IP Library Granted Patent US 8,877,905
Granted Patent B2
US 8,877,905 · App. 13/929,305 · Granted Nov 4, 2014

Nucleotides and nucleosides and methods for their use in DNA sequencing

Inventors: Vladislav A. Litosh (Cypress, TX); Megan N. Hersh (Houston, TX); Brian P. Stupi (Cypress, TX); Weidong Wu (Houston, TX); Michael L. Metzker (Houston, TX)
Assignee: LaserGen, Inc.
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Quick Facts
Patent No.
US 8,877,905
App. No.
13/929,305
Granted
Nov 4, 2014
Kind
B2
Abstract

The present invention relates generally to labeled and unlabeled cleavable terminating groups and methods for DNA sequencing and other types of DNA analysis. More particularly, the invention relates in part to nucleotides and nucleosides with chemically cleavable, photocleavable, enzymatically cleavable, or non-photocleavable groups and methods for their use in DNA sequencing and its application in biomedical research.

Claims (46)

1. A compound of formula:

wherein:

Z is —O—, —S—, —NH—, —OC(O)O—, —NHC(O)O—, —OC(O)NH— or —NHC(O)NH—;

R 1 is hydroxy, monophosphate, diphosphate, triphosphate, α-thiotriphosphate, or polyphosphate;

R 2 is hydrogen or hydroxy;

R 3 and R 4 are each independently:

hydrogen, hydroxy, halo or amino; or

alkyl (C≦12) , alkenyl (C≦12) , alkynyl (C≦12) , aryl (C≦12) , aralkyl (C≦12) , heteroaryl (C≦12) , heteroaralkyl (C≦12) , alkoxy (C≦12) , aryloxy (C≦12) , aralkoxy (C≦12) , heteroaryloxy (C≦12) , heteroaralkoxy (C≦12) , alkylamino (C≦12) , dialkylamino (C≦12) , arylamino (C≦12) , aralkylamino (C≦12) , or a substituted version of any of these groups; or

R 5 , R 6 , R 7 , R 8 and R 9 are each independently:

hydrogen, hydroxy, halo, amino, nitro, cyano or mercapto;

alkyl (C≦12) , alkenyl (C≦12) , alkynyl (C≦12) , aryl (C≦12) , aralkyl (C≦12) , heteroaryl (C≦12) , heteroaralkyl (C≦12) , acyl (C≦12) , alkoxy (C≦12) , alkenyloxy (C≦12) , alkynyloxy (C≦12) , aryloxy (C≦12) , aralkoxy (C≦12) , heteroaryloxy (C≦12) , heteroaralkoxy (C≦12) , acyloxy (C≦12) , alkylamino (C≦12) , dialkylamino (C≦12) , alkoxyamino (C≦12) , alkenylamino (C≦12) , alkynylamino (C≦12) , arylamino (C≦12) , aralkylamino (C≦12) , heteroarylamino (C≦12) , heteroaralkylamino (C≦12) , alkylsulfonylamino (C≦12) , amido (C≦12) , alkylthio (C≦12) , alkenylthio (C≦12) , alkynylthio (C≦12) , arylthio (C≦12) , aralkylthio (C≦12) , heteroarylthio (C≦12) , heteroaralkylthio (C≦12) , acylthio (C≦12) , thioacyl (C≦12) , alkylsulfonyl (C≦12) , arylsulfonyl (C≦12) , alkylammonium (C≦12) , alkylsulfonium (C≦12) , alkylsilyl (C≦12) , or a substituted version of any of these groups;

a group of formula:

wherein

 X is

 —O—, —S—, or —NH—; or

 alkanediyl (C≦12) , alkenediyl (C≦12) , alkynediyl (C≦12) , arenediyl (C≦12) , heteroarenediyl (C≦12) , or a substituted version of any of these groups;

 Y is —O—, —NH—, alkanediyl (C≦12) or substituted alkanediyl (C≦12) ;

 n is an integer from 0-12; and

 m is an integer from 0-12; or

a -linker-reporter;

or a salt thereof.

2. The compound of claim 1 , wherein Z is —O—.

3. The compound of claim 1 , wherein R 1 is hydroxy.

4. The compound of claim 1 , wherein R 1 is a triphosphate.

5. The compound of claim 1 , wherein R 2 is hydrogen.

6. The compound of claim 1 , wherein R 3 is alkyl (C≦12) or a substituted version thereof.

7. The compound of claim 6 , wherein R 3 is selected from the group consisting of methyl, ethyl, n-propyl, isopropyl and tert-butyl.

8. The compound of claim 7 , wherein R 3 is tert-butyl.

9. The compound of claim 1 , wherein R 4 is hydrogen.

10. The compound of claim 1 , wherein R 5 is alkoxy (c≦12) or a substituted version thereof.

11. The compound of claim 10 , wherein R 5 is methoxy.

12. The compound of claim 1 , wherein R 6 is a -linker-reporter.

13. The compound of claim 12 , wherein the linker is:

wherein

X is

—O—, —S—, or —NH—; or

alkanediyl (c≦12) , alkenediyl (c≦12) , alkynediyl (c≦12) , arenediyl (c≦12) , heteroarenediyl (c≦12) , or a substituted version of any of these groups; and

n is an integer from 0-12.

14. The compound of claim 13 , wherein X is —C≡C—.

15. The compound of claim 13 , wherein n is zero.

16. The compound of claim 12 , wherein the reporter is based on a dye, wherein the dye is zanthene, fluorescein, rhodamine, BODIPY, cyanine, coumarin, pyrene, phthalocyanine, phycobiliprotein, ALEXA FLUOR® 350, ALEXA FLUOR® 405, ALEXA FLUOR® 430, ALEXA FLUOR® 488, ALEXA FLUOR® 514, ALEXA FLUOR® 532, ALEXA FLUOR® 546, ALEXA FLUOR® 555, ALEXA FLUOR® 568, ALEXA FLUOR® 568, ALEXA FLUOR® 594, ALEXA FLUOR® 610, ALEXA FLUOR® 633, ALEXA FLUOR® 647, ALEXA FLUOR® 660, ALEXA FLUOR® 680, ALEXA FLUOR® 700, ALEXA FLUOR® 750, or a squaraine dye.

17. The compound of claim 12 , wherein the reporter is:

18. The compound of claim 1 , wherein R 7 is hydrogen.

19. The compound of claim 1 , wherein R 8 is nitro.

20. The compound of claim 1 , wherein R 9 is hydrogen.

21. The compound of claim 1 , wherein R 1 is α-thiotriphosphate.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 14, 2018
From: LASERGEN, INC.
To: AGILENT TECHNOLOGIES, INC.
Reel/Frame 047494/0278 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2018
From: LITOSH, VLADISLAV A.; HERSH, MEGAN N.; STUPI, BRIAN P.; WU, WEIDONG; METZKER, MICHAEL L.
To: LASERGEN, INC.
Reel/Frame 046930/0154 →
Continuity (5)
Division 13406934 · Feb 28, 2012
Division 12483080 · Jun 11, 2009
Provisional Application 61060795 · Jun 11, 2008
Provisional Application 61184779 · Jun 5, 2009
Related Publication 20140051848A1 · Feb 20, 2014