发明名称 Substituted phenoxy N-alkylated thiazolidinediones 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 US9034852(B2) 申请公布日期 2015.05.19
申请号 US201213346808 申请日期 2012.01.10
申请人 Janssen Pharmaceutica N.V. 发明人 Gaul Michael;Searle Lily Lee;Rentzeperis Dionisios
分类号 C07D277/34;C07D417/06 主分类号 C07D277/34
代理机构 代理人 McKown Jeremy K.
主权项 1. A method of treating a subject suffering from or diagnosed with a disease, disorder, or condition mediated by ERR-α, comprising administering to the subject a therapeutically effective amount of at least one compound of formulawherein X is S or O; n is 1-4 R1 is halo, optionally substituted C1-4alkyl, optionally substituted C1-4alkoxy, or hydroxyl; R2 is selected from halo substituted C1-3alkyl, cyano, halo, —C(O)NH2, and —C(O)O—C1-4alkyl, or alternatively R2 is linked together to R3 to form an aryl fused to the phenyl ring to which R2 and R3 are shown attached; R3 is H, or alternatively R3 is linked together to R2 to form an aryl ring fused to the phenyl ring to which R3 and R2 are shown attached; R4 is halo, cyano, halo substituted C1-3alkyl, —C≡CH, —C(O)O—C1-4alkyl, —C(O)NH2, or —S(O2)—C1-4alkyl; and R5 and R6 are independently H or optionally substituted C1-4alkyl, or alternatively R5 and R6 are linked together with the N atom to which they are attached to form an optionally substituted 5-9 membered N-containing heteroaryl or optionally substituted 5-7 membered N-containing heterocyclyl; or an optical isomer, enantiomer, diastereomer, cis-trans isomer, racemate, or pharmaceutically acceptable salt thereof, wherein the disease, disorder, or medical condition is selected from the group consisting of obesity, diabetes, lipid disorders, artherosclerosis, hyperglycemia, elevated blood glucose level, and insulin resistance.
地址 Beerse BE