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 21, 2018
Date of Patent:
December 15, 2020
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 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:
May 28, 2020
Publication date:
November 5, 2020
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 heterocyclic-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
Abstract: This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
Type:
Application
Filed:
May 18, 2020
Publication date:
September 10, 2020
Applicant:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, Ricky D. Gaston, Robert C. Gadwood
Abstract: This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
Abstract: This invention is a benzothiophene estrogen receptor modulator or its pharmaceutically acceptable salt or a pharmaceutically acceptable composition thereof to treat an estrogen-related medical disorder.
Abstract: This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
Type:
Grant
Filed:
December 21, 2018
Date of Patent:
May 19, 2020
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, Ricky D. Gaston, Robert C. Gadwood
Abstract: This invention is a benzothiophene estrogen receptor modulator or its pharmaceutically acceptable salt or a pharmaceutically acceptable composition thereof to treat an estrogen-related medical disorder.
Abstract: This invention provides an unexpectedly stable, highly crystalline form of the di-HCl salt of 2?-((5-(4-isopropylpiperazin-1-yl)pyridin-2-yl)amino)-7?,8?-dihydro-6?H-spiro[cyclohexane-1,9?-pyrazino[1?,2?:1,5]pyrrolo[2,3-d]pyrimidin]-6?-one for advantageous therapeutic pharmaceutical efficacy and dosage form stability.
Type:
Application
Filed:
December 19, 2019
Publication date:
April 23, 2020
Applicant:
G1 Therapeutics, Inc.
Inventors:
Alexander Smith, Hannah S. White, Patrica Andres, Xufeng Sun, Lei Zhu, Petinka I. Vlahova
Abstract: This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
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:
August 21, 2019
Publication date:
December 12, 2019
Applicant:
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:
Application
Filed:
July 2, 2019
Publication date:
October 24, 2019
Applicants:
G1 Therapeutics, Inc., The Board of Trustees of the University of Illinois
Inventors:
JAY C. STRUM, Gregory R. Thatcher, Rui Xiong, Jiong Zhao, Debra A. Tonetti
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:
June 5, 2019
Publication date:
October 24, 2019
Applicant:
G1 Therapeutics, Inc.
Inventors:
Jessica A. Sorrentino, Ann Y. Lai, Jay C. Strum, Patrick Joseph Roberts
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:
August 24, 2018
Date of Patent:
October 8, 2019
Assignee:
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 therapeutic combinations for and methods of treating selected retinoblastoma (Rb)-negative cancers and Rb-negative abnormal cellular proliferative disorders using particular topoisomerase inhibitors and specific cyclin-dependent kinase 4/6 (CDK4/6) inhibitors. In one aspect, the improved treatment of select Rb-negative cancers is disclosed using specific compounds disclosed herein in combination with a topoisomerase I inhibitor.
Type:
Grant
Filed:
September 26, 2018
Date of Patent:
September 17, 2019
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John E. Bisi, Patrick Joseph Roberts, Jessica A. Sorrentino
Abstract: This invention is in the area of tricyclic lactam 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, treatment of select Rb-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as selective cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.
Type:
Grant
Filed:
July 31, 2017
Date of Patent:
August 13, 2019
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Ricky D. Gaston, Robert C. Gadwood