Cytovia, Inc.

Irm LLC

Novartis Ag

Shire Biochem, Inc.

Myrexis, Inc.

Epicept Corporation

Myriad Pharmaceuticals, Inc.

Songchun Jiang

Sui Xiong Cai

Hong Zhang

Thomas H Marsilje, Iii

Bei Chen

Wenshuo Lu

John A Drewe

Xiaohui He

Pierre-Yves Michellys

Kunyong Yang

Richard Storer

William E Kemnitzer

Pingda Ren

Yun He

Shailaja Kasibhatla

Han-Zhong Zhang

Giorgio Attardo

Robert Epple

Phillip B Alper

Daniel Mutnick

Nilantha Sudath Sirisoma

Gerald Lelais

Christopher Cow

Christian Cho-Hua Lee

Pamela Ann Albaugh

Tao Jiang

Xiaolin Li

Valentina Molteni

Xiaodong Wang

Yun Long

Yi Zhang

Xing Wang

Guobao Zhang

Yongping Xie

Jon Christopher Loren

Juliet Nabakka

Zuosheng Liu

Xiaodong Liu

Badry Bursulaya

Donatella Chianelli

Taebo Sim

Xia Wang

Mark B Anderson

Mihai Azimioara

Shuli You

Wei Pei

Rabindra Rej

Katayoun Jessen

Victor Ivanovich Nikulin

Rachel M Slade

Real Denis

Yevgeniya Klimova

Robert J Halter

Jared Kuemmerle

Ben Y Tseng

Azra Pervin

Thomas Knoepfel

Adam Willardsen

Réal Denis

Matthew McNeill

Jonathan Deane

Thomas H Marsilje

Matthew H McNeill

Peter Syka

Lucas Westcott-Baker

Chris Pleiman

Nicole Marion English

Serguei Maliartchouk

Matthew H Mcneill

Phillip Alper

Iii Thomas H Marsilje

The invention disclosed herein relates to 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridinyl compounds and 4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridinyl compounds of Formula (A), pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of autoimmune diseases. 

Compounds and compositions as inhibitors of endosomal toll-like receptors

The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating EGFR activity, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated EGFR activity.

Compounds and compositions for modulating EGFR Activity

The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or analplastic lymphoma kinase (ALK).

Compounds and compositions as kinase inhibitors

The invention provides novel pyrimidine derivatives of formula I and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK). 

Pyrimidine derivatives as kinase inhibitors

The invention provides novel pyrimidine derivatives of formula (I) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK). 

The invention provides compounds of Formula I: wherein A, L, m, q, Q, R, R, R, Rand Rare defined in the Summary of the Invention. The invention further provides for pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.

Compounds and compositions as modulators of GPR119 activity

The invention provides a novel class of compounds of the Formula I: in which the symbols have the meanings given in the description and claims, to pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of FGFR3 kinase.

[4,5']Bipyrimidinyl-6,4&#x2032;-diamine derivatives as protein kinase inhibitors

Disclosed are 1-arylamino-phthalazines, 4-arylamino-benzo[d][1,2,3]triazines, and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Pharmaceutical compounds as activators of caspases and inducers of apoptosis and the use thereof

The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR&#x3b1;, PDGFR&#x3b2;, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF&#x3b2;, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2&#x3b2;, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.

Compositions and methods for modulating c-kit and PDGFR receptors

The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Derivatives of gambogic acid and analogs as activators of caspases and inducers of apoptosis

Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

4-arylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof

The present invention relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using Apoptosis Inducing Proteins (AIPs) as a target for the discovery of apoptosis activators useful as anticancer agents. The screening methods of the present invention can employ homogenous or heterogeneous binding assays using purified or partially purified AIPs; or whole cell assays using cells with altered levels of one or more AIPs. The invention also contemplates use of gambogic acid or GA-related compounds which bind AIPs and can accordingly be used to raise antibodies useful for drug discovery. Alternatively, labeled GA is used for competitive binding assays for drug discovery. Such assays afford high throughput screening of chemical libraries for apoptosis activators.

Methods of treating diseases responsive to induction of apoptosis and screening assays

The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the Formula (I): wherein R, R-R, A, D, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Substituted 4-aryl-4h-pyrrolo[2,3-h]chromenes and analogs as activators of caspases and inducers of apoptosis and the use thereof

The present invention is directed to substituted 4H-chromenes, 2H-chromenes, chromans and analogs thereof, represented by the general Formula (I) wherein R, A, B, X, Y, Z and dotted lines are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Substituted 4H-chromens, 2H-chromenes, chromans and analogs as activators of caspases and inducers of apoptosis and the use thereof

The present invention is directed to substituted coumarins and quinolines and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Substituted coumarins and quinolines and analogs as activators of caspases and inducers of apoptosis and the use thereof

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San Diego, CA, United States of America

Songchun Jiang