Michael P Groziak

6339151, Jan 15, 2002

Jan 22, 1999

09/235961

H. Michael Shepard - Rancho Santa Fe CA
Michael P. Groziak - Palo Alto CA

NewBiotics, Inc. - San Diego CA

C07H 19073

536 268, 536 2854, 536 2855, 536 2711, 514 50, 514 51

This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with a prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.

6683061, Jan 27, 2004

Oct 10, 2001

09/856127

H. Michael Shepard - Encinitas CA
Ming Fai Chan - Encinitas CA
Michael P. Groziak - Palo Alto CA

NewBiotics, Inc. - San Diego CA

A01N 4304

514 50, 514 42, 514 49, 514 43, 514 44, 514 45, 514 51, 536 172, 536 173

This invention provides novel substrate compounds that selectively inhibit the proliferation of pathological cells, for example, pathological calls that endogenously overexpress a target enzyme that confers resistance to biologic and chemotherapeutic agents. The enzyme acts on a substrate compound to 1) convert it to a cellular toxin and/or 2) release a toxic byproduct. In one embodiment, the activity of the target enzyme has been greatly enhanced in a target cell as a result of loss of tumor suppressor function and/or selection resulting from previous exposure to chemotherapy. In another embodiment, the pathological cell contains a target enzyme that is an expression product of an infectious agent in the cell. Further provided by this invention is a method for treating a subject by delivering to the subject a prodrug as described herein. The prodrugs of this invention may be used alone or in combination with other chemotherapeutics or alternative anti-cancer therapies such as radiation.

7601703, Oct 13, 2009

Feb 12, 2001

09/782721

H. Michael Shepard - Rancho Sante Fe CA, US
Michael P. Groziak - Palo Alto CA, US

Celmed Oncology (USA), Inc. - Quebec

A61K 31/70
C07H 19/10

514 51, 536 268

This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with a prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.

7605144, Oct 20, 2009

Oct 7, 2003

10/681418

H. Michael Shepard - Encinitas CA, US
Ming Fai Chan - Encinitas CA, US
Michael P. Groziak - Palo Alto CA, US

Celmed Oncology (USA), Inc. - Quebec

A61K 31/70
C07H 19/10
C12Q 1/66
C12P 29/00
C12P 31/00

514 51, 536 268, 435 8, 435 63, 435 64

This invention provides novel compounds selected from the group consisting of a 1,5-substituted pyrimidine derivative or analog and substituted furano-pyrimidone analogs. The compounds are useful to treat or prevent diseases such as cancer.

60839368, Jul 4, 2000

Jan 25, 1999

9/236948

Michael P. Groziak - Palo Alto CA

SRI International - Menlo Park CA

A01N 5558
C07C 6996
C07F 504
C07F 502

514 64

Boron heterocycle steroid mimics are provided that are useful as pharmaceutical agents, particularly in the treatment of estrogen-dependent disorders such as estrogen-dependent cancers. The compounds are also useful in diagnostic techniques such as magnetic resonance imaging (MRI) and magnetic resonance spectroscopy (MRS), in boron neutron capture therapy, and in fluorescence emission-based modalities. Pharmaceutical formulations and methods of using the novel compounds are provided as well.

62483056, Jun 19, 2001

Jan 25, 2000

9/490601

Michael P. Groziak - Palo Alto CA

SRI International - Menlo Park CA

A61K 5100
A61K 3169
A61B 5055
C07F 504
C07F 502

424 161

Boron heterocycle steroid mimics are provided that are useful as pharmaceutical agents, particularly in the treatment of estrogen-dependent disorders such as estrogen-dependent cancers. The compounds are also useful in diagnostic techniques such as magnetic resonance imaging (MRI) and magnetic resonance spectroscopy (MRS), in boron neutron capture therapy, and in fluorescence emission-based modalities. Pharmaceutical formulations and methods of using the novel compounds are provided as well.