发明名称 ROR modulators and their uses
摘要 The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR. The invention is based in part on the discovery of ROR modulators which interact with RORa and/or RORy and thereby inhibit or induce RORa and/or RORy-activity, and RORa- and/or RORy-regulated target gene and protein expression.
申请公布号 US9321750(B2) 申请公布日期 2016.04.26
申请号 US201314394777 申请日期 2013.04.22
申请人 INNOV17 LLC 发明人 Gaweco Anderson;Tilley Jefferson W.;Walker John;Palmer Samantha;Blinn James
分类号 C07D209/08;C07D403/10;C07D215/38;C07D401/10;C07D405/10;C07D405/12 主分类号 C07D209/08
代理机构 代理人
主权项 1. A compound of formula Ia: wherein A is phenyl optionally substituted with C1-C4 alkyl, halogen, OH, CN, or N(R4)2; R1 is absent, H, OH, halogen, N(R4)2, O-alkyl, CN, —S(O)2-alkyl, —O—C1-C4 alkyl optionally substituted with halogen, OH, O-alkyl, CN, or N(R4)2, or C1-C4 alkyl optionally substituted with halogen, OH, O-alkyl, CN, or N(R4)2; R2 and R3 are independently selected from H, halogen, or C1-C4 alkyl optionally substituted with halogen, OH, CN, N(R4)2, or R2 and R3, taken together may form a 4-7 membered saturated or unsaturated ring, optionally incorporating 1-3 N, O, or S atoms; wherein the 4-7 membered ring is optionally substituted with C1-C4 alkyl, halogen, OH, carbonyl, CN, halogen, or N(R4)2, or R2 and R3, can be taken together to form a carbonyl; each R4 is independently H, alkyl, aryl, or can be taken together to form a 4-7 membered ring, optionally incorporating an additional N, O, S atom; wherein the 4-7 membered ring is optionally substituted with C1-C4 alkyl, halogen, OH, CN, halogen, or N(R4)2; R6 is H or alkyl; R7 is H, alkyl, optionally substituted acyl, alkyl-O-acyl, substituted or unsubstituted aminoacyl, carbamoyl, carbamido, alkyl sulfonyl, aryl sulfonyl, heteroaryl sulfonyl, 4-7 membered heterocycle sulfonyl, or C4-C7 cycloalkyl-acyl; and p is 1 or 2; or a pharmaceutically acceptable salt, hydrate, solvate, or tautomer thereof.
地址 Brooklyn NY US