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    • 1. 发明申请
    • MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KB ACTIVITY AND USE THEREOF
    • GLUCOCORTICOID受体的调节剂,AP-1和/或NF-κB活性及其用途
    • WO2008057855A2
    • 2008-05-15
    • PCT/US2007083083
    • 2007-10-31
    • SQUIBB BRISTOL MYERS CODHAR T G MURALIXIAO HAI-YUNSHEPPECK JAMES E
    • DHAR T G MURALIXIAO HAI-YUNSHEPPECK JAMES E
    • C07D471/04
    • 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 (R x )(R y ); is heterocyclo or heteroaryl; E is -N-, -NR 1 -, -O-, -C(=O), -S-, -SO 2 -, or -CR 2 -; F is -N-, -NR 1a , -O-, -C(=O), -S-, -SO 2 -, or -CR 2a -; G is independently N, -NR 1b -, -O-, -C(=O), -S-, -SO 2 - or -CR 2b - 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, R x , R y , R 1 , R 1a , R 1b , R 2 , R 2a , R 2b , R 4 , R 5a , R 6 , R 7 , X, Z a and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases employing said compounds.
    • 提供了新的非甾体化合物,其可用于治疗与糖皮质激素受体的调节有关的疾病和/或AP-1和/或NF-κB活性,包括具有式I结构的炎性和免疫疾病,肥胖症和糖尿病 :其对映异构体,非对映异构体或其药学上可接受的盐或水合物,其中基团X为O或(R x x)O(R y); 是杂环基或杂芳基; E是-N-,-NR 1 - , - O - , - C(= O),-S - , - SO 2 - 或-CR 2 - ; F是-N,-NR 1a,-O - , - C(= O), - S - , - SO 2 - 或-CR 图2a - ; G独立地为N,-NR1B1 - , - O - , - C(= O),-S-,-SO2-或-CR2b - 条件是所形成的杂环不含有SS或SO键,并且E,F和G中的至少一个为杂原子; 和M a,R x,R y,R 1,R 1a,R 1b, R 2,R 2,R 2a,R 2b,R 4,R 5a, R 6,R 6,R 7,X,Z a a和Z如本文所定义。 还提供了使用所述化合物治疗炎性或免疫相关疾病的药物组合物和方法。
    • 7. 发明申请
    • HETEROCYCLIC COMPOUNDS AS MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-I, AND/OR NP-KAPPA-B ACTIVITY
    • 作为GLUCOCORTICOID受体,AP-I和/或NP-KAPPA-B活性的调节剂的杂环化合物
    • WO2008057855A9
    • 2009-06-18
    • PCT/US2007083083
    • 2007-10-31
    • SQUIBB BRISTOL MYERS CODHAR T G MURALIXIAO HAI-YUNSHEPPECK JAMES E
    • DHAR T G MURALIXIAO HAI-YUNSHEPPECK JAMES E
    • C07D471/04A61K31/437A61P3/00A61P29/00A61P37/00
    • C07D471/04
    • 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.
    • 提供新的非甾体化合物,其可用于治疗与糖皮质激素受体和/或AP-1和/或NF-κB活性相关的疾病,包括具有结构式(1)的炎性和免疫疾病,肥胖症和糖尿病 I):其对映异构体,非对映异构体或其药学上可接受的盐或水合物,其中基团X为O或(Rx)(Ry); 是杂环基或杂芳基; E是-N-,-NR1 - , - O - , - C(= O),-S-,-SO2-或-CR2-; F是-N-,-NR1a,-O-,-C(= O),-S-,-SO2 - 或-CR2a; G独立地为N,-NR1b - , - O - , - C(= O), - S - , - SO2-或-CR2b-,条件是所形成的杂环不含有SS或SO键, E,F和G是杂原子; 并且Ma,Rx,Ry,R1,R1a,R1b,R2,R2a,R2b,R4,R5a,R6,R7,X,Za和Z如本文所定义。 还提供了使用所述化合物治疗炎性或免疫相关疾病的药物组合物和方法。