发明名称 5-aminopyrazole-4-carboxamide inhibitors of CDPK1 from <i>T. gondii </i>and <i>C. parvum</i>
摘要 The present disclosure is generally directed to compositions and methods for treating apicomplexan protozoan related disease, such as toxoplasmosis and cryptosporidiosis.
申请公布号 US9518026(B2) 申请公布日期 2016.12.13
申请号 US201414891237 申请日期 2014.05.20
申请人 University of Washington Through its Center For Commercialization 发明人 Fan Erkang;Van Voorhis Wesley C.;Zhang Zhongsheng;Huang Wenlin;Ojo Kayode K.
分类号 C07D217/00;C07D231/38;C07D311/20;C07D235/08;C07D235/12;C07D487/04;C07D231/14;C07D401/04;C07D401/06;C07D403/04;C07D405/04;C07D405/14 主分类号 C07D217/00
代理机构 McDonnell Boehnen Hulbert & Berghoff LLP 代理人 McDonnell Boehnen Hulbert & Berghoff LLP
主权项 1. A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is one of the formulas: wherein n is 0;each R7 is independently halogen, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, —OR10, —SR10, —N(R10)2, —C(O)R10, —C(O)OR10, —C(O)N(R10)2, —S(O)2R10, —OC(O)R10, —OC(O)OR10, —OC(O)N(R10)2, —N(R10)C(O)R10, —N(R10)C(O)OR10, or —N(R10)C(O)N(R10)2, wherein each R10 is independently hydrogen or C1-6 alkyl;R8 is halogen, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, or -Q-R8′;Q is —O—, —S—, —NH—, or —N(C1-6 alkyl)-;R8′ is hydrogen, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, C3-8 cycloalkyl, heterocyclyl, aryl, arylC1-6 alkyl, heteroaryl, or heteroarylC1-6 alkyl, wherein the alkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl are optionally substituted with one, two, three, or four groups that are each independently halogen, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, —OR14, —SR14, —N(R14)2, —C(O)R14, —C(O)OR14, —C(O)N(R14)2, —S(O)2R14, —OC(O)R14, —OC(O)OR14, —OC(O)N(R14)2, —N(R14)C(O)R14, —N(R14)C(O)OR14, or —N(R14)C(O)N(R14)2, wherein each R14 is independently hydrogen or C1-6 alkyl; andeach R9 is independently hydrogen or C1-6 alkyl; R2 is hydrogen, C1-6 alkyl, C1-6 haloalkyl, —C1-4 alkyl-R12, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, monocyclic heterocyclyl, monocyclic heteroaryl, or phenyl, wherein the alkyl, cycloalkyl, heterocyclyl, heteroaryl, and phenyl groups are each optionally substituted with one or two R13 groups; each R13 is independently C1-6 alkyl, C1-6 haloalkyl, —OR, —SR, —NR2, —C(O)R, —C(O)OR, —C(O)NR2, —S(O)2NR2, or —S(O)2R; andwhere R12 is —OR, —SR, —NR2, —C(O)R, —C(O)OR, —C(O)NR2, —S(O)2R, —OC(O)R, —OC(O)OR, —OC(O)NR2, —N(R)C(O)R, —N(R)C(O)OR, —N(R)C(O)NR2, phenyl, monocyclic heteroaryl, C3-8 cycloalkyl, or monocyclic heterocyclyl, wherein the aryl, heteroaryl, C3-8 cycloalkyl, and heterocyclyl groups are each optionally substituted by one, two, or three groups that are each independently halogen, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, —OR, —SR, —NR2, —C(O)R, —C(O)OR, —C(O)NR2, —S(O)2R, —OC(O)R, —OC(O)OR, —OC(O)NR2, —N(R)C(O)R, —N(R)C(O)OR, or —N(R)C(O)NR2; and each R is independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, C3-8 cycloalkyl, heterocyclyl, aryl, arylC1-6 alkyl, heteroaryl, or heteroarylC1-6 alkyl, wherein the alkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl are optionally substituted with one, two, three, or four groups that are each independently halogen, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, —OR0, —SR0, —N(R0)2, —C(O)R0, —C(O)OR0, —C(O)N(R0)2, —S(O)2R0, —OC(O)R0, —OC(O)OR0, —OC(O)N(R0)2, —N(R0)C(O)R0, —N(R0)C(O)OR0, or —N(R0)C(O)N(R0)2, wherein each R0 is independently hydrogen or C1-6 alkyl;or R2 and R3 together with the atoms to which they are attached form 2-oxo-2,3-dihydro-imidazolyl ring; R3 and R4 are independently hydrogen; and R5 and R6 are independently hydrogen.
地址 Seattle WA US