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EP0010668A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

3-Deazaadenosine and pharmaceutical compositions containing it

Assignee: Wellcome Foundation Ltd
•
Filing: 1979-10-12
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Granted: —
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Expires: 1999-10-12
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Abstract

Abstract Adenosine derivatives for inhibition of immune response are disclosed. Adenosine derivatives of formula(I) Wherein R 1 is amino or lower alkyl amino; R 2 is hydrogen or an aliphatic carboxylic acid residue; and R 3 is hydrogen, aliphatic carboxylic acid residue or a phosphoric acid residue, are useful as inhibitors of immune response. The activity is potentiated by derivatives of homocysteine and homocystine. Particularly useful is 3-deaza-adenosine both alone and in combination with L-homocysteine thio- lacetone, Pharmaceutical formulations of compounds of formula (I) alone and with potentiators are provided.

Inventors

  • 👤 Gerald Wolberg
  • 👤 Thomas Paul Zimmerman

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-08 15:29
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/052; A; A61; A61P; A61P37/00; A61P37/02; A61P37/06; A61P43/00

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 48 words
A compound of the formula (I) or pharmaceutically acceptable salts thereof wherein R 1 is amino or lower alkylamino; R 2 is hydrogen or an aliphatic carboxylic acid residue; and R 3 is hydrogen, and aliphatic carboxylic acid residue or a phosphoric acid residue, for use in medicine.
Claim 2
Dependent Claim 48 words
A compound of the formula (I) or pharmaceutically acceptable salts thereof wherein R 1 is amino or lower alkylamino; R 2 is hydrogen or an aliphatic carboxylic acid residue; and R 3 is hydrogen, and aliphatic carboxylic acid residue or a phosphoric acid residue, for use in medicine.
Claim 3
Dependent Claim 11 words
3-Deazaadenosine or a pharmaceutically acceptable salt thereof for use in medicine.
Claim 4
Dependent Claim 11 words
3-Deazaadenosine or a pharmaceutically acceptable salt thereof for use in medicine.
Claim 5
Dependent Claim 25 words
A pharmaceutical formulation comprising a compound of formula (I) or a salt thereof as defined in claim 1, together with a pharmaceutically acceptable carrier therefore.
Claim 6
Dependent Claim 17 words
A pharmaceutical formulation as claimed in claim 3 in which the compound of formula (1) is 3-deazaadenosine.
Claim 7
Dependent Claim 17 words
5 A pharmaceutical formulation as claimed in either claim 3 or claim 4 in unit dosage form.
Claim 8
Dependent Claim 36 words
6 A combination comprising a compound of formula (I) or a salt thereof as defined in claim I together with a potentiator selected from L-homocysteine, D-homocysteine, L-homocysteine thiolactone, D-homocysteine thiolactone, L-homocystine, D-homocystine and their selenium analogues.
Claim 9
Dependent Claim 13 words
A combination comprising 3-deazaadenosine or a pharmaceutically acceptable salt thereof and L-homocysteine thiolactone.
Claim 10
Dependent Claim 13 words
A combination comprising 3-deazaadenosine or a pharmaceutically acceptable salt thereof and L-homocysteine thiolactone.
Claim 11
Dependent Claim 27 words
A combination as claimed in either claim 6 or claim 7 wherein the two components are respectively present in a weight ratio of from 1:100 to 1:10.
Claim 12
Dependent Claim 16 words
A combination as claimed in any one of claims 6 to 8 for use in medicine.
Claim 13
Dependent Claim 24 words
10 A pharmaceutical formulation comprising a combination as defined in any one of claims 6 to 8 together with a pharmaceutically acceptable carrier therefor.
Claim 14
Dependent Claim 13 words
11 A pharmaceutical formulation as claimed in claim 10 in unit dosage form.
Claim 15
Dependent Claim 41 words
12 A pharmaceutical formulation as claimed in claim 11 wherein the compound of formula (I) is present in an amount of from 5 mg to 100 mg and the potentiator is present in an amount of from 50 mg to 1g.
Claim 16
Dependent Claim 33 words
13 A method for the preparation of a pharmaceutical formulation as defined in any one of claims 3,4,5,10,11 or 12 which comprises admixture of the active ingredient(s) with a pharmaceutcially acceptable carrier therefor.

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