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EP0038569A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Deazapurine nucleosides, formulations and preparation thereof

Assignee: Wellcome Foundation Ltd
•
Filing: 1981-04-22
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Granted: —
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Expires: 2001-04-22
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Abstract

Abstract 4-Amino-1-(2-deoxy-β-D-ribofuranosyl)-1H-imidazo [4,5-c] pyridine, esters thereof and pharmaceutical salts thereof, methods for the preparation thereof, pharmaceutical formulations thereof and the use thereof in medicine, in particular in the treatment of inflammation, are disclosed. Also disclosed are intermediates for use in preparing the title compound and methods for the preparation of the intermediates.

Inventors

  • 👤 Janet Litster Rideout
  • 👤 Thomas Anthony Krenitsky

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-01 12:16
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/052; A; A61; A61P; A61P29/00

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 19 words
A compound of the formula (I) organic esters thereof and pharmaceutically acceptable salts of the compound or its ester.
Claim 2
Dependent Claim 19 words
A compound of the formula (I) organic esters thereof and pharmaceutically acceptable salts of the compound or its ester.
Claim 3
Dependent Claim 1 words
4-Amino-1-(2-deoxy-β-D-ribofuranosyl)-1H-imidazo-[4,5-c]-pyridine.
Claim 4
Dependent Claim 1 words
4-Amino-1-(2-deoxy-β-D-ribofuranosyl)-1H-imidazo-[4,5-c]-pyridine.
Claim 5
Dependent Claim 13 words
A compound of the formula (HA) wherein R is halogen or substituted amino.
Claim 6
Dependent Claim 13 words
A compound of the formula (HA) wherein R is halogen or substituted amino.
Claim 7
Independent Claim 49 words
A method for the preparation of a compound of the formula (II) wherein R is halogen, amino or substituted amino, which comprises reacting a 4-substituted-1H-[4,5-c]-pyridine base of formuia (III) 00385 wherein R is as defined above, with a 2-deoxyribosyl donor system comprising 2-deoxyribose-1-phosphate and a purine nucleoside phosphorylase enzyme.
Claim 8
Independent Claim 49 words
A method for the preparation of a compound of the formula (II) wherein R is halogen, amino or substituted amino, which comprises reacting a 4-substituted-1H-[4,5-c]-pyridine base of formuia (III) 00385 wherein R is as defined above, with a 2-deoxyribosyl donor system comprising 2-deoxyribose-1-phosphate and a purine nucleoside phosphorylase enzyme.
Claim 9
Dependent Claim 41 words
A method for the preparation of a compound of formula (I) as defined in claim 1 which comprises the conversion of the 4-substituent of a compound of formula (IV) wherein R 2 is halogen or protected amino, into an amino group.
Claim 10
Dependent Claim 26 words
A method as claimed in claim 5 wherein the compound of formula (IV) was obtained by reaction of the corresponding 4-substituted-IH-imidazo-[4,5-c]-pyrimidine with a 2-deoxyribose donor system.
Claim 11
Dependent Claim 69 words
A method for the preparation of a compound of formula (II) as defined in claim 4 which process comprises reacting a compound of formula wherein R is halogen, amino or substituted amino and Q is a leaving group capable of being replaced with a 2-deoxyribosyl moiety, with a compound of formula (VI) wherein A is an acyloxy group or a halogen atom and Z is a suitable protecting group.
Claim 12
Dependent Claim 35 words
A pharmaceutical formulation comprising the compound of formula (I) as defined in claim or an ester thereof or a pharmaceutically acceptable salt of the compound or ester thereof in association with a pharmaceutically acceptable carrier.
Claim 13
Dependent Claim 21 words
The compound of formula (I), its esters and pharmaceutically acceptable salts of the compounds or its esters for use in medicine.
Claim 14
Dependent Claim 21 words
The compound of formula (I), its esters and pharmaceutically acceptable salts of the compounds or its esters for use in medicine.
Claim 15
Dependent Claim 24 words
The compound of formula (I), its esters and pharmaceutically acceptable salt of the compound or its esters for use in the treatment of inflammation.
Claim 16
Dependent Claim 24 words
The compound of formula (I), its esters and pharmaceutically acceptable salt of the compound or its esters for use in the treatment of inflammation.

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