Tri-institutional Therapeutics Discovery Institute

Cornell University

The Rockefeller University

Sloan-kettering Institute for Cancer Research

Memorial Sloan Kettering Cancer Center

Mayako Michino

Rei Okamoto

Thomas Tuschl

Peter T Meinke

Toshihiro Imaeda

Yasutomi Asano

Taku Kamei

Jumpei Aida

Michael Andrew Foley

Dinshaw J Patel

Lonny Levin

Jochen Buck

Kazuyoshi Aso

Maurizio Scaltriti

Ayumu Sato

Lavoisier Ramos-Espiritu

Clemens Steegborn

J Fraser Glickman

Michael Miller

Yosef Shamay

Makoto Fushimi

Daniel Alan Heller

Shogo Hashizume

Carles Monterrubio Martinez

Amaia Arruabarrena Aristorena

Hiroki Takahagi

Jose Manuel Baselga Torres

Lodoe Lama

Daisuke Tomita

Takanobu Kuroita

Yusuke Sasaki

JFraser Glickman

Taku Kamel

The development of a new, targeted drug delivery paradigm coupled to improved PI3K inhibitors (e.g., PI3Kα inhibitors) represents a significant advance in cancer therapy. Provided herein are compounds, such as compounds of Formula (I) and (II), and pharmaceutically acceptable salts, hydrates, solvates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The compounds provided herein are PI3K (e.g., PI3Kα) inhibitors and are therefore useful for the treatment and/or prevention of various diseases (e.g., proliferative diseases such as cancer). Also provided herein are nanoparticles and nanogels (e.g., P-selectin targeting nanoparticles) comprising PI3K inhibitors, such a compound described herein. In certain embodiments, a nanoparticle or nanogel described herein encapsulates a compound described herein for targeting delivery to cancer cells or tumors.

PI3K inhibitors and uses thereof

1-(3,4-Dihydro-1H-pyrido[4, 3-b]indol-2(5H)-yl)-2-hydroxyethanones are disclosed. The compounds are inhibitors of human cGAS in interferon-producing cell types. They are thus useful as therapeutic agents for treating cGAS-related autoimmune diseases in humans.

Substituted pyrido[4,3-b]indoles and azepino[4,5-b]indoles as inhibitors of cGAS

Provided are 6-amino substituted 2,6-diamino-4-chloropyrimidine compounds which are specific inhibitors of soluble adenylyl cyclase. The compounds can be formulated with pharmaceutical carriers and used for reducing cyclic AMP levels. The compositions can be used for treatment of various conditions including ocular hypotony.

Inhibitors of soluble adenylyl cyclase

Growing community of inventors

New York, NY, United States of America

Mayako Michino