Cgi Pharmaceuticals, Inc.

Neurogen Corporation

Other

Gilead Connecticut, Inc.

Cellular Genomics, Inc.

James William Darrow

Scott A Mitchell

Kevin S Currie

Robert W DeSimone

Douglas A Pippin

George D Maynard

Raymond F Horvath

Jennifer N Tran

Charles A Blum

David Andrew Griffith

Peter A Blomgren

Jeffrey E Kropf

Philip Albert Carpino

Stephane De Lombaert

St&eacute;phane De Lombaert

Mark Giangiordano

Alan J Hutchison

Xiaozhang Zheng

Jianjun Xu

Rajagopal Bakthavatchalam

Seung H Lee

Aaron C Schmitt

David R Brittelli

Douglas Gregory Stafford

Marlys Hammond

Richard Louis Elliott

Harry Brielmann

Douglas A I Pippin

Xiaobing Qian

Mark Velleca

Dapeng Qian

M Diana Danca

Tony Lee

Steven L Gallion

At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.

Certain substituted amides, method of making, and method of use thereof

At least one chemical entity chosen from compounds of Formula 2 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.

Compounds of Formula I-a and all pharmaceutically-acceptable forms thereof, are described herein. The variables R, R, R, Z, Q, and A shown in Formula I-a are defined herein. Pharmaceutical compositions containing one or more compounds of Formula I-a, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Methods of treating patients suffering from certain diseases responsive to inhibition of tyrosine kinase activity are also given. In certain embodiments the diseases are responsive to inhibition of Btk activity and/or B-cell proliferation. Such methods comprise administering to such patients an amount of a compound of Formula I-a effective to reduce signs or symptoms of the disease. These diseases include cancer, an autoimmune and/or inflammatory disease, or an acute inflammatory reaction. Thus methods of treatment include administering a sufficient amount of a compound or salt as provided herein to decrease the symptoms or slow the progression of these diseases.

Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds

A novel composition comprises a compound of Formula 1 the pharmaceutically acceptable salts, hydrates, solvates, crystal forms, diastereomers, prodrugs, or mixtures thereof. The composition is of particular utility in the treatment of kinase-implicated disorders.

6-aryl-imidazo[1,2-a] pyrazin-8-ylamines, method of making, and method of use thereof

Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a pharmaceutically acceptable salt of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents, are also provided herein.  Methods of treating patients suffering from certain diseases and disorders responsive to EphB4 kinase modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder are disclosed. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with a compound of Formula I under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.

Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity

This invention pertains to compounds of Formula I: and the pharmaceutically-acceptable forms thereof. The variables R, R, R, Z, Z, W, and X shown in Formula I are defined herein. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to Hsp90 complex modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including chronic myeloid leukemia, melanoma, breast, ovarian, brain, thyroid, colorectal, prostate, and bladder cancer, heart disease, stroke, autoimmune/inflammatory diseases, and neurodegenerative diseases. Thus methods of treatment include administering a sufficient amount of a compound of Formula I or form thereof to decrease the symptoms or slow the progression of these diseases or disorders. The invention also encompasses methods of treating non-human patients, including livestock and domesticated companion animals, suffering from a disease or disorder responsive to Hsp90 complex modulation. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agent. The invention also includes a method for determining the presence of certain kinases or Hsp90 complex in a sample, comprising contacting the sample with a compound of Formula I or form thereof, and detecting Hsp9O complex activity in the sample.

Certain 6, 8-(heteroaryl or aryl) disubstituted imidazo[1,2-a]pyrazines as modulators of Hsp90 complex activity

A composition comprises a compound of Formula 1:a pharmaceutically acceptable salt, hydrate, solvate, crystal form, diastereomer, prodrug, or mixture thereof, wherein W is a nitrogen-substituted 5- or 6-membered monocyclic ring. The compounds are of utility as modulators of kinase activity.

Certain amino-substituted monocycles as kinase modulators

A novel composition comprises a compound of Formula 1the pharmaceutically acceptable salts, hydrates, solvates, crystal forms, diastereomers, prodrugs, or mixtures thereof. The composition is of particular utility in the treatment of kinase-implicated disorders.

Imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof

Substituted spiro&lsqb;isobenzofuran-1,4&prime;-piperidin&rsqb;-3-ones and 3H-spiroisobenzofuran-1,4&prime;-piperidines capable of modulating NPY5 receptor activity are provided. Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.

Spiro&lsqb;isobenzofuran-1,4&prime;-piperidin&rsqb;-3-ones and 3H-spiroisobenzofuran-1,4&prime;-piperidines

Amino substituted pyrazolo&lsqb;1,5,-a&rsqb;-1,5-pyrimidines and pyrazolo&lsqb;1,5-a&rsqb;-1,3,5-triazines

Aminoalkyl substituted 5,6,7,8-Tetrahydro-9H-Pyridino &lsqb;2,3-B&rsqb;indole derivatives

Certain alkylene diamine-substituted pyrazlo (1,5-a)-1,5-pyrimidines and pyrazolo (1,5-a) 1,3,5-triazines

Aminoalkyl substituted 9H-phridino&lsqb;2,3-b&rsqb; indole and 9H-pyrimidino&lsqb;4,5-b&rsqb; indole derivatives

Aminoalkyl substituted 5,6,7,8-tetrahydro-9H-pyridino &lsqb;2, 3-B&rsqb; indole and 5,6,7,8-tetrahydro-9H-pyrimidino &lsqb;4, 5-B&rsqb; indole derivatives: CRF1 specific ligands

Substituted 9H-pyridino &lsqb;2,3-B&rsqb;indole and 9H-pyrimidino &lsqb;4,5-B&rsqb;indole derivatives: selective neuropeptide Y receptor ligands

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Wallingford, CT, United States of America

James William Darrow