EP0049072A1
Expired / Lapsed
EP
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Guanine compounds and their use for the preparation of anti-viral agents
Assignee: Syntex USA LLC
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Filing: 1981-09-15
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Granted: —
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Expires: 2001-09-15
Abstract
Abstract Nucleoside analogues having a ring-open structure of general formula where R and R' may be hydrogen, silyl, substituted alkyl or benzyl, and X is an optionally substituted base such as guanine or adenine, have been shown to exhibit anti-viral and other biological activities at non-toxic levels. Many phosphate-linked dinucleotides thereof are also novel compounds.
Inventors
- 👤 Kelvin K. Ogilvie
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-02 10:27
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/47; A; A61; A61P; A61P31/00; A61P31/12; C07D239/52; C07D239/54; C07D239/545; C07D239/553; C07D251/00; C07D251/02; C07D251/12; C07D251/14; C07D251/16; C07D473/00; C07D473/02; C07D473/18; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/18; C07F7/1804; C07F9/00; C07F9/02; C07F9/547; C07F9/645; C07F9/6509; C07F9/6512; C07F9/6561; C07F9/65616; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/10; C07H19/16; C07H19/20
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
43 words
A purine or pyrimidine compound of the formula wherein X represents a uracil, 5-fluorouracil, cytosine, 5-azacytosine, adenine, guanine or 2-N-acetylguanine group; and R and R' are independently selected from hydrogen, benzyl, monomethoxytrityl and tert-butyldimethylsilyl; with the proviso that the compound is not 9-[[2-hydroxy-1-(hydroxymethyl)ethoxy]methyl]adenine.
Claim 2
Dependent Claim
43 words
A purine or pyrimidine compound of the formula wherein X represents a uracil, 5-fluorouracil, cytosine, 5-azacytosine, adenine, guanine or 2-N-acetylguanine group; and R and R' are independently selected from hydrogen, benzyl, monomethoxytrityl and tert-butyldimethylsilyl; with the proviso that the compound is not 9-[[2-hydroxy-1-(hydroxymethyl)ethoxy]methyl]adenine.
Claim 3
Dependent Claim
10 words
A pyrimidine compound according to claim 1, wherein X is
Claim 4
Dependent Claim
10 words
A pyrimidine compound according to claim 1, wherein X is
Claim 5
Dependent Claim
10 words
A pyrimidine compound according to claim 1, wherein X is
Claim 6
Dependent Claim
10 words
A pyrimidine compound according to claim 1, wherein X is
Claim 7
Dependent Claim
10 words
A urine compound according to claim 1, wherein X is
Claim 8
Dependent Claim
18 words
A purine compound according to claim 1, wherein X is and R and R' are not both hydrogen.
Claim 9
Dependent Claim
18 words
A compound according to any of claims 2, 3 and 6, wherein R and R' are each hydrogen.
Claim 10
Dependent Claim
19 words
A compound according to any of claims 2, 4 and 5, . wherein R and R' are each benzyl.
Claim 11
Dependent Claim
17 words
A compound according to claim 7, wherein R is hydrogen or tert-butyldimethylsilyl and R' is tert-butyl- dimethylsilyl.
Claim 12
Dependent Claim
129 words
A purine or pyridine compound of the formula wherein B and B' represent purine or pyrimidine base compounds independently selected from adenine, cytosine, thymine, guanine and uracil; either each of (Z) and (Y) represents a methylene group or (Z) and (Y) together represent the group -CH-CH 2 -CH- completing a deoxyribose ring; and either each of (Z') and (Y') represents a methylene group or (Z') and (Y') together represent the group -CH-CH 2 -CH- completing a deoxyribose ring; with the proviso that the compound contains no more than one deoxyribose ring; Q is 0, S or a bond; and R 2 , R3 and R are each independently selected from hydrogen, optionally substituted C 1-6 alkyl in which any substituent is phenyl or halogen, monomethoxytrityl and optionally substituted silyl.
Claim 13
Dependent Claim
129 words
A purine or pyridine compound of the formula wherein B and B' represent purine or pyrimidine base compounds independently selected from adenine, cytosine, thymine, guanine and uracil; either each of (Z) and (Y) represents a methylene group or (Z) and (Y) together represent the group -CH-CH 2 -CH- completing a deoxyribose ring; and either each of (Z') and (Y') represents a methylene group or (Z') and (Y') together represent the group -CH-CH 2 -CH- completing a deoxyribose ring; with the proviso that the compound contains no more than one deoxyribose ring; Q is 0, S or a bond; and R 2 , R3 and R are each independently selected from hydrogen, optionally substituted C 1-6 alkyl in which any substituent is phenyl or halogen, monomethoxytrityl and optionally substituted silyl.
Claim 14
Dependent Claim
10 words
A compound according to claim 10, wherein B represents adenine.
Claim 15
Dependent Claim
19 words
A compound according to any preceding claim, for use in the treatment of viral infections in live mammalian cells.
Claim 16
Dependent Claim
14 words
9-[[2-Hydroxy-1-(hydroxymethyl)ethoxylmethyl- adenine, for use in the treatment of viral infections in live mammalian cells.
Claim 17
Dependent Claim
14 words
9-[[2-Hydroxy-1-(hydroxymethyl)ethoxylmethyl- adenine, for use in the treatment of viral infections in live mammalian cells.
Claim 18
Dependent Claim
19 words
A pharmaceutical composition which comprises a compound according to any preceding claim in admixture with a pharmaceutically acceptable carrier.
Claim 19
Dependent Claim
15 words
A pharmaceutical composition which comprises the compound 9-[[2-hydroxy-l-(hydroxymethyl)ethoxy]methyl]-adenine in admixture with a pharmaceutically acceptable carrier.
Claim 20
Dependent Claim
15 words
A pharmaceutical composition which comprises the compound 9-[[2-hydroxy-l-(hydroxymethyl)ethoxy]methyl]-adenine in admixture with a pharmaceutically acceptable carrier.
Claim 21
Dependent Claim
14 words
A composition according to claim 15 or claim 16, wherein the carrier is water.
Claim 22
Dependent Claim
20 words
A composition according to any of claims 15 to 17, wherein the carrier comprises sodium chloride and a phosphate buffer.
Claim 23
Dependent Claim
21 words
A composition according to any of claims 15 to 18, which comprises from 1 to 20% by weight of the compound.
References Cited (Backward Citations)
GB1523865A
Cited
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