Ronald Lee Schultz

US Patent:

7321029, Jan 22, 2008

Filed:

Jan 19, 2001

Appl. No.:

10/181823

Inventors:

Sergei Gryaznov - San Mateo CA, US
Ronald G. Schultz - Urbana MO, US

Assignee:

Geron Corporation - Menlo Park CA

International Classification:

C07H 21/00
C07H 21/02
C07H 21/04
C12Q 1/68
C07G 3/00

US Classification:

536 231, 536 243, 536 253, 536 266, 536 41, 435 6

Abstract:

Oligonucleotides with a novel sugar-phosphate backbone containing at least one 2′-arabino-fluoronucleoside and an internucleoside 3′-NH—P(—O)(OR)—O-5′ linkage, where R is a positively charged counter ion or hydrogen, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive phosphoramidate 2′-arabino-fluorooligonucleotides have a high RNA binding affinity to complementary nucleic acids and are base and acid stable.

US Patent:

7989603, Aug 2, 2011

Filed:

Dec 20, 2007

Appl. No.:

12/004123

Inventors:

Sergei Gryaznov - San Mateo CA, US
Ronald G. Schultz - Urbana MO, US

Assignee:

Geron Corporation - Menlo Park CA

International Classification:

C07H 19/00
C07H 19/06
C07H 19/09
C07H 19/16
C07H 19/19

US Classification:

536 221, 536 261, 536 281, 536 284, 536 2781, 536 276, 514 42

Abstract:

Oligonucleotides with a novel sugar-phosphate backbone containing at least one 2′-arabino-fluoronucleoside and an internucleoside 3′-NH—P(═O)(OR)—O-5′ linkage, where R is a positively charged counter ion or hydrogen, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive phosphoramidate 2′-arabino-fluorooligonucleotides have a high RNA binding affinity to complementary nucleic acids and are base and acid stable.

US Patent:

8377644, Feb 19, 2013

Filed:

Jul 27, 2011

Appl. No.:

13/192035

Inventors:

Sergei Gryaznov - San Mateo CA, US
Ronald G. Schultz - Urbana MO, US

Assignee:

Geron Corporation - Menlo Park CA

International Classification:

G01N 33/53
C12Q 1/68
C07G 3/00
C07H 21/02
C07H 21/00

US Classification:

435 72, 435 61, 536 41, 536 231, 536 253

Abstract:

Oligonucleotides with a novel sugar-phosphate backbone containing at least one 2′-arabino-fluoronucleoside and an internucleoside 3′-NH—P(═O)(OR)—O-5′ linkage, where R is a positively charged counter ion or hydrogen, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive phosphoramidate 2′-aribino-fluorooligonucleotides have a high RNA binding affinity to complementary nucleic acids and are base and acid stable.

US Patent:

20130253034, Sep 26, 2013

Filed:

Feb 15, 2013

Appl. No.:

13/769090

Inventors:

Sergei Gryaznov - San Mateo CA, US
Ronald G. Schultz - Urbana MO, US

International Classification:

C12N 15/113

US Classification:

514 44 A, 435375

Abstract:

Oligonucleotides with a novel sugar-phosphate backbone containing at least one 2′-arabino-fluoronucleoside and an internucleoside ′-NH—P(═O)(OR)—O-5′ linkage, where R is a positively charged counter ion or hydrogen, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive phosphoramidate 2′-aribino-fluorooligonucleotides have a high RNA binding affinity to complementary nucleic acids and are base and acid stable.

US Patent:

58378359, Nov 17, 1998

Filed:

Jun 6, 1995

Appl. No.:

8/477306

Inventors:

Sergei M. Gryaznov - San Mateo CA
Ronald G. Schultz - Fremont CA

Assignee:

Lynx Therapeutics, Inc. - Hayward CA

International Classification:

C07H 2104
C12Q 168
A61K 3133

US Classification:

536 231

Abstract:

Modified oligonucleotides 3'-NHP(O)(O. sup. -)O-5' phosphoramidates were synthesized on a solid phase support. The phosphoramidate analogs were found to have significantly increased resistance toward phosphodiesterase digestion. Thermal dissociation experiments demonstrated that these compounds form more stable duplexes than phosphodiesters with complementary DNA and particularly RNA strands. Further, the phosphoramidate analogs can also form stable triplexes with double-stranded DNA target, where under similar conditions parent phosphodiester compounds failed to do so.

US Patent:

57262977, Mar 10, 1998

Filed:

Jun 5, 1995

Appl. No.:

8/465368

Inventors:

Sergei M. Gryaznov - San Mateo CA
Ronald G. Schultz - Hayward CA

Assignee:

Lynx Therapeutics, Inc. - Hayward CA

International Classification:

C07H 2102
C07H 2104
C12Q 168

US Classification:

536 221

Abstract:

Modified oligodeoxyribonucleotide 3'--NHP (O) (O. sup. -) O-5' phosphoramidates were synthesized on a solid phase support. The phosphoramidate analogs were found to have significantly increased resistance toward phosphodiesterase digestion. Thermal dissociation experiments demonstrated that these compounds form more stable duplexes than phosphodiesters with complementary DNA and particularly RNA strands. Further, the phosphoramidate analogs can also form stable triplexes with double-stranded DNA target, where under similar conditions parent phosphodiester compounds failed to do so.

US Patent:

59657200, Oct 12, 1999

Filed:

Jan 10, 1997

Appl. No.:

8/700448

Inventors:

Sergei M. Gryaznov - San Mateo CA
Ronald G. Schultz - Urbana MO

Assignee:

Lynx Therapeutics, Inc. - Hayward CA

International Classification:

C12Q 168

US Classification:

536 231

Abstract:

Modified oligonucleotides 3'-NHP(O)(O. sup. -)O-5' phosphoramidates were synthesized on a solid phase support. The phosphoramidate analogs were found to have significantly increased resistance toward phosphodiesterase digestion. Thermal dissociation experiments demonstrated that these compounds form more stable duplexes than phosphodiesters with complementary DNA and particularly RNA strands. Further, the phosphoramidate analogs can also form stable triplexes with double-stranded DNA target, where under similar conditions parent phosphodiester compounds failed to do so.

US Patent:

61691704, Jan 2, 2001

Filed:

Sep 3, 1997

Appl. No.:

8/923386

Inventors:

Sergei M. Gryaznov - San Mateo CA
Ronald G. Schultz - Urbana MO

Assignee:

Lynx Therapeutics, Inc. - Hayward CA

International Classification:

C07H 2100
C12Q 168

US Classification:

536 231

Abstract:

Modified oligonucleotides 3'-NHP(O)(O. sup. -)O-5' phosphoramidates were synthesized on a solid phase support. The phosphoramidate analogs were found to have significantly increased resistance toward phosphodiesterase digestion. Thermal dissociation experiments demonstrated that these compounds form more stable duplexes than phosphodiesters with complementary DNA and particularly RNA strands. Further, the phosphoramidate analogs can also form stable triplexes with double-stranded DNA target, where under similar conditions parent phosphodiester compounds failed to do so.