Patent US5512470A successfully refreshed from Google Patents.
US5512470A
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Method for inhibiting sialidase activity
Assignee: EIDP Inc
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Filing: 1995-05-19
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Granted: 1996-04-30
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Expires: 2015-05-19
Abstract
Abstract Novel NeuAc-Gal dissacharide sialidase substrates and inhibitors which are locked into rigid conformation by the attachment of an alkyl group at the C-6 arm of the galactose core are provided. Also provided is a method for the inhibition of sialidase activity.
Inventors
- 👤 Subramaniam Sabesan
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 10:40
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/02; C07H15/04; C07H15/10; C07H15/14; C07H23/00; C07H3/00; C07H3/06
Claims Analysis
Total Claims: 3
Claim 1
Independent Claim
240 words
A method for inhibiting sialidase activity comprising contacting sialidase with a compound of Formula I ##STR8## wherein R is H or C 1 to C 20 hydrocarbyl or substituted hydrocarbyl; R 1 is H, a C 1 to C 20 alkyl, a mono, di or polyvalent cation of an alkali metal, alkaline earth metal or transition metal, or an ammonium or substituted ammonium ion; X is O, S, CR 4 R 5 or NR 6 , wherein R 4 , R 5 , R 6 are each independently H or a C 1 to C 20 hydrocarbyl or substituted hydrocarbyl; R 2 is a C 1 to C 20 hydrocarbyl or substituted hydrocarbyl; R 3 and R 3' are H, OH, a C 1 to C 20 alkoxy or substituted alkoxy, a mono, di or oligosaccharide, or a C 1 to C 20 alkylideneoxy taken together with R 7' when R 7' is not H; provided that one of R 3 or R 3' must be H but R 3 and R 3' may not both be H; R 7 and R 7' are independently H, a C 1 to C 20 acyl, a C 1 to C 20 alkyl, or a C 1 to C 20 alkylidene taken together with an adjacent R 3' , R 7 or R7'; and R 8 is H, a C 1 to C 20 acyl, or a C 1 to C 20 alkyl.
Claim 2
Independent Claim
240 words
A method for inhibiting sialidase activity comprising contacting sialidase with a compound of Formula I ##STR8## wherein R is H or C 1 to C 20 hydrocarbyl or substituted hydrocarbyl; R 1 is H, a C 1 to C 20 alkyl, a mono, di or polyvalent cation of an alkali metal, alkaline earth metal or transition metal, or an ammonium or substituted ammonium ion; X is O, S, CR 4 R 5 or NR 6 , wherein R 4 , R 5 , R 6 are each independently H or a C 1 to C 20 hydrocarbyl or substituted hydrocarbyl; R 2 is a C 1 to C 20 hydrocarbyl or substituted hydrocarbyl; R 3 and R 3' are H, OH, a C 1 to C 20 alkoxy or substituted alkoxy, a mono, di or oligosaccharide, or a C 1 to C 20 alkylideneoxy taken together with R 7' when R 7' is not H; provided that one of R 3 or R 3' must be H but R 3 and R 3' may not both be H; R 7 and R 7' are independently H, a C 1 to C 20 acyl, a C 1 to C 20 alkyl, or a C 1 to C 20 alkylidene taken together with an adjacent R 3' , R 7 or R7'; and R 8 is H, a C 1 to C 20 acyl, or a C 1 to C 20 alkyl.
Claim 3
Dependent Claim
74 words
The process of claim 1 wherein in formula I R is methyl; R 1 is Na or CH 3 ; R 2 i s CH 3 ; R 8 is H or acetyl; R 7 is H or alkylidene taken together with R 3 ' ; R 7' is acetyl or benzyl; R 3 is OH when R 3' is H; R 3' is OH when R 3 is H; and X is S.
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| 3.5 Years (Year 4) | 1999-04-30 | 1999-10-30 | 2000-04-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2003-04-30 | 2003-10-30 | 2004-04-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2007-04-30 | 2007-10-30 | 2008-04-30 | $7700.00 | Window Closed / Lapsed |