Bristol-Myers Squibb Compnay

Universitéde Montreal

Shoshana L Posy

Sanjeev Gangwar

Prasanna Sivaprakasam

Yam B Poudel

Alaric J Dyckman

Dharmpal S Dodd

Christopher P Mussari

Sreekantha Ratna Kumar

Laxman Pasunoori

Tasir Shamsul Haque

Subramanya Hegde

R Michael Lawrence

Edward H Ruediger

Liqi He

Michael Matthew Miller

Trevor C Sherwood

Marc Gagnon

Daniel H Deon

Jacques Banville

Eldon Scott Priestley

John E Macor

Louis John Lombardo

Ramesh Kumar Sistla

Brian K Whiteley

John L Gilmore

David R Tortolani

Roger Remillard

Alain Martel

Michael A Poss

Chunjian Liu

Annapurna Pendri

Alicia Regueiro-Ren

Anne Marinier

Ashok Vinayak Purandare

Naidu S Chowdari

Jean-Francois Lavallee

Pancras C Wong

Anupama Kandhi Ramachandra Reddy

Julia Guy

Brad D Maxwell

Laurence Dube

Rushith Kumar Anumula

Ian Scott Young

Roger Rémillard

François Tremblay

Laurence Dubé

Honghe Wan

Dietmar A Seiffert

Louis J Lombardo

Haibo Liu

David S Yoon

Srinivasan Kunchithapatham Duraisamy

Swanee E Jacutin-Porte

Pitani Veera Venkata Srinivas

Michael R Lawrence

Francois Tremblay

Laura Akullian D'Agostino

Tasir Shamsul Hague

Michael Mandler

Jean-François Lavallée

Anupama Ramachandra

Subramaya Hegde

Laurence DubÉ

Dietmar Alfred Seiffert

The present invention relates to 1H-benzo[d]imidazole 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, non-alcoholic 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).

1H-benzo[D]imidazole derivatives as TLR9 inhibitors for the treatment of fibrosis

Disclosed are compounds of Formula (I) or salts thereof, wherein R, R, R, R, and Rare defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Substituted carbazole compounds

Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein X is CRor N; and G, A, R; and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Substituted indole and indazole compounds

Disclosed are compounds of Formula (I) pharmaceutically acceptable salts thereof are defined herein, and pharmaceutical compositions thereof and combinations thereof, and methods of using the same as inhibitors of protein tyrosine phosphatases (PTPN2). These compounds are useful in treating cancer and diseases susceptible to PNPT2 inhibition.

Inhibitors of protein tyrosine phosphatase, compositions, and methods of use

The present invention provides thiazole compounds of Formula I wherein W, Y, R, R, R, R, R, R, X, X, Xand Xare as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.

Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation

Disclosed are compounds of Formula (I) or a salt thereof, wherein R, R, R, R, R, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

[1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds

Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R, R, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Substituted indole compounds useful as TLR inhibitors

Disclosed are compounds of Formula (I) or salts thereof, wherein Ring Het, R, R, R, R, R, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Substituted indole compounds

Compounds having a structure according to formula are modulators of TLR7 activity and can be used to treat conditions amenable to treatment by the modulation of TLR7 activity. 

Macrocyclic toll-like receptor 7 (TLR7) agonists

N-oxides, or salts thereof, wherein G, L, R, R, R, R, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases. 

Amide substituted indole compounds useful as TLR inhibitors

Disclosed are compounds of Formula (I) or salts thereof, wherein A, G, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases. 

Aryl and heteroaryl substituted indole compounds

Disclosed are compounds of Formula (I) or salts thereof, wherein G, R1, R5, R7, R8, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases. 

Amino indole compounds useful as TLR inhibitors

Compounds having a structure according to formula (I), (II), or (III) where R, R, R, RX, X, and Xare as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Toll-like receptor 7 (TLR7) agonists having a tricyclic moiety, conjugates thereof, and methods and uses therefor

Compounds having a structure according to formula (I) where R, R, and Rare as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Toll-like receptor 7 (TLR7) agonists having a benzotriazole moiety, conjugates thereof, and methods and uses therefor

Growing community of inventors

Highland Park, NJ, United States of America

Shoshana L Posy