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Gamma related retinal (ROR gamma) receptor modulators for the treatment of autoimmune and inflammatory diseases
专利权人:
GLAXO GROUP LIMITED
发明人:
HAN, FANGBIN,LEI, HUI,LIN, XICHEN,MENG, QINQHUA,WANG, YONGHUI
申请号:
PE2015000712
公开号:
PE20151144A1
申请日:
2013.12.05
申请国别(地区):
PE
年份:
2015
代理人:
摘要:
The invention refers to a formula compound as the modulator of gamma iris bone receptor and a formula compound for the treatment of rogamma vector diseases such as multiple sclerosis, rheumatoid arthritis and psychosis, wherein R1 is tar such as C1-C6, C3-C7, R2 is halogen or C1-C3 tar; R3 is halogen or methyl; R4 is h or methyl; R5 is C1-C3 tar; R6 is C1-C3 tar; R7 is C1-C7 tar, etc.; 0 or 1 per K; 0 or 1 per P. The preferred compounds are: (s) - N - (3 - ((4 - (cyclopentantan carbazone) - 3-methylpyridine-1-il) methyl) - 5-fluoro-2-methylphenyl) - 2-methylpyridine-5-carboxyamine (E20);Y (s) - N - (5-chloro-3 - ((4 - (cyclopentantan carbohydrates) - 3-methylpyridine-1-il) methyl) - 2-methylphenyl) - 6-methylnicotine (E62);Among other thingsLa invencion se refiere a compuestos de formula I como moduladores del receptor huerfano gamma relacionado con retinoides (RORgamma) y su uso en el tratamiento de enfermedades mediadas por RORgamma, como esclerosis multiple, artritis reumatoide, psoriasis, etc. Donde R1 es alquilo C1-C6, cicloalquilo C3-C7, etc; R2 es halo o alquilo C1-C3; R3 es halo o metilo; R4 es H o metilo; R5 es alquilo C1-C3; R6 es alquilo C1-C3; R7 es alquilo C1-C7, etc; cada K es 0 o 1 y cada p es 0 o 1. Los compuestos preferidos son: (S)-N-(3-((4-(ciclopentancarbonil)-3-metilpiperazin-1-il)metil)-5-fluoro-2-metilfenil)-2-metilpirimidin-5-carboxamida(E20); y (S)-N-(5-cloro-3-((4-(ciclopentancarbonil)-3-metilpiperazin-1-il)metil)-2-metilfenil)-6- metilnicotinamida (E62); entre otros
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