发明名称 HETEROCYCLIC DERIVATIVES AND USE THEREOF
摘要 A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.
申请公布号 US2016108056(A1) 申请公布日期 2016.04.21
申请号 US201414892378 申请日期 2014.06.03
申请人 C&C RESEARCH LABORATORIES 发明人 Park Chan Hee;Lee Sang Hwi;Im Junhwan;Lee Soon Ok;Kim Hoe Moon;Moon Sung Hyun;Kim Seunghee;Kim Jongmin;Ko Kwang Seok;Choi Bu Young;Kim Byungho
分类号 C07D495/04;C07D409/12;C07D471/04;C07D277/68;C07D209/42;C07D333/70 主分类号 C07D495/04
代理机构 代理人
主权项 1. A compound selected from the group consisting of a heterocyclic derivative represented by formula (I), and a pharmaceutically acceptable salt and a stereoisomer thereof:wherein A is present or absent, and, if present, A is a saturated or unsaturated C3-10 carbocycle or a 5- to 10-membered heterocycle, and if A is absent, X3 and X4 are each independently optionally substituted with R1 or R2; B is a benzene or a 5- to 12-membered heterocycle; C is a benzene, a 5- to 12-membered heterocycle, or C3-6 carbocycle; Y is —C(═O)— connected to X2 or X5; X1 is —O—, —S—, —S(═O)—, —S(═O)2—, or —N(W1)—; X2 is a carbon atom connected to Y, or —N═, —NH—, —C(W2)═ or —CH(W2)— not connected to Y; X3 and X4 are each independently a carbon or nitrogen atom; X5 is a carbon atom connected to Y, or —CH═ not connected to Y; wherein the 5-membered ring comprising X1 to X5 is aromatic or non-aromatic; W is hydrogen, halogen, C1-6 alkyl, or 5- or 6-membered heterocyclyl-C1-3 alkyl; W1 is hydrogen, C1-6 alkyl, C1-6 alkoxycarbonyl, or 5- to 8-membered heterocyclyl-C1-4 alkyl; W2 is hydrogen, halogen, C1-6 alkyl, or 5- to 8-membered heterocyclyl-C1-4 alkyl; L is —(CR9R10)m—, —(CR9R10)m—O—, —NH—, —N(C1-6 alkyl)-, —S(═O)2—, —C(CH2)—, or C3-7 cycloalkylene, wherein m is an integer of 0 to 3, and R9 and R10 are each independently hydrogen, hydroxy, halogen, or C1-6 alkyl; R1 is nitro, amino, C1-6 alkylsulfonyl, haloC1-6 alkoxy, or any one of the following structural formulae i) to iv): R2 is hydrogen, halogen, nitro, amino, C1-6alkoxy, haloC1-6 alkoxy, C1-6 alkylsulfonyl, or 5- or 6-membered heterocycloalkyl; R3 is hydrogen, halogen, cyano, C1-6 alkyl, haloC1-6 alkyl, cyanoC1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkoxy, haloC1-6 alkoxy, cyanoC1-6 alkoxy, C1-6 alkylamino, diC1-6 alkylamino, C1-6 alkylthio, C1-6 alkylaminocarbonyl, diC1-6 alkylaminocarbonyl, C2-8 alkynyl, C6-10 aryl, haloC6-10 aryl, 5- to 10-membered heterocyclyl, or 5- to 10-membered heterocyclylcarbonyl, wherein the heterocyclyl moiety is optionally substituted with one to three substituents selected from the group consisting of halogen, hydroxy, cyano, amino, C1-6 alkyl, haloC1-6 alkyl, C1-6 alkoxy and C1-6 alkoxycarbonyl; R4 is hydrogen, halogen, hydroxy, cyano, nitro, amino, oxo, aminosulfonyl, sulfonylamido, C1-6 alkylamino, C1-6 alkyl, haloC1-6 alkyl, cyanoC1-6 alkyl, C1-6 alkoxy, haloC1-6 alkoxy, cyanoC1-6 alkoxy, C3-8cycloalkyl-oxy, C2-8 alkynyl, C1-6 alkylamino-C1-6 alkoxy, diC1-6 alkylamino-C1-6 alkoxy, C1-6 alkoxy-carbonyl, carbamoyl, carbamoyl-C1-6 alkoxy, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, 5- to 10-membered heterocyclyl, 5- to 10-membered heterocyclyl-C1-6 alkyl, 5- to 10-membered heterocyclyl-C1-6 alkoxy, or 5- to 10-membered heterocyclyl-oxy, wherein the heterocyclyl moiety is optionally substituted with one or two substituents selected from the group consisting of hydroxy, oxo, C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylsulfonyl, diC1-3 alkylsulfonyl, C1-6 alkylcarbonyl, C1-6 alkylaminocarbonyl, diC1-3 alkylaminocarbonyl, C1-6 alkylaminosulfonyl, and non-substituted or C1-6 alkyl-substituted 5- to 10-membered heterocyclyl; R5 is hydrogen, C1-6 alkyl, carbamoylC1-6 alkyl, C1-6 alkylaminoC1-6 alkyl, diC1-6 alkylaminoC1-6 alkyl, or 5- to 10-membered heterocyclylC1-6 alkyl, or is fused with R6 to form C3-4 alkylene; R6 is C1-6 alkyl, haloC1-6 alkyl, C1-6 alkoxyC1-6 alkyl, C1-6 alkylcarbonylC1-6 alkyl, C2-7 alkenyl, amino, aminoC1-6 alkyl, C3-7 cycloalkyl, 5- to 10-membered heterocyclyl, or 5- to 10-membered heterocyclyl-C1-6 alkyl, or is fused with R5 to form C3-4 alkylene, wherein the amino moiety is optionally substituted with one or two substituents selected from hydroxy or C1-6 alkyl, and the heterocyclyl moiety is optionally substituted with one to four substituents selected from the group consisting of oxo, C1-6 alkyl and C1-6 alkylcarbonyl; R7 and R8 are each independently hydrogen or C1-6 alkyl; p and q are each independently 0 or 1; r is an integer of 0 to 3, and, when r is 2 or higher, R3 moieties are the same or different; and s is an integer of 0 to 3, and, when s is 2 or higher, R4 moieties are the same or different; all of said heterocycle or heterocyclyl moieties each independently have a saturated or unsaturated single or multiple ring and contain one to three heteroatoms selected from N, O or S; and all of said aryl moieties each independently have an aromatic single or multiple ring.
地址 Gyeonggi-do KR
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