Amgen Inc.

Biogen Ma Inc.

The Broad Institute, Inc.

Skyhawk Therapeutics, Inc.

Sling Media Inc.

Brian Stuart Lucas

Lawrence R McGee

Felix Gonzalez Lopez De Turiso

Joseph P Lyssikatos

Jay Patrick Powers

Jason A Duquette

Ming Yu

Brian M Fox

Ana Zurisadai Gonzalez Buenrostro

Yi Heng Chen

Gnanasambandam Kumaravel

Kevin Guckian

Xiaodong Wang

Timothy David Cushing

Michael G Johnson

Xiaolin Hao

Xiao He

Jermaine Thomas

Julio Cesar Medina

Tiansheng Wang

Michael Luzzio

Frank Kayser

Xiaoqi Chen

Edward Holson

Robert Michael Rzasa

Liusheng Zhu

Jeffrey Thomas Mihalic

Xuelei Yan

Dustin L McMinn

David John Kopecky

Zice Fu

Jiwen Liu

Xianghong Wang

Sean P Brown

Youngsook Shin

Zhili Xin

Ilya Asnis

Daqing Sun

Robert J Zamboni

Florence Fevrier Wagner

Zhihua Ma

Dawei Zhang

Yosup Rew

Jonathan Dante Low

Michael D Bartberger

Richard J Austin

Zhihong Li

Tracy J Jenkins

Timothy Raymond Chan

Benjamin Fisher

Jiang Zhu

Robert Meissner

Irina Leaf

Jeremy Duffield

John Eksterowicz

Hilary Plake Beck

Jeffrey Deignan

Julie Anne Heath

Richard V Connors

Darin J Gustin

Steven H Olson

Michel Weiwer

Yingcai Wang

Andreas Reichelt

Joel McIntosh

Sebastien Caille

Nick A Paras

Mike Elias Lizarzaburu

Marc Vimolratana

Yunxiao Li

Jennifer L Seganish

Jiasheng Fu

Matthew Bio

XianYun Jiao

Manuel Zancanella

Joshua Taygerly

Yihong Li

Yuanqing Fang

Michael W Gribble, Jr

Xin Huang

Philip M Roveto

SuJen Lai

TeYu Chen

Sean H Wiedemann

Jeffery Vessels

Arthur J Campbell

Edward Yin-Shiang Lin

John Howard Jones

Minna Bui

Jeffrey Vessels

Istvan J Enyedy

Edward Yin Shiang Lin

Nathan Genung

Filisaty Vounatsos

Brian McNeil Cochran

Sarah Wortman

Kurt D Van Vloten

Joshua R Sacher

The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intellectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder).

Tricyclic compounds as glycogen synthase kinase 3 (GSK3) inhibitors and uses thereof

Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, pharmaceutical compositions comprising the same, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.

Methods and compositions for modulating splicing

Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use as Nrf2 activators and for their production. 

Tetrahydronaphthalene derivatives useful as Nrf2 activators

Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production. Formula (I) The compounds are IRAK-4 inhibitors useful for treating an inflammatory disease, an autoimmune disease, cancer, a cardiovascular disease, a disease of the central nervous system, a disease of the skin, an ophthalmic disease and condition, and a bone disease. 

IRAK4 inhibiting agents

The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intellectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder). 

Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are Mcl-1 inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

Compounds that inhibit Mcl-1 protein

Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.

NRF2 activator

Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

Compounds that inhibit MCL-1 protein

Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110&#x3b4; activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

Heterocyclic compounds and their uses

The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

Processes of making and crystalline forms of a MDM2 inhibitor

Growing community of inventors

Arlington, MA, United States of America

Brian Stuart Lucas