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EP0174447A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

16-Keto-17-substituted thio-17-alkyl (or alkenyl)-androstenes

Assignee: ER Squibb and Sons LLC
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Filing: 1985-06-18
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Granted: —
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Expires: 2005-06-18
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Abstract

Abstract Antiinflammatory activity is exhibited by new steroids having the formula and the 1,2-dehydro derivatives thereof, wherein R, is alkyl, mono-, di- or trifluoroalkyl, aryl or alkylthioalkyl, wherein R 6 is alkyl or aryl and m is 1, 2, 3 or 4; wherein R 7 , R 8 and R 9 are each independently hydrogen or alkyl of 1 to 4 carbon atoms; R 3 is carbonyl or β-hydroxymethylene; R 4 is hydrogen or halogen; R 5 is hydrogen, methyl or fluorine; and n is 0, 1 or 2; with the proviso that if R 1 is alkylthioalkyl, n is 0.

Inventors

  • 👤 Ravi K. Varma
  • 👤 Donald S. Karanewsky

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-05 10:17
CPC Classifications
C; C07; C07J; C07J31/00; C07J31/003; A; A61; A61P; A61P29/00

Claims Analysis

Total Claims: 13
Claim 1
Independent Claim 107 words
A steroid having the formula or a 1,2-dehydro derivative thereof, wherein R 1 is alkyl, mono-, di- or trifluoroalkyl, O R 6 -C-O-(CH 2 ) m -, aryl or alkylthioalkyl, wherein R 6 is alkyl or aryl and m is 1, 2, 3 or 4; R 2 is wherein R 7 , R 8 and R 9 are each independently hydrogen or alkyl of 1 to 4 carbon atoms; R 3 is carbonyl or β-hydroxymethylene; R 4 is hydrogen or halogen; R 5 is hydrogen, methyl or fluorine; and n is 0, 1 or 2; with the proviso that if R 1 is alkylthioalkyl, n is 0.
Claim 2
Dependent Claim 107 words
A steroid having the formula or a 1,2-dehydro derivative thereof, wherein R 1 is alkyl, mono-, di- or trifluoroalkyl, O R 6 -C-O-(CH 2 ) m -, aryl or alkylthioalkyl, wherein R 6 is alkyl or aryl and m is 1, 2, 3 or 4; R 2 is wherein R 7 , R 8 and R 9 are each independently hydrogen or alkyl of 1 to 4 carbon atoms; R 3 is carbonyl or β-hydroxymethylene; R 4 is hydrogen or halogen; R 5 is hydrogen, methyl or fluorine; and n is 0, 1 or 2; with the proviso that if R 1 is alkylthioalkyl, n is 0.
Claim 3
Dependent Claim 12 words
A steroid in accordance with claim 1 wherein R 1 is alkyl.
Claim 4
Dependent Claim 15 words
A steroid in accordance with claim 1 wherein R 1 is mono-, di- or trifluoroalkyl.
Claim 5
Dependent Claim 11 words
A steroid in accordance with claim 1 wherein R 1 is
Claim 8
Dependent Claim 12 words
A steroid in accordance with claim 1 wherein R 1 is aryl.
Claim 9
Dependent Claim 16 words
A steroid in accordance with claim 1 wherein R 1 is alkylthioalkyl and n is 0.
Claim 10
Dependent Claim 16 words
A steroid in accordance with any one of Claims 1 to 6 wherein R 2 is
Claim 11
Dependent Claim 16 words
A steroid in accordance with any one of Claims 1 to 6 wherein R 2 is
Claim 12
Dependent Claim 16 words
A steroid in accordance with any one of Claims 1 to 6 wherein R 2 is
Claim 13
Dependent Claim 15 words
A steroid in accordance with any one of Claims 1 to 9 having the formula
Claim 14
Dependent Claim 8 words
The steroid in accordance with claim 1, (11β,17β)-9-fluoro-11-hydroxy-17-(methylthio)-17-(2-propenyl)androsta-1,4-dien-3,16-dione.
Claim 15
Dependent Claim 28 words
A steroid useful as an intermediate in the preparation of a steroid of any one of Claims 1 to 11 having the formula or a 1,2-dehydro derivative thereof.

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