Dana-farber-cancer Institute Inc.

Children's Medical Center Corporation

Cornell University

The Schepens Eye Research Institute, Inc.

David A Scott

Nathanael Schiander Gray

John M Hatcher

Michael Eck

Jaebong Jang

Nathanael S Gray

Ofer Levy

Ari Matthew Melnick

David J Dowling

Francesco Borriello

Spencer E Brightman

Lorena Fontan Gabas

Pasi Antero Janne

Yongbo Hu

Courtney A Cullis

Guangyan Du

Alyssa Verano

Dries De Clercq

Shih-Chung Huang

Ciric To

David Heppner

Frederic Feru

Tyler Beyett

Thomas Gero

Jamie A Saxon

Eric S Fischer

Radoslaw Nowak

Katherine Donovan

Krista E Gipson

Calla M Olson

Patricia A D'Amore

Behnam Nabet

Brian Groendyke

Hao Wu

Yin Shan Eric Ng

Qi Qiao

Spandan Chennamadhavuni

Ashley Mackey

Steve Stroud

Mikaela Mohardt

Zhengnian Li

Benika J Pinch

Gopalan Gnanaguru

The disclosure relates to compounds that act as allosteric inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.

Allosteric EGFR inhibitors and methods of use thereof

The disclosure relates to a compound of Formula (I), which acts as an allosteric inhibitor of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compound; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.

Disclosed are compounds that possess inhibitory activity against FAK. Also disclosed are pharmaceutical compositions containing the compounds and methods of using the compounds to treat cancer mediated by aberrant FAK activity.

Small-molecule focal adhesion kinase (FAK) inhibitors

Disclosed are bifunctional compounds (degraders) that target Wee1 tyrosine kinase for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat disease.

Degraders of WEE1 kinase

Provided herein are Toll-like receptor 2 (TLR2) agonists for use in enhancing human immune response and/or as adjuvants in vaccines. The TLR2 agonists include thiophenes, imidazoles, or phenyl-containing compounds, which may be compounds of Formulae (I), (II), (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. The compounds described herein are used as enhancers of an immune response (e.g., innate and/or adaptive immune response), and are useful in treating and/or preventing a disease, as adjuvants in a vaccine for the disease. (e.g., proliferative disease, inflammatory disease, autoimmune disease, infectious disease, or chronic disease). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

Use of toll-like receptor 2 (TLR-2) agonist for modulating human immune response

The application relates to compounds, or pharmaceutically acceptable salts, hydrates, solvates, or stereoisomers thereof, which modulate the activity of EGFR, a pharmaceutical composition comprising said compounds, and methods of treating or preventing a disease in which EGFR plays a role.

Inhibitors of EGFR and methods of use thereof

The application relates to a compound having Formula X: which modulates the activity of HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, plays a role.

Inhibitors of EGFR and/or HER2 and methods of use

Provided herein are imidazopyrimidine compounds, such as compounds of Formula (I), for use in enhancing human immune response and/or as adjuvants in vaccines.

Composition comprising an antigen and a substituted imidazo[1,2-a]pyrimidine for enhancing human immune response

The present disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. The compounds described herein are used as enhancers and/or modifiers of an immune response (e.g., innate and/or adaptive immune response), and are useful in treating and/or preventing a disease, as adjuvants in a vaccine for the disease, (e.g., proliferative disease, inflammatory disease, autoimmune disease, infectious disease, or chronic disease), or as stand alone anti-infective or immune response modifying agents. Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein. 

Imidazopyrimidine compounds and uses thereof

There are provided inter alia compounds capable of inhibiting retinal pigment epithelium (RPE) degeneration or geography atrophy (GA) associated with age-related macular degeneration (AMD), and methods of using the same.

Compounds and compositions for inhibiting retinal pigment epithelium degeneration and methods using the same

Provided herein are compounds that inhibit MALT1, a protein whose activity is responsible for constitutive NF-&#x3ba;B signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating MALT1-related diseases and disorders (e.g., cancer) with the compounds in a subject, by administering the compounds and/or compositions described herein.

Inhibitors of MALT1 and uses thereof

The application relates to a compound having Formula X: which modulates the activity of HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, plays a role. 

Provided herein are compounds of Formula (I) and pharmaceutical compositions thereof, which may be useful as MALT1 inhibitors. Also provided are for the treatment of proliferative disorders (e.g., cancer (e.g., non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, MALT lymphoma), benign neoplasm, a disease associated with angiogenesis, an autoimmune disease, an inflammatory disease, an autoinflammatory disease) by administering a compound of Formula (I). 

MALT1 inhibitors and uses thereof

Provided herein are bifunctional compounds that inhibit MALT1 and/or promote targeted ubiquitination for the degradation of MALT1. In particular, provided are compounds that can bind MALT1, a protein whose activity is responsible for constitutive NF-KB signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)), and can assist in its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon, VHL), which can ubiquitinate MALT1, marking it for proteasome degradation. Also provided are pharmaceutical compositions comprising the bifunctional compounds, methods of treating cancer with the bifunctional compounds, methods of promoting the degradation of MALT1, and methods of binding E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.

Compounds for MALT1 degredation

Growing community of inventors

Newton, MA, United States of America

David A Scott