Patent EP0122707A1 successfully refreshed from Google Patents.
EP0122707A1
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EP
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Improvements in or relating to novel difluoro antiviral agents
Assignee: Eli Lilly and Co
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Filing: 1984-03-06
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Granted: —
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Expires: 2004-03-06
Abstract
Abstract The invention provides novel nucleosides and novel 2,2-difluoro-2-desoxycarbohydrates useful in the preparation of such nucleosides.
Inventors
- 👤 Larry Wayne Hertel
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-09 03:02
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07D; C07D307/00; C07D307/02; C07D307/26; C07D307/30; C07D307/32; C07D307/33; A; A61; A61P; A61P31/00; A61P31/12; C07D317/00; C07D317/08; C07D317/10; C07D317/14; C07D317/30; C07H11/00; C07H19/16; C07H5/00; C07H5/02; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 32
Claim 1
Independent Claim
50 words
A nucleoside of formula (I) a protected derivative thereof, or a pharmaceutically-acceptable salt thereof, in which R is a base of one of the formulae: in which R 1 is hydrogen, methyl, bromo, fluoro, chloro or iodo; R 2 is hydroxy or amino; R 3 is bromo, chloro or iodo.
Claim 2
Dependent Claim
50 words
A nucleoside of formula (I) a protected derivative thereof, or a pharmaceutically-acceptable salt thereof, in which R is a base of one of the formulae: in which R 1 is hydrogen, methyl, bromo, fluoro, chloro or iodo; R 2 is hydroxy or amino; R 3 is bromo, chloro or iodo.
Claim 3
Dependent Claim
15 words
A nucleoside as claimed in claim 1 in which the carbohydrate moiety is 2-desoxy-2,2-difluoro- ribosyl.
Claim 4
Dependent Claim
29 words
A nucleoside as claimed in claim 1 or claim 2, or a pharmaceutically-acceptable salt thereof, in which R is in which R 1 is as defined in claim 1.
Claim 5
Dependent Claim
31 words
A nucleoside as claimed in any one of claims 1 to 3, or a pharmaceutically-acceptable salt thereof in which R is , and R 1 is as defined in claim 1.
Claim 6
Dependent Claim
6 words
1-(5-methyl-2,4-dioxo-1H,3H-pyrimidin-1-yl)-1,2-desoxy-2,2-difluororibose, or a pharmaceutically-acceptable salt thereof.
Claim 7
Dependent Claim
6 words
1-(5-methyl-2,4-dioxo-1H,3H-pyrimidin-1-yl)-1,2-desoxy-2,2-difluororibose, or a pharmaceutically-acceptable salt thereof.
Claim 8
Dependent Claim
6 words
1-(4-amino-2-oxo-1H-pyrimidin-1-yl)-2- desoxy-2,2-difluororibose, or a-pharmaceutically-acceptable salt thereof.
Claim 9
Dependent Claim
6 words
1-(4-amino-2-oxo-1H-pyrimidin-1-yl)-2- desoxy-2,2-difluororibose, or a-pharmaceutically-acceptable salt thereof.
Claim 10
Dependent Claim
6 words
1-(4-amino-5-iodo-2-oxo-lH-pyrimidin-1-yl)-2-desoxy-2,2-difluororibose, or a pharmaceutically-acceptable salt thereof.
Claim 11
Dependent Claim
6 words
1-(4-amino-5-iodo-2-oxo-lH-pyrimidin-1-yl)-2-desoxy-2,2-difluororibose, or a pharmaceutically-acceptable salt thereof.
Claim 12
Dependent Claim
6 words
1-(2,4-dioxo-5-fluoro-1H,3H-pyrimidin-1-yl)-2-desoxy-2,2-difluororibose, or a pharmaceutically-acceptable salt thereof.
Claim 13
Dependent Claim
6 words
1-(2,4-dioxo-5-fluoro-1H,3H-pyrimidin-1-yl)-2-desoxy-2,2-difluororibose, or a pharmaceutically-acceptable salt thereof.
Claim 14
Dependent Claim
38 words
A difluoro-desoxy carbohydrate of formula (II): in which Q is CHOH, CHX in which X is a leaving group, or > C = O ; and Y 1 and Y 2 , independently, are hydrogen or hydroxy-protecting groups.
Claim 15
Dependent Claim
38 words
A difluoro-desoxy carbohydrate of formula (II): in which Q is CHOH, CHX in which X is a leaving group, or > C = O ; and Y 1 and Y 2 , independently, are hydrogen or hydroxy-protecting groups.
Claim 16
Dependent Claim
12 words
A carbohydrate as claimed in claim 9 in which Q is CHOH.
Claim 17
Dependent Claim
19 words
A carbohydrate as claimed in claim 9 or 10 in which the carbohydrate possesses the same configuration as ribose.
Claim 18
Dependent Claim
12 words
A carbohydrate as claimed in claim 9 in which Q is >C=O.
Claim 19
Dependent Claim
21 words
A carbohydrate as claimed in claim 9 in which X of CH X is a sulfonate leaving group, chloro or bromo.
Claim 20
Dependent Claim
26 words
A carbohydrate as claimed in any one of claims 9 to 13 in which Y 1 and Y 2 are hydrogen, or a protected derivative thereof.
Claim 21
Dependent Claim
6 words
2-Desoxy-2,2-difluoro-1-oxo-ribose, or a protected derivative thereof.
Claim 22
Dependent Claim
6 words
2-Desoxy-2,2-difluoro-1-oxo-ribose, or a protected derivative thereof.
Claim 23
Dependent Claim
6 words
1-Methanesulfonyloxy-2-desoxy-2,2-difluororibose, or a protected derivative thereof.
Claim 24
Dependent Claim
6 words
1-Methanesulfonyloxy-2-desoxy-2,2-difluororibose, or a protected derivative thereof.
Claim 25
Dependent Claim
6 words
2-Desoxy-2,2-difluororibose, or a protected derivative thereof.
Claim 26
Dependent Claim
6 words
2-Desoxy-2,2-difluororibose, or a protected derivative thereof.
Claim 27
Dependent Claim
32 words
A process for preparing a compound of Formula (I) as defined in claims 1 to 8 which comprises the removal of the protecting groups from a correspondingly protected nucleoside of Formula (I).
Claim 28
Dependent Claim
61 words
A process for preparing a compound of Formula (I) as defined in claims 1 to 8 which comprises coupling a compound of Formula (II), as defined in claim 9, in which Q is CHX, and Y 1 and y2 are hydroxy, or a protected derivative thereof, with a base as defined in claim 1, and, if desired, removing the protecting groups.
Claim 29
Dependent Claim
42 words
A process for preparing a compound of Formula (II), as defined in claim 9, in which Q is CHOH, or a protected derivative thereof, which comprises reducing a compound of Formula (II), in which Q is >C=O, or a protected derivative thereof.
Claim 30
Dependent Claim
26 words
A nucleoside of formula (I), or a pharmaceutically-acceptable salt thereof, as claimed in any one of claims 1 to 8, for use as an antiviral agent.
Claim 31
Dependent Claim
28 words
A nucleoside of formula (I), or a pharmaceutically-acceptable salt thereof, as claimed in any one of claims 1 to 8, for use in the treatment of herpes infections.
Claim 32
Dependent Claim
39 words
A pharmaceutical formulation which comprises as an active ingredient, a nucleoside of formula (I), or a pharmaceutically-acceptable salt thereof, as claimed in any one of claims 1 to 8, associated with one or more physiologically-acceptable carriers or vehicles therefor.
References Cited (Backward Citations)
EP0010205A1
Cited
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