Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.
Type:
Application
Filed:
August 7, 2023
Publication date:
November 30, 2023
Applicant:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
Abstract: This invention is in the area of improved compounds for and methods of treating selected RB-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, improved treatment of select RB-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as highly selective and, in certain embodiments, short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.
Type:
Application
Filed:
March 6, 2023
Publication date:
November 16, 2023
Applicant:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis X. Tavares
Abstract: The addition of a selective, fast-acting, short half-life CDK 4/6 inhibitor in a very specific dosage regimen to the combination of chemotherapy with a checkpoint inhibitor provides superior results in the treatment of a tumor or cancer. The unexpected discovery is that the short pulsatile specifically-timed administration of a selective, fast-acting, short half-life CDK 4/6 inhibitor during administration of the chemotherapy portion of the triple combination therapy has a profound effect on the immune cells in the cancer microenvironment.
Type:
Application
Filed:
December 1, 2022
Publication date:
September 28, 2023
Applicant:
G1 Therapeutics, Inc.
Inventors:
Jessica A. Sorrentino, Anne Y. Lai, Jay C. Strum, Patrick Joseph Roberts
Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.
Type:
Grant
Filed:
April 5, 2021
Date of Patent:
August 8, 2023
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
Abstract: This invention directed to methods for treating select RB-positive cancers and other Rb-positive abnormal cellular proliferative disorders using CDK4/6 inhibitors in specific dosing and combination or alternation regimes. In one aspect, treatments of select RB-positive cancers are disclosed using specific CDK4/6 inhibitors in combination or alternation with a Bruton's tyrosine kinase (BTK) inhibitor.
Type:
Application
Filed:
August 29, 2022
Publication date:
August 3, 2023
Applicant:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John E. Bisi, Patrick Joseph Roberts, Jessica A. Sorrentino, Hannah S. White
Abstract: This invention provides a process for preparing 1,4-diazaspiro[5.5]undecan-3-one and analogues thereof that are useful in the preparation of pharmaceutical compound, including for the treatment of disorders involving abnormal cellular proliferation. Chemical intermediates in the process are also provided.
Type:
Grant
Filed:
February 24, 2021
Date of Patent:
July 25, 2023
Assignee:
G1 Therapeutics, Inc.
Inventors:
Stephen E. Schneider, Hannah White, Thomas Fessard, Sagar Beldar
Abstract: This invention is in the area of improved compounds for and methods of treating selected RB-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, improved treatment of select RB-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as highly selective and, in certain embodiments, short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.
Type:
Grant
Filed:
February 22, 2021
Date of Patent:
May 23, 2023
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis X. Tavares
Abstract: A G1T38 human oral dosage regime that provides a (mean AUC(0-24),ss (h*ng/mL))/(dose (mg)) ratio of less than 5 and/or a (mean AUC(0-24),ss (h*ng/mL))/(Absolute Neutrophil Count (cells/mm3)) ratio on day 22 of dosing of not greater than 1.25.
Abstract: The present invention provides methods for treating a EGFR-mutant cancer in a patient by administering a selective CDK4/6 inhibitor described herein in combination or alternation with an EGFR-TKI to delay or reverse acquired resistance to previously administered EGFR-TKIs. In addition, methods for treating a EGFR-mutant cancer in a patient by administering a selective CDK4/6 inhibitor described herein in combination or alternation with an EGFR-TKI are provided wherein an intrinsically EGFR-TKI resistant EGFR-mutant cancer is sensitized to the effects of the EGFR-TKI.
Type:
Application
Filed:
June 30, 2022
Publication date:
May 11, 2023
Applicant:
G1 Therapeutics, Inc.
Inventors:
Jessica A. Sorrentino, Jay Copeland Strum, John E. Bisi, Andrew Beelen
Abstract: This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.
Abstract: This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
Type:
Grant
Filed:
December 14, 2020
Date of Patent:
April 18, 2023
Assignee:
G1 Therapeutics, Inc.
Inventors:
Alexander Smith, Hannah S. White, Francis Xavier Tavares, Sergiy Krasutsky, Jian-Xie Chen, Roberta L. Dorrow, Hua Zhong
Abstract: This invention provides an unexpectedly stable, highly crystalline form of the di-HCl salt of for advantageous therapeutic pharmaceutical efficacy and dosage form stability.
Type:
Application
Filed:
February 28, 2022
Publication date:
February 9, 2023
Applicant:
G1 Therapeutics, Inc.
Inventors:
Alexander Smith, Hannah S. White, Patricia Andres, Xufeng Sun, Lei Zhu, Petinka I. Vlahova
Abstract: The addition of a selective, fast-acting, short half-life CDK 4/6 inhibitor in a very specific dosage regimen to the combination of chemotherapy with a checkpoint inhibitor provides superior results in the treatment of a tumor or cancer. The unexpected discovery is that the short pulsatile specifically-timed administration of a selective, fast-acting, short half-life CDK 4/6 inhibitor during administration of the chemotherapy portion of the triple combination therapy has a profound effect on the immune cells in the cancer microenvironment.
Type:
Grant
Filed:
June 5, 2019
Date of Patent:
December 20, 2022
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jessica A. Sorrentino, Anne Y. Lai, Jay C. Strum, Patrick Joseph Roberts
Abstract: This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.
Abstract: This invention directed to methods for treating select RB-positive cancers and other Rb-positive abnormal cellular proliferative disorders using CDK4/6 inhibitors in specific dosing and combination or alternation regimes. In one aspect, treatments of select RB-positive cancers are disclosed using specific CDK4/6 inhibitors in combination or alternation with a Bruton's tyrosine kinase (BTK) inhibitor.
Type:
Grant
Filed:
January 22, 2019
Date of Patent:
September 20, 2022
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John E. Bisi, Patrick Joseph Roberts, Jessica A. Sorrentino, Hannah S. White
Abstract: The present invention provides methods for treating a EGFR-mutant cancer in a patient by administering a selective CDK4/6 inhibitor described herein in combination or alternation with an EGFR-TKI to delay or reverse acquired resistance to previously administered EGFR-TKIs. In addition, methods for treating a EGFR-mutant cancer in a patient by administering a selective CDK4/6 inhibitor described herein in combination or alternation with an EGFR-TKI are provided wherein an intrinsically EGFR-TKI resistant EGFR-mutant cancer is sensitized to the effects of the EGFR-TKI.
Type:
Grant
Filed:
August 21, 2019
Date of Patent:
July 26, 2022
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jessica A. Sorrentino, Jay Copeland Strum, John E. Bisi, Andrew Beelen
Abstract: Compositions, combinations and methods comprising a CDK4/6 inhibitor of Formula D with a selective estrogen receptor downregulator of Formula A, B or C that are advantageous for the treatment of abnormal cellular proliferation, including a cancer or a tumor.
Type:
Grant
Filed:
July 2, 2019
Date of Patent:
June 21, 2022
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jay C. Strum, Gregory R. Thatcher, Rui Xiong, Jiong Zhao, Debra A. Tonetti
Abstract: A G1T38 human oral dosage regime that provides a (mean AUC(0-24),ss (h*ng/mL))/(dose (mg)) ratio of less than 5 and/or a (mean AUC(0-24),ss (h*ng/mL))/(Absolute Neutrophil Count (cells/mm3)) ratio on day 22 of dosing of not greater than 1.25.