Bristol-myers Squibb Compnay

Bristol-myers Squibb Pharma Company

Zhonghui Lu

Jingwu Duan

Bin Jiang

T G Murali Dhar

William John Pitts

Lihua Chen

Arun Kumar Gupta

Ananta Karmakar

Stephen T Wrobleski

David S Weinstein

Hai-Yun Xiao

Gregory R Ott

Shuqun Lin

Chu-Biao Xue

Thomas P Maduskuie, Jr

John T Hynes

Steven H Spergel

Carl P Decicco

Hong Wu

Bingwei Vera Yang

Junqing Guo

Joseph Barbosa

Hua Gong

James Kempson

Gregory D Brown

Carolyn A Weigelt

Jagabandhu Das

Joseph Anthony Tino

John S Tokarski

Matthew Ernst Voss

Xiao-Tao Chen

Andrew J Tebben

Khehyong Ngu

Lidia M Doweyko

Murali T G Dhar

Ning Li

TG Murali Dhar

There are described ROR&#x3b3; modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR&#x3b3; activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR&#x3b3; activity, for example, autoimmune and/or inflammatory disorders.

ROR &#x3b3; modulators

Disclosed are compounds of Formula (I) or a salt thereof, wherein: A is CRor N; B is CRor N; D is CRor N; Lis &#x2014;(CRR)&#x2014;; Lis &#x2014;(CRR)&#x2014;; and X, Z, R, R, R, R, R, and Rare define herein. Also disclosed are methods of using such compounds as modulators of TNF&#x3b1;, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases. 

Heterocyclic compounds useful as modulators of TNF alpha

Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: &#x2014;(CR3R3)2-5-, &#x2014;(CR3R3)x-Y&#x2014;(CR3R3)y-, &#x2014;Y&#x2014;(CR3R3)2-3-Y&#x2014;, &#x2014;CR3R3-Y&#x2014;(CR3R3)2-Y&#x2014;, &#x2014;Y&#x2014;(CR3R3)2-Y&#x2014;CR3R3-; and Y, R1, R2, R3, R5, R6, R8, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNF&#x3b1;, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Tricyclic heterocyclic compounds useful as inhibitors of TNF

Described are ROR&#x3b3; modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR&#x3b3; activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR&#x3b3; activity, for example, autoimmune and/or inflammatory disorders. 

Carbocyclic sulfone ROR&#x3b3; modulators

Described are ROR&#x3b3; modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR&#x3b3; activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR&#x3b3; activity, for example, autoimmune and/or inflammatory disorders. 

ROR&#x3b3; modulators

Cyclohexyl sulfone ROR&#x3b3; modulators

Described are ROR&#x3b3; modulators of the formula (I), [INSERT CHEMICAL STRUCTURE HERE] or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR&#x3b3; activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR&#x3b3; activity, for example, autoimmune and/or inflammatory disorders. 

Heterocyclic sulfone ROR&#x3b3; modulators

Described are ROR&#x3b3; modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR&#x3b3; activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR&#x3b3; activity, for example, autoimmune and/or inflammatory disorders.

Pyrrolidinyl sulfone ROR&#x3b3; modulators

The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases. 

Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases

Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases. 

Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, (I) are useful as kinase modulators, including Btk modulation, wherein A, A, A, Rare as defined herein. 

Azaindazoles as kinase inhibitors and use thereof

Non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-&#x3ba;B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or hydrate thereof, where J is selected from NRor C(R)(R); K is selected from NRor C(R)(R); L is selected from NRor C(R)(R); and A, X, Y, R, R, R, R, R, R, R, R, R, R, R, R, and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.

Modulators of glucocorticoid receptor, AP-1, and/or NF-&#x3ba;B activity, and use thereof

The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R, R, R, R, R, n, W, U, X, Y, Z, U, X, Y, and Zare defined in the present specification, which are useful as TNF-&#x3b1; converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.

Barbituric acid derivatives as inhibitors of TNF-&#x3b1; converting enzyme (TACE) and/or matrix metalloproteinases

Growing community of inventors

King of Prussia, PA, United States of America

Zhonghui Lu