Srdan Verstovsek

US Patent:

6995188, Feb 7, 2006

Filed:

Jan 13, 2005

Appl. No.:

11/035178

Inventors:

Ralph A. Zingaro - College Station TX, US
Emil J. Freireich - Houston TX, US
Hatice Duzkale - Houston TX, US
Hagop Kantarjian - Bellaire TX, US
Srdan Verstovsek - Houston TX, US
Merida Sotelo-Lerma - Hermosillo, MX

Assignee:

Board of Regents, The University of Texas System - Austin TX
The Texas A&M University System - College Station TX

International Classification:

A61K 31/285
A61K 33/36
C07F 9/70

US Classification:

514504, 556 71, 556 77, 556 78, 556 80, 424629

Abstract:

Arsenic trioxide, an inorganic compound, is commercially available anti-cancer agent but it carries significant toxicity. Organic arsenicals, on the other hand, are much less toxic, to the extent that the methylation of inorganic arsenic in vivo into organic arsenicals has been considered a detoxification reaction. New organic arsenic derivatives have been synthesized, including S-dimethylarsino-glutathione, S-dimethylarsino-thiosuccinic acid and S-dimethylarsino-thiobenzoic acid, and established its potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia. Results form a basis for the development of S-dimethylarsino-glutathione, S-dimethylarsino-thiosuccinic acid, S-dimethylarsino-thiobenzoic acid, and other organic arsenicals as an anti-cancer therapy, combining high efficacy with very low, if any, toxicity.

US Patent:

7405314, Jul 29, 2008

Filed:

Oct 17, 2005

Appl. No.:

11/252966

Inventors:

Ralph A. Zingaro - College Station TX, US
Hatice Duzkale - Houston TX, US
Emil J. Freireich - Houston TX, US
Hagop Kantarjian - Bellaire TX, US
Merida Sotelo-Lerma - Hermosillo, MX
Srdan Verstovsek - Houston TX, US
Mingzhang Gao - Indianapolis IN, US

Assignee:

The Texas A&M University System - College Station TX
Board of Regents, The University of Texas System - Austin TX

International Classification:

A61K 61/285
C07F 9/00

US Classification:

556 71, 556 76, 514504

Abstract:

The present invention provides organic arsenicals. Many of these compounds have potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia.

US Patent:

7619000, Nov 17, 2009

Filed:

Feb 6, 2006

Appl. No.:

11/349043

Inventors:

Ralph A. Zingaro - College Station TX, US
Emil J. Freireich - Houston TX, US
Hatice Duzkale - Houston TX, US
Hagop Kantarjian - Bellaire TX, US
Srdan Verstovsek - Houston TX, US
Merida Sotelo-Lerma - Hermosillo, MX

Assignee:

The Texas A&M University System - College Station TX
Board of Regents, The University of Texas System - Austin TX

International Classification:

A61K 31/285
A61K 33/36
C07F 9/00

US Classification:

514504, 556 71, 556 77, 556 78, 556 80, 424629

Abstract:

Arsenic trioxide, an inorganic compound, is commercially available anti-cancer agent but it carries significant toxicity. Organic arsenicals, on the other hand, are much less toxic, to the extent that the methylation of inorganic arsenic in vivo into organic arsenicals has been considered a detoxification reaction. New organic arsenic derivatives have been synthesized, including S-dimethylarsino-glutathione, S-dimethylarsino-thiosuccinic acid and S-dimethylarsino-thiobenzoic acid, and established its potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia. Results form a basis for the development of S-dimethylarsino-glutathione, S-dimethylarsino-thiosuccinic acid, S-dimethylarsino-thiobenzoic acid, and other organic arsenicals as an anti-cancer therapy, combining high efficacy with very low, if any, toxicity.

US Patent:

20040034095, Feb 19, 2004

Filed:

Jan 7, 2003

Appl. No.:

10/337969

Inventors:

Ralph Zingaro - College Station TX, US
Emil Freireich - Houston TX, US
Hatice Duzkale - Houston TX, US
Hagop Kantarjian - Bellaire TX, US
Srdan Verstovsek - Houston TX, US
Merida Sotelo-Lerma - Hermosillo, MX

International Classification:

A61K031/285
C07F009/70

US Classification:

514/504000, 556/069000

Abstract:

Arsenic trioxide, an inorganic compound, is commercially available anti-cancer agent but it carries significant toxicity. Organic arsenicals, on the other hand, are much less toxic, to the extent that the methylation of inorganic arsenic in vivo into organic arsenicals has been considered a detoxification reaction. New organic arsenic derivatives have been synthesized, including S-dimethylarsino-glutathione, S-dimethylarsino-thiosuccinic acid and S-dimethylarsino-thiobenzoic acid, and established its potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia. Results form a basis for the development of S-dimethylarsino-glutathione, S-dimethylarsino-thiosuccinic acid, S-dimethylarsino-thiobenzoic acid, and other organic arsenicals as an anti-cancer therapy, combining high efficacy with very low, if any, toxicity.

US Patent:

20040192652, Sep 30, 2004

Filed:

Dec 8, 2003

Appl. No.:

10/729387

Inventors:

Francis Giles - Houston TX, US
Srdan Verstovsek - Houston TX, US

International Classification:

A61K031/675
A61K031/513

US Classification:

514/081000, 514/269000, 514/085000

Abstract:

In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of leukemia comprising at least one active compound of formula (I): and a Bcr-Abl tyrosine kinase inhibitor, and a method of treating a patient having leukemia comprising at least one active compound of formula (I), as defined above, and a Bcr-Abl tyrosine kinase inhibitor.

US Patent:

20080090793, Apr 17, 2008

Filed:

Aug 20, 2007

Appl. No.:

11/894766

Inventors:

Ralph Zingaro - College station TX, US
Hatice Duzkale - Houston TX, US
Emil Freireich - Houston TX, US
Hagop Kantarjian - Bellaire TX, US
Merida Sotelo-Lerma - Hermosillo, MX
Srdan Verstovsek - Houston TX, US
Mingzhang Gao - Indianapolis IN, US

Assignee:

The Texas A&M University System - College Station TX
Board of Regents, The University of Texas System - Austin TX

International Classification:

A61K 31/285
A61K 31/555
A61P 35/00
C07F 9/00
C07F 9/80

US Classification:

514188000, 514504000, 546003000, 556070000

Abstract:

The present invention provides organic arsenicals. Many of these compounds have potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia.

US Patent:

20080090904, Apr 17, 2008

Filed:

Aug 20, 2007

Appl. No.:

11/894807

Inventors:

Ralph Zingaro - College Station TX, US
Emil Freireich - Houston TX, US
Hatice Duzkale - Houston TX, US
Hagop Kantarjian - Bellaire TX, US
Srdan Verstovsek - Houston TX, US
Merida Sotelo-Lerma - Hermosillo, MX

Assignee:

The Texas A&M University System - College Station TX
Board of Regents, The University of Texas System - Austin TX

International Classification:

A61K 31/285
A61P 35/00
C07F 9/66

US Classification:

514504000, 556071000

Abstract:

Arsenic trioxide, an inorganic compound, is commercially available anti-cancer agent but it carries significant toxicity. Organic arsenicals, on the other hand, are much less toxic, to the extent that the methylation of inorganic arsenic in vivo into organic arsenicals has been considered a detoxification reaction. New organic arsenic derivatives have been synthesized, including S-dimethylarsino-glutathione, S-dimethylarsino-thiosuccinic acid and S-dimethylarsino-thiobenzoic acid, and established its potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia. Results form a basis for the development of S-dimethylarsino-glutathione, S-dimethylarsino-thiosuccinic acid, S-dimethylarsino-thiobenzoic acid, and other organic arsenicals as an anti-cancer therapy, combining high efficacy with very low, if any, toxicity.