Bristol-myers Squibb Compnay

Bristol Meyers Squibb Company

Andrew P Degnan

John E Macor

George O Tora

Gene Michael Dubowchik

Guanglin Luo

Prasad V Chaturvedula

Ling Chen

Xiaojun Han

Matthew D Hill

William D Schmitz

Hong Huang

Joanne J Bronson

John E Starrett, Jr

Wen-Ching Han

Fukang Yang

Graham S Poindexter

Kevin W Gillman

Michael Frederick Parker

Rita Civiello

Godwin Kwame Kumi

Xiang Jun J Jiang

Ashvinikumar V Gavai

Lawrence B Snyder

Wayne D Vaccaro

Derek J Norris

George V Delucca

Patrice Gill

Haiquan Fang

George N Karageorge

Derek John Denhart

Jeffrey A Deskus

Mikkel V DeBenedetto

James Aaron Balog

Yan Chen

Alicia Regueiro-Ren

John S Tokarski

Mark D Wittman

Weifang Shan

Audris Huang

Harold A Mastalerz

Francis Lee

Gang Wu

Ramkumar Rajamani

Ashok Vinayak Purandare

Ying Han

Mikkel V Debenedetto

Bradley C Pearce

Daniel O'Malley

Bireshwar Dasgupta

Vivekananda M Vrudhula

Stephen E Mercer

Claude A Quesnelle

Guifen Zhang

Guo Li

Yazhong Huang

Jonathan L Ditta

David S Yoon

George V De Lucca

Sunil Kumar Mandal

Shuanghua Hu

Erika M V Araujo

Shikha Vig

Darrell Maxwell

Francis Y Lee

John E Starrett

Charles Mark Conway

Jr John E Starrett

Daniel O'malley

The present invention relates to imidazo[1,2-a]pyridine and [1,2,4]triazolo[1, 5-a]pyridine derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic diseases, such as e.g. liver fibrosis, renal fibrosis, biliary fibrosis or pancreatic fibrosis, nonalcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), chronic kidney disease, diabetic kidney disease, primary sclerosing cholangitis (PSC) or primary biliary cirrhosis (PBC), or idiopathic pulmonary fibrosis (IPF).

Imidazo[1,2-A]pyridine and [1,2,4]triazolo[1,5-A]pyridine derivatives as TLR9 inhibitors for the treatment of fibrosis

The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.

Oxazolidinones as modulators of MGLUR5

Disclosed are compounds of Formula (I): or a salt thereof, wherein: Z is CRRor C&#x2550;O; Ring A is: and R, R, R, R, R, m, and n are defined herein. Also disclosed are methods of using such compounds to inhibit Helios protein, and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

Compounds useful as inhibitors of helios protein

Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CH or N; Y is CR5 or N; and R1, R2, R3, R4, and R5 are defined herein. Also disclosed are methods of using such compounds to modulate or inhibit the enzymatic activity of hematopoietic progenitor kinase 1 (HPK1), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer. 

Isofuranone compounds useful as HPK1 inhibitors

The present invention is directed to tricyclic compounds of formula (I), pharmaceutically acceptable compositions comprising compounds of the invention and said compositions for use in methods for the treatment of various disorders in particular cancer. 

5H-pyrido[3,2-B]indole compounds as anticancer agents

The present invention is directed to tricyclic compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Tricyclic compounds as anticancer agents

The present invention is directed to tricyclic compounds of the formula wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD). 

Substituted imidazo[1,5-a]pyrazines as CGRP receptor antagonists

The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system. 

Oxazolidinones as modulators of mGluR5

The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both. 

NK-1 and serotonin transporter inhibitors

The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders. 

Substituted heterocyclic ethers and their use in CNS disorders

The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors ('CGRP-receptor'), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.

Anti-migraine spirocycles

Therapeutic agents for the treatment of migraine

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Rocky Hill, CT, United States of America

Andrew P Degnan