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Therapeutic nucleosides and their preparation

Assignee: Wellcome Foundation Ltd
•
Filing: 1986-05-14
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Granted: —
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Expires: 2006-05-14
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Abstract

Abstract The present invention relates to certain 2',3'-dideoxy- nucleosides and pharmaceutically acceptable derivatives thereof, methods for preparing them, their use in the treatment and prophylaxis of viral, especially retroviral, infections, and pharmaceutical formulations containing them.

Inventors

  • 👤 George Walter Koszalka
  • 👤 Thomas Anthony Krenitsky

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-31 22:54
CPC Classifications
C; C07; C07D; C07D473/00; A; A61; A61P; A61P31/00; A61P31/12; A61P31/14; A61P31/18; C07D405/00; C07D405/02; C07D405/04; C07D473/02; C07D473/04; C07D473/06; C07D473/10; C07D473/26; C07D473/32; C07D473/36; C07D473/38; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/16

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 34 words
A compound of formula (I) wherein B is a purine or cytosine base linked to the sugar residue at the 9-or 1- position respectively, or a pharmaceutically acceptable derivative thereof, for use in therapy.
Claim 2
Dependent Claim 34 words
A compound of formula (I) wherein B is a purine or cytosine base linked to the sugar residue at the 9-or 1- position respectively, or a pharmaceutically acceptable derivative thereof, for use in therapy.
Claim 3
Dependent Claim 18 words
A compound as defined in claim 1 for use in the treatment or prophylaxis of a viral infection.
Claim 4
Dependent Claim 19 words
A compound as defined in claim 1 for use in the treatment or prophylaxis of retrovirus or retrovirus-like infection.
Claim 5
Dependent Claim 19 words
A compound as defined in claim 1 for use in the treatment or prophylaxis of PGL, ARC or AIDS.
Claim 6
Dependent Claim 18 words
A compound as defined in claim 1 for use in the treatment or prophylaxis of an AIDV infection.
Claim 7
Dependent Claim 18 words
A compound selected from: 2',3'-dideoxycytidine, 2',3'-dideoxyadenosine, 2',3'-dideoxyguanosine, 2',3'-dideoxyinosine, 6-methoxypurine-9-ß-D-2',3'-dideoxyribofuranoside, 6-methylthiopurine-9-P-D-2',3'-dideoxyribofuranoside, 2,6-diaminopurine-9-ß-D-2',3'-dideoxyribofuranoside and 2-aminopurine-9-ß-D-2',3'-dideoxyribofuranoside; and pharmaceutically acceptable derivatives thereof.
Claim 8
Dependent Claim 18 words
A compound selected from: 2',3'-dideoxycytidine, 2',3'-dideoxyadenosine, 2',3'-dideoxyguanosine, 2',3'-dideoxyinosine, 6-methoxypurine-9-ß-D-2',3'-dideoxyribofuranoside, 6-methylthiopurine-9-P-D-2',3'-dideoxyribofuranoside, 2,6-diaminopurine-9-ß-D-2',3'-dideoxyribofuranoside and 2-aminopurine-9-ß-D-2',3'-dideoxyribofuranoside; and pharmaceutically acceptable derivatives thereof.
Claim 9
Dependent Claim 17 words
A compound according to claim 6 for use as defined in any of claims 1 to 5.
Claim 10
Dependent Claim 32 words
Use of a compound as defined in either of claims 1 and 6 in the manufacture of a medicament for treatment or prophylaxis as defined in any of claims 1 to 5.
Claim 11
Dependent Claim 22 words
A pharmaceutical composition comprising a compound as defined in either of claims 1 and 6 together with a pharmaceutically acceptable carrier therefor.
Claim 12
Dependent Claim 183 words
A process for the preparation of a compound of formula (I) as defined in claim 1 and pharmaceutically acceptable derivatives thereof which comprises either: (A) reacting a compound of formula: wherein B is as defined in claim 1 and R is a precursor group for the hydroxy group, or for a pharmaceutically acceptable derivative group thereof, with an agent or under conditions serving to convert the said precursor group into the corresponding desired group; or (B) reacting a purine or cytosine base of formula wherein B is as defined in claim 1, or a functional equivalent thereof, with a compound serving to introduce the desired ribofuranosyl ring at the 9- or 1-position respectively of the purine or cystosine base of formula (III); and thereafter, or simultaneously therewith, effecting one or more of the following optional conversions:- (i) when a compound of formula (I) is formed, converting it into a pharmaceutically acceptable derivative thereof, and (ii) when a pharmaceutically acceptable derivative of a compound of formula (I) is formed, converting the said derivative into a compound of formula (I), or a different derivative thereof.
Claim 13
Dependent Claim 198 words
A process for the preparation of a compound of formula (I) wherein B is a purine or cytosine base linked to the sugar residue at the 9-or 1- position respectively, or a pharmaceutically acceptable derivative thereof, which comprises either: (A) reacting a compound of formula: wherein B is as defined in claim 1 and R is a precursor group for the hydroxy group, or for a pharmaceutically acceptable derivative group thereof, with an agent or under conditions serving to convert the said precursor group into the corresponding desired group; or (B) reacting a purine or cytosine base of formula wherein B is as defined in claim 1, or a functional equivalent thereof, with a compound serving to introduce the desired ribofuranosyl ring at the 9- or 1-position respectively of the purine or cystosine base of formula (III); and thereafter, or simultaneously therewith, effecting one or more of the following optional conversions:- (i) when a compound of formula (I) is formed, converting it into a pharmaceutically acceptable derivative thereof, and (ii) when a pharmaceutically acceptable derivative of a compound of formula (I) is formed, converting the said derivative into a compound of formula (I), or a different derivative thereof.
Claim 14
Dependent Claim 35 words
A process for the preparation of a compound according to claim 1, wherein the compound is selected from: 2',3'-dideoxycytidine, 2',3'-dideoxyadenosine, 2',3'-dideoxyguanosine, 2',3'-dideoxyinosine, 6-methoxypurine-9- ß-D-2',3'-dideoxyribofuranoside, 6-methylthiopurine-9-ß-D-2',3'-dideoxyribofuranoside, 2,6-diaminopurine-9- ß-D-2',3'-dideoxyribofuranoside and 2-aminopurine-9- ß-D-2',3'-dideoxyribofuranoside; and pharmaceutically acceptable derivatives thereof.

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