Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Type:
Application
Filed:
March 11, 2011
Publication date:
June 30, 2011
Applicant:
Merck & Co., Inc.
Inventors:
Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
Abstract: The Present invention relates to antibodies that immunospecifically bind to phospho-Akt and certain p-Akt substrates. The invention encompasses human and humanized forms of the antibodies and their use in treating cancers and other proliferative disorders. The invention also relates to p-Akt derived peptides useful for preparing the antibodies. Methods and compositions for detecting, diagnosing, treating or ameliorating a disease or disorder, especially cancer and other proliferative disorders using the present antibodies also are disclosed.
Abstract: The present invention relates to human Akt3 proteins and polypeptides. The invention also relates to isolated nucleic acids encoding human Akt3, to vectors containing them and to their therapeutic uses, in particular for gene therapy. Expression of Akt3 inhibits cell death associated with hypoxia, apoptosis or necrosis.
Type:
Application
Filed:
August 1, 2011
Publication date:
February 9, 2012
Applicant:
AVENTIS PHARMACEUTICALS INC.
Inventors:
Kun Guo, Marco F. Pagnoni, Kenneth L. Clark, Yuri D. Ivashchenko
Abstract: The instant invention provides for substituted thiazoles that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Abstract: The present invention relates to antibodies that immunospecifically bind to phospho-Akt and certain p-Akt substrates. The invention encompasses human and humanized forms of the antibodies and their use in treating cancers and other proliferative disorders. The invention also relates to p-Akt-derived peptides useful for preparing the antibodies. Methods and compositions for detecting, diagnosing, treating or ameliorating a disease or disorder, especially cancer and other proliferative disorders using the present antibodies also are disclosed.
Abstract: Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.
Type:
Application
Filed:
May 20, 2019
Publication date:
September 5, 2019
Inventors:
Samir N. Khleif, Mikayel Mkrtichyan, Iryna Lebedyeva
Abstract: Human EEF2K genes are identified as modulators of the PTEN/AKT pathway and thus are therapeutic targets for disorders associated with defective PTEN/AKT function. Methods for identifying modulators of PTEN/AKT comprising screening for agents that modulate the activity of EEF2K are provided.
Type:
Grant
Filed:
March 10, 2006
Date of Patent:
March 25, 2014
Assignee:
Exelixis, Inc.
Inventors:
Arthur Brace, Robert A. Blake, Lori S. Friedman, Lynn Margaret Bjerke, Kevin M. Ward, Susana Nieto-Bergman
Abstract: The present invention relates to human Akt3 proteins and polypeptides. The invention also relates to isolated nucleic acids encoding human Akt3, to vectors containing them and to their therapeutic uses, in particular for gene therapy. Expression of Akt3 inhibits cell death associated with hypoxia, apoptosis or necrosis.
Type:
Grant
Filed:
March 14, 2000
Date of Patent:
April 19, 2005
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Kun Guo, Marco F. Pagnoni, Kenneth L. Clark, Yuri D. Ivashchenko
Abstract: Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.
Type:
Application
Filed:
January 17, 2017
Publication date:
July 20, 2017
Inventors:
Samir N. Khleif, Mikayel Mkrtichyan, lryna Lebedyeva
Abstract: Provided herein are inhibitors of AKT1, pharmaceutical compositions comprising the inhibitory compounds, and methods for using the AKT1 inhibitory compounds for the treatment of disease.
Type:
Application
Filed:
September 26, 2023
Publication date:
May 30, 2024
Inventors:
Michael David BARTBERGER, Elena V. DNEPROVSKAIA, Yi FAN, Eric Anthony MURPHY, Xuefeng ZHU
Abstract: Methods for determining whether a cancer patient is likely to benefit from treatment with a taxane compound based on Akt-Ser473 phosphorylation status are provided, together with kits for determining Akt-Ser473 phosphorylation status and methods for improving treatment of a cancer patient that include obtaining a determination of the Akt-Ser473 phosphorylation status of the cancer.
Type:
Application
Filed:
May 21, 2010
Publication date:
June 7, 2012
Applicant:
The United States of America, as represented by the Secretary, Department of Health and Human Serv
Abstract: Methods for determining whether a cancer patient is likely to benefit from treatment with a taxane compound based on Akt-Ser473 phosphorylation status are provided, together with kits for determining Akt-Ser473 phosphorylation status and methods for improving treatment of a cancer patient that include obtaining a determination of the Akt-Ser473 phosphorylation status of the cancer.
Type:
Grant
Filed:
May 21, 2010
Date of Patent:
October 1, 2013
Assignee:
The United States of America, as represented by the Secretary, Department of Health and Human Services
Abstract: Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.
Type:
Grant
Filed:
October 2, 2019
Date of Patent:
May 25, 2021
Assignee:
Augusta University Research Institute, Inc.
Abstract: Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.
Type:
Grant
Filed:
January 17, 2017
Date of Patent:
May 21, 2019
Assignee:
Augusta University Research Institute, Inc.
Inventors:
Samir N. Khleif, Mikayel Mkrtichyan, Iryna Lebedyeva
Abstract: The instant invention provides for substituted fused pyrimidine compounds of Formula A that inhibit Akt activity: In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Type:
Grant
Filed:
March 29, 2010
Date of Patent:
April 8, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Qi Chen, Mingxiang Cui, Bin Hu, Shuangxi Hu, Zhifa Pu, Philip E. Sanderson, Richard Soll, Xue Tang, Jiabing Wang, Yongjin Yan, Jinfeng Yao, Hongjie Zhang
Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Type:
Grant
Filed:
March 11, 2011
Date of Patent:
October 16, 2012
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
Abstract: The present invention relates to antibodies that immunospecifically bind to phospho-Akt and certain p-Akt substrates. The invention encompasses human and humanized forms of the antibodies and their use in treating cancers and other proliferative disorders. The invention also relates to p-Akt-derived peptides useful for preparing the antibodies. Methods and compositions for detecting, diagnosing, treating or ameliorating a disease or disorder, especially cancer and other proliferative disorders using the present antibodies also are disclosed.
Abstract: Most human tumors find ways to resist anticancer drug monotherapy. Akt is considered a likely peptide providing such monotherapy drug resistance. Data indicates that Akt chemoresistance is induced in a p53-dependent manner and that inhibition of Akt may be an effective means of overcoming chemoresistance in cancer cells expressing wild-type p53. Breast, ovarian, lung cancer and leukemia cells lines were treated with combinations of Akt activation inhibitor Triciribine (TCN) or Triciribine phosphate (TCNP) and chemotherapeutic drugs to determine the efficiency of combination therapy. Additionally, cells were introduced into xenograft models to determine in vivo effects of combination treatment. Combining TCN or TCNP with other anticancer drugs overcame cytotoxic or treatment resistance. Thus, TCN and TCNP are shown to broaden the spectrum of human tumors that can be effectively treated.
Abstract: The instant invention provides for substituted fused pyrimidine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Type:
Application
Filed:
March 29, 2010
Publication date:
March 29, 2012
Inventors:
Qi Chen, Mingxiang Cui, Bin Hu, Shuangxi Hu, Zhifa Pu, Philip E. Sanderson, Richard Soll, Xue Tang, Jiabing Wang, Yongjin Yan, Jinfeng Yao, Hongjie Zhang
Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Type:
Grant
Filed:
December 4, 2007
Date of Patent:
August 18, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson