Robert W Brueggemeier

US Patent:

7572919, Aug 11, 2009

Filed:

Aug 26, 2005

Appl. No.:

11/212229

Inventors:

Robert W. Brueggemeier - Dublin OH, US
Young-Woo Kim - Columbus OH, US
John C. Hackett - Dublin OH, US

Assignee:

The Ohio State University Research Foundation - Columbus OH

International Classification:

C07D 311/04
C07D 311/74
C07D 401/02

US Classification:

5462831, 549400, 549401

Abstract:

Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I:.

US Patent:

7741520, Jun 22, 2010

Filed:

Feb 5, 2007

Appl. No.:

11/702276

Inventors:

Robert W Brueggemeier - Dublin OH, US
Bin Su - Columbus OH, US
Edgar S Diaz-Cruz - Columbus OH, US
Serena Landini - Columbus OH, US

Assignee:

The Ohio State University Research Foundation - Columbus OH

International Classification:

C07C 311/10
A61K 31/18

US Classification:

564 99, 564 84, 564 97, 514602, 514605

Abstract:

Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I:.

US Patent:

7829557, Nov 9, 2010

Filed:

Aug 28, 2006

Appl. No.:

11/511192

Inventors:

Robert W. Brueggemeier - Dublin OH, US
Young-Woo Kim - Columbus OH, US

Assignee:

The Ohio State University Research Foundation - Columbus OH

International Classification:

A61K 31/5377
C07D 413/02

US Classification:

5142335, 544151

Abstract:

The present invention provides 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of cancers, namely breast cancer. This invention further provides a method of synthesis of 2-(alkylthio)isoflavones that can be carried out at ambient conditions. This invention further provides a method of synthesis of the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one from a 2-(alkylthio)isoflavone. The invention further provides methods of using the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of breast cancer in mammals.

US Patent:

7960548, Jun 14, 2011

Filed:

May 1, 2006

Appl. No.:

11/414890

Inventors:

J. Thomas Pento - Norman OK, US
Robert W. Brueggemeier - Dublin OH, US
John C. Hackett - Dublin OH, US

Assignee:

The Ohio State University Research Foundation - Columbus OH
The Board of Regents of the University of Oklahoma - Norman OK

International Classification:

C07D 471/02
C07D 215/22
C07D 215/227

US Classification:

546 62, 546157, 546158

Abstract:

Compounds and methods for treating, inhibiting, or delaying the onset of cancer in a subject by administering a therapeutically effective amount of a keratinocyte growth factor receptor tyrosine kinase (KGFR TK) inhibitor to the subject in need of such treatment. Also provided are compounds and methods for the treating, inhibiting, or delaying the onset of metastasis in a subject with cancer by administering a therapeutically effective amount of a KGFR TK inhibitor to the subject in need of such treatment.

US Patent:

8476313, Jul 2, 2013

Filed:

May 26, 2009

Appl. No.:

12/471751

Inventors:

Robert W. Brueggemeier - Dublin OH, US
Young-Woo Kim - Belmont MA, US
John C. Hackett - Dublin OH, US

Assignee:

The Ohio State University Research Foundation - Columbus OH

International Classification:

A61K 31/352
A61K 31/44

US Classification:

514456, 514337, 549400, 549403, 5462831

Abstract:

Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I:.

US Patent:

20040087586, May 6, 2004

Filed:

Aug 4, 2003

Appl. No.:

10/634463

Inventors:

Robert Brueggemeier - Dublin OH, US
Young-Woo Kim - Columbus OH, US

International Classification:

A61K031/5377
A61K031/452
A61K031/4025
A61K031/353
C07D413/02
C 07D 4 5/02

US Classification:

514/232800, 514/320000, 514/422000, 514/456000, 544/151000, 546/196000, 548/525000, 549/406000

Abstract:

The present invention provides 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of cancers, namely breast cancer. This invention further provides a method of synthesis of 2-(alkylthio)isoflavones that can be carried out at ambient conditions. This invention further provides a method of synthesis of the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one from a 2-(alkylthio)isoflavone. The invention further provides methods of using the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of breast cancer in mammals.

US Patent:

20090181110, Jul 16, 2009

Filed:

Jul 9, 2008

Appl. No.:

12/169858

Inventors:

Marcy J. Balunas - Indicasat, PA
Bin Su - Glendora CA, US
Robert W. Brueggemeier - Columbus OH, US
Alan Douglas Kinghorn - Columbus OH, US

Assignee:

THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION - Columbus OH

International Classification:

A61K 36/38
C12N 9/99
A61K 31/352
C12N 9/00
A61P 35/00

US Classification:

424725, 435184, 514455, 435 4

Abstract:

Aromatase inhibitors (AIs) are disclosed which are useful in the treatment and prevention of post-menopausal breast cancer. New AIs derived from natural products are disclosed that are evaluated for clinical utility for treating post-menopausal breast cancer and may also act as chemopreventive agents for preventing breast cancer. Several pure compounds demonstrated AI activity using a noncellular, enzyme-based microsomal and a cell-based aromatase assay. Correlations are made between structural classes with levels of aromatase inhibition. The disclosure may be utilized to direct synthetic modification of natural product scaffolds to enhance aromatase inhibition or to standardize botanical dietary supplements for increased aromatase inhibition activity.