Patent number: 8198311
Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically acceptable salt, or hydrate, thereof, wherein X is (Ia); or X is (Ib); or X is (Ic); (Id) is heterocycle or heteroaryl; E is —N—, —NR1—, —O—, —S—, —SO2— or —CR2—; F is —N—, —NR1a—, —O—, —S—, —SO2— or —CR2a—; G is N, —NR1b—, —O—, —S—, —SO2— or —CR2b—, provided that the E-F-G containing heterocyclic ring formed does not contain a S—S or S—O bond, and at least one of E, F and G is a heteroatom; J, Ja, M, Ma, Q, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, and R3 to R21, Z, Za, Zb, and Zc are as defined above.
Type:
Grant
Filed:
October 31, 2007
Date of Patent:
June 12, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
James E. Sheppeck, John L. Gilmore, T. G. Murali Dhar, Hai-Yun Xiao, Jianmin Wang, Bingwei Vera Yang, Lidia M. Doweyko
Patent number: 7994190
Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1 and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I):, its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein the group X is O or (Rx)(Ry); is heterocyclo or heteroaryl; E is —N—, —NR1—, —O—, —C(?O), —S—, —SO2—, or —CR2—; F is —N—, —NR1a, —O—, —C(?O), —S—, —SO2—, or —CR2a—; G is independently N, —NR1b—, —O—, —C(?O), —S—, —SO2— or —CR2b— provided that the heterocyclic ring formed does not contain a S—S or S—O bond and at least one of E, F and G is a hetero atom; and Ma, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, R4, R5a, R6, R7, X, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases employing said compounds.
Type:
Grant
Filed:
October 31, 2007
Date of Patent:
August 9, 2011
Assignee:
Bristol-Myers Squibb Company
Inventors:
T. G. Murali Dhar, Hai-Yun Xiao, James E. Sheppeck
Publication number: 20100190820
Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1 and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I): its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein the group X is O or (Rx)(Ry); is heterocyclo or heteroaryl; E is —N—, —NR1—, —O—, —C(?O), —S—, —SO2—, or —CR2—; F is —N—, —NR1a, —O—, —C(?O), —S—, —SO2—, or —CR2a—; G is independently N, —NR1b—, —O—, —C(?O), —S—, —SO2— or —CR2b— provided that the heterocyclic ring formed does not contain a S—S or S—O bond and at least one of E, F and G is a hetero atom; and Ma, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, R4, R5a, R6, R7, X, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases employing said compounds.
Type:
Application
Filed:
October 31, 2007
Publication date:
July 29, 2010
Inventors:
T. G. Murali Dhar, Hai-Yun Xiao, James E. Sheppeck
Publication number: 20100075961
Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically acceptable salt, or hydrate, thereof, wherein X is (Ia); or X is (Ib); or X is (Ic); (Id) is heterocycle or heteroaryl; E is —N—, —NR1—, —O—, —S—, —SO2— or —CR2—; F is —N—, —NR1a—, —O—, —S—, —SO2— or —CR2a—; G is N, —NR1b—, —O—, —S—, —SO2— or —CR2b—, provided that the E-F-G containing heterocyclic ring formed does not contain a S—S or S—O bond, and at least one of E, F and G is a heteroatom; J, Ja, M, Ma, Q, Rx, Ry, R1, R1a, R1b, R2, R2a, R2b, and R3 to R21, Z, Za, Zb, and Zc are as defined above.
Type:
Application
Filed:
October 31, 2007
Publication date:
March 25, 2010
Inventors:
James E. Sheppeck, John L. Gilmore, T. G. Murali Dhar, Hai-Yun Xiao, Jianmin Wang, Bingwei Vera Yang, Lidia M. Doweyko