SUBSTITUTED PHENOXY N-ALKYLATED THIAZOLEDINEDIONE AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS

• Main Authors: DIONISIOS RENTZEPERIS, MICHAEL GAUL, LILY LEE SEARLE
• Format: Patent
• Language: Croatian; English
• Published: 31.03.2012
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

Spoj formule (I) naznačen time da X je S; n je 1-4R1 je halo, proizvoljno supstituiran C1-4alkil, proizvoljno supstituiran C1-4alkoksi, ilihidroksil; R2 je odabran od halo supstituiranog C1-3alkila, cijano, halo, -C(O)NH2, i -C(O)O-C1-4alkila, ili alternativno R2 je povezan sa R3 da se dobije aril kondenziran na fenilni prsten na koji su pridruženi prikazani R2 i R3;R3 je H, ili alternativno R3 je povezan sa R2 da se dobije arilni prsten kondenziran na fenilni prsten na koji su pridruženi prikazani R3 i R2;R4 je halo, cijano, halo supstituirani C1-3alkil, -C?CH, -C(O)O-C1-4alkil, -C(O)NH2, ili -S(O2)-C1-4alkil; iR5 i R6 su neovisno H ili proizvoljno supstituirani C1-4alkil, ili alternativno R5 i R6 su vezani zajedno sa atomom dušika na koji su spojeni da se dobije proizvoljno supstituiran 5-9 člani N-koji sadrži heteroaril ili proizvoljno supstituiran 5-7 člani N- koji sadrži heterociklil; ili optički izomer, enantiomer, diastereomer, cis-trans izomer, racemat ili njegova farmaceutski prihvatljiva sol. Patent sadrži još 33 patentna zahtjeva. 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.