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US4481197A Expired / Lapsed US ⏱️ 0.0 years remaining

Anti-inflammatory deoxyribosides

Assignee: SmithKline Beecham Corp
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Filing: 1982-06-17
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Granted: 1984-11-06
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Expires: 2002-06-17
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Abstract

Abstract The novel compounds 3-deaza-2'-deoxyadenosine and certain of its derivatives and their pharmaceutically acceptable salts have anti-inflammatory activity as well as immune response suppression activity. 3-Deaza-2'-deoxyadenosine and certain of its intermediates are synthesized by the enzyme catalyzed reaction of the appropriately substituted 3-deazapurine with a 2'-deoxyribose donor.

Inventors

  • 👤 Janet L. Rideout
  • 👤 Thomas A. Krenitsky

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-27 12:35
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/052; C12; C12P; C12P19/00; C12P19/26; C12P19/28

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 35 words
The compound of formula (I) ##STR8## the 5'-phosphate ester thereof, organic esters of the compound or its 5'-phosphate ester with lower alkanoic or benzoic acid and pharmaceutically acceptable salts of the compound or its esters.
Claim 2
Dependent Claim 35 words
The compound of formula (I) ##STR8## the 5'-phosphate ester thereof, organic esters of the compound or its 5'-phosphate ester with lower alkanoic or benzoic acid and pharmaceutically acceptable salts of the compound or its esters.
Claim 3
Dependent Claim 11 words
A compound of formula (IIA) ##STR9## wherein R 1 is halogen.
Claim 4
Dependent Claim 11 words
A compound of formula (IIA) ##STR9## wherein R 1 is halogen.
Claim 5
Independent Claim 69 words
A method for the treatment of inflammation comprising the administration to a human or other mammal suffering from an inflammatory condition an effective anti-inflammatory, non-toxic amount of an active ingredient selected from the compound of formula (I) ##STR10## the 5'-phosphate ester of said compound, organic esters of said compound or its 5'-phosphate ester with lower alkanoic or benzoic acid and pharmaceutically acceptable salts of said compound or its esters.
Claim 6
Independent Claim 69 words
A method for the treatment of inflammation comprising the administration to a human or other mammal suffering from an inflammatory condition an effective anti-inflammatory, non-toxic amount of an active ingredient selected from the compound of formula (I) ##STR10## the 5'-phosphate ester of said compound, organic esters of said compound or its 5'-phosphate ester with lower alkanoic or benzoic acid and pharmaceutically acceptable salts of said compound or its esters.
Claim 7
Dependent Claim 33 words
A method according to claim 3 wherein said active ingredient is administered orally or parenterally in a dosage of from about 0.05 mg/kg to about 10 mg/kg body weight of recipient per day.
Claim 8
Dependent Claim 19 words
A method according to claim 3 wherein said active ingredient is administered topically for the exertion of local action.
Claim 9
Dependent Claim 12 words
A method according to claim 3 wherein said inflammatory condition is arthritis.
Claim 10
Dependent Claim 25 words
A method according to claim 3 comprising the administration of a pharmaceutical formulation comprising the active ingredient in association with a pharmaceutically acceptable carrier therefor.
Claim 11
Independent Claim 68 words
A method for the suppression of the immune response in a human or other mammal comprising the administration of an immune response suppressing non-toxic amount of an active ingredient selected from the compound of formula (I), ##STR11## the 5'-phosphate ester of said compound, organic esters of said compound or its 5'-phosphate ester with lower alkanoic or benzoic acid and pharmaceutically acceptable salts of said compound or its esters.
Claim 12
Independent Claim 68 words
A method for the suppression of the immune response in a human or other mammal comprising the administration of an immune response suppressing non-toxic amount of an active ingredient selected from the compound of formula (I), ##STR11## the 5'-phosphate ester of said compound, organic esters of said compound or its 5'-phosphate ester with lower alkanoic or benzoic acid and pharmaceutically acceptable salts of said compound or its esters.
Claim 13
Dependent Claim 29 words
A method according to claim 8 wherein said active ingredient is administered orally or parenterally in a dosage of at least 10 mg/kg body weight of recipient per day.
Claim 14
Dependent Claim 16 words
A method according to claim 8 for treating autoimmune disease or preventing rejection of foreign cells.
Claim 15
Dependent Claim 73 words
A pharmaceutical formulation for use in treatment of inflammation or suppression of the immune response or both comprising an effective inflammation or immune response nontoxic treatment amount of an ingredient selected from the compound of formula (I) ##STR12## the 5'-phosphate ester thereof, organic esters of the compound or its 5'-phosphate ester with lower alkanoic or benzoic acid and pharmaceutically acceptable salts of the compound or its esters and a pharmaceutically acceptable carrier therefore.
Claim 16
Dependent Claim 73 words
A pharmaceutical formulation for use in treatment of inflammation or suppression of the immune response or both comprising an effective inflammation or immune response nontoxic treatment amount of an ingredient selected from the compound of formula (I) ##STR12## the 5'-phosphate ester thereof, organic esters of the compound or its 5'-phosphate ester with lower alkanoic or benzoic acid and pharmaceutically acceptable salts of the compound or its esters and a pharmaceutically acceptable carrier therefore.

References Cited (Backward Citations)

US4056674A Cited
US4210639A Cited
US4309419A Cited
US4322411A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1987-11-06 1988-05-07 1988-11-06 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1991-11-06 1992-05-07 1992-11-06 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1995-11-06 1996-05-07 1996-11-06 $7700.00 Window Closed / Lapsed

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