Janssen Pharmaceutica Nv

Zhejiang Dtrm Biopharma Co. Ltd.

Aventis Pharmaceuticals Inc.

Vitae Pharmaceuticals, Inc.

Aventis Pharmaceuticals Products Inc.

Ortho-mcneil Pharmaceutical Corp.

Wei He

Henry Joseph Breslin

Chaozhong Cai

Robert William Kavash

Steven J Coats

Alfred P Spada

Michael R Myers

Tamara A Miskowski

Alexey Borisovich Dyatkin

David A Claremon

Suresh B Singh

Colin M Tice

Wei Zhao

Yuanjie Ye

Scott L Dax

Li Liu

Zhenrong Xu

Salvacion Cacatian

Martin P Maguire

Mark J Schulz

Janet L Ralbovsky

Joseph Lisko

Linghang Zhuang

Yue-Mei Zhang

Shu-Chen Lin

Mark J Macielag

Peter J Connolly

Philip Michael Pitis

Haiyan Bian

Bart L DeCorte

Bin Benjamin Zhu

Gilles C Bignan

Bart L De Corte

Robert Simpson

Bruce E Maryanoff

Katerina Leftheris

William R Ewing

William Joel Hoekstra

William Alvin Kinney

Christopher J Burns

Timothy Francis Gallagher

Heinz W Pauls

Stephen M Condon

Kent W Neuenschwander

Joseph M Karpinski

Robert D Groneberg

Robert L Morris

Yong Mi Choi-Sledeski

Aiwen Li

Gregory Bernard Poli

Barbara Hanney

Gerard McGeehan

Jean-Francois Sabuco

Michael R Becker

Mark A Bobko

John Ziqi Jiang

Roderick S Davis

Wan F Lau

Mark Schulz

Cai Chaozhong

Robert D Simpson

Mark J Schultz

The present disclosure provides methods of treating lymphoid malignancies such as B cell malignancies using a BTK inhibitor in the described therapeutic regimens.

Methods for treating lymphoid malignancies

Described herein are combination therapies for cancer (such as lymphoid malignancies) and immune diseases (such as autoimmune diseases and inflammatory diseases). The therapies comprise the combined use of inhibitors of BTK, mTOR kinase, and Bcl-2 or their signaling pathways, and immunomodulatory drugs. Also described are pharmaceutical compositions and kits comprising these inhibitors.

Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases

Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.

Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors

The present invention is directed to novel opioid receptor modulators of Formula (I).  The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.

Compounds as opioid receptor modulators

The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.

This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih)1 (Ij), (Ik), (Il). (Im), (In), (Io), (Ip), (Iq), (Ir) and (Is), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11&#x3b2;-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell. 

Cyclic urea inhibitors of 11&#x3b2;-hydroxysteroid dehydrogenase 1

This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11&#x3b2;-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell. 

Inhibitors of 11&#x3b2;-hydroxysteroid dehydrogenase type 1

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R, Y, R, R, and Rare defined herein.

Phenoxy-substituted pyrimidines as opioid receptor modulators

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Audubon, PA, United States of America

Wei He