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US4435390A
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Hydrocortisone derivatives, the preparation and use thereof
Assignee: Bayer Pharma AG
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Filing: 1982-08-18
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Granted: 1984-03-06
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Expires: 2002-08-18
Abstract
Abstract Hydrocortisone derivatives of Formula I ##STR1## wherein is a single bond or a double bond, n is 1 or 2, R 1 is hydrogen or methyl, R 2 is alkyl of 1-6 carbon atoms, and R 3 is hydrogen or 1-oxoalkyl (alkanoyl) of 2-6 carbon atoms, are pharmacologically active compounds, e.g., as antiinflammatories.
Inventors
- 👤 Klaus Annen
- 👤 Henry Laurent
- 👤 Helmut Hofmeister
- 👤 Rudolf Wiechert
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 10:38
CPC Classifications
C; C07; C07J; C07J5/00; C07J5/0046; C07J5/0053; A; A61; A61P; A61P17/00; A61P37/00; A61P37/08
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
46 words
A hydrocortisone derivative of the formula ##STR4## wherein is a single bond or a double bond, n is 1 or 2, R 1 is hydrogen or methyl, R 2 is alkyl of 1-6 carbon atoms, and R 3 is hydrogen or alkanoyl of 2-6 carbon atoms.
Claim 2
Dependent Claim
46 words
A hydrocortisone derivative of the formula ##STR4## wherein is a single bond or a double bond, n is 1 or 2, R 1 is hydrogen or methyl, R 2 is alkyl of 1-6 carbon atoms, and R 3 is hydrogen or alkanoyl of 2-6 carbon atoms.
Claim 3
Dependent Claim
6 words
17-Ethoxyacetoxy-11β,21-dihydroxy-4-pregnene-3,20-dione, a compound of claim 1.
Claim 4
Dependent Claim
6 words
11β,21-Dihydroxy-17-methoxyacetoxy-4-pregnene-3,20-dione, a compound of claim 1.
Claim 5
Dependent Claim
6 words
17-(3-Ethoxypropionyloxy)-11β,21-dihydroxy-4-pregnene-3,20-dione, a compound of claim 1.
Claim 6
Dependent Claim
6 words
11β,21-Dihydroxy-17-(3-methoxypropionyloxy)-4-pregnene-3,20-dione, a compound of claim 1.
Claim 7
Dependent Claim
6 words
17-Ethoxyacetoxy-11β,21-dihydroxy-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 8
Dependent Claim
6 words
21-Acetoxy-11.beta.-hydroxy-17-(3-methoxypropionyloxy)-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 9
Dependent Claim
6 words
11β,21-Dihydroxy-17-(3-methoxypropionyloxy)-6α-methyl-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 10
Dependent Claim
6 words
21-Acetoxy-11β-hydroxy-17-(3-methoxypropionyloxy)-6α-methyl-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 11
Dependent Claim
6 words
21-Acetoxy-11.beta.-hydroxy-17-methoxyacetoxy-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 12
Dependent Claim
6 words
17-Ethoxyacetoxy-11β,21-dihydroxy-6α-methyl-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 13
Dependent Claim
6 words
17-(3-Ethoxypropionyloxy)-11β,21-dihydroxy-6α-methyl-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 14
Dependent Claim
6 words
21-Acetoxy-17-(3-ethoxypropionyloxy)-11β-hydroxy-6α-methyl-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 15
Dependent Claim
6 words
11β-Hydroxy-17-methoxyacetoxy-21-propionyloxy-6α-methyl-1,4pregnadiene-3,20-dione, a compound of claim 1.
Claim 16
Dependent Claim
6 words
21-Butyryloxy-11.beta.-hydroxy-17-methoxyacetoxy-6α-methyl-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 17
Dependent Claim
6 words
21-Acetoxy-11β-hydroxy-17-methoxyacetoxy-6α-methyl-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 18
Dependent Claim
6 words
11β-Hydroxy-21-isobutyryloxy-17-methoxyacetoxy-6α-methyl-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 19
Dependent Claim
6 words
21-Acetoxy-17-ethoxyacetoxy-11β-hydroxy-6α-methyl-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 20
Dependent Claim
6 words
11β,21-Dihydroxy-17-methoxyacetoxy-6α-methyl-4-pregnene-3,20-dione, a compound of claim 1.
Claim 21
Dependent Claim
6 words
17-Ethoxyacetoxy-11β,21-dihydroxy-6α-methyl-4-pregnene-3,20-dione, a compound of claim 1.
Claim 22
Dependent Claim
6 words
21-Acetoxy-11.beta.-hydroxy-17-methoxyacetoxy-6α-methyl-4-pregnene-3,20-dione, a compound of claim 1.
Claim 23
Dependent Claim
6 words
21-Acetoxy-11.beta.-hydroxy-17-(3-methoxypropionyloxy)-6α-methyl-4-pregnene-3,20-dione, a compound of claim 1.
Claim 24
Dependent Claim
6 words
11β,21-dihydroxy-17-methoxyacetoxy-6α-methyl-1,4-pregnadiene-3,20-dione, a compound of claim 1.
Claim 25
Dependent Claim
19 words
A pharmaceutical composition comprising an antiinflammatorily effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.
Claim 26
Dependent Claim
14 words
A pharmaceutical composition of claim 24 wherein the carrier is adapted for topical administration.
Claim 27
Dependent Claim
12 words
A pharmaceutical composition of claim 24 comprising 1 or 2 antiinflammatory agents.
Claim 28
Dependent Claim
27 words
A method of treating inflammation in a patient in need of such treatment comprising administering an amount of a compound of claim 1 effective for such treatment.
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) | 1987-03-06 | 1987-09-05 | 1988-03-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-03-06 | 1991-09-05 | 1992-03-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-03-06 | 1995-09-05 | 1996-03-06 | $7700.00 | Window Closed / Lapsed |