Bristol-myers Squibb Compnay

Bin Jiang

Jingwu Duan

Zhonghui Lu

T G Murali Dhar

David S Weinstein

William John Pitts

Hai-Yun Xiao

Bingwei Vera Yang

Arun Kumar Gupta

Ananta Karmakar

Stephen T Wrobleski

John T Hynes

Steven H Spergel

James Edward Sheppeck

Hong Wu

Junqing Guo

Shuqun Lin

Hua Gong

Lihua Chen

James Kempson

Jagabandhu Das

John S Tokarski

John L Gilmore

Joseph Barbosa

Lidia M Doweyko

Carolyn A Weigelt

Ping Chen

Chu-Biao Xue

Joseph Anthony Tino

Khehyong Ngu

Andrew J Tebben

Gregory D Brown

Tg Murali Dhar

Arthur M Doweyko

Murali T G Dhar

Ning Li

Murali TG Dhar

TG Murali Dhar

Das Jagabandhu

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: Ring A is 3- to 6-membered carbocyclic or heterocyclic ring; X is CRor N; Y is &#x2014;(CRR)&#x2014;; Z is &#x2014;(CRR)&#x2014;; and q, R, R, R, R, R, R, R, R, and Rare defined 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. 

Cyclic compounds useful as modulators of TNF &#x3b1;

Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: (i) &#x2014;(CRR)&#x2014;; (ii) &#x2014;(CRR)&#x2014;Y&#x2014;(CRR)&#x2014;; Or (iii) &#x2014;Y&#x2014;(CRR)&#x2014;Y&#x2014;; and Y, R, R, R, R, R, R, x, and y are defined 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.

Substituted tricyclic heterocyclic compounds

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

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. 

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

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. 

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

Novel non-steroidal compounds are provided that 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 having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is AQA-; Q is a bond, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;OC(O)&#x2014;, &#x2014;C(&#x2550;O)NR&#x2014;, &#x2014;SO&#x2014;, &#x2014;SONR&#x2014;, &#x2014;C(O)O&#x2014;, &#x2014;NRC(O)&#x2014;, &#x2014;OC(O)NR&#x2014;, &#x2014;NRC(O)O&#x2014;, &#x2014;S(O)NRC(O)&#x2014;, &#x2014;C(O)NRS(O)&#x2014; &#x2014;NRS(O)&#x2014;, or &#x2014;NRC(&#x2550;O)NR&#x2014;. Y is selected from hydrogen, Calkyl, OR, substituted Calkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. Aand Aare independently selected from a bond, Calkylene, or Calkenylene, and R-Rare defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.

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

Growing community of inventors

Norristown, PA, United States of America

Bin Jiang