Exelixis, Inc.

Cellerant Therapeutics, Inc.

Ph Pharma Co., Ltd.

Symphony Evolution, Inc.

Exelixis Patent Company LLC

Exelixus, Inc.

Vasu Jammalamadaka

John M Nuss

Lynne Canne Bannen

Wei Xu

Richard George Khoury

Morrison B Mac

Jason Jevious Parks

Yong Wang

James William Leahy

Larry Wayne Mann

Diva Sze-Ming Chan

Lisa Esther Dalrymple

Moon Jung Kim

Timothy Patrick Forsyth

Jeff Z Chen

Grace Mann

Tai Phat Huynh

Craig Stacy Takeuchi

Erick Wang Co

Donna Tra Le

Shumeye Mamo

Wie Xu

Jagath Reddy Junutula

Sanjeev Satyal

S David Brown

Amy Lew Tsuhako

Morrisson B Mac

Hoyoung Huh

Michael P Prisbylla

Zhaoyang Wen

Amy Lew

Lynne Canne-Bannen

Rickard George Khoury

Raju Mohan

Matthew A Williams

Richard Martin

Neel Kumar Anand

Tsze Tsang

Tie-Lin Wang

Kenneth D Rice

Joerg Bussenius

Ping Huang

Charles M Blazey

Brett Bradley Busch

Simona Costanzo

Atwood Kim Cheung

Xiao-Hui Gu

Larisa Dubenko

Brant Clayton Boren

Owen Joseph Bowles

Brian Hugh Ridgway

Edwin J Schweiger

Sergey Epshteyn

Gary Lee Lewis

William C Stevens, Jr

Joan C Sangalang

Xian Shi

Mohamed Ibrahim

Steven Charles Defina

Wei Cheng

Yinong Xie

Kimberly Ann Tipton

Rhett Ronald Klein

Shao Po Lu

Robin Tammie Noguchi

Kevin Luke Schnepp

Shao-Po Lu

Jeff Chen

Baili Chen

Maurizio Franzini

Moon Hwan Kim

Larry W Mann

Erick W Co

The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.

Thailanstatin analogs

The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

C-met modulators and methods of use

This disclosure provides novel isoquinolidinobenzodiazepines. These compounds can also be incorporated into antibody-drug conjugates.

Isoquinolidinobenzodiazepines

c-Met modulators and methods of use

The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

C-met modulators and method of use

c-Met modulators and method of use

The present invention relates to compounds of the Formula (I) and (II) wherein R, R, R-R, m, n, X-X, and Qare defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention. 

Kinase modulators and methods of use

The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Tie-2. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.

Tie-2 modulators and methods of use

Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R, R, R, R, J, J, G, G, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. 

LXR and FXR modulators

The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.

Human ADAM-10 inhibitors

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Pleasanton, CA, United States of America

Vasu Jammalamadaka