发明名称 ROR GAMMA MODULATORS
摘要 The present invention relates to compounds of formula I, or a pharmaceutically acceptable salt thereof,;;for use in the treatment or prevention, suppression or amelioration of a disease mediated by the ROR gamma receptor in a subject in need thereof, in particular diabetes and diabetes-related disorders, specifically type II diabetes, methods of their production, as well as methods of treatment or prevention of such diseases.
申请公布号 US2014343023(A1) 申请公布日期 2014.11.20
申请号 US201214345597 申请日期 2012.09.18
申请人 ETH ZÜRICH, ETH TRANSFER 发明人 Wolfrum Christian;Carriera Erick;Meissburger Bettina
分类号 C07J9/00;C07J71/00;A61K31/58;A61K31/575 主分类号 C07J9/00
代理机构 代理人
主权项 1. A compound of formula I for use as modulator of the ROR gamma receptor, having the general formula I or pharmaceutically acceptable salts or stereoisomers thereof wherein R1, R2, R2′ are independently of each other H, hal, —ORa, —SRa, —NRaRb, —COOR1, —CONRaRb, wherein Ra and Rb are independently of each other H or (C1-6)alkyl, or R1, R2 form together with the C-atoms to which they are linked an epoxy group; R3, R4, R5, R6, are independently of each other H, hal, —ORa, —SRa, —NRaRb, —COORa, —CONRaRb, oxo, thio wherein Ra and Rb are independently of each other H or (C1-6)alkyl; R7, R8, R9 are independently of each other H, (C1-10)alkyl, wherein one or more non neighbouring CH2 groups may be replaced with —O—, —S—, —CO—, —CO—O—, —O—CO—, —NRa—, —CO—NRa—, —NRa—CO—, —C═C—, or —C≡C—; wherein Ra is H or (C1-6)alkyl; L is a linking group, such as straight-chain or branched 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 independently be replaced by a group selected from —O—, —CO—, —CO—O—, —O—CO—, —NRa—, —NRa—CO—, —CO—NRa—, —CH═CH—, —C≡C—, wherein Ra and Rb are independently of each other H or C(1-6)alkyl, X is H, —ORa, —SRa, —NRaRb, —COORc, —CONRaRc; wherein Ra and Rb are independently of each other H or (C1-6)alkyl and Rc is —H, —(C1-6)alkyl, —NH—(CH2)n—CO2Ra or —NH—(CH2)p—SO3Ra, wherein n, p is 1, 2, or 3 and Ra is —H or —(C1-6)alkyl; m is 0 to 5.
地址 Zürich CH