Takeda San Diego, Inc.

Takeda Pharmaceutical Company Limited

Biophysica, Inc.

Biophysica Foundation

Jerome C Bressi

Jeffrey Alan Stafford

Anthony R Gangloff

Phong H Vu

Jason W Brown

Sheldon Cao

Andrew John Jennings

Xiao-Yi Xiao

Lily Kwok

Milos Sovak

James Gordon Douglass, Iii

Michael Brennan Wallace

Stephen W Kaldor

Wolfgang J Wrasidlo

Zhiyuan Zhang

John David Lawson

Robert J Skene

Mallareddy Komandla

Shaosong Chu

Brian Campion

Philip Erickson

Sanjib Das

Allen Seligson

Compounds of the following formula are provided for use with cMET: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using the compounds.

cMET inhibitors

Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.

Histone deacetylase inhibitors

Compounds, pharmaceutical compositions, kits and methods useful for inhibiting HDAC, thereby treating a disease state for which HDAC possess activity that contributes to the pathology and/or symptomology of the disease state. The compound is selected from the group consisting of: 

Compounds, pharmaceutical compositions, kits and methods are provided for use with histone deacetylases (HDACs) that comprise a compound of the formulae: wherein the variables are as defined herein.

Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R, R, Rand Rare each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained Calkyl, Caminoalkyl or Coxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that Rand Rare not both hydrogen; Ris selected from the group consisting of a carbonyl, a substituted or unsubstituted Calkyl, a substituted or unsubstituted &#x2014;Calkyl-C(O), a substituted or unsubstituted &#x2014;C(O)&#x2014;Calkyl, and a substituted or unsubstituted &#x2014;C(O)C(O)Calkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3-12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.

Compounds that may be used to inhibit histone deacetylase having the formulaZ-Q-L-M or Z-L-Mwherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0-10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.

Compounds that may be used to inhibit histone deacetylase having the formulaZ-Q-L-M or Z-L-Mwherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0&#x2013;10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.

Histone deacetylase inhibitors and uses thereof are provided that have the general formula 

Novel taxoids are provided having enhanced water solubility and/or improved pharmacological properties as compared to paclitaxel. The subject taxoids comprise a functional group attached to a paclitaxel at the C-2' and/or C-7 position by a linking group. Functional groups present in the subject taxoids may be hydrophilic chains, groups capable of in vivo conversion to hydrophilic chains, targeting moieties capable of specifically binding with cellular receptors and water soluble polymers of at least 5 kD. The subject taxoids find use in the treatment of hosts suffering from a cellular proliferative disease.

Taxoids

Substituted phenylthiohydantoins are provided for use in detecting the presence of tumor cells having androgenic receptors and providing for cytostatic and cytotoxic activity toward such cells. The subject compounds provide for vehicles for specific targeting to the androgenic receptor containing cells of cytostatic and/or cytotoxic agents, heavy or light radioactive or radioopaque atoms, and the like for detection and treatment of cancer cells involving androgenic receptors or blocking androgenic receptors.

Growing community of inventors

San Diego, CA, United States of America

Jerome C Bressi