发明名称 Substituted thiazolidinedione indazoles, indoles and benzotriazoles as estrogen-related receptor-α modulators
摘要 The present invention relates to compounds of Formula (I),; methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
申请公布号 US8796256(B2) 申请公布日期 2014.08.05
申请号 US201113114084 申请日期 2011.05.24
申请人 Janssen Pharmaceutica NV 发明人 Bignan Gilles;Cheung Wing;Gaul Micheal;Huang Hui;Li Xun;Patch Raymond;Patel Sharmila;Player Mark;Xu Guozhang;Zhao Bao-Ping;Liu Jian
分类号 C07D417/06 主分类号 C07D417/06
代理机构 代理人 McKown Jeremy K.
主权项 1. A compound of Formula (I) wherein X is CR4;Y is N;L is a bond;R1 is an optionally substituted heterocyclyl group;R2 is halo-substituted C1-3alkyl, or alternatively R2 is linked together to R5 to form a cycloalkyl fused to the phenyl ring to which R2 is shown attached;R3 is halo, cyano, halo-substituted C1-3alkyl, or C1-4alkoxyl;R4 is H, hydroxyl, halo, C1-4alkyl, C1-4alkoxyl, optionally substituted phenyl, cyano, or —C(O)NH2;R5 is H, or alternatively R5 is linked together to R2 to form a cycloalkyl fused to the phenyl ring to which R2 is shown attached;R6 is H or F; andR7 is H or F;or an enantiomer, diastereomer, cis-trans isomer, racemate, prodrug or pharmaceutically acceptable salt thereof.
地址 Beerse BE