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US4091036A
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17-Alkylthio (and arylthio)-1',2',3',4'-tetrahydroandrosteno [16 α, 17 α-b]naphthalenes and derivatives
Assignee: ER Squibb and Sons LLC
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Filing: 1977-05-12
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Granted: 1978-05-23
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Expires: 1997-05-12
Abstract
Abstract pg,1 Steroids having the formula ##STR1## wherein X is ##STR2## R 1 is alkyl, aryl or acyloxyalkyl; R 2 and R 3 are the same or different and are hydrogen, alkyl, alkoxy, carboalkoxy, formyl, ##STR3## hydroxy, halogen, phenyl or cyano, with the proviso that when R 2 and R 3 are different, one of R 2 and R 3 is hydrogen; R 4 is carbonyl, β-hydroxymethylene or β-acyloxymethylene; R 5 is hydrogen or halogen; and R 6 is hydrogen or fluorine; can be used as antiinflammatory agents.
Inventors
- 👤 Ravi K. Varma
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 08:28
CPC Classifications
C; C07; C07J; C07J31/00; C07J31/003; A; A61; A61P; A61P29/00; C07J53/00; C07J53/002
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
137 words
A steroid having the formula ##STR19## or the 1,2-dehydro derivative thereof, wherein X is ##STR20## R 1 is alkyl, aryl or acyloxyalkyl; R 2 and R 3 are the same or different and are hydrogen, alkyl, alkoxy, carboalkoxy, formyl, ##STR21## hydroxy, halogen, phenyl or cyano, with the proviso that when R 2 and R 3 are different, one of R 2 and R 3 is hydrogen; R 4 is carbonyl, β-hydroxymethylene or β-acyloxymethylene; R 5 is hydrogen or halogen; and R 6 is hydrogen or fluorine; wherein the term "aryl" refers to phenyl or phenyl substituted with one or two alkyl, alkoxy or halogen substituents; the term "acyloxy" refers to a group having the formula ##STR22## wherein Y is alkyl or aryl; and the terms "alkyl" and "alkoxy" refer to groups having 1 to 10 carbon atoms.
Claim 2
Dependent Claim
137 words
A steroid having the formula ##STR19## or the 1,2-dehydro derivative thereof, wherein X is ##STR20## R 1 is alkyl, aryl or acyloxyalkyl; R 2 and R 3 are the same or different and are hydrogen, alkyl, alkoxy, carboalkoxy, formyl, ##STR21## hydroxy, halogen, phenyl or cyano, with the proviso that when R 2 and R 3 are different, one of R 2 and R 3 is hydrogen; R 4 is carbonyl, β-hydroxymethylene or β-acyloxymethylene; R 5 is hydrogen or halogen; and R 6 is hydrogen or fluorine; wherein the term "aryl" refers to phenyl or phenyl substituted with one or two alkyl, alkoxy or halogen substituents; the term "acyloxy" refers to a group having the formula ##STR22## wherein Y is alkyl or aryl; and the terms "alkyl" and "alkoxy" refer to groups having 1 to 10 carbon atoms.
Claim 3
Dependent Claim
11 words
A steroid in accordance with claim 1 wherein X is --S--.
Claim 4
Dependent Claim
11 words
A steroid in accordance with claim 1 wherein X is ##STR23##
Claim 5
Dependent Claim
11 words
A steroid in accordance with claim 1 wherein X is ##STR24##
Claim 6
Dependent Claim
12 words
A steroid in accordance with claim 1 wherein R 1 is alkyl.
Claim 7
Dependent Claim
12 words
A steroid in accordance with claim 1 wherein R 1 is aryl.
Claim 8
Dependent Claim
12 words
A steroid in accordance with claim 1 wherein R 1 is acyloxyalkyl.
Claim 9
Dependent Claim
15 words
A steroid in accordance with claim 1 wherein R 2 and R 3 are hydrogen.
Claim 10
Dependent Claim
21 words
A steroid in accordance with claim 1 wherein R 4 is β-hydroxymethylene, R 5 is fluorine, and R 6 is hydrogen.
Claim 11
Dependent Claim
8 words
The steroid in accordance with claim 1, 9-fluoro-1',2',3',4'-tetrahydro-11β-hydroxy-17-(methylthio)androsta-1,4-dieno[16α,17α-b]naphthalene-3-one.
Claim 12
Dependent Claim
8 words
The steroid in accordance with claim 1, 9-fluoro-1',2',3',4'-tetrahydro-11β-hydroxy-17-(methylsulfonyl)androsta-1,4-dieno[16α,17α-b]naphthalene-3-one.
Claim 13
Dependent Claim
8 words
The steroid in accordance with claim 1, 4'β-ethoxy-9-fluoro-1',2',3',4'-tetrahydro-11β-hydroxy-17-(methylsulfonyl)-androsta-1,4-dieno[16α,17α-b]naphthalene-3-one.
Claim 14
Dependent Claim
8 words
The steroid in accordance with claim 1, 17-[[(acetyloxy)methyl]sulfonyl]-9-fluoro-1',2',3',4'-tetrahydro-11β-hydroxyandrosta-1,4-dieno[16α,17α-b]naphthalene-3-one.
Claim 15
Dependent Claim
8 words
The steroid in accordance with claim 1, 17-[[(acetyloxy)methyl]sulfonyl]-4'β-ethoxy-9-fluoro-1',2',3',4'-tetrahydro-11β-hydroxyandrosta-1,4-dieno[16α,17α-b]naphthalene-3-one.
Claim 16
Dependent Claim
8 words
The steroid in accordance with claim 1, 9-fluoro-1',2',3',4'-tetrahydro-11β-hydroxy-17-(methylsulfinyl)-androsta-1,4-dieno[16α,17α-b]naphthalene-3-one.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-05-22 | 1981-11-21 | 1982-05-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-05-22 | 1985-11-21 | 1986-05-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-05-22 | 1989-11-21 | 1990-05-23 | $7700.00 | Window Closed / Lapsed |