G1 Therapeutics, Inc.

Gi Therapeutics, Inc.

Smithkline Beecham Corporation

Novatarg, Inc.

Other

Resilio Therapeutics, LLC

Harvard College

The Scripps Research Institute

Sorrento Therapeutics, Inc.

Symberix, Inc.

Pharmacosmos A/s

Tavares, Francis Xavier

Francis Xavier Tavares

Jay Copeland Strum

Patrick Joseph Roberts

John Emerson Bisi

Jeffery Edmond Cobb

Kristjan S Gudmundsson

Kenneth Batchelor

Scott Howard Dickerson

Alexander Smith

Hannah S White

Brad Richard Henke

Sergiy Krasutsky

Jian-Xie Chen

Roberta L Dorrow

Hua Zhong

Michael Peter Vitek

James Marvin Veal

Kim D Janda

Philip Anthony Harris

Stephen Andrew Thomson

David Kendall Jung

David Norman Deaton

Aaron Bayne Miller

Michael Robert Peel

Tara Renae Rheault

Jennifer Gabriel Badiang

Kirk Stevens

John George Catalano

Jennings Franklin Worley, Iii

Jeff T Hutchins

Ward Peterson

Peter K Vogt

Bret D Wallace

Brad R Henke

Huiqiang Zhou

Michael John Reno

Juergen Mollenhauer

Susan Chubinskaya

The present invention provides novel fused bicyclic alkylene linked imidodicarbonimidic diamides. In particular, described herein are N-[2-(indol-3-yl)alkylene]-linked imidodicarbonimidic diamides and N-[2-(pyrrolopyridin-3-yl)alkylene]-linked imidodicarbonimidic diamides (compound of formula (I) or formula (II)), and uses therefor. The compounds of the present invention are believed to be organic cation transporter selective compounds, useful for the treatment of diseases and conditions caused by reduced activity of 5' adenosine monophosphate-activated protein kinase (AMPK).

Fused bicyclic alkylene linked imidodicarbonimidic diamides, methods for synthesis, and uses in therapy

The present disclosure describes compounds and compositions that inhibit β-glucuronidase activity, and methods for attenuating the side effects of one or more drugs and improving the efficacy of drugs by administration of selective β-glucuronidase inhibitors.

Compounds, compositions, and methods for selectively inhibiting β-glucuronidases and alleviating side effects associated with drug treatment induced diarrhea

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.

Transient protection of normal cells during chemotherapy

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.

HSPC-sparing treatments for RB-positive abnormal cellular proliferation

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.

Synthesis of N-(heteroaryl)-pyrrolo[3,2-d]pyrimidin-2-amines

Novel compounds of formula (II) are disclosed. Compounds of formula (II) comprise ornithine derivatives or compounds that can metabolize under physiological conditions to ornithine. The pH and plasma stability of compounds of formula (II) is also described. Also disclosed are methods for the treatment of neurodegenerative diseases such as Alzheimer's Disease using compounds of formula (II).

Compounds and methods for the treatment of neurodegenerative diseases

This invention provides small molecule Myc-inhibitors. Also provided in the invention are therapeutic applications of these compounds for treating Myc-driven cancer and other related methods.

Small molecule c-Myc inhibitors

Methods for the synthesis of lactams are presented whereby a carboxylic acid of the formula HOOC&#x2014;OR&#x2014;NH-LG, wherein OR is an organic moiety and LG is a leaving group, is reacted with an acid, such as an organic acid, in particular a strong acid, and a dehydrating agent, which may be one in the same such as a strong acid anhydride, such that the amount of acid added allows for the desired transformation to take place without the loss of the leaving group (LG) before the cyclization, and recovering the lactam.

Synthesis of lactams

Compounds of Formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

CDK inhibitors

Synthesis of n-(heteroaryl)-pyrrolo[3,2-d]pyrimidin-2-amines

Growing community of inventors

Durham, NC, United States of America

Francis Xavier Tavares