Novartis Ag

Yangtze River Pharmaceutical Group Co., Ltd.

Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

Jiangsu Hengrui Medicine Company Ltd.

Shanghai Hengrui Pharmaceutical Co., Ltd.

Neurogen Corporation

Novartis Vaccines & Diagnostics, Gmbh

Jiangsu Hansoh Pharmaceutical Co., Ltd.

Jiong Lan

Fusheng Zhou

Matthew T Burger

Hengyuan Lang

Gisele A Nishiguchi

Yunfeng Fang

Qing Dong

Mika Lindvall

Yunzhou Jin

Jing Xie

Edcon Chang

Wooseok Han

Jinzhu Zhao

Qiang Lv

Olga M Fryszman

Xing Liu

James Clifford Sutton

Yang Liu

Xiang Chen

Dong Huang

Yi Hu

Shuchun Guo

Xiangyu He

Bonian Liu

Xiaotao Li

Kai Zhang

Hong Yang

Piaoyang Sun

Weibo Wang

Martin Sendzik

Savithri Ramurthy

Keith Bruce Pfister

Allan S Wagman

Simon C Ng

Xuejun Zhang

Marion Wiesmann

Jianbiao Peng

Qi Yang He

Chong Wen

Yaoping Zhu

Elizabeth J Mieuli

Anu Sharma

Victoria Sung

Wan He

Michelle Tetalman

Liana M Klivansky

William Lenahan

Susan Kaufman

Ping Bu

Changjiang Qiao

Shuhui Chen

Yu Wang

Haiying He

Yuan Chen

Cynthia Shafer

Christopher McBride

John M Peterson

Qiyue Hu

Yang Gao

Guoqing Cao

Nicholas M Valiante

Linghong Xie

Annette Olga Walter

Hui Xu

Jianqiang Wang

Ping Ge

Zhiyuan Zhang

Tatiana Zavorotinskaya

Songliang Wu

Pablo Dominguez Garcia

Wallace C Pringle

Yuhe Wang

Yingtao Liu

Gordana Babic Atallah

Kay Huh

Yufeng Li

Wei Peng

Fangfang Jin

Lei Chen

Taotao Jiang

Biao Ma

Feng Xu

Joseph W Ochterski

Sida Shen

Jing Lei

Chunyan Gu

Chunzhou Han

Cornelia Bellamacina

Pengfei Cheng

Leitao Zhang

Ming Weng

Xia Shi

William Antonios-McCrea, Jr

Daofei Li

Lixiao Wang

Zhihua Fang

Zonglei Fei

Liang Zhang

The present invention relates to a 1,2-dihydropyrrol[3,4-c]pyridin/pyrimidin-3-one derivative substituted by N-(3-aminophenyl)acrylamide and a preparation method and pharmaceutical use thereof. In particular, the present invention relates to a compound of formula (II) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof and a preparation method and application of the same. The definition of each substituent in the formula is described in detail in the specification and claims. 

Aniline-substituted 1,2-dihydropyrrol[3,4-C]pyridin/pyrimidin-3-one derivative and use thereof

The present disclosure relates to 4,6,7-trisubstituted 1,2-dihydropyrrolo[3,4-c]pyridin/pyrimidin-3-one derivatives, and their preparations and medicinal use. Specifically, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof, wherein the definition of each group is as described in the specification and claims. 

4,6,7-trisubstituted 1,2-dihydropyrrolo[3,4-c]pyridin/pyrimidin-3-one derivatives and uses thereof

Provided are 4,5,6-tri-substituted indazoles derivatives, a preparation method therefor, and a use thereof in medicines. Specifically, provided are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates, or prodrugs thereof, a preparation method therefor, and a use thereof. 

4,5,6-trisubstituted indazole derivatives, and preparation method and pharmaceutical use thereof

The present invention discloses an N-sulfonyl benzamide derivative with a heterocyclic substituent, and a preparation method therefor and a pharmaceutical application thereof. More specifically, the invention discloses a compound represented by formula (II) or a pharmaceutically acceptable salt, stereoisomer, solvent compound, or prodrug thereof, and a preparation method therefor and an application thereof. Refer to the specification for definitions of each group in the formula. 

N-sulfonyl benzamides as voltage-gated sodium channel inhibitors

The present invention relates to a sulfuryl-substituted benzoheterocyclic derivative, a preparation method and medical use thereof. Particularly, disclosed is a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, and a preparation method and application thereof. The definition of each group in the formula can be found in the specification and the claims. 

Sulfuryl-substituted benzoheterocyclic derivative, preparation method and medical use thereof

It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain. 

Benzobicycloalkane derivatives, their preparation and pharmaceutical use thereof

Provided is an EGFR inhibitor and a pharmaceutically acceptable salt and a polymorph thereof, and a use thereof. In particular, provided is a polymorph, a pharmaceutically acceptable salt or a prodrug of N-(2-(4-(dimethylamino)piperid-1-yl)-5-(5-fluoro-4-(1-methyl-1H-pyrazol-4-yl) pyrimidin-2-ylamino)-4-methoxy phenyl) acrylamide. In addition, also provided is a pharmaceutical composition containing the inhibitor and a use thereof.

EGFR inhibitor and pharmaceutically acceptable salt and polymorph thereof, and use thereof

The present invention provides a class of 2,4-substituted phenylene-1,5-diamine derivatives, having an inhibiting effect on EGFR tyrosine kinases, and pharmaceutically acceptable salt, stereoisomer, solvate or prodrug of said derivatives. See the description for the definition of each group in the formula. In addition, the present invention also discloses pharmaceutical compositions, pharmaceutically acceptable compositions and applications thereof.

2,4-disubstituted phenylene-1,5-diamine derivatives and applications thereof, and pharmaceutical compositions and pharmaceutically acceptable compositions prepared therefrom

A pyrrole six-membered heteroaryl ring derivative, and the medicinal uses thereof are described. Specifically, the pyrrole six-membered heteroaryl ring derivative is a compound of formula (I), wherein the variable groups are as described in the specification. 

Pyrrole heteroaryl ring derivative and method of use thereof

The present invention discloses a series of piperidine derivatives as orexin receptor antagonists and compositions thereof, and relates to the application thereof in preparing medications for the treatment of insomnia, chronic obstructive pulmonary disease, obstructive sleep apnea, hypersomnia, anxiety, obsessive-compulsive disorder, panic attack, nicotine addiction, or binge eating disorder.

Piperidine derivatives as orexin receptor antagonist

Azabicyclo derivatives, a preparation process, and medical use thereof are provided. In particular, azabicyclo derivatives of formula (I), pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs thereof are described. The azabicyclo derivatives of formula (I) are useful as Epidermal Growth Factor Receptor (EGFR) inhibitors. The definitions of the variable R groups in the azabicyclo derivatives of formula (I) are described in the specification. 

Azabicyclo derivatives, process for preparation thereof and medical use thereof

The present invention relates to a 2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, a preparation method and a medicinal use thereof. In particular, the present invention discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. For the definition of each group in formula (I), see the description tbr details. 

2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, preparation method and medicinal use thereof

The present invention relates to 2,3,4,6-tetra-substituted benzene-1,5-diamine derivatives, a preparation method therefor and a medicinal use thereof. Specifically, disclosed are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, preparation method therefor and application thereof. Definition of each group in the formula can be found in the specification for details. 

2,3,4,6-tetra-substituted benzene-1,5-diamine derivatives, preparation method therefor and medicinal use thereof

Cycloalkyl acid derivatives, a preparation method thereof, and a pharmaceutical application thereof are described. In particular, a cycloalkyl acid derivative represented by general formula (I) and a medical salt thereof, a preparation method thereof, and an application of the cycloalkyl acid derivative and the medical salt thereof as URAT1 inhibitors, and particularly as therapeutic agents for diseases related to an abnormal uric acid level are described, wherein definitions of substituent groups in general formula (I) are the same as the definitions in the specification. 

Cycloalkyl acid derivative, preparation method thereof, and pharmaceutical application thereof

The present invention relates to a pyrrole six-membered heteroaryl ring derivative, the preparation method therefor, and the medicinal uses thereof. Specifically, the present invention relates to a new pyrrole six-membered heteroaryl ring derivative as represented by formula (I), the preparation method therefor, a medicinal composition comprising the derivative, and a therapeutic method using same, and, in particular, the uses as a JAK inhibitor and an immunosuppressor. Substituents in formula (I) have the same definitions as in the description. 

Pyrrole six-membered heteroaryl ring derivative, preparation method thereof, and medicinal uses thereof

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Moraga, CA, United States of America

Jiong Lan