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1. 发明授权

US08569310B2 Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use 有权
标题翻译：五氟硫基亚氨基杂环化合物作为BACE-1抑制剂，组合物及其用途
公开(公告)号：US08569310B2
公开(公告)日：2013-10-29
申请号：US13391441
申请日：2010-10-06
申请人： Ulrich Iserloh , Andrew W. Stamford , Jared N Cumming
发明人： Ulrich Iserloh , Andrew W. Stamford , Jared N Cumming
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04
CPC分类号： C07D239/22 , C07D405/04
摘要： In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (a) and pharmaceutically acceptable salts thereof. Compounds of Formula (a) have the general structure: (a) wherein each variable is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供某些五氟硫亚氨基杂环化合物，包括式（a）化合物及其药学上可接受的盐。式（a）的化合物具有通式结构：（a）其中每个变量是独立选择的，如本文所定义。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和用于治疗与包括阿尔茨海默病在内的淀粉样蛋白β（Abeta）蛋白相关的病理学的方法。

2. 发明申请

US20120148603A1 PENTAFLUOROSULFUR IMINO HETEROCYCLIC COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
标题翻译： PENTAFLUOROSULFUR IMINO杂环化合物作为BACE-1抑制剂，组合物及其使用
公开(公告)号：US20120148603A1
公开(公告)日：2012-06-14
申请号：US13390856
申请日：2010-10-06
申请人： Andrew W. Stamford , Jared N Cumming
发明人： Andrew W. Stamford , Jared N Cumming
IPC分类号： A61K31/505 , C07D409/04 , A61K31/506 , A61K31/55 , A61P7/00 , A61P25/28 , A61P25/16 , A61P25/00 , A61P3/10 , C07D239/04 , A61K39/395
CPC分类号： C07D239/22 , C07D409/04
摘要： In its many embodiments, the present invention provides provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-, L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了某些五氟硫亚胺杂环化合物，包括式（I）化合物及其互变异构体，以及所述化合物和所述互变异构体的溶剂化物，前药，酯和氘代，以及所述化合物的药学上可接受的盐，互变异构体，溶剂合物，前药，酯和氘代，其中R1，R2，R3，R4，R5，R9，R11，环A，环B，m，n，p，q，r，-L1， - 和L3-是独立选择的，如本文所定义。还公开了包含一种或多种这样的化合物（单独并与一种或多种其它活性剂组合）的药物组合物及其制备和用于治疗与包括阿尔茨海默病在内的淀粉样蛋白β（A＆bgr））蛋白相关的病理学的方法。

3. 发明授权

US08557826B2 Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use 有权
标题翻译：五氟硫基亚氨基杂环化合物作为BACE-1抑制剂，组合物及其应用
公开(公告)号：US08557826B2
公开(公告)日：2013-10-15
申请号：US13390856
申请日：2010-10-06
申请人： Andrew W. Stamford , Jared N Cumming
发明人： Andrew W. Stamford , Jared N Cumming
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04
CPC分类号： C07D239/22 , C07D409/04
摘要： In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-, L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供某些五氟硫亚氨基杂环化合物，包括式（I）化合物及其互变异构体，以及所述化合物和所述互变异构体的溶剂合物，前药，酯和氘代，以及所述化合物的药学上可接受的盐，互变异构体，溶剂化物，前药，酯和氘代，其中R1，R2，R3，R4，R5，R9，R11，环A，环B，m，n，p，q，r，-L1-，和L3-是独立选择的，如本文所定义。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和用于治疗与包括阿尔茨海默病在内的淀粉样蛋白β（Abeta）蛋白相关的病理学的方法。

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