Tri-Institutional Therapeutics Discovery Institute

Cornell University

Other

The Rockefeller University

Sloan-Kettering Institute for Cancer Research

Kazuyoshi Aso

Michael Andrew Foley

Gang Herbert Lin

Carl F Nathan

Toshihiro Imaeda

Tzu-Tshin Wong

Kenjiro Sato

Rei Okamoto

Wenhu Zhan

Trevor Morgan

Ryoma Hara

Takafumi Yukawa

Akinori Toita

Laura Kirkman

Masanori Kawasaki

John D Ginn

Peter T Meinke

Tomohiro Okawa

Hideki Furukawa

Yuta Tanaka

Moriteru Asano

Maurizio Scaltriti

Tarun M Kapoor

Yoshiyuki Fukase

Mayako Michino

Yayoi Yoshitomi

Hiroki Takahagi

Jose Manuel Baselga Torres

Yusuke Sasaki

Yasutomi Asano

Amaia Arruabarrena Aristorena

Sachie Takashima

Yosef Shamay

Makoto Fushimi

Daniel Alan Heller

Yashuhiro Hirata

Carles Monterrubio Martinez

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

The compounds of the present invention are represented by the following compounds having Formula I and Formula (I′): where the substituents R, R, R, R, R, R, R', R″, X, Y, and Z are as defined herein and where the substituents R, R, R, R, R, R', R″, X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.

Macrocyclic compounds as proteasome inhibitors

The compounds of the present invention are represented by the following compounds having Formula I and Formula (I'): where the substituents R, R, R, R, R, R, R&#x2032;, R&#x2033;, X, Y, and Z are as defined herein and where the substituents R, R, R, R, R, R&#x2032;, R&#x2033;, X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.

The compounds of the present invention are represented by the following compounds having Formula (I) and Formula (I'): where the substituents R, R, R, R, R, W, X, Y, Z, k, and m are as defined herein and where the substituents R, R, R, R, R, X, Y, Z, and m are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.

Peptidomimetic proteasome inhibitors

The compounds of the present invention are represented by the following compounds having Formula (I) and Formula (I'): where the substituents R, R, RR, R&#x2032;, W, X, Y, Z, k, and m are as defined herein and where the substituents R, R, R, R, R, X, Y, Z, and m are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues. 

Compounds of formula: are useful as antitumor agents. In these compounds, Ris (a) (C-C) hydrocarbyl, (C-C)halohydrocarbyl, (C-C)hydroxyalkyl, or or Ris (b) in which Q and A are linkers and Ar is optionally substituted monocyclic or bicyclic aryl or heteroaryl.

Pyrazoloquinazolinone antitumor agents

Growing community of inventors

Kanagawa, Japan

Kazuyoshi Aso