David A Boykin

US Patent:

6486200, Nov 26, 2002

Filed:

Jul 7, 2000

Appl. No.:

09/612138

Inventors:

David W. Boykin - Atlanta GA
M. Syed Rahmathullah - Mississauga, CA
Richard R. Tidwell - Pittsboro NC
James E. Hall - Chapel Hill NC

Assignee:

The University of North Carolina at Chapel Hill - Chapel Hill NC
Georgia State University Research Foundation, Inc. - Atlanta GA

International Classification:

A61K 31357

US Classification:

514467, 514473, 549448, 549450, 549451

Abstract:

A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): wherein: X may be O, S, or NRâ wherein Râ is H or loweralkyl; R and R may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R and R are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R is represented by a formula selected from the group consisting of: âwherein: X , X , and X are independently selected from O and S; and R and R are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.

US Patent:

6503940, Jan 7, 2003

Filed:

Jul 31, 2001

Appl. No.:

09/918787

Inventors:

David W. Boykin - Atlanta GA
M. Syed Rahmathullah - Mississauga, CA
Richard R. Tidwell - Pittsboro NC
James E. Hall - Chapel Hill NC

Assignee:

The University of North Carolina at Chapel Hill - Chapel Hill NC
Georgia State University Research Foundation, Inc. - Atlanta GA

International Classification:

A61K 3140

US Classification:

514422, 548541, 548556, 549448, 549449, 549450, 549451, 514423

Abstract:

A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): wherein: X may be O, S, or NRâ wherein Râ is H or loweralkyl, R and R may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R and R are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R is represented by a formula selected from the group consisting of: wherein: X , X , and X are independently selected from O and S; and R and R are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.

US Patent:

6613787, Sep 2, 2003

Filed:

Dec 20, 2000

Appl. No.:

09/745004

Inventors:

W. David Wilson - Atlanta GA
David W. Boykin - Atlanta GA
Richard R. Tidwell - Pittsboro NC

Assignee:

The University of North Carolina at Chapel Hill - Chapel Hill NC
Georgia State University Research Foundation, Inc. - Atlanta GA

International Classification:

A61K 31415

US Classification:

514394, 5483047, 549472

Abstract:

Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.

US Patent:

6649652, Nov 18, 2003

Filed:

Jul 30, 2002

Appl. No.:

10/208947

Inventors:

David W. Boykin - Atlanta GA
M. Syed Rahmathullah - Mississauga, CA
Richard R. Tidwell - Pittsboro NC
James E. Hall - Chapel Hill NC

Assignee:

The University of North Carolina at Chapel Hill - Chapel Hill NC
Georgia State University Research Foundation, Inc. - Atlanta GA

International Classification:

C07D31704

US Classification:

514467, 514473, 549229, 549448, 549449, 549451

Abstract:

A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I).

US Patent:

6737440, May 18, 2004

Filed:

Nov 6, 2001

Appl. No.:

10/008535

Inventors:

David W. Boykin - Atlanta GA
Richard R. Tidwell - Pittsboro NC
W. David Wilson - Atlanta GA
John R. Perfect - Durham NC
Chad F. Stephens - Villa Rica GA

Assignee:

The University of North Carolina at Chapel Hill - Chapel Hill NC
Georgia State University Research Foundation, Inc. - Atlanta GA
Duke University - Durham NC

International Classification:

A61K 3127

US Classification:

514491, 514472, 549491, 549472

Abstract:

The present invention relates to novel 2,5-bis {[alkyl(or aryl)imino]aminophenyl}furans and thiophenes of the general formula in which R , R , R and R are each independently selected from the group consisting of H, alkyl, alkoxy, halide, and alkylhalide groups; R is H, alkyl or aryl; R is H, alkyl, aryl, or NR R , in which R and R are each independently selected from the group consisting of H, alkyl and aryl; and X is O, S or NR , in which R is H or alkyl, and to the use of such compounds.

US Patent:

6867227, Mar 15, 2005

Filed:

Sep 2, 2003

Appl. No.:

10/653677

Inventors:

W. David Wilson - Atlanta GA, US
David W. Boykin - Atlanta GA, US
Richard R. Tidwell - Pittsboro NC, US

Assignee:

The University of North Carolina at Chapel Hill - Chapel Hill NC
Georgia State University Research Foundation, Inc. - Atlanta GA

International Classification:

A61K031/423
A61K031/4184
C07D235/15
C07D263/57
C07D413/04

US Classification:

514375, 514394, 548224, 5483047

Abstract:

Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.

US Patent:

7160914, Jan 9, 2007

Filed:

Jan 14, 2005

Appl. No.:

11/035627

Inventors:

W. David Wilson - Atlanta GA, US
David W. Boykin - Atlanta GA, US
Richard R. Tidwell - Pittsboro NC, US

Assignee:

The University of North Carolina at Chapel Hill - Chapel Hill NC
Georgia State University Research Foundation, Inc. - Atlanta GA

International Classification:

A61K 31/4184
A61K 31/4164
C07D 403/04
C12Q 1/04
C12Q 1/24

US Classification:

514393, 5483061, 435 6

Abstract:

Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.

US Patent:

7241795, Jul 10, 2007

Filed:

Mar 2, 2004

Appl. No.:

10/791425

Inventors:

David W. Boykin - Atlanta GA, US
Richard R. Tidwell - Pittsboro NC, US
W. David Wilson - Atlanta GA, US
John R. Perfect - Durham NC, US
Chad F. Stephens - Villa Rica GA, US

Assignee:

The University of North Carolina at Chapel Hill - Chapel Hill NC
Georgia State University Research Foundation, Inc. - Atlanta GA
Duke University - Durham NC

International Classification:

A61K 31/40
A61K 31/38
C07D 207/04
C07D 333/38
C07D 307/34

US Classification:

514408, 514438, 514471, 548577, 549 71, 549491, 546258, 5462841

Abstract:

The present invention relates to novel 2,5-bis{[alkyl (or aryl) imino]aminophenyl}furans and thiophenes of the general formula.