Jiri Z Zemlicka

US Patent:

6352991, Mar 5, 2002

Filed:

Mar 12, 1999

Appl. No.:

09/267839

Inventors:

Jiri Zemlicka - Warren MI
Yao-Ling Qiu - Detroit MI
John C. Drach - Ann Arbor MI
Roger G. Ptak - New Market MD

Assignee:

Wayne State University
The Regents of the University of Michigan

International Classification:

C07D47316

US Classification:

514262, 514261, 544276, 544277

Abstract:

Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R and R are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R X and/or R X can also be amino acid residues with X as NH.

US Patent:

6790841, Sep 14, 2004

Filed:

Jan 14, 2002

Appl. No.:

10/047202

Inventors:

Jiri Zemlicka - Warren MI
Yao-Ling Qiu - Detroit MI
John C. Drach - Ann Arbor MI
Roger G. Ptak - New Market MD

Assignee:

Wayne State University - Detroit MI
The Regents of the University of Michigan - Ann Arbor MI

International Classification:

C07D47340

US Classification:

514 81, 514151, 5142633, 51426334, 51426337, 5142634, 544244, 544264, 544265, 544276, 544277, 544280, 544254, 544317, 544309, 544182, 546118

Abstract:

Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R and R are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R X and/or R X can also be amino acid residues with X as NH.

US Patent:

6958345, Oct 25, 2005

Filed:

Aug 6, 2004

Appl. No.:

10/913219

Inventors:

Jiri Zemlicka - Warren MI, US
Yao-Ling Qiu - Hamburg PA, US
John C. Drach - Ann Arbor MI, US
Roger G. Ptak - New Market MI, US

Assignee:

The Regents of the University of Michigan - Ann Arbor MI
Wayne State University - Detroit MI

International Classification:

C07D239/47
C07D239/54
A61K031/505

US Classification:

514274, 544314, 544317

Abstract:

Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, Rand Rare alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The RX and/or RX can also be amino acid residues with X as NH.

US Patent:

7183268, Feb 27, 2007

Filed:

Sep 15, 2004

Appl. No.:

10/942314

Inventors:

Jiri Zemlicka - Warren MI, US
John C. Drach - Ann Arbor MI, US
Xinchao Chen - Schenectady NY, US

Assignee:

Wayne State University - Detroit MI
The Regents of the University of Michigan - Ann Arbor MI

International Classification:

C07D 473/32
C07D 473/16
C07D 473/18
A61K 31/522
A61K 31/52

US Classification:

514 81, 5142634, 544244, 544276, 544277

Abstract:

Compounds which are active against viruses have the following Formulas:.

US Patent:

7393855, Jul 1, 2008

Filed:

Sep 15, 2004

Appl. No.:

10/942313

Inventors:

Jiri Zemlicka - Warren MI, US
Shaoman Zhou - Detroit MI, US
John C. Drach - Ann Arbor MI, US

Assignee:

The Regents of the University of Michigan - Ann Arbor MI
Wayne State University - Detroit MI

International Classification:

C07D 473/32
C07D 473/16
A61K 31/522

US Classification:

5142631, 51426337, 5142634, 544265, 544276, 544278

Abstract:

Compounds which are active against viruses have the following formulas:.

US Patent:

7888330, Feb 15, 2011

Filed:

Nov 9, 2006

Appl. No.:

12/092999

Inventors:

Anthony F. Shields - Bloomfield Hills MI, US
Jiri Zemlicka - Warren MI, US
Sridhar Nimmagadda - Baltimore MD, US

Assignee:

Wayne State University - Detroit MI

International Classification:

A01N 43/04
A61K 31/70
A61K 49/04
A61K 51/00
C07H 19/10
C07H 19/048

US Classification:

514 51, 424 173, 424 943, 536 268

Abstract:

The present invention provides phosphoramidate derivatives of a furanosyluracil analog, FAU, that can effectively deliver FAU monophosphate, or a derivative thereof, intracellularly. FAU-Phosphoramidate diesters can bypass the first step of phosphorylation and be activated intracellularly so as to be converted to nucleoside monophosphates. This results in improved formation of nucleoside triphosphates, and higher incorporation into DNA. The compounds of the invention can be used to treat cancer.

US Patent:

8232275, Jul 31, 2012

Filed:

Jul 15, 2011

Appl. No.:

13/183722

Inventors:

Jiri Zemlicka - Warren MI, US
Shaoman Zhou - Atlanta GA, US
John C. Drach - Ann Arbor MI, US

Assignee:

Wayne State University - Detroit MI
The Regents of the University of Michigan - Ann Arbor MI

International Classification:

C07D 239/52
A61K 31/505

US Classification:

514242, 5142651, 514274, 514303, 5142611, 544182, 544254, 544280, 544309, 544311, 544312, 544314, 546118

Abstract:

Compounds which are active against viruses have the following formulas:.

US Patent:

20060122203, Jun 8, 2006

Filed:

Oct 25, 2005

Appl. No.:

11/257776

Inventors:

Jiri Zemlicka - Warren MI, US
Yao-Ling Qiu - Hamburg PA, US
John Drach - Ann Arbor MI, US
Roger Ptak - New Market MI, US

International Classification:

A61K 31/513

US Classification:

514269000, 544314000

Abstract:

Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, Rand Rare alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The RX and/or RX can also be amino acid residues with X as NH.