合物，其制备和含有它们的药物组合物
公开(公告)号：EP0057401B1
公开(公告)日：1984-08-01
申请号：EP82100490.0
申请日：1982-01-25
申请人： SCHERING CORPORATION
发明人： Shapiro, Elliot L.
CPC分类号： C07J33/002 , C07J17/00 , C07J43/003
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2.发明公开Aromatic heterocyclic esters of steroids, their preparation and pharmaceutical compositions containing them 失效芳香族杂环类固醇酯，其制备方法和含有它们的药物组合物。
公开(公告)号：EP0057401A1
公开(公告)日：1982-08-11
申请号：EP82100490.0
申请日：1982-01-25
申请人： SCHERING CORPORATION
发明人： Shapiro, Elliot L.
CPC分类号： C07J33/002 , C07J17/00 , C07J43/003
摘要： Disclosed herein are novel 3,20-dioxo-1,4-pregnadiene-17-01-17-aromatic heterocyclic carboxylates (and the 6-dehydro and 1,2-dihydro derivatives thereof) of general formula I:
wherein:
A is hydrogen or, provided that Y is (H,βOH), A may also be chloro, fluoro or methyl;
X is hydrogen or a halogen atom having an atomic weight less than 100;
Y is oxygen, (H,βOH) or, provided that X is hydrogen, Y may also be (H,H) or, provided X is chloro or bromo, Y may also be (H,β-halogen), the β-halogen having an atomic weight less than 100 and being at least as electronegative as X;
Z is hydrogen, methyl, chloro or fluoro;
Z' is hydrogen or, provided that Z is hydrogen, may also be halogen having an atomic weight of less than 100;
V is an acyl radical of a thiophenecarboxylic acid, pyrrolecarboxylic acid or furancarboxylic acid or the methyl- or halogen-substituted derivatives thereof;
W is (H,H), (H, lower alkyl) or (H, aOV,) where V, is hydrogen or specified acyl radicals, or W is a methylene or substituted methylene group; and
G is hydrogen, a halogen atom having an atomic weight of less than 100 or is -QV 2 where Q is oxygen or sulfur and V 2 is specified acyl radicals.
The novel compounds exhibit anti-inflammatory activity and their use for this purpose is disclosed. Also disclosed are methods for the preparation of the novel compounds.
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