发明名称 Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists
摘要 Embodiments of the invention include substituted indole compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition.
申请公布号 US9572794(B2) 申请公布日期 2017.02.21
申请号 US201514820488 申请日期 2015.08.06
申请人 Vanderbilt University 发明人 Hamm Heidi E.;Stauffer Shaun R.;Lindsley Craig W.;Wen Wandong;Young Summer E.;Duvernay Matthew T.;Temple Kayla J.
分类号 A61K31/404;A61K31/407;A61K31/437;C07D209/10;C07D209/30;C07D239/00;C07D401/04;C07D513/04;A61K31/4985;A61K31/519;A61K31/5025;C07D221/00;C07D237/00;C08L67/02;C08L69/00 主分类号 A61K31/404
代理机构 Stites & Harbison PLLC 代理人 Stites & Harbison PLLC ;Myers, Jr. Richard S.
主权项 1. A compound having a structure represented by formula (I): wherein: Q1 is selected from N and CR1a;Q2 is selected from N and CR1b, or can optionally cyclize with Q3 to form a C5 or C6 saturated heterocycle;Q3 is selected from N and CR1c, or can optionally cyclize with Q2 to form a C5 or C6 saturated heterocycle;Q4 is selected from N and CR1d; and wherein 0, 1, or 2 of Q1, Q2, Q3 and Q4 are N;R1a, R1b, R1c, and R1d, when present, are each independently selected from hydrogen, halogen, hydroxyl, cyano, C1-C3 alkyl sulfone, C1-C3 polyhaloalkyl sulfone, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 polyhaloalkyl, C1-C6 alkoxy, (C1-C6) alkoxy-(C1-C6) alkyl, (C1-C6) alkylamino, (C1-C6) haloalkyl-oxy-(C1-C6) alkyl, (C1-C6) polyhaloalkyl-oxy-(C1-C6) alkyl, (C1-C6) polyhaloalkyl-(C1-C6) alkoxy, and (C1-C6) dialkylamino; n is 0-5;X is independently selected from optionally substituted CH2-aryl, CH2-heteroaryl, CH2-biaryl, or wherein:Q5 is selected from N, CR1a, and R1a; andn is 0-5;R2 is selected from hydrogen, C1-C3 alkyl, C1-C3 haloalkyl, and C1-C3 polyhaloalkyl, (C1-C3) polyhaloalkyl-oxy-(C1-C3) alkyl, and (C1-C3) haloalkyl-oxy-(C1-C3) alkyl, andA is optionally substituted and chosen from imidazolyl, oxadiazolyl, oxazolyl, pyrazinyl, pyrazolyl, pyridinyl, pyrimidinyl, thiadiazolyl, thiazolyl, imidazothiadiazolyl, imidazooxadiazole, imidazothiazole, thiazolotriazole, and triazolyl;or a pharmaceutically acceptable salt, solvate, or polymorph thereof.
地址 Nashville TN US