Eli Lilly and Company

Jiangsu Hengrui Medicine Company Ltd.

Bristol-myers Squibb Compnay

Shanghai Hengrui Pharmaceutical Co., Ltd.

Wyeth

Karo Bio Ab

Impact Therapeutics, Inc.

Jiangsu Hansoh Pharmaceutical Co., Ltd.

Eternity Bioscience Inc.

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Minsheng Zhang

Daniel Jon Sall

Gerald Floyd Smith

Ho-Shen Lin

Richard Waltz Harper

Kumiko Takeuchi

Jefferson Ray McCowan

Matthew Joseph Fisher

Nickolay Y Chirgadze

Alan David Palkowitz

Dong Liu

Denis E Ryono

Todd J Friends

Michael Robert Wiley

Michael Enrico Richett

Jolie Anne Bastian

Jon J Hangeland

Robert J Foglesong

Johan Malm

Michael Lyle Denney

Mary George Johnson

Michael P Lynch

Yolanda V Caringal

Boyd Lynn Harrison

Derek Cecil Cole

Anthony Frank Kreft

Valentine Joseph Klimkowski

Scott Christian Mayer

Jennifer Marie Tinsley

Yinfa Yan

George Diamantidis

Lynn Resnick

Todd Jonathan Kohn

Molly Hoke

Rocco John Galante

Yi-Lin Li

Tingzhong Wang

Ye Liu

Feng He

Pratik Devasthale

Qiyue Hu

Arthur M P Doweyko

Tamara Dejneka

Rumin Zhang

Kan He

Shawn Christopher Miller

Fengqi Zhang

Konrad Koehler

Neeraj Garg

Mingxun He

Chris Litten

Biao Lu

Andrei Sanin

Xiaodong Shen

Ana Maria Garcia Collazo

Suxing Liu

William R Ewing

Nicholas J Bach

Weikang Tao

Natesan Murugesan

Gregory S Bisacchi

Guixue Yu

Baihua Hu

Zhengxiang Gu

Jeffrey Thomas Mullaney

Lianshan Zhang

Asa Hedfors

Charlotta Mellin

Jolie Ann Bastian

The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (RORγ) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of RORγ-mediated diseases or disorders.

Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (RORγ) and pharmaceutical use thereof

The present invention relates to benzimidazole derivatives of formula (I) as inhibitors of retinoid-related orphan receptor gamma (ROR&#x3b3;) protein, pharmaceutical compositions containing the compounds, preparation methods thereof, and the use of the compounds as therapeutic agents for the treatment of ROR&#x3b3;-mediated diseases or disorders. 

Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (ROR&#x3b3;) and pharmaceutical uses thereof

A benzofuran derivative, a preparation method thereof and a use thereof in medicine are described. In particular, a benzofuran derivative as shown by general formula (I), the preparation method thereof, a pharmaceutical composition containing the derivative, and uses thereof as an EZH2 inhibitor and in the prevention and/or treatment of diseases such as tumours and cancers, etc., and in particular, uses thereof in the prevention and/or treatment of non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, follicular lymphoma and synovial sarcoma, are described. 

Benzofuran derivative, preparation method thereof and use thereof in medicine

The present invention relates to a benzofuran derivative, a preparation method thereof and a use thereof in medicine. In particular, the present invention relates to the benzofuran derivative as shown by general formula (I), the preparation method thereof, a pharmaceutical composition containing the derivative, and uses thereof as an EZH2 inhibitor and in the prevention and/or treatment of diseases such as tumours and cancers, etc., and in particular, uses thereof in the prevention and/or treatment of non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, follicular lymphoma and synovial sarcoma, wherein the definitions of the substituents in the general formula (I) are the same as those defined in the description. 

The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis. 

Aminopyridazinone compounds as protein kinase inhibitors

Substituted ethynyl heterobicyclic compounds as tyrosine kinase inhibitors

The present disclosure provides novel furanone compounds, or pharmaceutically acceptable salts, solvates or prodrugs thereof, as Raf kinase, especially BRAF kinase, inhibitors, which are useful therapeutic agents for treatment of Raf kinase related diseases or disorders, such as melanomas, cancers, and leukemia. The disclosure also provides methods and processes for preparing these novel furanone compounds, pharmaceutical compositions containing these furanone compounds, and methods of treatment using these furanone compounds.

Furanone compounds as kinase inhibitors

The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP. 

Quinazolinediones and their use

The present invention relates to compounds represented by formula (I), which can modulate the activity of protein kinases. The invention also relates to a composition containing a compound of formula (I), and a method for synthesizing and using such compound for preventing or treating ALK or cMet mediated disorders or conditions. 

Phosphorus containing compounds as protein kinase inhibitors

A method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a Tregulated gene, wherein a compound as described in the general formula I below is administered in a therapeutically effective amount: 

Thyroid receptor ligands

Compounds of Formula (I), are provided where T is CHO, COR, or C(OH)RR; Rand Rare hydrogen, optionally substituted lower alkyl, CF, optionally substituted alkenyl, or optionally substituted alkynyl; Ris hydrogen or optionally substituted lower alkyl; Ris (CF)alkyl, (CF)(substitutedalkyl), (CF)alkylphenyl, (CF)alkyl(substitutedphenyl), or (F)cycloalkyl; n=1-3; Ris hydrogen, halogen, CF, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CRor N where at least one of W, Y or Z are C; Ris hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO, or NR; Ris hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and Ris lower alkyl, CF, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof

Thyroid receptor ligands are provided which have the general formula I wherein:   In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a Tregulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

Compounds of Formula (I), are provided where T is CHO, COR, or C(OH)RR; Rand Rare hydrogen, optionally substituted lower alkyl, CF, optionally substituted alkenyl, or optionally substituted alkynyl; Ris hydrogen or optionally substituted lower alkyl; Ris (CF)alkyl, (CF)(substituted alkyl), (CF)alkylphenyl, (CF)alkyl(substituted phenyl), or (F)cycloalkyl; n=1-3; Ris hydrogen, halogen, CF, diene fused to Y when Y&#x2550;C, or substituted diene fused to Y when Y&#x2550;C; W, Y and Z are C, CRor N where at least one of W, Y or Z are C; Ris hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO, or NR; Ris hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and Ris lower alkyl, CF, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

Compounds of Formula (I), are provided where T is CHO, CON, or C(OH)RR; Rand Rare hydrogen, optionally substituted lower alkyl, CF, optionally substituted alkenyl, or optionally substituted alkynyl; Ris hydrogen or optionally substituted lower alkyl; Ris (CF)alkyl, (CF)(substitutedalkyl), (CF)alkylphenyl, (CF)alkyl(substitutedphenyl), or (F)cycloalkyl; n=1-3; Ris hydrogen, halogen, CF, diene fused to Y when Y&#x2550;C, or substituted diene fused to Y when Y&#x2550;C; W, Y and Z are C, CRor N where at least one of W, Y or Z are C; Ris hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO, or NR; Ris hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and Ris lower alkyl, CF, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.

Growing community of inventors

Warren, NJ, United States of America

Minsheng Zhang