Abstract: The present application provides stable peptide-based Akt capture agents and methods of use as detection and diagnosis agents and in the treatment of diseases and disorders. The application further provides methods of manufacturing Akt capture agents using iterative on-bead in situ click chemistry.
Type:
Application
Filed:
May 5, 2015
Publication date:
December 3, 2015
Inventors:
Kaycie Deyle, Blake Farrow, James R. Heath
Abstract: The subject invention relates to peptide inhibitors of Akt as well as to uses of these inhibitors. More specifically, the inhibitors may be used, for example, to induce apoptosis in cells and sensitize tumor cells to cancer therapies. The peptides may also be used to purify Akt.
Type:
Application
Filed:
March 21, 2002
Publication date:
September 25, 2003
Inventors:
Yan Luo, Vincent L. Giranda, Paul L. Richardson, Richard A. Smith
Abstract: The instant invention provides for substituted fused naphthyridine derivatives 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 10, 2010
Date of Patent:
December 24, 2013
Assignees:
Merck Sharp & Dohme Corp., MSD K.K.
Inventors:
Weiming Fan, Thomas F. N. Haxell, Matthew G. Jenks, Nobuhiko Kawanishi, Shuliang Lee, Hao Liu, Michael J. Malaska, Joseph A. Moore, III, Yoshio Ogino, Yu Onozaki, Bharathi Pandi, Michael R. Peel, Toshihiro Sakamoto, Tony Siu
Abstract: The administration of an Akt inhibitor in a suitable carrier to a rheumatoid arthritis synovial fibroblast affords a process for inducing rheumatoid arthritis synovial fibroblast apoptosis. The Akt inhibitor is administered either as an active molecule or as a gene sequence expressible within rheumatoid arthritis synovial fibroblast cells. The gene sequence can be encompassed within a gene vector such as an adenovirus. A process for assaying rheumatoid arthritis drug candidates for apoptosis affect includes exposing a culture of rheumatoid arthritis synovial fibroblast cells to a drug candidate and monitoring apoptosis in the culture in the presence of the drug candidate. Apoptosis in the culture is compared to apoptosis induced in a duplicate culture in the presence of a known Akt inhibitor.
Type:
Application
Filed:
November 16, 2004
Publication date:
May 18, 2006
Inventors:
John Mountz, Huang-Ge Zhang, Hui-Chen Hsu
Abstract: Compounds and compositions for selectively modulating Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
Type:
Application
Filed:
August 10, 2020
Publication date:
December 17, 2020
Inventors:
Samir N. KHLEIF, Mikayel MKRTICHYAN, Iryna LEBEDYEVA, Thomas ALBERS
Abstract: The subject invention concerns materials and methods for inhibiting the Akt/PKB pathway. In one embodiment, a compound of the invention inhibits kinase activity and/or phosphorylation levels of Akt proteins. The subject invention also concerns methods for inhibiting or killing a cancer cell or other cell in which expression of an Akt protein is elevated or constitutively active, comprising contacting the cell with an effective amount of a compound of formula I. The subject invention also concerns methods for treating cancer or a tumor in a person or animal comprising administering all effective amount of a compound of formula I to the person or animal.
Abstract: Provided is a compound as an Akt kinase inhibitor. The present invention specifically relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition containing the compound, and the use thereof in the preparation of a drug for treating Akt kinase-related diseases.
Abstract: The present invention discloses an AKT inhibitor, and specifically relates to a compound represented by formula I or a pharmaceutically acceptable salt thereof. The present invention further provides a preparation method thereof, and the use thereof in prevention and/or treatment of a disease mediated by AKT protein kinase.
Type:
Application
Filed:
January 22, 2020
Publication date:
May 12, 2022
Inventors:
Changyou Ma, He Tian, Jie An, Jianliang Zhao, Donghui Chen, Jian Wu, Dan Xu, Chunxia Zhu, Zhoushan Tian
Abstract: Compounds and compositions for selectively inhibiting Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
Type:
Grant
Filed:
January 17, 2017
Date of Patent:
July 9, 2019
Assignee:
Augusta University Research Institute, Inc.
Abstract: Compounds and compositions for selectively inhibiting Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
Type:
Grant
Filed:
February 20, 2018
Date of Patent:
December 25, 2018
Assignee:
Augusta University Research Institute, Inc.
Abstract: Relapse in adoptive cell transfer of CAR-T cells is often the result of CAR-T cells disappearance. Disclosed herein a method for enhancing CAR-T cell therapy in a subject, comprising administering to a subject undergoing adoptive cell transfer of therapeutic CAR-T cells an Akt inhibitor in an amount effective to increase the persistence of the CAR-T cells. As a consequence, a subject treated with a combination of CAR-T cells and an Akt inhibitor is less likely to relapse. Therefore, also disclosed herein is a method for treating a subject, comprising adoptively transferring to the subject an effective amount of a composition comprising a CAR-T cell, and administering to the subject an Akt inhibitor in an amount effective to increase the persistence of the CAR-T cells.
Abstract: The present application provides stable peptide-based Akt capture agents and methods of use as detection and diagnosis agents and in the treatment of diseases and disorders. The application further provides methods of manufacturing Akt capture agents using iterative on-bead in situ click chemistry.
Type:
Application
Filed:
August 17, 2017
Publication date:
March 15, 2018
Inventors:
Kaycie Deyle, Blake Farrow, James R. Heath
Abstract: Compounds and compositions for selectively inhibiting Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
Type:
Grant
Filed:
February 6, 2019
Date of Patent:
March 17, 2020
Assignee:
Augusta University Research Institute, Inc.
Abstract: The subject invention concerns materials and methods for inhibiting the Akt/PKB pathway. In one embodiment, a compound of the invention inhibits kinase activity and/or phosphorylation levels of Akt proteins. The subject invention also concerns methods for inhibiting or killing a cancer cell or other cell in which expression of an Akt protein is elevated or constitutively active, comprising contacting the cell with an effective amount of a compound of formula I. The subject invention also concerns methods for treating cancer or a tumor in a person or animal comprising administering an effective amount of a compound of formula I to the person or animal.
Abstract: The present invention provides compounds of Formula I including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as Akt protein kinase inhibitors and for the treatment of Akt-mediated diseases, for example, hyperproliferative diseases such as cancer.
Abstract: In certain aspects, the invention relates to methods for identifying compounds which modulate Akt activity mediated by the rictor-mTOR complex and methods for treating or preventing a disorder that is associated with aberrant Akt activity.
Type:
Application
Filed:
July 15, 2008
Publication date:
July 8, 2010
Inventors:
David M. Sabatini, Dos D. Sarbassov, Michael Andreeff, Marina Konopleva, Zhihong Zeng, Francis J. Giles
Abstract: The instant invention provides for 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:
January 25, 2010
Publication date:
November 24, 2011
Inventors:
Donna J. Armstrong, Yasuhiro Goto, Takashi Hashihayata, Tetsuya Kato, Michael J. Kelly, III, Mark E. Layton, Craig W. Lindsley, Yoshio Ogino, Yu Onozaki, Kenvin J. Rodzinak, Michael A. Rossi, Philip E. Sanderson, Jiabing Wang, Melissa M. Yaroschak
Abstract: Compounds and compositions for selectively inhibiting Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
Type:
Grant
Filed:
February 5, 2020
Date of Patent:
April 20, 2021
Assignee:
Augusta University Research Institute, Inc.
Inventors:
Samir N. Khleif, Mikayel Mkrtichyan, Iryna Lebedyeva, Thomas Albers
Abstract: The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases.