Gliatech, Inc.

The Cleveland Clinic Foundation

Chiron Corporation

Glaxosmithkline LLC

Anacor Pharmaceuticals, Inc.

James G Phillips

Jacob J Plattner

Yong-Kang Zhang

Tsutomu Akama

Rajeshwar Singh

Vincent S Hernandez

Stephen J Baker

Yi Xia

Michael Richard Kevin Alley

Clark E Tedford

Amin Mohammed Khan

Syed M Ali

Babal Kant Jha

Anand Dev Tiwari

Nishith C Chaturvedi

Stephen L Yates

Kwok Peng Ng

Rustum S Boyce

Jason Daniel Speake

Huchen Zhou

Rashmi Sharma

Yogenthiran Saunthararajah

Jaroslaw Maciejewski

Rahim Mohammad

Thomas Radivoyevitch

Yihong Guan

Jennifer Carew

Minh Ha

El Mehdi Keramane

James A Nieman

Xiasong Lu

A method of treating cancer is described. The method includes administering a therapeutically effective amount of a TET2 activating compound or pharmaceutically acceptable salt thereof to a subject in need of treatment. The TET2 activating compounds are α-ketoglutarate derivatives. A method of treating or preventing cancer in a subject that includes the step of analyzing a biological sample to determine if cells of the biological sample exhibit a TET2 mutation in addition to administering a TET2 activator is also described.

Antitumor TET2 modulating compounds

Imidazopyridine derivatives according to formula I are described 

Antitumor derivatives for differentiation therapy

Autophagy inhibitors useful for the treatment of cancer and other diseases are described. The autophagy inhibitors are a compound of formula: I wherein Ris a group selected from lower alkyl, lower alkyl amide, lower alkyl ester, lower alkyl ketone, and lower alkyl ether; Rand Rare H or a group selected from cycloalkyl, lower alkyl, lower alkyl amide, lower alkyl ester, lower alkyl ketone, and lower alkyl ether; Ris a heteroaryl group; and L is a &#x2014;(CH)&#x2014;X&#x2014;(CH)&#x2014; group, wherein n is 1, 2, 3, or 4, X is absent, O, S, or N&#x2014;R, wherein Ris H or a lower alkyl group, or a pharmaceutically acceptable salt thereof. 

Substituted thioxanthenone autophagy inhibitors

A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the formula IA and IB. IA and IB have the following structures where Z has the formula shown below and the rest of the variables are defined herein 

Quinazolinone compounds with reduced bioaccumulation

1H-4(5)-substituted imidazole derivatives

The present invention provides, in its principal aspect, compounds of the general formula: ##STR1## when A is --NHCO--, --N(CH.sub.3)--CO--, --NHCH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --CH.dbd.CH--, --COCH.sub.2 --, CH.sub.2 CH.sub.2 --, --CH(OH)CH.sub.2 -- or --C.tbd.C--;

1H-4(5)-cyclo-substituted imidazole derivatives as histamine H.sub.3

The present invention provides compounds having H.sub.3 histamine receptor antagonist activity of the general formula: ##STR1## R.sub.2 is a hydrogen or a methyl or ethyl group; R.sub.3 is a hydrogen or a methyl or ethyl group; n is 1, 2, 2, 3, 4, 5, or 6; and R.sub.1 is selected from the group consisting of (a) C.sub.3 to C.sub.8 cycloalkyl; (b) phenyl or substituted phenyl; (c) alkyl; (d) heterocyclic; (e) decahydronapthalene; and (f) octahydroindene; with the provisos that

2-(1H-4(5)-imidazoyl) cyclopropyl derivatives

2-(1H-4(5)-imidazoyl) cyclopropyl compounds

The present invention provides compounds having H.sub.3 histamine receptor antagonist activity of the general formula: ##STR1## where X is H, A is --CH.sub.2 CH.sub.2 --, --COCH.sub.2 --, --CONH--, --CON(CH.sub.3)--, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 --NH--, --CH.sub.2 --NCH.sub.3 --, --CH(OH)CH.sub.2 --, --NH--CH.sub.2 --, --N(CH.sub.3) --CH.sub.2 --, --NHSO.sub.2 --, --CH.sub.2 O--, --CH.sub.2 S--, CH.sub.2 SO.sub.2 --, or --CH.sub.2 S(O)--;

2-(4-imidazoyl) cyclopropyl derivatives

Growing community of inventors

Bay Village, OH, United States of America

James G Phillips