Exelixis, Inc.

Chiron Corporation

Symphony Evolution, Inc.

Escalier Biosciences B.v.

Zomagen Biosciences Ltd

Novartis Vaccines & Diagnostics, Gmbh

Vimalan Biosciences, Inc.

Ventyx Biosciences, Inc.

Novartis Ag

Daiichi Sankyo Company, Limited

Oppilan Pharma Ltd.

Exelixus, Inc.

John M Nuss

Wei Xu

James William Leahy

Lynne Canne Bannen

Raju Mohan

Yong Wang

Vasu Jammalamadaka

Larry Wayne Mann

Morrison B Mac

Richard George Khoury

Jason Harris

Jason Jevious Parks

Erick Wang Co

Timothy Patrick Forsyth

Shendong Yuan

Donna Tra Le

Diva Sze-Ming Chan

Moon Jung Kim

Savithri Ramurthy

Jeff Z Chen

Grace Mann

Tai Phat Huynh

Craig Stacy Takeuchi

Lisa Esther Dalrymple

Amy Lew Tsuhako

Wie Xu

David B Ring

Allan S Wagman

Stephen David Harrison

S David Brown

Mohamed Ibrahim

Morrisson B Mac

Rhett Ronald Klein

Matthew A Williams

Paul A Renhowe

Kirk William Johnson

Keith Bruce Pfister

Shumeye Mamo

Rustum S Boyce

Chris Allen Buhr

Sunghoon Ma

Lynn Seely

Gary Lee Lewis

Joan C Sangalang

Xian Shi

Wei Cheng

Tae-Gon Baik

Kevin Luke Schnepp

Xiaohui A Zhou

Zerom Tesfai

Dane A Goff

Sharadha Subramanian

Longcheng Wang

Patrick C Kearney

Sergey Epshteyn

Zhaoyang Wen

William Bajjalieh

Robin Tammie Noguchi

Amy Lew

Manoj C Desai

Richard Martin

Neel Kumar Anand

Kazumasa Aoki

Tsze Tsang

Tie-Lin Wang

Kenneth D Rice

Joerg Bussenius

Michael P Prisbylla

Atwood Kim Cheung

Larisa Dubenko

Barry Haskell Levine

Hiroyuki Tsuruoka

Brian Hugh Ridgway

Charles K Marlowe

Bryan K S Yeung

Tsuyoshi Homma

Baili Chen

Lynne Canne-Bannen

Rickard George Khoury

Sean P Brown

Rajinder Paul Singh

Noriyuki Hayashi

Sabina Pecchi

Csaba J Peto

Keiji Saito

David J Matthews

Ping Huang

Abigail R Kennedy

Charles M Blazey

Simona Costanzo

Peter Lamb

Owen Joseph Bowles

Steven Charles Defina

Kerry L Spear

Yusuke Asoh

Joon Won Jeong

Katherine Lara

Henry William Beecroft Johnson

Lutz Richter

Barbara O Scott

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

The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

C-met modulators and methods of use

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

Heterocyclic compounds for the treatment of disease

c-Met modulators and methods of use

The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.

Phosphatidylinositol 3-kinase inhibitors and methods of their use

This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.

Acetanilide sphingosine-1-phosphate receptor antagonists

Growing community of inventors

Danville, CA, United States of America

John M Nuss