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US4816570A
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Biologically reversible phosphate and phosphonate protective groups
Assignee: The University of Texas System
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Filing: 1986-04-04
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Granted: 1989-03-28
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Expires: 2006-04-04
Abstract
Abstract Protective groups are provided which are suitable for masking phosphates and phosphonates. The protected compositions can be introduced in a biological system and then demasked under certain biological conditions. This method permits phosphates and phosphonates which would themselves degrade in the biological system and therefore be ineffective to be introduced in a protected form and late released under the proper conditions.
Inventors
- 👤 David Farquhar
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 18:54
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/10; C07F; C07F9/00; C07F9/02; C07F9/06; C07F9/08; C07F9/09; C07F9/091; C07F9/12; C07F9/547; C07F9/645; C07F9/6509; C07F9/6512; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
74 words
A bioreversibly protected phosphate compound having the formula: ##STR12## where R 1 is selected from the group consisting of hydrogen, alkyl hydrocarbons having from 1-10 carbon atoms, aryl or alkaryl hydrocarbons having from 6-10 carbon atoms, and amines having the formula NR 4 R 5 where R 4 and R 5 are independently hydrogen or an alkyl hydrocarbon having from 1-10 carbon atoms; R 2 is nucleosid-5'-yl; and R 3 is hydrogen or methyl.
Claim 2
Dependent Claim
74 words
A bioreversibly protected phosphate compound having the formula: ##STR12## where R 1 is selected from the group consisting of hydrogen, alkyl hydrocarbons having from 1-10 carbon atoms, aryl or alkaryl hydrocarbons having from 6-10 carbon atoms, and amines having the formula NR 4 R 5 where R 4 and R 5 are independently hydrogen or an alkyl hydrocarbon having from 1-10 carbon atoms; R 2 is nucleosid-5'-yl; and R 3 is hydrogen or methyl.
Claim 3
Dependent Claim
51 words
The compound of claim 1, wherein R 1 is selected from the group consisting of H, CH 3 , C 2 H 5 , C 3 H 7 , C 4 H 9 , C 6 H 5 , NH 2 , NHCH 3 , and N(CH 3 ) 2 .
Claim 4
Dependent Claim
74 words
A bioreversibly protected phosphate compound having the formula: ##STR13## where R 1 is selected from the group consisting of hydrogen, alkyl hydrocarbons having from 1-10 carbon atoms, aryl or alkaryl hydrocarbons having from 6-10 carbon atoms, and amines having the formula NR 4 R 5 where R 4 and R 5 are independently hydrogen or an alkyl hydrocarbon having from 1-10 carbon atoms; R 2 is 2'-deoxynucleosid-5'-yl; and R 3 is hydrogen or methyl.
Claim 5
Dependent Claim
74 words
A bioreversibly protected phosphate compound having the formula: ##STR13## where R 1 is selected from the group consisting of hydrogen, alkyl hydrocarbons having from 1-10 carbon atoms, aryl or alkaryl hydrocarbons having from 6-10 carbon atoms, and amines having the formula NR 4 R 5 where R 4 and R 5 are independently hydrogen or an alkyl hydrocarbon having from 1-10 carbon atoms; R 2 is 2'-deoxynucleosid-5'-yl; and R 3 is hydrogen or methyl.
Claim 6
Dependent Claim
51 words
The compound of claim 3, where R 1 is selected from the group consisting of H, CH 3 , C 2 H 5 , C 3 H 7 , C 4 H 9 , C 6 H 5 , NH 2 , NHCH 3 , and N(CH 3 ) 2 .
Claim 7
Dependent Claim
90 words
A bioreversibly protected phosphate compound, having the formula: ##STR14## where R 1 is selected from the group consisting of hydrogen, alkyl hydrocarbons having from 1-10 carbon atoms, aryl or alkaryl hydrocarbons having from 6-10 carbon atoms, and amines having the formula NR 4 R 5 where R 4 and R 5 are independently hydrogen or an alkyl hydrocarbon having from 1-10 carbon atoms; R 2 is selected from the group consisting of ' -deoxy-5-fluorouridin-5'-yl 2'-deoxy-3'-O-acetyl-5-fluorouridin-5'-yl 2'-deoxyuridin-5'-yl 2'-deoxy-5-bromouridin-5'-yl 2'-deoxy-5-iodouridin-5'-yl ' -deoxy-t-(bromovinyl)-uridin-5'-yl thymidin-5'-yl, and 3'-O-acetylthymidin-5'-yl; and R 3 is hydrogen or methyl.
Claim 8
Dependent Claim
90 words
A bioreversibly protected phosphate compound, having the formula: ##STR14## where R 1 is selected from the group consisting of hydrogen, alkyl hydrocarbons having from 1-10 carbon atoms, aryl or alkaryl hydrocarbons having from 6-10 carbon atoms, and amines having the formula NR 4 R 5 where R 4 and R 5 are independently hydrogen or an alkyl hydrocarbon having from 1-10 carbon atoms; R 2 is selected from the group consisting of ' -deoxy-5-fluorouridin-5'-yl 2'-deoxy-3'-O-acetyl-5-fluorouridin-5'-yl 2'-deoxyuridin-5'-yl 2'-deoxy-5-bromouridin-5'-yl 2'-deoxy-5-iodouridin-5'-yl ' -deoxy-t-(bromovinyl)-uridin-5'-yl thymidin-5'-yl, and 3'-O-acetylthymidin-5'-yl; and R 3 is hydrogen or methyl.
Claim 9
Dependent Claim
51 words
The compound of claim 5, where R 1 is selected from the group consisting of H, CH 3 , C 2 H 5 , C 3 H 7 , C 4 H 9 , C 6 H 5 , NH 2 , NHCH 3 , and N(CH 3 ) 2 .
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-03-27 | 1992-09-26 | 1993-03-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-03-27 | 1996-09-26 | 1997-03-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-03-27 | 2000-09-26 | 2001-03-28 | $7700.00 | Window Closed / Lapsed |