发明名称 NOVEL FAP INHIBITORS
摘要 The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.;
申请公布号 US2014357650(A1) 申请公布日期 2014.12.04
申请号 US201314372798 申请日期 2013.01.17
申请人 UNIVERSITEIT ANTWERPEN ;Fox Chase Cancer Center 发明人 Jansen Koen;De Meester Ingrid;Heirbaut Leen;Cheng Jonathan D.;Joossens Jurgen;Augustyns Koen;Van Der Veken Pieter
分类号 C07D487/04;C07D471/04;C07D417/12;C07D413/12;C07D401/12;C07D403/12 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of Formula X or a stereoisomer, tautomer, racemic, salt, hydrate, or solvate thereof, Wherein R1 and R2 are each independently selected from the group consisting of —H, OH, -halo, C1-6alkyl, —O—C1-6alkyl, and S—C1-6alkyl; R3 is selected from the group consisting of —H, —CN, —B(OH)2, —C(O)alkyl, —C(O)aryl-, —C═C—C(O)aryl, —C═C—S(O)2aryl, —CO2H, —SO3H, —SO2NH2, —PO3H2, and 5-tetrazolyl; R4 is —H; R5, R6 and R7 are each independently selected from the group consisting of —H, —OH, -oxo, -halo, —C1-6alkyl, —O—C1-6alkyl, —S—C1-6alkyl, —NR8R9, —OR12 -Het2 and —Ar2; each of said C1-6alkyl being optionally substituted with from 1 to 3 substituents selected from —OH and -halo; R8, R9 and R12 are each independently selected from the group consisting of —H, —OH, -halo, —C1-6alkyl, —O—C1-6alkyl, —S—C1-6alkyl, and —Ar3; R10, R11, R13 and R14 are each independently selected from the group consisting of —H, —OH, -halo, —C1-6alkyl, —O—C1-6alkyl, and —S—C1-6alkyl; Ar1, Ar2 and Ar3 are each independently a 5- or 6-membered aromatic monocycle optionally comprising 1 or 2 heteroatoms selected from O, N and S; each of said Ar1, Ar2 and Ar3 being optionally and independently substituted with from 1 to 3 substituents selected from —NR10R11, —C1-6alkyl, —O—C1-6alkyl, and —S—C1-6alkyl; Het2 is a 5- or 6-membered non-aromatic monocycle optionally comprising 1 or 2 heteroatoms selected from O, N and S; said Het2 being optionally substituted with from 1 to 3 substituents selected from —NR13R14, —C1-6alkyl, —O—C1-6alkyl, and —S—C1-6alkyl; n is 0, 1, 2, or 3; andrepresents a 5 to 10-membered N-containing aromatic or non-aromatic mono- or bicyclic heterocycle, said heterocycle optionally further comprising 1, 2 or 3 heteroatoms selected from O, N and S.
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