Patents by Inventor Kirk R. Gustafson
Kirk R. Gustafson has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
-
Patent number: 10246463Abstract: Embodiments of small molecule inhibitors of hypoxia inducible factor 1 (HIF-1) and pharmaceutical compositions thereof are disclosed. The disclosed compounds suppress HIF-1 activity by inhibiting the interaction between the HIF-1 ? subunit and transcriptional co-activator protein p300. Embodiments of methods for making and using the small molecule inhibitors are also disclosed.Type: GrantFiled: April 6, 2016Date of Patent: April 2, 2019Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Kirk R. Gustafson, Martin J. Schnermann, Susanna T. S. Chan, Paresma R. Patel, William D. Figg, James B. McMahon
-
Publication number: 20180093995Abstract: Embodiments of small molecule inhibitors of hypoxia inducible factor 1 (HIF-1) and pharmaceutical compositions thereof are disclosed. The disclosed compounds suppress HIF-1 activity by inhibiting the interaction between the HIF-1 a subunit and transcriptional co-activator protein p300. Embodiments of methods for making and using the small molecule inhibitors are also disclosed.Type: ApplicationFiled: April 6, 2016Publication date: April 5, 2018Applicant: The United States of America, as represented by the Secretary, Department of Health and Human ServInventors: Kirk R. Gustafson, Martin J. Schnermann, Susanna T. S. Chan, Paresma R. Patel, William D. Figg, James B. McMahon
-
Patent number: 9820965Abstract: The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.Type: GrantFiled: September 10, 2015Date of Patent: November 21, 2017Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Michael R. Boyd, Kirk R. Gustafson, Charles L. Cantrell
-
Patent number: 9314448Abstract: Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): wherein R1, R2, R3, X1, X2, X3, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.Type: GrantFiled: June 5, 2013Date of Patent: April 19, 2016Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Curtis J. Henrich, Heidi R. Bokesch, Laura K. Cartner, Richard W. Fuller, Kirk R. Gustafson, Kentaro Takada, James B. McMahon, Susan E. Bates, Robert W. Robey, Suneet Shukla, Suresh V. Ambudkar, Michael C. Dean
-
Patent number: 9238069Abstract: Disclosed is a method of enhancing the response of cancer cells in a mammal to treatment with a death receptor ligand, which method comprises contacting the cancer cells with a death receptor ligand in conjunction with an effective amount of a compound described herein, for example, a cucurbitacin (I) or a withanolide (II). Also disclosed is a method of inducing apoptosis in cancer cells in a mammal, comprising contacting the cancer cells with a compound described herein, for example, a cucurbitacin (I) or a withanolide (II) and also contacting the cancer cells with a death receptor ligand, whereby apoptosis is induced in the cancer cells.Type: GrantFiled: December 16, 2010Date of Patent: January 19, 2016Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Thomas Joseph Sayers, Nancy Lynn Booth, Curtis J. Henrich, Alan David Brooks, Kirk R. Gustafson, Karen L. Erickson
-
Publication number: 20150374661Abstract: The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.Type: ApplicationFiled: September 10, 2015Publication date: December 31, 2015Applicant: The United States of America, as represented by the Secretary, Department of Health and Human ServInventors: Michael R. Boyd, Kirk R. Gustafson, Charles L. Cantrell
-
Patent number: 9139595Abstract: The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.Type: GrantFiled: May 12, 2014Date of Patent: September 22, 2015Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Michael R. Boyd, Kirk R. Gustafson, Charles L. Cantrell
-
Publication number: 20140243284Abstract: The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.Type: ApplicationFiled: May 12, 2014Publication date: August 28, 2014Applicant: The United States of America, as represented by the Secretary, Department of Health and Human ServInventors: Michael R. Boyd, Kirk R. Gustafson, Charles L. Cantrell
-
Patent number: 8741947Abstract: The present invention provides a compound of the formula (I) or (II, wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.Type: GrantFiled: August 6, 2010Date of Patent: June 3, 2014Assignee: The United States of America, as represented by the Secretary of the Department of Health and Human ServicesInventors: Michael R. Boyd, Kirk R. Gustafson, Charles L. Cantrell
-
Patent number: 8729053Abstract: An embodiment of the invention provides a pharmaceutical composition comprising a compound of formula (I) a pharmaceutically acceptable salt, prodrug, hydrate, or solvate thereof. Another embodiment of the invention provides a method of treating or preventing a condition associated with increased expression and/or activity of an NF?B pathway using same compounds. A further embodiment of the invention provides a method of diagnosing a condition in an individual using same compounds.Type: GrantFiled: September 22, 2009Date of Patent: May 20, 2014Assignee: The United States of America, as represented by the Secretary of the Department of Health and Human ServicesInventors: Curtis J. Henrich, Moon-II Kang, Heidi R. Bokesch, Kirk R. Gustafson, Nancy H. Colburn, Matthew R. Young, James B. McMahon
-
Patent number: 8609716Abstract: A composition comprising a substantially purified compound of the formula: in combination with at least one additional therapeutic agent, and methods of preventing or treating cancer and a condition treatable by the inhibition of vacuolar-type (H+)-ATPase.Type: GrantFiled: October 1, 2012Date of Patent: December 17, 2013Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Michael R. Boyd, Kirk R. Gustafson
-
Publication number: 20130274323Abstract: Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): wherein R1, R2, R3, X1, X2, X3, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.Type: ApplicationFiled: June 5, 2013Publication date: October 17, 2013Inventors: Curtis J. Henrich, Heidi R. Bokesch, Laura K. Cartner, Richard W. Fuller, Kirk R. Gustafson, Kentaro Takada, James B. McMahon, Susan E. Bates, Robert W. Robey, Suneet Shukla, Suresh V. Ambudkar, Michael C. Dean
-
Patent number: 8470888Abstract: Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): Formula (I), wherein R1, R2, R3, X1, X2, X3, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.Type: GrantFiled: December 29, 2008Date of Patent: June 25, 2013Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Curtis J. Henrich, Heidi R. Bokesch, Laura K. Cartner, Richard W. Fuller, Kirk R. Gustafson, Kentaro Takada, James B. McMahon, Susan E. Bates, Robert W. Robey, Suneet Shukla, Suresh V. Ambudkar, Michael C. Dean
-
Publication number: 20130039883Abstract: Disclosed is a method of enhancing the response of cancer cells in a mammal to treatment with a death receptor ligand, which method comprises contacting the cancer cells with a death receptor ligand in conjunction with an effective amount of a compound described herein, for example, a cucurbitacin (I) or a withanolide (II). Also disclosed is a method of inducing apoptosis in cancer cells in a mammal, comprising contacting the cancer cells with a compound described herein, for example, a cucurbitacin (I) or a withanolide (II) and also contacting the cancer cells with a death receptor ligand, whereby apoptosis is induced in the cancer cells.Type: ApplicationFiled: December 16, 2010Publication date: February 14, 2013Applicant: THE UNITED STATES OF AMERICAInventors: Thomas Joseph Sayers, Nancy Lynn Booth, Curtis J. Henrich, Alan David Brooks, Kirk R. Gustafson, Karen L. Erickson
-
Patent number: 8278348Abstract: A composition comprising a substantially purified compound of the formula: in combination with at least one additional therapeutic agent, and methods of preventing or treating cancer and a condition treatable by the inhibition of vacuolar-type (H+)-ATPase.Type: GrantFiled: October 22, 2010Date of Patent: October 2, 2012Assignee: The United States of America, as represented by the Secretary of the Department of Health and Human ServicesInventors: Michael R. Boyd, Kirk R. Gustafson
-
Publication number: 20110190240Abstract: An embodiment of the invention provides a pharmaceutical composition comprising a compound of formula (I)a pharmaceutically acceptable salt, prodrug, hydrate, or solvate thereof. Another embodiment of the invention provides a method of treating or preventing a condition associated with increased expression and/or activity of an NF?B pathway using same compounds. A further embodiment of the invention provides a method of diagnosing a condition in an individual using same compounds.Type: ApplicationFiled: September 22, 2009Publication date: August 4, 2011Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPT. OF HEALTH AND HUMAN SERVICESInventors: Curtis J. Henrich, Moon-Il Kang, Heidi R. Bokesch, Kirk R. Gustafson, Nancy H. Colburn, Matthew R. Young, James B. McMahon
-
Publication number: 20110034547Abstract: A composition comprising a substantially purified compound of the formula: in combination with at least one additional therapeutic agent, and methods of preventing or treating cancer and a condition treatable by the inhibition of vacuolar-type (H+)-ATPase.Type: ApplicationFiled: October 22, 2010Publication date: February 10, 2011Applicants: Department of Health and Human ServicesInventors: Michael R. Boyd, Kirk R. Gustafson
-
Publication number: 20100317732Abstract: Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): Formula (I), wherein R1, R2, R3, X1, X2, X3, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.Type: ApplicationFiled: December 29, 2008Publication date: December 16, 2010Applicant: THE UNITED STATES OF AMERICA,AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICEInventors: Curtis J. Henrich, Heidi R. Bokesch, Laura K. Cartner, Richard W. Fuller, Kirk R. Gustafson, Kentaro Takada, James B. McMahon, Susan E. Bates, Robert W. Robey, Suneet Shukla, Suresh V. Ambudkar, Michael C. Dean
-
Publication number: 20100298248Abstract: The present invention provides a compound of the formula (I) or (II, wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.Type: ApplicationFiled: August 6, 2010Publication date: November 25, 2010Applicant: The U.S.A., as represented by the secretary, Department of Health and Human ServicesInventors: Michael R. Boyd, Kirk R. Gustafson, Charles L. Cantrell
-
Patent number: 7790764Abstract: The present invention provides a compound of formula (II). The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.Type: GrantFiled: May 16, 2006Date of Patent: September 7, 2010Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Michael R Boyd, Kirk R Gustafson, Charles L Cantrell