Patent number: 8222247
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 metabolic and inflammatory or immune associated diseases or disorders having the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups, R1, R2, R3, and/or R4; provided that (i) A is not tetrazole or (ii) if A is thienyl or furanyl then Z M is selected from alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl; Z is selected from alkyl, CF3, OH, cycloalkyl, heterocyclo, aryl, heteroaryl, —C(?O)NR8R9, —C(?O)R8, —C(NCN)NR8R9, —C(?O)OR8, —SO2R8, and —SO2NR8R9.
Type:
Grant
Filed:
October 31, 2007
Date of Patent:
July 17, 2012
Assignee:
Bristol-Myers Squibb Company
Inventors:
Bingwei Vera Yang, Lidia M. Doweyko
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: 8034940
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, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted
Type:
Grant
Filed:
August 8, 2007
Date of Patent:
October 11, 2011
Assignee:
Bristol-Myers Squibb Company
Inventors:
David S. Weinstein, Ping Chen, T. G. Murali Dhar, Jingwu Duan, Hua Gong, Bin Jiang, Bingwei Vera Yang, Arthur M. Doweyko
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
Publication number: 20090075995
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, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B is a cycloalkyl, cycloalkenyl, aryl, heterocyclo, or heteroaryl ring, wherein each ring is fused to the A ring on adjacent atoms and optionally substituted by one to four groups which are the same or different and are independently selected from R5, R6, R7, and R8; J1, J2, and J3 are at each occurrence the same or different and are independently -A1QA2-; Q is a bond, O, S, S(O), or S(O)2; A1 and A2 are the same or different and are at each occurrence independently selected from a bond, C1-3alkylene, substituted
Type:
Application
Filed:
August 8, 2007
Publication date:
March 19, 2009
Inventors:
David S. Weinstein, Ping Chen, T.G. Murali Dhar, Jingwu Duan, Hua Gong, Bin Jiang, Bingwei Vera Yang, Arthur M. Doweyko
