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Oligonucleotide analogs containing sulfur linkages

Assignee: Individual
•
Filing: 1988-06-06
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Granted: 1993-06-01
•
Expires: 2008-06-06
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Abstract

Abstract Analogs of DNA containing sulfides, sulfoxides, and sulfones as linking groups between subunits capable of forming bonds with natural oligonucleotides are described. The analogs are lipophilic, stable to chemical degradation under a wide range of conditions and stable to enzymatic degradation in vivo.

Inventors

  • 👤 Steven A. Benner

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-05 08:26
CPC Classifications
C; C07; C07D; C07D473/00; C07H; C07H19/00; C07H19/02; C07H19/04; C07H21/00

Claims Analysis

Total Claims: 6
Claim 1
Independent Claim 88 words
A compound having a formula selected from the group consisting of ##STR4## wherein V is selected from the group consisting of --O-- and --CH 2 --; B is a base analog that can form hydrogen bonds to natural oligonucleoside bases, wherein B is selected from the group consisting of adenine, 7-deazaadenine, 7-deaza-8-azaadenine, 3,7-dideazaadenine, 8-deazaadenine, guanine, 3-deazaguanine, 7-deaza-8-azaguanine, 3,7-dideazaaguanine, 3,7-dideaza-8-azaguanine, 7-deazaguanine, 8-azaguanine, purine, azapurine, 2,6-diaminopurine, hypoxanthine, uracil, 5-azauracil, 6-azauracil, 5-fluorouracil, 5-bromouracil, 5-iodouracil, thymine, 6-azathymine, cytosine, 6-azacytosine, 5-azacytosine, pyrimidine, azapyrimidine, pyrrolopyrimidine, pyrazolopyrimidine, triazolopyrimidine, imidazolopyrimidine, pyridine, imidazolopyridine, pyrrolopyridine, pyrazolopyridine and triazolopyridine.
Claim 2
Dependent Claim 88 words
A compound having a formula selected from the group consisting of ##STR4## wherein V is selected from the group consisting of --O-- and --CH 2 --; B is a base analog that can form hydrogen bonds to natural oligonucleoside bases, wherein B is selected from the group consisting of adenine, 7-deazaadenine, 7-deaza-8-azaadenine, 3,7-dideazaadenine, 8-deazaadenine, guanine, 3-deazaguanine, 7-deaza-8-azaguanine, 3,7-dideazaaguanine, 3,7-dideaza-8-azaguanine, 7-deazaguanine, 8-azaguanine, purine, azapurine, 2,6-diaminopurine, hypoxanthine, uracil, 5-azauracil, 6-azauracil, 5-fluorouracil, 5-bromouracil, 5-iodouracil, thymine, 6-azathymine, cytosine, 6-azacytosine, 5-azacytosine, pyrimidine, azapyrimidine, pyrrolopyrimidine, pyrazolopyrimidine, triazolopyrimidine, imidazolopyrimidine, pyridine, imidazolopyridine, pyrrolopyridine, pyrazolopyridine and triazolopyridine.
Claim 3
Dependent Claim 275 words
A compound having the formula: S.sub.1 (J.sub.1 --A.sub.1 --J.sub.2 --A.sub.2).sub.n S.sub.2 wherein n is an integer less than 25; wherein S 1 is selected from the group consisting of alkyl and aralkyl and S 2 is selected from the group consisting of hydroxyl, S-alkyl and S-aralkyl; J 1 and J 2 are linking groups independently selected from the group consisting of sulfide, sulfoxide, and sulfone whereby J 1 and J 2 may be different in each n subunit; A 1 and A 2 may be different in each n subunit and are independently selected from the formulae consisting of: ##STR5## wherein V is independently selected from --O-- or --CH 2 --; E is a base analog independently selected from the group consisting of adenine, 7-deazaadenine, 7-deaza-8-azaadenine, 3,7-dideazaadenine, 8-deazaadenine, guanine, 3-deazaguanine, 7-deaza-8-azaguanine, 3,7-dideazaaguanine, 3,7-dideaza-8-azaguanine, 7-deazaguanine, 8-azaguanine, purine, azapurine, 2,6-diaminopurine. hypoxanthine, uracil, 5-azauracil, 6-azauracil, 5-fluorouracil, 5-bromouracil, 5-iodouracil, thymine, 6-azathymine, cytosine, 6-azacytosine, 5-azacytosine, pyrimidine, azapyrimidine, pyrrolopyrimidine, pyrazolopyrimidine, triazolopyrimidine, imidazolopyrimidine, pyridine, imidazolopyridine, pyrrolopyridine, pyrazolopyridine and triazolopyridine; L 1 is a linking roup containing from zero to four linking units independently selected from the group consisting of --CH 2 --and --O--; L 2 is a linking group containing from 1 to 5 linking units independently selected from the group consisting of --CH 2 and --O--; L 3 is a linking group containing from 0 to 5 linking units independently selected from the group consisting of --CH 2 -- and --O--; whereby for each A 1 or A 2 of formula (II), the number of linking units in L 1 is less than or equal to the sum of the number of linking units in L 2 and L 3 .
Claim 4
Dependent Claim 275 words
A compound having the formula: S.sub.1 (J.sub.1 --A.sub.1 --J.sub.2 --A.sub.2).sub.n S.sub.2 wherein n is an integer less than 25; wherein S 1 is selected from the group consisting of alkyl and aralkyl and S 2 is selected from the group consisting of hydroxyl, S-alkyl and S-aralkyl; J 1 and J 2 are linking groups independently selected from the group consisting of sulfide, sulfoxide, and sulfone whereby J 1 and J 2 may be different in each n subunit; A 1 and A 2 may be different in each n subunit and are independently selected from the formulae consisting of: ##STR5## wherein V is independently selected from --O-- or --CH 2 --; E is a base analog independently selected from the group consisting of adenine, 7-deazaadenine, 7-deaza-8-azaadenine, 3,7-dideazaadenine, 8-deazaadenine, guanine, 3-deazaguanine, 7-deaza-8-azaguanine, 3,7-dideazaaguanine, 3,7-dideaza-8-azaguanine, 7-deazaguanine, 8-azaguanine, purine, azapurine, 2,6-diaminopurine. hypoxanthine, uracil, 5-azauracil, 6-azauracil, 5-fluorouracil, 5-bromouracil, 5-iodouracil, thymine, 6-azathymine, cytosine, 6-azacytosine, 5-azacytosine, pyrimidine, azapyrimidine, pyrrolopyrimidine, pyrazolopyrimidine, triazolopyrimidine, imidazolopyrimidine, pyridine, imidazolopyridine, pyrrolopyridine, pyrazolopyridine and triazolopyridine; L 1 is a linking roup containing from zero to four linking units independently selected from the group consisting of --CH 2 --and --O--; L 2 is a linking group containing from 1 to 5 linking units independently selected from the group consisting of --CH 2 and --O--; L 3 is a linking group containing from 0 to 5 linking units independently selected from the group consisting of --CH 2 -- and --O--; whereby for each A 1 or A 2 of formula (II), the number of linking units in L 1 is less than or equal to the sum of the number of linking units in L 2 and L 3 .
Claim 5
Dependent Claim 130 words
A compound having the formula: ##STR6## wherein is an integer less than 25; wherein S 1 is selected from the group consisting of alkyl and aralkyl and S 2 is selected from the group consisting of hyroxyl, 8-alkyl and 8-aralkyl, J is a linking group independently selected from the group consisting of sulfide, sulfoxide, and sulfone, V is independently selected from --O-- or CH 2 --; and B is a base analog independently selected from the group consisting of adenine, 7-deazaadenine, 7-deaza-8-azaadenine, 3,7-dideazaadenine, 8-deazaadenine, guanine, 3-deazaguanine, 7-deaza-8-azaguanine, 3,7-dideazaaguanine, 3,7-dideaza-8-azaguanine, 7-deazaguanine, 8-azaguanine, purine, azapurine, 2,6-diaminopurine, hypoxanthine, uracil, 5-azauracil, 6-azauracil, 5-fluorouracil, 5-bromouracil, 5-iodouracil, thymine, 6-azathymine, cytosine, 6-azacytosine, 5-azacytosine, pyrimidine, azapyrimidine, pyrrolopyrimidine, pyrazolopyrimidine, triazolopyrimidine, imidazolopyrimidine, pyridine, imidazolopyridine, pyrrolopyridine, pyrazolopyridine and triazolopyridine, whereby J, V, and B may be different in each n subunit.
Claim 6
Dependent Claim 130 words
A compound having the formula: ##STR6## wherein is an integer less than 25; wherein S 1 is selected from the group consisting of alkyl and aralkyl and S 2 is selected from the group consisting of hyroxyl, 8-alkyl and 8-aralkyl, J is a linking group independently selected from the group consisting of sulfide, sulfoxide, and sulfone, V is independently selected from --O-- or CH 2 --; and B is a base analog independently selected from the group consisting of adenine, 7-deazaadenine, 7-deaza-8-azaadenine, 3,7-dideazaadenine, 8-deazaadenine, guanine, 3-deazaguanine, 7-deaza-8-azaguanine, 3,7-dideazaaguanine, 3,7-dideaza-8-azaguanine, 7-deazaguanine, 8-azaguanine, purine, azapurine, 2,6-diaminopurine, hypoxanthine, uracil, 5-azauracil, 6-azauracil, 5-fluorouracil, 5-bromouracil, 5-iodouracil, thymine, 6-azathymine, cytosine, 6-azacytosine, 5-azacytosine, pyrimidine, azapyrimidine, pyrrolopyrimidine, pyrazolopyrimidine, triazolopyrimidine, imidazolopyrimidine, pyridine, imidazolopyridine, pyrrolopyridine, pyrazolopyridine and triazolopyridine, whereby J, V, and B may be different in each n subunit.

References Cited (Backward Citations)

US3846402A Cited
US4469863A Cited
US4415732A Cited
GB2122197A Cited
GB2122198A Cited
US4808708A Cited
US4837311A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1996-05-31 1996-11-30 1997-06-01 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2000-05-31 2000-11-30 2001-06-01 $3760.00 Window Closed / Lapsed
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