US4004004A
Expired / Lapsed
US
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Fusidic acid derivatives
Assignee: Leo Pharma AS
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Filing: 1975-08-12
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Granted: 1977-01-18
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Expires: 1995-08-12
Abstract
Abstract The present invention relates to a series of new fusidic acid derivatives and salts or easily hydrolysable esters thereof, to the preparation of these compounds and to pharmaceutical compositions containing the compounds. The new compounds have the general formula: <IMAGE> I in which R1 and R2 stand for an alkanoyl, aralkanoyl or aroyl radical and R2 also can be hydrogen; the dotted line between C-24 and C-25 indicates a double bond or a single bond, and the wavy line at C-3 indicates that OR1 is either alpha -oriented or beta -oriented. The compounds of the invention have a remarkable anti-inflammatory effect and cause a pronounced relief on patients suffering from arthritis.
Inventors
- 👤 Welf von Daehne
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 12:29
CPC Classifications
C; C07; C07J; C07J13/00; C07J13/007; C07J17/00; C07J41/00; C07J41/0033; C07J41/0088; C07J41/0094
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
139 words
A pharmaceutical composition in dosage unit form for the treatment of patients suffering from arthritis, which comprises as therapeutical ingredient at least one compound of the formula: ##STR11##in which R 1 and R 2 stand for a lower alkanoyl radical having from 2 to 8 carbon atoms, a mono- or bicyclic, carbocyclic aryl-lower alkanoyl radical, or a mono- or bicyclic, carbocyclic aroyl radical; and R 2 also stands for hydrogen; the dotted line between C-24 and C-25 indicates a double bond or a single bond; and the wavy line at C-3 indicates that OR 1 is α- or β-oriented; and pharmaceutically acceptable, non-toxic salts or easily hydrolyzable esters thereof, said compound being admixed with an atoxic, pharmaceutically acceptable carrier, and the dosage unit being between 100 to 1000 mg calculated as the free acid of the therapeutically active compound.
Claim 2
Dependent Claim
139 words
A pharmaceutical composition in dosage unit form for the treatment of patients suffering from arthritis, which comprises as therapeutical ingredient at least one compound of the formula: ##STR11##in which R 1 and R 2 stand for a lower alkanoyl radical having from 2 to 8 carbon atoms, a mono- or bicyclic, carbocyclic aryl-lower alkanoyl radical, or a mono- or bicyclic, carbocyclic aroyl radical; and R 2 also stands for hydrogen; the dotted line between C-24 and C-25 indicates a double bond or a single bond; and the wavy line at C-3 indicates that OR 1 is α- or β-oriented; and pharmaceutically acceptable, non-toxic salts or easily hydrolyzable esters thereof, said compound being admixed with an atoxic, pharmaceutically acceptable carrier, and the dosage unit being between 100 to 1000 mg calculated as the free acid of the therapeutically active compound.
Claim 3
Dependent Claim
17 words
A composition as claimed in claim 1 wherein the dosage unit is in the form of tablets.
Claim 4
Dependent Claim
17 words
A composition as claimed in claim 1 wherein the dosage unit is in the form of capsules.
Claim 5
Dependent Claim
17 words
A composition as claimed in claim 1 wherein the dosage unit is in the form of pills.
Claim 6
Dependent Claim
35 words
A composition as claimed in claim 1 wherein the dosage unit is in the injectable form of preparation and contains from 50 to 500 mg, calculated as the free acid, of the therapeutically active compound.
Claim 7
Dependent Claim
32 words
A composition as claimed in claim 1 wherein the dosage unit is a suspension for oral use and containing the therapautically active compound in an amount of from 2 to 25 percent.
Claim 8
Dependent Claim
25 words
A composition according to claim 1 in which the active ingredient is 3-O-acetyl-16-epideacetylfusidic acid or a pharmaceutically acceptable, non-toxic salt or easily hydrolyzable ester thereof.
Claim 9
Independent Claim
105 words
A method of treating acute or chronic arthritis which comprises administering into the body an effective amount of a compound of the formula: ##STR12##in which R 1 and R 2 stand for a lower alkanoyl radical having from 2 to 8 carbon atoms, a mono- or bicyclic, carbocyclic aryl-lower alkanoyl radical, or a mono- or bicyclic, carbocyclic aroyl radical; and R 2 also stands for hydrogen; the dotted line between C-24 and C-25 indicates a double bond or a single bond; and the wavy line at C-3 indicates that OR 1 is α- or β-oriented; and pharmaceutically acceptable, non-toxic salts or easily hydrolyzable esters thereof.
Claim 10
Independent Claim
105 words
A method of treating acute or chronic arthritis which comprises administering into the body an effective amount of a compound of the formula: ##STR12##in which R 1 and R 2 stand for a lower alkanoyl radical having from 2 to 8 carbon atoms, a mono- or bicyclic, carbocyclic aryl-lower alkanoyl radical, or a mono- or bicyclic, carbocyclic aroyl radical; and R 2 also stands for hydrogen; the dotted line between C-24 and C-25 indicates a double bond or a single bond; and the wavy line at C-3 indicates that OR 1 is α- or β-oriented; and pharmaceutically acceptable, non-toxic salts or easily hydrolyzable esters thereof.
Claim 11
Dependent Claim
35 words
A method according to claim 8 in which the therapeutically active compound is administered by the oral route, in amounts from 200 to 4000 mg per day, preferably from 500 to 2000 mg per day.
Claim 12
Dependent Claim
109 words
A pharmaceutical composition in dosage unit form for the treatment of arthritis comprising an effective amount of a compound of the formula: ##STR13##in which R 1 and R 2 stand for a lower alkanoyl radical having from 2 to 8 carbon atoms, a mono- or bicyclic, carbocyclic aryl-lower alkanoyl radical, or a mono- or bicyclic, carbocyclic aroyl radical; and R 2 also stands for hydrogen; the dotted line between C-24 and C-25 indicates a double bond or a single bond; and the wavy line at C-3 indicates that OR 1 is α- or β-oriented; and pharmaceutically acceptable, non-toxic salts or easily hydrolyzable esters thereof and an inert carrier therefor.
Claim 13
Dependent Claim
109 words
A pharmaceutical composition in dosage unit form for the treatment of arthritis comprising an effective amount of a compound of the formula: ##STR13##in which R 1 and R 2 stand for a lower alkanoyl radical having from 2 to 8 carbon atoms, a mono- or bicyclic, carbocyclic aryl-lower alkanoyl radical, or a mono- or bicyclic, carbocyclic aroyl radical; and R 2 also stands for hydrogen; the dotted line between C-24 and C-25 indicates a double bond or a single bond; and the wavy line at C-3 indicates that OR 1 is α- or β-oriented; and pharmaceutically acceptable, non-toxic salts or easily hydrolyzable esters thereof and an inert carrier therefor.
References Cited (Backward Citations)
US3867413A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-01-18 | 1980-07-19 | 1981-01-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-01-18 | 1984-07-19 | 1985-01-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-01-18 | 1988-07-19 | 1989-01-18 | $7700.00 | Window Closed / Lapsed |