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EP0287313A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Acid stable dideoxynucleosides active against the cytopathic effects of human immunodeficiency virus

Assignee: United States Department of Commerce
•
Filing: 1988-04-12
•
Granted: —
•
Expires: 2008-04-12
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Abstract

Abstract 2ʹ3,ʹ-dideoxynucleosides which are effective in inhibiting the infectivity of the human immunodeficiency virus and which are stable in an acidic environment are disclosed, which compounds conform to the formula: wherein X      is selected from the group consisting of hydrogen, F, CN, N₃ and NO₂; Y      is either H or F; with the proviso that Y is F only when X=H. Also disclosed is a compound of the formula: Also disclosed are compounds conforming to the formula: wherein R      may be either OH or NH₂; and L is NH₂. Also disclosed are compounds conforming to the formula: wherein A      is selected from the group consisting of OH and NH₂ B      is selected from the group consisting of H, CH₃, CF₃, CH=CHBr, and halogen.

Inventors

  • 👤 Victor E. Marquez
  • 👤 John S. Driscoll
  • 👤 Christopher Kuo-Hou Tseng

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-30 20:44
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/16; A; A61; A61P; A61P31/00; A61P31/12; A61P31/14; A61P31/18

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 41 words
A compound characterized in that it con­forms to the formula: wherein X      is selected from the group consisting of hydrogen, F, CN, and NO₂; Y      is either H or F; with the proviso that X and Y cannot both be H.
Claim 2
Dependent Claim 41 words
A compound characterized in that it con­forms to the formula: wherein X      is selected from the group consisting of hydrogen, F, CN, and NO₂; Y      is either H or F; with the proviso that X and Y cannot both be H.
Claim 3
Dependent Claim 9 words
A compound according to claim 1 which is 2ʹ,3ʹ-dideoxy-2ʹ-beta-fluoroadenosine.
Claim 4
Dependent Claim 9 words
A compound according to claim 1 which is 2ʹ,3ʹ-dideoxy-2ʹ-alpha-fluoroadenosine.
Claim 5
Dependent Claim 32 words
A composition for inhibiting the infec­tivity of the human immunodeficiency virus characterized in that it comprises a compound according to any one of claims 1 to 3 and a pharmaceutically acceptable carrier.
Claim 6
Dependent Claim 15 words
A process for preparing 2ʹ,3ʹ-dideoxy-2ʹ-­beta-fluoroinosine characterized in that it comprises treating 2ʹ,3ʹ-dideoxy-2ʹ-beta-fluoroadenosine with adenosine deaminase.
Claim 7
Dependent Claim 15 words
A process for preparing 2ʹ,3ʹ-dideoxy-2ʹ-­beta-fluoroinosine characterized in that it comprises treating 2ʹ,3ʹ-dideoxy-2ʹ-beta-fluoroadenosine with adenosine deaminase.
Claim 8
Dependent Claim 25 words
A compound characterized in that it conforms to the formula wherein R      is selected from the group consisting of OH and NH₂ L      is NH₂.
Claim 9
Dependent Claim 25 words
A compound characterized in that it conforms to the formula wherein R      is selected from the group consisting of OH and NH₂ L      is NH₂.
Claim 10
Dependent Claim 8 words
A compound characterized in that it is 2ʹ,3ʹ-dideoxy-2ʹ-beta-fluoroinosine.
Claim 11
Dependent Claim 8 words
A compound characterized in that it is 2ʹ,3ʹ-dideoxy-2ʹ-beta-fluoroinosine.
Claim 12
Dependent Claim 27 words
A composition for inhibiting the infec­tivity of the human immunodeficiency virus characterized in that it comprises the compound of claim 7 and a pharmaceutically acceptable carrier therefor.
Claim 13
Dependent Claim 36 words
The compound characterized in that it conforms to the formula: wherein A      is selected from the group consisting of OH and NH₂; B      is selected from the group consisting of H, CH₃, CF₃, CH=CHBr, and halogen.
Claim 14
Dependent Claim 36 words
The compound characterized in that it conforms to the formula: wherein A      is selected from the group consisting of OH and NH₂; B      is selected from the group consisting of H, CH₃, CF₃, CH=CHBr, and halogen.

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