Berlex Laboratories, Inc.

Schering Aktiengesellschaft

Exelixis, Inc.

Exelixis Patent Company LLC

Ralexar Therapeutics, Inc.

Akarna Therapeutics, Ltd.

Bristol-myers Squibb Compnay

Escalier Biosciences B.v.

Zomagen Biosciences Ltd

Other

Daiichi Sankyo Company, Limited

Bayer Schering Pharma Ag

X-ceptor Therapeutics, Inc.

Schering Aktiengessellschaft

Sankyo Company, Limited

Raju Mohan

Michael M Morrissey

Shendong Yuan

Richard Martin

Brad Owen Buckman

John M Nuss

Tie-Lin Wang

Brenton Todd Flatt

Jason Harris

Wei Xu

Brett Bradley Busch

Imadul Islam

Xiao-Hui Gu

Judi Bryant

Michael Charles Nyman

Edwin J Schweiger

William C Stevens, Jr

Guo Ping Wei

Benjamin Pratt

Yinong Xie

Howard P Ng

Monica J Kochanny

Venkataiah Bollu

Alan Thomas Johnson

Shao Po Lu

Jason H Wu

Kenneth Jay Shaw

Ellen K Kick

Brant Clayton Boren

Christopher D Bayne

Weiya Yun

Shao-Po Lu

Brett Murphy

Gary Bruce Phillips

Matthew A Williams

David D Davey

Kazumasa Aoki

Yong Wang

Timothy Patrick Forsyth

John T Martin

Damian O Arnaiz

Lynne Canne Bannen

Christoph-Stephan Hilger

Nicholas Ronald Wurtz

Larry Wayne Mann

Morrison B Mac

Jeff Z Chen

Grace Mann

Richard Horuk

Jackaline Dalgard Julien

Joseph E Hesselgesser

Lisa Esther Dalrymple

Karen B May

Haixia Wang

Hiroyuki Tsuruoka

Brian D Griedel

Yuo-Ling Chou

Nadia Haq

Meriah Neissel Valente

Mandar Shrikrishna Bodas

Harald Dinter

Tsuyoshi Homma

Bernd Johannsen

Peter Maeding

Andrew I Chitty

Sarah Hudson

Christopher West

Kumar Emayan

Joerg Steinbach

Meredith Halks-Miller

William C Stevens

Paul W Erhardt

Noriyuki Hayashi

Keiji Saito

Vasu Jammalamadaka

Ping Huang

Ronald Griffith

Peter Ordentlich

John W Lampe

Sharanabasappa Patil

Claudia Averbuj

Satoru Kaneko

Yusuke Asoh

Prasanna Savanor Maddu Rao

Jackline Eve Dalgard

Haiying Zhang

Jeff Chen

Jeevanprakash Shetty

Alla Venu

Kozo Oda

Robert Guo-Ping Wei

Ron H Bihovsky

Xiao Hui Gu

Tie Lin Wang

Masatoshi Honzumi

William Stevens

Alan T Johnson

Described herein are N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl) carbamoyl)-4,5,6,7-tetrahydrobenzofuran-2-sulfonamide derivatives and related compounds of formula (I) wherein R1 is formulae (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX) and R2 is formulae (X) or (XI) as NLRP3 (pyrin domain-containing protein 3) modulators for the treatment of e.g. metabolic diseases (e.g. type 2 diabetes or obesity), liver diseases (e.g. NAFLD or cirrhosis), lung diseases (e.g. asthma or CORD), central nervous system diseases (e.g. Alzheimer's disease or multiple sclerosis), inflammatory or autoimmune diseases (e.g. rheumatoid arthritis or psoriasis), cardiovascular diseases (e.g. atherosclerosis or stroke). The present description discloses the synthesis and characterization of exemplary compounds as well as pharmacological data thereof. An exemplary compound is e.g. N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl) carbamoyl)-4-hydroxy-4-methyl-4,5,6,7-tetrahydrobenzofuran-2-sulfonamide (Example 1; compound (5)).

N-((1,2,3,5,6,7-hexahydro-S-indacen-4-yl)carbamoyl)-4, 5, 6, 7-tetrahydrobenzofuran-2-sulfonamide derivatives and related compounds as NLPR3 modulators for the treatment of multiple sclerosis (MS)

Described herein are NLRP3 modulators of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, and methods of utilizing said NLRP3 modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing said NLRP3 modulators.

NLRP3 modulators

Described herein are TYK2 pseudokinase ligands and methods of utilizing TYK2 pseudokinase ligands in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

TYK2 pseudokinase ligands

Described herein are TYK2 pseudokinase ligands of Formula (I'), methods of utilizing these TYK2 pseudokinase ligands in the treatment of diseases, disorders or conditions, and pharmaceutical compositions containing such compounds: wherein X, Y, L, R, R, R, R, R, R, and Rare defined in the specification.

Substituted pyrazolo[1,5-a]pyrimidines as TYK2 pseudokinase ligands

Described herein are NLRP3 modulators and methods of utilizing NLRP3 modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds. 

Described herein are Janus kinase (JAK) inhibitors of the Formula (I'): 

Substituted pyrrolo[2,3-d]pyrimidines as JAK inhibitors

Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing ROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Spirocyclic ROR-gamma modulators

Bicyclic ROR&#x3b3; modulators

Described herein are Janus kinase (JAK) inhibitors of Formula (I'): Also described herein are methods of utilizing JAK inhibitors of Formula (I&#x2032;) in the treatment of diseases, disorders or conditions and pharmaceutical compositions containing such compounds.

JAK inhibitors

Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of LXR-associated diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Liver X receptor (LXR) modulators

Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators of Formula (I) and pharmaceutical compositions thereof, and methods of utilizing these ROR&#x3b3; modulators in the treatment of dermal diseases, disorders or conditions:  Amendment to the abstract of disclosure showing mark-up: Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators of Formula (I) and pharmaceutical compositions thereof, and methods of utilizing these ROR&#x3b3; modulators in the treatment of dermal diseases, disorders or conditions: 

Substituted piperazines as ROR-gamma modulators

Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.

Fused bicyclic compounds for the treatment of disease

Described herein are heterocyclic compounds, compositions, and methods for their use for the treatment of disease.

Heterocyclic compounds for the treatment of disease

Growing community of inventors

Encinitas, CA, United States of America

Raju Mohan