发明名称 SODIUM CHANNEL MODULATORS FOR THE TREATMENT OF PAIN AND DIABETES
摘要 Provided herein are sodium channel modulating Compounds, in particular NaV1.7 modulating compounds of Formula I or compounds of Formula I′:;;In particular, provided herein are processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions comprising, and therapeutic methods comprising administering such compounds. In particular, provided herein are compounds for the treatment of pain and diabetes.
申请公布号 US2016221974(A1) 申请公布日期 2016.08.04
申请号 US201415021153 申请日期 2014.09.09
申请人 CHROMOCELL CORPORATION 发明人 BABICH Olga;GARYANTES Tina;LUO Robert Z.;PALLING David J.;VENKATACHALAN Srinivasan P.;WANG-FISCHER Yanlin
分类号 C07D277/52;C07D471/04;C07D487/04;C07D417/12;C07D285/08 主分类号 C07D277/52
代理机构 代理人
主权项 1. A compound of Formula (I), or a pharmaceutically acceptable salt, or a stereoisomeric or tautomeric form thereof, wherein: Z is —O— or —S—; Y is —X—C(═O)NR4R5, —(CH2)3—NR9R10, or 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-(2-yl or 3-yl); X is (C6-C10)aryl or 5- or 6-membered heteroaryl; R1 is a partially unsaturated or aromatic 5- or 6-membered heterocycle; R2 is independently at each occurrence —F, —Cl, —Br, —CH3 or —CN; R3 is independently at each occurrence —H, —F, —Cl, —Br, —CF3, —OCF3, —CN, (C1-C12)alkyl, or (C1-C12)alkoxy; R4 and R5 are each independently H, (C1-C9)alkyl, (C4-C12)cycloalkyl, or R4 and R5 together form a 5- to 7-membered heterocycloalkyl ring; with the proviso that: R4 and R5 are not both H; andat least one of R4 and R5 independently or said heterocycloalkyl ring formed by R4 and R5 together is substituted with 1 or 2 substituents selected from the group consisting of —CO2H, —CO2R6, —CN, —OH, —CONR7R8, and —NR7R8; wherein: R6 is (C1-C12)alkyl;R7 and R8 are each independently H, (C1-C12)alkyl, or R7 and R8 together form a 4- to 7-membered heterocycloalkyl ring; R9 is (C1-C6)alkyl, (C3-C8)cycloalkyl, pyrazolyl or pyridinyl; wherein R9 is optionally further substituted with 1 or 2 substituents selected from the group consisting of —COOH, —COOR11, —CONR11R12, —SO2R11, —SO2NR11R12, —OH, —CN, —OR11, and —NR11R12; wherein R11 and R12 may form a 6 membered heterocycloalkyl ring R10 is R11, —COR11, —COOR11, —SO2R11, 5-methyl-2-oxo-1,3-dioxol-4-yl,—COO—CH(CH3)OCOCH(CH3)2; or R9 and R10 together form a piperazinone or a 4- to 8-membered heterocycloalkyl ring, wherein said heterocycloalkyl ring is substituted with 1 or 2 substituents selected from the group consisting of —COOH, —COOR11, —CH2—COOR11, —OH, —NH2, —CN, and (C1-C8)alkoxy; R11 and R12 are independently H or (C1-C6)alkyl, optionally substituted with 4- to 8-membered heterocycloalkyl ring; and m and n are each independently 1, 2, 3, or 4.
地址 North Brunswick NJ US