发明名称 AMIDE DERIVATIVES OF ANILINE-RELATED COMPOUNDS AND COMPOSITIONS THEREOF
摘要 Amide derivatives of aniline-related compounds are disclosed, including salts thereof, and compositions, preparations and uses thereof. In certain embodiments, the amide derivatives and/or salts thereof show higher solubility in water compared to the corresponding parent aniline-related compounds.
申请公布号 US2015284360(A1) 申请公布日期 2015.10.08
申请号 US201514677753 申请日期 2015.04.02
申请人 C&C BIOPHARMA, LLC 发明人 CHEN Lin;WU Yongqing;GAI Dahai;CHEN Xiaojiang
分类号 C07D401/04;C07C235/74;C07D213/56 主分类号 C07D401/04
代理机构 代理人
主权项 1. A compound comprising a structure of Structure X:including crystals, stereoisomers, pharmaceutically acceptable solvates, and pharmaceutically acceptable salts thereof, further including mixtures thereof in all ratios, wherein: each RA1-RA4 are independently selected from the group consisting of H, F, Cl, Br, and I; X2 is selected from the group consisting of —C(═O)—NH— and —NH—C(═O)—; L1 is —(CH2)n—, wherein n is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, and any one or more of the —CH2— may be replaced by a group selected from the group consisting of aryl, heteroaryl, cycloalkyl, heterocycloalkyl, substituted aryl, substituted heteroaryl, substituted cycloalkyl, substituted heterocycloalkyl, —O—, —S—, —C(═O)—, —S(═O)—, —S(═O)2—, —NH—C(═O)—, —C(═O)—NH—, —NR—, —C═C—, and —C≡C—; X1 is selected from the group consisting of —C(═O)—NH—, —NH—C(═O)—, and —NH—; Y1 is selected from the group consisting of H, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, substituted aryl, substituted heteroaryl, substituted cycloalkyl, substituted heterocycloalkyl, —OH, —SH, and —NH2; Y2 is —(CH2)p—, wherein p is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10, and any one or more of the —CH2— may be replaced by a group selected from the group consisting of alkyl, —C═C—, —C≡C—, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, substituted aryl, substituted heteroaryl, substituted cycloalkyl, substituted heterocycloalkyl, —O—, —S—, —N—, —C(═O)—, and —C(═S)—; X is S, P or C, wherein: when X is S, and m is 2, Rx is selected from the group consisting of H, alkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, substituted alkyl, substituted aryl, substituted heteroaryl, substituted cycloalkyl, and substituted heterocycloalkyl; and Ry is nothing; when X is P, and m is 1, Rx and Ry are independently selected from the group consisting of H, alkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, substituted alkyl, substituted aryl, substituted heteroaryl, substituted cycloalkyl, and substituted heterocycloalkyl; when X is C, and m is 0, Rx is H, and Ry is  and when X is C, and m is 1, Rx is nothing, and Ry is alkyl, alkyl carboxyl,  whereinR1 selected from the group consisting of H,alkyl, and alkyl further substituted with aryl, heteroaryl, amino, hydroxide, hydroxide aryl, hydroxide carbonyl, amino carbonyl, thiol, alkyl-S—, or guanidinyl; and R3 is alkyl.
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