Tri-institutional Therapeutics Discovery Institute

Cornell University

The Rockefeller University

Other

Sloan-kettering Institute for Cancer Research

Icahn School of Medicine at Mount Sinai

Michael Andrew Foley

Kazuyoshi Aso

Gang Herbert Lin

Carl F Nathan

Toshihiro Imaeda

Tzu-Tshin Wong

Kenjiro Sato

Rei Okamoto

Ryoma Hara

Trevor Morgan

Wenhu Zhan

Takafumi Yukawa

Akinori Toita

Laura Kirkman

Yoshiyuki Fukase

Masanori Kawasaki

John D Ginn

Peter T Meinke

Barry S Coller

Tomohiro Okawa

Hideki Furukawa

Yuta Tanaka

Moriteru Asano

Marta Filizola

Timothy Hla

Maurizio Scaltriti

Mayako Michino

Tarun M Kapoor

Yayoi Yoshitomi

Ayumu Sato

Yasutomi Asano

Yasufimi Wada

Asato Kina

Hideyuki Igawa

William J Polvino

Andrew Stamford

Hiroki Takahagi

Irina Jilishitz

Yusuke Sasaki

Jose Manuel Baselga Torres

Amaia Arruabarrena Aristorena

Carles Monterrubio Martinez

Daniel Alan Heller

Makoto Fushimi

Yosef Shamay

Yashuhiro Hirata

Sachie Takashima

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 various examples presented herein are directed to compounds of the formula A-L-Het-L-Cyor a pharmaceutical acceptable salt, polymorph, prodrug, solvate or clathrate thereof, wherein: A is cycloalkyl, aryl, arylalkyl or heterocyclyl; Hetis heterocyclyl containing at least two heteroatoms; Cyis a heterocyclyl; Lis a bond, alkyl, alkenyl or alkynyl linker; Lis an acyl or alkyl linker; and A and Cyare different. The compounds are useful in the treatment of fibrotic diseases, abnormal vascular leak and pathological angiogenesis.

Pyridinone- and pyridazinone-based compounds 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&#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

Tetrahydronaphthyridines of formula are disclosed. These compounds selectively inhibit &#x3b1;V&#x3b2;3 without activating the &#x3b1;V&#x3b2;3 receptor. They are useful for treating osteoporosis, acute myelogenous leukemia, sickle cell disease, focal segmental glomerulosclerosis, fibrosis, supravalvular aortic stenosis associated with Williams syndrome, tumors expressing &#x3b1;V&#x3b2;3, tumor metastasis, bone resorption, T-cell lymphoma, retinal disease, age-related macular degeneration, diabetic retinitis, and herpes simplex virus infection. They may also be used for inhibiting tumor angiogenesis.

Tetrahydronaphthyridinepentanamide integrin antagonists

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Michael Andrew Foley