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EP0138683A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Purine derivatives, their application in anti-viral compositions

Assignee: Merck and Co Inc
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Filing: 1984-09-24
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Granted: —
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Expires: 2004-09-24
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Abstract

Abstract Compounds of the formula and the pharmaceutically acceptable salts thereof are disclosed. In these compounds, R 1 is halogen, -SR 4 wherein R 4 is H or alkyl of 1 to 4 carbon atoms, - OCH 3 , - OSO 2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms, -NR 4 R 5 wherein R 4 is as defined above and R 5 is H, alkyl of 1 to 4 carbon atoms, amino, alkanoyl of 1 to 8 carbon atoms, benzoyl, methoxy or hydroxy or R 1 is - N(CH 3 ) 3 + X - wherein X is halogen or -OSO 2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms; R 2 is H, alkanoyl of 1 to 8 carbon atoms or benzoyl; R 3 is A or B wherein A is wherein R 6 and R 7 are independently selected from wherein R 6 and R 9 are independently selected from pharmaceutically acceptable cations and H, H, or R 6 and R 7 taken together are wherein R 10 is selected from pharmaceutically acceptable cations and H; with the proviso that R 4 is not H when: R S is H, R 3 is A, and R 6 and R 7 are H. The compounds have anti-viral activity.

Inventors

  • 👤 Richard L. Tolman
  • 👤 Wallace Ashton
  • 👤 Malcolm Maccoss

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-09 16:09
CPC Classifications
C; C07; C07D; C07D473/00; A; A61; A61P; A61P31/00; A61P31/12; A61P31/20; A61P31/22; C07F; C07F9/00; C07F9/02; C07F9/547; C07F9/6561; C07F9/65616

Claims Analysis

Total Claims: 6
Claim 1
Independent Claim 226 words
A compound of the formula: and the pharmaceutically acceptable salts thereof wherein R 1 is halogen, -SR 4 wherein R 4 is H or alkyl of 1 to 4 carbon atoms, -OCH 3 , -OS0 2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms, - NR 4 R 5 wherein R 4 is as defined above and R 5 is H, alkyl of 1 to 4 carbon atoms, amino, alkanoyl of 1 to 8 carbon atoms, benzoyl, methoxy or hydroxy, or R 1 is -N(CH 3 ) + 3 X - wherein X is halogen or -OS0 2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms; R 2 is H or alkanoyl of 1 to 8 carbon atoms or benzoyl; R 3 is A or B wherein A is wherein R 6 and R 7 are independently selected from H and wherein R 8 and R 9 are independently selected from pharmaceutically acceptable cations and H , or R 6 and R 7 taken together are wherein R 10 is selected from pharmaceutically acceptable cations and H; with the proviso that R 4 is not H when: R 5 is H , R 3 is A, and R 6 and R 7 are H.
Claim 2
Dependent Claim 226 words
A compound of the formula: and the pharmaceutically acceptable salts thereof wherein R 1 is halogen, -SR 4 wherein R 4 is H or alkyl of 1 to 4 carbon atoms, -OCH 3 , -OS0 2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms, - NR 4 R 5 wherein R 4 is as defined above and R 5 is H, alkyl of 1 to 4 carbon atoms, amino, alkanoyl of 1 to 8 carbon atoms, benzoyl, methoxy or hydroxy, or R 1 is -N(CH 3 ) + 3 X - wherein X is halogen or -OS0 2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms; R 2 is H or alkanoyl of 1 to 8 carbon atoms or benzoyl; R 3 is A or B wherein A is wherein R 6 and R 7 are independently selected from H and wherein R 8 and R 9 are independently selected from pharmaceutically acceptable cations and H , or R 6 and R 7 taken together are wherein R 10 is selected from pharmaceutically acceptable cations and H; with the proviso that R 4 is not H when: R 5 is H , R 3 is A, and R 6 and R 7 are H.
Claim 3
Dependent Claim 43 words
A compound according to Claim 1, wherein R 1 is -NH 2 , -NHCH 3 or -SH; R 2 is H; and R 6 and Rare H or R 6 and R 7 taken together are wherein R 10 is as defined above.
Claim 4
Dependent Claim 13 words
A compound according to Claim 1, wherein R 1 is -OSO 2 Ar.
Claim 5
Dependent Claim 23 words
An anti-viral pharmaceutical composition comprising an effective amount of a compound of one of claims 1 to 3 and a pharmaceutically acceptable carrier.
Claim 6
Dependent Claim 15 words
Application of a compound according to one of claims 1 to 3 as anti-viral agent.

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