Schering Corporation

Merck Sharp + Dohme Corp.

Pharmacopeia Inc.

Pharmacopeia Drug Discovery, Inc.

Western University of Health Sciences

Schering-plough Corporation

Schering Coporation

Honeywell International Inc.

Ying Huang

Andrew William Stamford

Ulrich Iserloh

Guoqing Li

Jared N Cumming

Yusheng Wu

Corey Strickland

Tao Guo

Zhaoning Zhu

Brian Alexander McKittrick

Suresh D Babu

Johannes H Voigt

Kurt William Saionz

William J Greenlee

Anandan Palani

Robert G Aslanian

Zhong-Yue Sun

Jianping Pan

Robert D Mazzola, Jr

Xiao Chen

Thuy X H Le

Xianhai Huang

Elizabeth M Smith

Douglas Walsh Hobbs

Lingyan Wang

Ashwin Umesh Rao

Yuefei Shao

Xiaoxiang Liu

Gang Qian

Johannes H Voight

Samuel Chackalamannil

Dong Xiao

Yan Xia

John P Caldwell

Yuanzan C Ye

Rachael Catherine Hunter

Michelle Lee Morris

Jun Qin

Huizhong Gu

Dawit Tadesse

Gaifa Lai

Jeffrey A Misiaszek

Jingqi Duo

Chuanxing Qu

Neng-Yang Shih

Pauline C Ting

Ning Shao

Thuy X E Le

Joseph P Vacca

F George Njoroge

Frank W Bennett

Qun Dang

Stuart W McCombie

Stephane L Bogen

Kevin D McCormick

Joseph Michael Kelly

David Brian Olsen

Craig D Boyle

Ian W Davies

Dmitri A Pissarnitski

Vinay M Girijavallabhan

Latha G Nair

Vishal Verma

Angela Dawn Kerekes

Jianhua Cao

Sylvia Joanna Degrado

Ashok Arasappan

Jason D Brubaker

David J Blythin

Michael Berlin

Hongjun Zhang

Gerald Wayne Shipps, Jr

Phieng Siliphaivanh

Joshua Close

Ho-Jane Shue

Eric J Gilbert

Purakkattle J Biju

Jing Su

Rongze Kuang

Wing C Tom

Peter Orth

Li Xiao

Joon Jung

John W Butcher

Robert Jason Herr

Junying Zheng

Wei Zhou

Chen Chen

Haiqun Tang

Mwangi W Mutahi

Xiaohua Huang

Michelle Martinez

Robert Mazzola

John H Schwerdt

Rachel Nicola MacCoss

Li Dong

Scott Peterson

Youhao Dong

Lana Michele Rossiter

The invention provides compositions comprising wilforlide A for overcoming drug resistance in cancer therapy, particularly in the treatment of cancers which have exhibited resistance to treatment by chemotherapeutic drugs. Methods and compositions for treating a cancer are disclosed. The method administers to a patient in need thereof a combination of wilforlide A and a chemotherapeutic drug. Wilforlide A and chemotherapeutic drug are administered in a combined amount effective to treat the cancer. The cancer being treated is at least in part resistant to treatment by the chemotherapeutic drug alone.

Use of wilforlide A for overcoming chemotherapy resistance

The invention provides extracts and compositions derived fromfor overcoming drug resistance in cancer therapy. This invention relates to organic solvent extracts ofand their use in cancer treatment, particularly in the treatment of cancers which have exhibited resistance to treatment by chemotherapeutic drugs. Methods of treating a cancer are disclosed. The method administers to a patient in need thereof a combination of (a) an organic solvent extract ofand (b) a chemotherapeutic drug. The organic solvent extract of(a) and chemotherapeutic drug (b) are administered in a combined amount effective to treat the cancer. The cancer being treated is at least in part resistant to treatment by the chemotherapeutic drug (b) alone. Also disclosed are chemotherapeutic compositions comprising a combination of (a) an organic solvent extract ofand (b) a chemotherapeutic drug, wherein (a) and (b) are administered in a combined amount effective to treat the cancer; and a pharmaceutically acceptable carrier.

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The invention provides pharmaceutical compositions containing a vehicle for the targeted delivery of therapeutic and diagnostic agents for the treatment of hyperproliferative diseases. The targeting component of the vehicle is a cystine molecule that is coupled to the cargo component, which can be either a therapeutic or diagnostic agent or to a nanoparticle composition that contains the therapeutic agent or diagnostic. The invention also provides methods of treating hyperproliferative disorders by targeting hyperproliferative disease cells for the targeted delivery of a therapeutic or diagnostic agent.

Targeted liposomes in cancer therapy

The present invention relates to 2'-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R, Rand Rare as defined herein. The present invention also relates to compositions comprising at least one 2&#x2032;-Azido Substituted Nucleoside Derivative, and methods of using the 2&#x2032;-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. 

2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

The present invention relates to 2'-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R, Rand Rare as defined herein. The present invention also relates to compositions comprising at least one 2&#x2032;-Cyano Substituted Nucleoside Derivative, and methods of using the 2&#x2032;-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient. 

2'-cyano substituted nucleoside derivatives and methods of use thereof useful for the treatment of viral diseases

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein  and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a &#x3b2;-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

Cyclic amide BACE-1 inhibitors having a benzamide substituent

The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein ('FABP') inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

Substituted quinoxalines as inhibitors of fatty acid binding protein

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic magonist or mantagonist.

Heterocyclic aspartyl protease inhibitors

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein

Substituted isoindolines as aspartyl protease inhibitors

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula I are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic magonist or mantagonist.

Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R, R, R, R, Rand Rare as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic magonist or mantagonist.

Aspartyl protease inhibitors

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein Ris  R is &#x2014;C(O)&#x2014;N(R)(R) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a &#x3b2;-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

Cyclic amine BACE-1 inhibitors having a benzamide substituent

The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R, R, R, R, R, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTHfunction.

Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of &#x3b2;-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.

Substituted amide beta secretase inhibitors

Growing community of inventors

East Brunswick, NJ, United States of America

Ying Huang