EP0486477A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
1-( -D-Arabinofuranosyl)-5-propynyluracil as a VZV-antiviral compound
Assignee: Wellcome Foundation Ltd
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Filing: 1987-12-14
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Granted: —
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Expires: 2007-12-14
Abstract
Abstract The present invention relates to certain 5-substituted pyrimidine nucleosides and pharmaceutically acceptable derivatives thereof and their use in the treatment and prophylaxis of varicella zoster virus, cytomegalovirus and Epstein Barr virus infections. Also provided are pharmaceutical formulations and processes for the preparation of the compounds according to the invention.
Inventors
- 👤 Saad George Rahim
- 👤 Dorothy Jane Martin Purifoy
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-29 14:43
CPC Classifications
C; C07; C07D; C07D405/00; C07D405/02; C07D405/04; A; A61; A61K; A61K31/00; A61K31/70; A61P; A61P31/00; A61P31/12; A61P31/20; A61P31/22; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06
Claims Analysis
Total Claims: 37
Claim 1
Independent Claim
95 words
A compound of the general formula (I): wherein R¹ represents an oxo or imine group; R² represents a hydrogen atom or a methyl group; R³ represents a hydrogen atom or a C₁₋₄ alkanoyl or benzoyl group optionally substituted by one or more halogen or alkyl substituents; and R⁴ represents a hydrogen atom or a hydroxy group; providing that when R², R³ and R⁴ each represent a hydrogen atom, R¹ does not represent an oxo group, and pharmaceutically acceptable salts, esters or salts of such esters for use in the treatment or prophylaxis of viral infections.
Claim 2
Dependent Claim
28 words
A compound as claimed in claim 1 and pharmaceutically acceptable salts, esters or salts of such esters for use in the treatment or prophylaxis of herpes viral infections.
Claim 3
Dependent Claim
29 words
A compound as claimed in claim 1 and pharmaceutically acceptable salts, esters or salts of such esters for use in the treatment or prophylaxis of varicella zoster viral infections.
Claim 4
Dependent Claim
23 words
A compound for uses as claimed in claims 1 to 3 which is of the general formula (I) as defined in claim 1.
Claim 5
Dependent Claim
103 words
Use of a compound of the general formula (I): wherein R¹ represents an oxo or imine group; R² represents a hydrogen atom or a methyl group; R³ represents a hydrogen atom or a C₁₋₄ alkanoyl or benzoyl group optionally substituted by one or more halogen or alkyl substituents; and R⁴ represents a hydrogen atom or a hydroxy group; providing that when R², R³ and R⁴ each represent a hydrogen atom, R¹ does not represent an oxo group, and pharmaceutically acceptable salts, esters or salts of such esters for use in the preparation of a medicament for the treatment of varicella zoster viral infections.
Claim 6
Dependent Claim
95 words
A pharmaceutical formulation comprising a compound of the general formula (I): wherein R¹ represents an oxo or imine group; R² represents a hydrogen atom or a methyl group; R³ represents a hydrogen atom or a C₁₋₄ alkanoyl or benzoyl group optionally substituted by one or more halogen or alkyl substituents; and R⁴ represents a hydrogen atom or a hydroxy group; providing that when R², R³ and R⁴ each represent a hydrogen atom, R¹ does not represent an oxo group, and pharmaceutically acceptable salts, esters or salts of such esters together with a pharmaceutically acceptable carrier.
Claim 7
Dependent Claim
17 words
Pharmaceutically acceptable esters or salts of such esters of 1-(β-D-arabinofuranosyl)-5-propynyluracil except the 5-prop-1-ynyl-1-(2',3', 5'-tri-O-toluoyl-β-D-arabinofuranosyl)uracil and 5-prop-1-ynyl-1-(2', 3',5'-tri-O-acetyl-β-D-arabinofuranosyl).
Claim 8
Dependent Claim
20 words
A pharmaceutical formulation comprising pharmaceutically acceptable esters or salts of such esters of 1-(β-D-arabinofuranosyl)-5-propynyluracil together with a pharmaceutically acceptable carrier.
Claim 9
Dependent Claim
20 words
Pharmaceutically acceptable esters or salts of such esters of 1-(β-D-arabinofuranosyl)-5-propynyluracil for use in the treatment or prophylaxis of viral infections.
Claim 10
Dependent Claim
24 words
Pharmaceutically acceptable esters or salts of such esters as claimed in claim 9 for use in the treatment or prophylaxis of herpes viral infections.
Claim 11
Dependent Claim
28 words
Use of pharmaceutically acceptable esters or salts of such esters of 1-(β-D-arabinofuranosyl)-5-propynyluracil in the manufacture of a medicament for the treatment or prophylaxis of varicella zoster virus infections.
Claim 12
Dependent Claim
10 words
A pharmaceutical formulation comprising 1-(β-D-arabinofuranosyl)-5-propynyluracil and a pharmaceutically acceptable carrier.
Claim 13
Dependent Claim
15 words
A pharmaceutical formulation comprising a pharmaceutically acceptable salt of 1-(β-D-arabinofuranosyl)-5-propynyluracil and a pharmaceutically acceptable carrier.
Claim 14
Dependent Claim
19 words
A pharmaceutical formulation as claimed in claim 13 wherein the pharmaceutically acceptable salt is a pharmaceutically acceptable base salt.
Claim 15
Dependent Claim
18 words
A pharmaceutical formulation as claimed in claim 14 wherein the pharmaceutically acceptable base salt is a sodium salt.
Claim 16
Dependent Claim
16 words
A pharmaceutical formulation as claimed in any of claims 12 to 15 adapted for oral administration.
Claim 17
Dependent Claim
17 words
A pharmaceutical formulation as claimed in claim 16 in the form of a tablet or a capsule.
Claim 18
Dependent Claim
25 words
A pharmaceutical formulation as claimed in claim 16 in the form of a solution or a suspension in an aqueous liquid or a non-aqueous liquid.
Claim 19
Dependent Claim
16 words
A pharmaceutical formulation as claimed in any of claims 12 to 15 adapted for parenteral administration.
Claim 20
Dependent Claim
19 words
A pharmaceutical formulation as claimed in claim 19 in the form of an aqueous or non-aqueous sterile injection solution.
Claim 21
Dependent Claim
19 words
A pharmaceutical formulation as claimed in either of claims 19 or 20 presented in a sealed ampoule or vial.
Claim 22
Dependent Claim
17 words
A pharmaceutical formulation as claimed in any of claims 19 to 21 presented in a freeze-dried condition.
Claim 23
Dependent Claim
17 words
A pharmaceutical formulation as claimed in any claims 12 to 15 presented in a unit dosage form.
Claim 24
Dependent Claim
29 words
A pharmaceutical formulation as claimed in claim 23 in which each unit dosage form contains 10-1000mg of the compound or a salt thereof defined in claims 12 to 15.
Claim 25
Dependent Claim
30 words
A pharmaceutical formulations as claimed in claim 24 in which each unit dosage form contains 20-500mg of the compound or a salt thereof as defined in claims 12 to 15.
Claim 26
Dependent Claim
29 words
A pharmaceutical formulation as claimed in claim 25 in which each unit dosage form contains 100-400mg of the compound or a salt thereof defined in claims 12 to 15.
Claim 27
Dependent Claim
23 words
A pharmaceutical formulation as claimed in any of claims 12 to 15 in a form of an ointment or cream for topical application.
Claim 28
Dependent Claim
32 words
A pharmaceutical formulation as claimed in claim 27 wherein the active compound or salt thereof as defined in claims 12 to 15 is present in an amount of 0.075 to 20% w/w.
Claim 29
Dependent Claim
25 words
A pharmaceutical formulation as claimed in claim 28 wherein the active compound or salt thereof is present in an amount of 0.2 to 15% w/w.
Claim 30
Dependent Claim
22 words
A pharmaceutical formulation as claimed in any of claims 12 to 15 for use in the treatment or prophylaxis of viral infections.
Claim 31
Dependent Claim
19 words
A pharmaceutical formulation as claimed in claim 30 for use in the treatment or prophylaxis of herpes viral infections.
Claim 32
Dependent Claim
20 words
A pharmaceutical formulation as claimed in claim 31 for use in the treatment or prophylaxis of varicella zoster viral infections.
Claim 33
Dependent Claim
18 words
A pharmaceutical formulation as claimed in claim 32 for use in the treatment or prophylaxis of chicken pox.
Claim 34
Dependent Claim
17 words
A pharmaceutical formulation as claimed in claim 32 for use in the treatment or prophylaxis of shingles.
Claim 35
Dependent Claim
44 words
A process for the preparation of a formulation as claimed in any one of claims 12 to 34 which comprises bringing the compound or a pharmaceutically acceptable salt thereof as defined in claims 12 to 15 into association with the said pharmaceutically acceptable carrier.
Claim 36
Dependent Claim
12 words
1-(β-D-arabinofuranosyl)-5-propynyluracil or a pharmaceutically acceptable salt thereof for use in medical therapy.
Claim 37
Dependent Claim
18 words
1-(β-D-arabinofuranosyl)-5-propynyluracil or a pharmaceutically acceptable salt thereof for use in the treatment of prophylaxis of a viral infection.
References Cited (Backward Citations)
No citation records indexed.
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