Exelixis, Inc.

Exelixis Patent Company LLC

Luoxin Pharmaceutical (Shanghai) Co., Ltd.

Novartis Ag

Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.

X-Ceptor Therapeutics, Inc.

University of Kentucky Research Foundation

Daiichi Sankyo Company, Limited

Medshine Discovery Inc.

Tie-Lin Wang

Richard Martin

Brenton Todd Flatt

Raju Mohan

Xiao-Hui Gu

Brett Bradley Busch

Michael Charles Nyman

Edwin J Schweiger

Jiaqiang Dong

Jason H Wu

Shuhui Chen

Charles Z Ding

Lihong Hu

William C Stevens, Jr

Jianyu Lu

Yinong Xie

Huijun He

Xuechun Zhang

Mark G Bock

Matthew A Williams

John M Nuss

Yong Wang

Kazumasa Aoki

Timothy Patrick Forsyth

Venkataiah Bollu

Lynne Canne Bannen

Piotr Henryk Karpinski

Dario Braga

Yves Auberson

Thomas Josef Troxler

Larry Wayne Mann

Jeff Z Chen

Morrison B Mac

Grace Mann

Stephanie Kay Dodd

Brant Clayton Boren

Ronald Griffith

Hiroyuki Tsuruoka

Lisa Esther Dalrymple

Stefano Luca Giaffreda

Xiaoyang Wang

Jeffrey Dean Kahl

Shao Po Lu

Tsuyoshi Homma

Brett Murphy

Marco Curzi

William C Stevens

Jian Li

Wei Xu

Michael M Morrissey

Yves Pommier

Noriyuki Hayashi

Guoping Hu

Kevin X Chen

Keiji Saito

Vasu Jammalamadaka

Ping Huang

Weidong Li

Xu Zeng

Benjamin Pratt

Thomas G Burke

Jackaline Dalgard Julien

Nadia Haq

Xiaobing Yan

Shenyi Shi

Yusuke Asoh

Jackline Eve Dalgard

Shao-Po Lu

Sarah Hudson

Haiyang Jiang

Jeff Chen

Ashok J Chavan

Ayhan S Demir

Masatoshi Honzumi

Hayang Jiang

Jianglei Huang

Yuekun Nie

Cihangir Tanyeli

Zhijuan Chen

William Stevens

Jeffery Dean Kahl

Disclosed is a novel class of MDM2-p53 inhibitor compounds having an imidaxopyrolone structure, and specifically disclosed are compounds represented by formulas (I-1) and (I-2) and pharmaceutically acceptable salts thereof. 

Substituted pyrrolo[3,4-d]imidazoles as MDM2-p53 inhibitors

Disclosed are a crystal form of an estrogen receptor inhibitor and a preparation method therefor, in particular disclosed are a crystal form A of a compound of formula (I) and a preparation method therefor, and the use of the crystal form in the preparation of a drug for treating breast cancer. 

Crystal form of estrogen receptor inhibitor and preparation method therefor

Disclosed in the present invention is a type of indole substituted piperidine compounds as an estrogen receptor down-regulator. Specifically disclosed are a compound as shown in formula (I), a pharmaceutically acceptable salt, hydrate or prodrug thereof, a preparation method therefor, a pharmaceutical composition thereof, and a use thereof as an estrogen receptor down-regulator in the treatment of estrogen receptor positive breast cancers. 

Indolo substituted piperidine compound as estrogen receptor down-regulator

Disclosed is a new indole compound, in particular, the compound as shown in formula (I), and a preparation method, pharmaceutical composition and use thereof as an estrogen receptor down-regulator in preparing drugs for treating estrogen receptor-positive breast cancer. 

Substituted-indole-compounds as estrogen receptor down-regulators

The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.

Carbamate/urea derivatives

The invention relates to compound of the formula I (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation and to medicaments comprising it for treating diseases connected to the inhibition of H3 receptor. 

Carbamate/urea derivatives containing piperidin and piperazin rings as H3 receptor inhibitors

Methods of using compounds of the invention, such as compounds of Formulae IIa, IIb, IIc, or IId and pharmaceutically acceptable salts thereof are disclosed. The compounds are useful in treating, preventing, inhibiting or ameliorating the symptoms of a disease or disorder that is modulated or otherwise affected by nuclear receptor activity, or in which nuclear receptor activity is implicated.

Imidazole based LXR modulators

The present invention comprises TGR5 agonists of structural formula I, wherein X, R, R, and Rare defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.

Triazole and imidazole derivatives for use as TGR5 agonists in the treatment of diabetes and obesity

The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein Rrepresents a C1-C3 alkyl group; Rrepresents a hydroxy-C1-C4 alkyl group and the like; Rrepresents a halogeno group, a halogeno-C1-C3 alkyl group and the like; Rrepresents a hydrogen atom, a halogeno group and the like, &#x2014;Rrepresents a sulfamoyl group or a C1-C3 alkylsulfonyl group; Rrepresents a hydrogen atom, a halogeno group and the like] or an N-oxide, atropisomer of the foregoing, or pharmaceutically acceptable salt of the foregoing. 

1-phenylpyrrole derivatives

Compounds of the invention, such as compounds of Formulae IIa, IIb, IIc or IId, and pharmaceutically acceptable salts, isomers, and prodrugs thereof, are useful as modulators of the activity of liver X receptors, where R, R, R, Rand G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. 

Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Azepinoindole derivatives as pharmaceutical agents

The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I): wherein Rrepresents a C1-C3 alkyl group; Rrepresents a 2-hydroxy-C4-C6 alkyl group; Rrepresents a halogeno group, a halogeno-C1-C3 alkyl group and the like; Rrepresents a hydrogen atom, a halogeno group and the like; Rrepresents a C1-C3 alkyl group; and Rrepresents a hydrogen atom, a halogeno group and the like] or atropisomers thereof. 

Atropisomers of (hydroxyalkyl) pyrrole derivatives

Compounds, compositions and methods are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder related to the activity of the receptors.

Azepine derivatives as pharmaceutical agents

Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Pyrrole derivatives as pharmaceutical agents

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San Diego, CA, United States of America

Tie-Lin Wang