发明名称 SUBSTITUTED GEMCITABINE BICYCLIC AMIDE ANALOGS AND TREATMENT METHODS USING SAME
摘要 In one aspect, the invention relates to substituted gemcitabine aryl amide analogs, derivatives thereof, and related compounds; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating viral disorders and disorders of uncontrolled cellular proliferation using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
申请公布号 US2016052952(A1) 申请公布日期 2016.02.25
申请号 US201414783199 申请日期 2014.03.15
申请人 SUO Zucai 发明人 Suo Zucai;Vyavhare Vinod P.;Taggart David J.
分类号 C07H19/06 主分类号 C07H19/06
代理机构 代理人
主权项 1. A compound having a structure represented by a formula: wherein Ar1 is a bicyclic fused ring system comprising an aryl ring fused to a 5-, 6-, or 7-membered heterocycloalkyl; wherein the aryl ring is selected from phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, and triazinyl;wherein the aryl ring is substituted with 0, 1, 2, or 3 groups independently selected from halogen, —OH, —CN, —NH2, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 monohaloalkyl, C1-C6 polyhaloalkyl, C1-C6 alkylamino, and C1-C6 dialkylamino;wherein the heterocycloalkyl is substituted with 0, 1, 2, 3, 4, or 5 groups independently selected from halogen, —OH, —CN, —NH2, oxo, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 monohaloalkyl, C1-C6 polyhaloalkyl, C1-C6 alkylamino, C1-C6 dialkylamino, C1-C6 aminoalkyl, C1-C6 hydroxyalkyl, —(C=0)OR5, and —(C═O)NR6aR6b;wherein each R5 is independently selected from hydrogen, C1-C8 alkyl, and a hydroxyl protecting group;wherein each of R6a and R6b is independently selected from hydrogen, C1-C4 alkyl, and an amine protecting group; wherein R2 is selected from hydrogen, C1-C4 alkyl, and an amine protecting group; wherein R3 is selected from hydrogen and a hydroxyl protecting group; and wherein R4 is selected from hydrogen, C1-C8 alkyl, and a hydroxyl protecting group, or wherein R3 and R4 together comprise a divalent moiety having a structure represented by a formula: wherein each of R7a, R7b, R7c, and R7d is independently selected from methyl, ethyl, propyl, and butyl; or stereoisomer, a pharmaceutically acceptable salt, solvate, or polymorph thereof.
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