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Gamma ROR modulators to treat complications of diabetes II
专利权人:
ETH Zürich
发明人:
WOLFRUM, Christian,CARREIRA, Erick,MEISSBURGER, Bettina
申请号:
ES12759466
公开号:
ES2659455T3
申请日:
2012.09.18
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound for use as a modulator of the gamma ROR receptor having the formula II and pharmaceutically acceptable salts or stereoisomers thereof, preferably having formula IIa, ** (See formula) ** wherein R1, R2, are independently from each other H , hal, -ORa, -SRa, -NRaRb, -COORa, -CONRaRb, where Ra and Rb are independently from each other H or (C1-6) alkyl, or R1, R2 form an epoxy group together with atoms C a those who are united; R2 'is H, hal, R4, R5 are independently from each other H, hal, -ORa, -SRa, -NRaRb, -COORa, -CONRaRb, oxo, uncle where Ra and Rb are independently from each other H or alkyl (C1 -6); L is a linking group, such as straight or branched chain C (1-12) alkyl, which is unsubstituted or substituted by at least one CN, hal, OH, NRaRb, COORa, NO2, and wherein one or more of the non-adjacent CH2 groups may be independently replaced by a group selected from -O-, -CO -, - CO-O-, - O-CO-, -NRa-, -NRa-CO-, -CO-NRa -, -CH>; = CH-, -C≡C-, where Ra and Rb are independently from each other H or C (1-6) alkyl, X is H, -ORa, -SRa, -NRaRb, -COORc, -CONRaRc; wherein Ra and Rb are independently H or C1-6 alkyl and Rc is -H, -C1-6 alkyl, -NH- (CH2) n-CO2Ra or -NH- (CH2) p-SO3Ra , where n, p are 1, 2 or 3 and Ra is -H or -C 1-6 alkyl; m is 0 to 5. where R3 and R6 are -ORa, where Ra is H or C (1-6) alkyl and said compound is for use in the treatment or prevention, suppression or improvement of diabetes type II and / or diseases, disorders and conditions that are related to type II diabetes in a subject in need, specifically low glucose tolerance, insulin resistance and / or hyperglycemia.Un compuesto para su uso como modulador del receptor ROR gamma que tiene la fórmula II y sales o esteroisómeros farmacéuticamente aceptables del mismo, preferiblemente que tienen fórmula IIa, **(Ver fórmula)** en donde R1, R2, son independientemente entre sí H, hal, -ORa, -SRa, -NRaRb, -COORa, -CONRaRb, en donde Ra y Rb son independientemente entre sí H o alquilo (C1-6), o R
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