Cytovia, Inc.

State of Oregon

Euro-celtique S.a.

University of California

Cocensys Inc.

Other

Acea Pharmaceuticals, Inc.

Purdue Neuroscience Company

Warner-lambert Company

Shire Biochem, Inc.

Myrexis, Inc.

University of Oregon

Epicept Corporation

Myriad Pharmaceuticals, Inc.

Sui Xiong Cai

John A Drewe

Eckard Weber

Han-Zhong Zhang

Yan Wang

Nancy C Lan

John F Keana

John F W Keana

Shailaja Kasibhatla

Hong Zhang

Songchun Jiang

Christopher Franklin Bigge

Nilantha Sudath Sirisoma

Anthony P Guzikowski

Jared Kuemmerle

P Sanjeeva Reddy

Zhang-Lin Zhou

William E Kemnitzer

Richard Woodward

David B Fick

Richard Storer

Ben Y Tseng

Azra Pervin

Wu Yang

Sunil Kher

Gordon B Mills

Giorgio Attardo

Mark B Anderson

Ravi Upasani

Douglas R Green

Mingdi Yan

Martin N Wybourne

John Guastella

George Field

Kristin P Ollis

Adam Willardsen

Bao Vinh Nguyen

Gian Luca Araldi

Jonathan L Wright

Bao Ngoc Nguyen

Daniel F Nogales

Christopher S Konkoy

Victor I Ilyin

Donald Lamunyon

Po-wai Yuen

Martin Sendzik

Joane Litvak

Rabindra Rej

Katayoun Jessen

Rachel M Slade

Real Denis

Robert J Halter

Yevgeniya Klimova

Jeffrey R Spencer

Henriette Gourdeau

Federico Gaeta

Haiji Xia

Denis Labrecque

Charles Blais

Réal Denis

John Fw Keana

Kazuyuki Suzuki

Soo Hong-Bae

Nancy F Lan

Jong Wu

James M Navratil

Chris Pleiman

Nicole Marion English

Serguei Maliartchouk

Sungchun Jiang

Emma Jane Shelton

David Sperandio

Lifen Xu

Lufeng Guan

William D Kemnitzer

The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Substituted 2-aminoacetamides and the use thereof

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, and in particular to the use of these compounds in treating brain cancer.

Method of treating brain cancer

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-arylamin-or-4-heteroarylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof

The present invention is directed to a substituted 4H-chromene represented by the Formula 1R, substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.

Substituted 4-aryl-chromene as activator of caspases and inducer of apoptosis and as antivascular agent and the use thereof

The invention is directed to substituted-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

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

Disclosed are 3-aryl-6-aryl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles and related compounds thereof, represented by the Formula I: wherein Ar, Ar, and X are defined herein. The present invention 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 may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

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The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.

Substituted 1(2H)-phthalazinones and pharmaceutical compositions thereof

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

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 invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

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-chromene and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, Z and Rare 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.

Disclosed are protease inhibitors for coronaviruses and SARS-CoV, or picornaviruses, and the use of these protease inhibitors for preventing, reducing, ameliorating and treating a disease or condition caused by coronaviruses and SARS-CoV, or picornaviruses. Also disclosed are methods of reducing or preventing the spread of coronavirus, or picornaviruses, and preventing or reducing the replication of coronavirus, or picornaviruses, with the compounds of the present invention.

Protease inhibitors for coronaviruses and SARS-CoV and the use thereof

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San Diego, CA, United States of America

Sui Xiong Cai