首页> 外国专利> Oxo compounds AZA anthracene Derivatives, Pharmaceutical composition comprising these Compounds, and their use for treating Transplant rejection, rheumatoid arthritis, psoriatic arthritis,Multiple Sclerosis and Asthma, among others.

Oxo compounds AZA anthracene Derivatives, Pharmaceutical composition comprising these Compounds, and their use for treating Transplant rejection, rheumatoid arthritis, psoriatic arthritis,Multiple Sclerosis and Asthma, among others.

机译:含氧化合物AZA蒽衍生物,包含这些化合物的药物组合物,及其在治疗移植排斥,类风湿性关节炎,银屑病关节炎,多发性硬化症和哮喘中的用途。

摘要

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 C1-3alkylene, C2-4alkenylene, and substituted C2-4alkenylene, provided that A1 and A2 are chosen so that ring A is a 5- to 8-membered carbocyclic or heterocyclic ring; R1 to R11 are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
机译:提供了新颖的非类固醇化合物,其可用于治疗与糖皮质激素受体,AP-1和/或NF-B活性调节有关的疾病,包括炎性和免疫性疾病,具有式(I)结构:对映体,其非对映异构体或其互变异构体,或其前药酯或其药学上可接受的盐,其中:Z为杂环或杂芳基; A为5至8元碳环或5至8元杂环。 B为环烷基,环烯基,芳基,杂环或杂芳基环,其中每个环与相邻原子上的A环稠合,并且任选地被1-4个相同或不同且独立地选自R5,R6, R7和R8; J1,J2和J3在每次出现时相同或不同,并且独立地为-A1QA2-; Q是键,O,S,S(O)或S(O)2; A1和A2相同或不同,并且每次选择独立地选自键,C1-3亚烷基,取代的C1-3亚烷基,C2-4亚烯基和取代的C2-4亚烯基,条件是选择A1和A2以使环A为5至8元碳环或杂环; R1至R11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以及肥胖症和糖尿病的药物组合物和方法。

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