Memorial Sloan Kettering Cancer Center

Sloan-kettering Institute for Cancer Research

The Rockefeller University

Other

Columbia University

Cornell University

Gabriela Chiosis

Tony Taldone

Stefan O Ochiana

Huazhong He

Pallav Patel

Yanlong Kang

Weilin Sun

Anna Rodina

Peter Smith-Jones

Laura Llauger-Bufi

Hardik J Patel

Joungnam Kim

Steven M Larson

NagaVarakishore Pillarsetty

Steve Larson

Maulik Patel

Liza Shrestha

Mark Dunphy

W Clark Still

Ivo Boneca

Chenghua Yang

Pengrong Yan

Danuta Zatorska

Mary L Alpaugh

Erica M Gomes-Dagama

Paul Greengard

Jason S Lewis

Neal Rosen

Naga Vara Kishore Pillarsetty

Monica L Guzman

Wenjie Luo

Fei Dou

H William Strauss

Hongliang Zong

John Koren

Nagavarakishore Pillarsetty

Neal c/o Office Of Industrial Affairs Rosen

Treatment of neurodegenerative diseases is achieved using small molecule purine scaffold compounds that inhibit Hsp90 and that possess the ability to cross the blood-brain barrier or are otherwise delivered to the brain.

Treatment of neurodegenerative diseases through inhibiton of Hsp90

This invention concerns various methods of using labeled HSP90 inhibitors to improve treatment of cancer patients with HSP90 inhibitors, including ex vivo and in vivo methods for determining whether a tumor will likely respond to therapy with an HSP90 inhibitor.

Uses of labeled HSP90 inhibitors

The disclosure relates to novel selective Grp94 inhibitors, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as cancer, comprising administering to an animal in need thereof an effective amount of such compounds.

Selective Grp94 inhibitors and uses thereof

The present invention provides new methods for inflammation and infection imaging and related medical applications thereof. In some embodiments, the present invention provides a method for the diagnosis of inflammation and/or infection. In some embodiments, the present invention provides a method for the treatment or prevention of inflammation and/or infection. In some embodiments, the present invention provides methods for monitoring the effect of inflammation and/or infection treatment, and/or methods for monitoring an inflammation and/or infection treatment regimen. In some embodiments, the present invention provides a method for selecting subjects for an inflammation and/or infection treatment. In some embodiments, the present invention provides a method for determining the dosage of a drug for the treatment of inflammation and/or infection.

HSP90-targeted inflammation and infection imaging and therapy

The present invention provides methods for radiolabeling compounds useful as Hsp90 inhibitors. The present invention also provides intermediates useful in such methods, and compositions of radiolabeled compounds. The present invention provides, among other things novel methods for the synthesis of radiolabeled compounds. In certain embodiments, the present invention provides compounds of formula I.

Methods and reagents for radiolabeling

The present subject matter relates to a compound represented by the general formula (I) or (I') or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).

Heat shock protein binding compounds, compositions, and methods for making and using same

Purine scaffold Hsp90 inhibitors are useful in therapeutic applications and as radioimaging ligands.

Small-molecule HSP90 inhibitors

The present invention, among other things, provides compounds and compositions thereof for use in the modulation of Hsp70. In some embodiments, the present invention provides a method for inhibiting Hsp70 activity. In some embodiments, the present invention provides a method of treating a subject suffering from or susceptible to a disease, disorder, or condition responsive to Hsp70 inhibition comprising administering to the subject a therapeutically effective amount of a provided compound. In some embodiments, the present invention provides a method for treating or preventing cancer in a subject suffering therefrom, comprising administering to a patient in need thereof a therapeutically effective amount of a provided compound.

Hsp70 modulators and methods for making and using the same

Hsp9O-targeted inflammation and infection imaging and therapy

Treatment of neurodegenerative diseases is achieved using small molecule purine scaffold compounds that inhibit Hsp90 and that possess the ability to cross the blood-brain barrier or are other wise delivered to the brain.

Treatment of neurodegenerative diseases through inhibition of HSP90

The present invention provides new methods for cardiac imaging and related medical applications thereof. In some embodiments, the present invention provides a method for the diagnosis of cardiovascular diseases, conditions, or disorders. In some embodiments, the present invention provides a method for the treatment or prevention of cardiovascular diseases, conditions, or disorders. In some embodiments, the present invention provides methods for monitoring the effect of cancer treatment on the heart, and/or methods for monitoring a cancer treatment regimen. In some embodiments, the present invention provides a method for selecting subjects for a test or treatment. In some embodiments, the present invention provides a method for determining the dosage of a drug. In some embodiments, the present invention provides methods for determining the risk of a cardiovascular disease, for assessing risk of a cardiovascular disease, and/or for determining the risk of heart attack.

HSP90-targeted cardiac imaging and therapy

The present application provides substituted purine derivatives and related compounds of the formulas shown. These compounds are useful as inhibitors of HSP90, and hence in the treatment of related diseases. (Formulae) Z-Z, X-X, X, X, Y and R are as defined in the specification. 

Purine derivatives useful as HSP90 inhibitors

Hsp90 inhibitors havin are provided havin the formula: (I) with a 2',4&#x2032;,5&#x2032;-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4&#x2032; and 5&#x2032; positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SOalkyl, COO-alkyl, KH, OH, CN, SOX, NO, NO, C&#x2550;SRNSOX, C&#x2550;OR, where Xis F, NH2, alkyl or H, and Ris alkyl, NH, NH-alkyl or O-alkyl, Cto Calkyl or alkoxy; or wherein Xhas the formula &#x2014;O&#x2014;(CH)&#x2014;O&#x2014;, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5&#x2032;-position and the other at the 4&#x2032;-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands. 

Growing community of inventors

New York, NY, United States of America

Gabriela Chiosis