Schering Aktiengesellschaft

Blade Therapeutics, Inc.

Zomagen Biosciences Ltd

Bayer Intellectual Property Gmbh

Escalier Biosciences B.v.

Vimalan Biosciences, Inc.

Ventyx Biosciences, Inc.

Elan Pharmaceuticals, Inc.

Bayer Schering Pharma Ag

Imago Pharmaceuticals, Inc.

Schering Aktiengessellschaft

Shendong Yuan

Raju Mohan

Brad Owen Buckman

Judi Bryant

John M Nuss

Imadul Islam

Jason Harris

Wei Xu

Michael M Morrissey

Guo Ping Wei

Marc Adler

John Beamond Nicholas

Monica J Kochanny

Kumaraswamy Emayan

Christopher West

Jingyuan Ma

Gary Bruce Phillips

Ying-Zi Xu

Damian O Arnaiz

Richard L Feldman

Karen B May

Yuo-Ling Chou

Wheeseong Lee

Seock-Kyu Khim

Paul Hrvatin

Kumar Emayan

Hing L Sham

Andrei William Konradi

Hans Briem

Markus Follmann

Alexandros Vakalopoulos

Katja Zimmermann

Dirk Kosemund

Dean R Artis

Joachim Kuhnke

Martina Schäfer

Simeon Bowers

Roy K Hom

Bin Ye

Mario Lobell

Nicole Teusch

Martin Krueger

Martin Michels

Peter Esperling

Lars Wortmann

Stefan Baeurle

Christoph Huwe

Ming Chen

David Wone

Michael Mamounas

Janet Meurer Ogden

Victor Selchau

Ulf Bomer

Emil Eckle

Robert Guo-Ping Wei

Mark Polokoff

Hongyi Yu

Michael Morrissey

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

Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

Calpain modulators and therapeutic uses thereof

Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to macrocyclic &#x3b1;-keto amide derivatives and their use as therapeutic agents.

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 technology relates to cyclic keto-amide compounds of general formulae I to XXXII, compositions and kits thereof as calpain modulators and methods useful for the treatment of various diseases or disorders such as fibrotic disease or cancer which are associated or mediated, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is also applicable to cyclic keto-amide compounds which inhibit myofibroblast differentiation.

Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof

Compounds are provided having a structure according to Formula (I): wherein A, A, A, Y, R, R, R, R, R, R, m, n and p are defined herein. Further provided are pharmaceutical compositions including the compounds provided and methods of making and using the compounds and compositions as provided, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease. 

Spirocyclic dihydro-thiazine and dihydro-oxazine BACE inhibitors, and compositions and uses thereof

This invention relates to novel bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.

Bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives and uses thereof

Growing community of inventors

San Ramon, CA, United States of America

Shendong Yuan