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公开(公告)号：US07858642B2
公开(公告)日：2010-12-28
申请号：US12396989
申请日：2009-03-03
申请人： Varghese John , Michel Maillard , John Tucker , Jose Aquino , Barbara Jagodzinska , Louis Brogley , Jay S. Tung , Simeon Bowers , Darren Dressen , Gary Probst , Neerav Shah
发明人： Varghese John , Michel Maillard , John Tucker , Jose Aquino , Barbara Jagodzinska , Louis Brogley , Jay S. Tung , Simeon Bowers , Darren Dressen , Gary Probst , Neerav Shah
IPC分类号： A61K31/427 , A61K31/4709 , C07D215/58 , C07D285/04
CPC分类号： C07D419/12 , C07C215/28 , C07C215/50 , C07C217/30 , C07C217/34 , C07C217/48 , C07C217/52 , C07C217/58 , C07C225/06 , C07C225/20 , C07C229/16 , C07C229/42 , C07C229/60 , C07C233/43 , C07C237/20 , C07C237/30 , C07C271/12 , C07C311/24 , C07C317/28 , C07C323/25 , C07C323/30 , C07C323/32 , C07C2601/02 , C07C2601/14 , C07C2602/04 , C07C2602/10 , C07C2602/42 , C07C2603/18 , C07C2603/74 , C07D207/323 , C07D207/325 , C07D213/38 , C07D215/42 , C07D231/12 , C07D231/38 , C07D233/54 , C07D233/64 , C07D233/88 , C07D239/42 , C07D239/48 , C07D249/04 , C07D249/06 , C07D249/14 , C07D257/04 , C07D263/34 , C07D271/113 , C07D275/02 , C07D277/42 , C07D285/08 , C07D285/10 , C07D285/135 , C07D307/52 , C07D309/14 , C07D311/74 , C07D333/36 , C07D335/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D495/04
摘要： The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
摘要翻译： 本发明涉及新化合物，还涉及使用这些化合物治疗与淀粉样变性相关的至少一种疾病，病症或病症的方法。 淀粉样变性是指与A-β蛋白异常沉积相关的疾病，病症和病症的集合。
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公开(公告)号：US20050239836A1
公开(公告)日：2005-10-27
申请号：US11075312
申请日：2005-03-09
申请人： Varghese John , Michel Maillard , John Tucker , Jose Aquino , Barbara Jagodzinska , Louis Brogley , Jay Tung , Simeon Bowers , Darren Dressen , Gary Probst , Neerav Shah
发明人： Varghese John , Michel Maillard , John Tucker , Jose Aquino , Barbara Jagodzinska , Louis Brogley , Jay Tung , Simeon Bowers , Darren Dressen , Gary Probst , Neerav Shah
IPC分类号： A61K31/382 , A61K31/453 , C07D207/32 , C07D207/325 , C07D233/54 , C07D257/04 , C07D335/06 , C07D403/12 , C07D405/12 , C07D419/12 , C07D49/02
CPC分类号： C07D419/12 , C07C215/28 , C07C215/50 , C07C217/30 , C07C217/34 , C07C217/48 , C07C217/52 , C07C217/58 , C07C225/06 , C07C225/20 , C07C229/16 , C07C229/42 , C07C229/60 , C07C233/43 , C07C237/20 , C07C237/30 , C07C271/12 , C07C311/24 , C07C317/28 , C07C323/25 , C07C323/30 , C07C323/32 , C07C2601/02 , C07C2601/14 , C07C2602/04 , C07C2602/10 , C07C2602/42 , C07C2603/18 , C07C2603/74 , C07D207/323 , C07D207/325 , C07D213/38 , C07D215/42 , C07D231/12 , C07D231/38 , C07D233/54 , C07D233/64 , C07D233/88 , C07D239/42 , C07D239/48 , C07D249/04 , C07D249/06 , C07D249/14 , C07D257/04 , C07D263/34 , C07D271/113 , C07D275/02 , C07D277/42 , C07D285/08 , C07D285/10 , C07D285/135 , C07D307/52 , C07D309/14 , C07D311/74 , C07D333/36 , C07D335/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D495/04
摘要： The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
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公开(公告)号：US20050239790A1
公开(公告)日：2005-10-27
申请号：US11075294
申请日：2005-03-09
申请人： Varghese John , Michel Maillard , John Tucker , Barbara Jagodzinska , Louis Brogley , Jay Tung , Neerav Shah , R. Neitz
发明人： Varghese John , Michel Maillard , John Tucker , Barbara Jagodzinska , Louis Brogley , Jay Tung , Neerav Shah , R. Neitz
IPC分类号： A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4747 , A61K31/4965 , C07C215/70 , C07C237/20 , C07D233/54 , C07D257/04 , C07D263/32 , C07D285/00 , C07D285/12 , C07D285/135 , C07D333/20 , C07D333/24 , C07D405/12 , C07D413/06 , C07D417/12
CPC分类号： C07D333/24 , C07C211/40 , C07C215/44 , C07C215/70 , C07C237/20 , C07C2601/14 , C07C2602/10 , C07D233/64 , C07D257/04 , C07D263/32 , C07D285/08 , C07D285/135 , C07D333/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/06 , C07D417/12
摘要： The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
摘要翻译： 本发明涉及新化合物，还涉及使用这些化合物治疗与淀粉样变性相关的至少一种疾病，病症或病症的方法。 淀粉样变性是指与A-β蛋白异常沉积相关的疾病，病症和病症的集合。
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4.发明申请OXIME DERIVATIVE SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS 审中-公开OXIME衍生的取代羟基乙酰胺ASPARTYL蛋白酶抑制剂公开(公告)号：US20090042961A1
公开(公告)日：2009-02-12
申请号：US12117094
申请日：2008-05-08
申请人： Varghese John , Michel Maillard , Barbara Jagodzinska , Jose Aquino , Gary Probst , Jay Tung
发明人： Varghese John , Michel Maillard , Barbara Jagodzinska , Jose Aquino , Gary Probst , Jay Tung
IPC分类号： A61K31/165 , A61P43/00 , C07D257/04 , C07C233/36 , C07C243/20 , C07D405/10 , A61K31/4155 , A61K31/41 , C07D231/12 , A61K31/415 , C07D231/54 , A61K31/416
CPC分类号： C07D285/08 , C07C233/36 , C07C237/20 , C07C251/44 , C07C251/54 , C07C251/84 , C07C255/42 , C07C255/58 , C07C2601/04 , C07C2601/14 , C07D213/40 , C07D231/12 , C07D231/56 , C07D233/64 , C07D257/04 , C07D261/20 , C07D271/10 , C07D335/06 , C07D405/10
摘要： The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
摘要翻译： 本发明涉及治疗与淀粉样变性相关的疾病，病症和病症的新化合物和方法。 淀粉样变性是指与A-β蛋白异常沉积相关的疾病，病症和病症的集合。
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5.发明申请Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors 失效肟衍生物取代的羟乙基胺天冬氨酰蛋白酶抑制剂公开(公告)号：US20070149584A9
公开(公告)日：2007-06-28
申请号：US11177324
申请日：2005-07-11
申请人： Varghese John , Michel Maillard , Barbara Jagodzinska , Jose Aquino , Gary Probst , Jay Tung
发明人： Varghese John , Michel Maillard , Barbara Jagodzinska , Jose Aquino , Gary Probst , Jay Tung
IPC分类号： A61K31/42 , A61K31/416 , A61K31/165
CPC分类号： C07D285/08 , C07C233/36 , C07C237/20 , C07C251/44 , C07C251/54 , C07C251/84 , C07C255/42 , C07C255/58 , C07C2601/04 , C07C2601/14 , C07D213/40 , C07D231/12 , C07D231/56 , C07D233/64 , C07D257/04 , C07D261/20 , C07D271/10 , C07D335/06 , C07D405/10
摘要： The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
摘要翻译： 本发明涉及治疗与淀粉样变性相关的疾病，病症和病症的新化合物和方法。 淀粉样变性是指与A-β蛋白异常沉积相关的疾病，病症和病症的集合。
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6.发明申请Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors 失效肟衍生物取代的羟乙基胺天冬氨酰蛋白酶抑制剂公开(公告)号：US20060135581A1
公开(公告)日：2006-06-22
申请号：US11177324
申请日：2005-11-17
申请人： Varghese John , Michel Maillard , Barbara Jagodzinska , Jose Aquino , Gary Probst , Jay Tung
发明人： Varghese John , Michel Maillard , Barbara Jagodzinska , Jose Aquino , Gary Probst , Jay Tung
IPC分类号： A61K31/42 , A61K31/416 , A61K31/165
CPC分类号： C07D285/08 , C07C233/36 , C07C237/20 , C07C251/44 , C07C251/54 , C07C251/84 , C07C255/42 , C07C255/58 , C07C2601/04 , C07C2601/14 , C07D213/40 , C07D231/12 , C07D231/56 , C07D233/64 , C07D257/04 , C07D261/20 , C07D271/10 , C07D335/06 , C07D405/10
摘要： The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
摘要翻译： 本发明涉及治疗与淀粉样变性相关的疾病，病症和病症的新化合物和方法。 淀粉样变性是指与A-β蛋白异常沉积相关的疾病，病症和病症的集合。
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7.发明授权Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors 失效肟衍生物取代的羟乙基胺天冬氨酰蛋白酶抑制剂公开(公告)号：US07385085B2
公开(公告)日：2008-06-10
申请号：US11177324
申请日：2005-07-11
申请人： Varghese John , Michel Maillard , Barbara Jagodzinska , Jose Aquino , Gary Probst , Jay Tung
发明人： Varghese John , Michel Maillard , Barbara Jagodzinska , Jose Aquino , Gary Probst , Jay Tung
IPC分类号： C07C237/04
CPC分类号： C07D285/08 , C07C233/36 , C07C237/20 , C07C251/44 , C07C251/54 , C07C251/84 , C07C255/42 , C07C255/58 , C07C2601/04 , C07C2601/14 , C07D213/40 , C07D231/12 , C07D231/56 , C07D233/64 , C07D257/04 , C07D261/20 , C07D271/10 , C07D335/06 , C07D405/10
摘要： The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
摘要翻译： 本发明涉及治疗与淀粉样变性相关的疾病，病症和病症的新化合物和方法。 淀粉样变性是指与A-β蛋白异常沉积相关的疾病，病症和病症的集合。
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公开(公告)号：US20070213316A1
公开(公告)日：2007-09-13
申请号：US11636903
申请日：2006-12-11
申请人： Varghese John , Michel Maillard , Barbara Jagodzinska , James Beck , Andrea Gailunas , John Freskos , John Mickelson , Lakshman Samala , Jennifer Sealy , Ruth TenBrink , Lawrence Fang , Roy Hom
发明人： Varghese John , Michel Maillard , Barbara Jagodzinska , James Beck , Andrea Gailunas , John Freskos , John Mickelson , Lakshman Samala , Jennifer Sealy , Ruth TenBrink , Lawrence Fang , Roy Hom
IPC分类号： A61K31/553 , A61K31/554 , A61K31/55 , A61K31/54 , A61K31/5377 , A61K31/275 , A61K31/4965
CPC分类号： C07D263/32 , C07C233/36 , C07C233/40 , C07C233/58 , C07C233/78 , C07C235/20 , C07C235/50 , C07C235/74 , C07C237/04 , C07C237/06 , C07C237/08 , C07C237/22 , C07C237/42 , C07C251/38 , C07C255/58 , C07C271/28 , C07C271/44 , C07C311/08 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/37 , C07C317/46 , C07C317/50 , C07C323/60 , C07C323/62 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/267 , C07D207/27 , C07D209/42 , C07D211/58 , C07D211/60 , C07D211/96 , C07D213/71 , C07D213/80 , C07D213/82 , C07D213/85 , C07D215/36 , C07D215/42 , C07D215/48 , C07D215/56 , C07D217/22 , C07D231/14 , C07D231/38 , C07D233/84 , C07D233/90 , C07D237/14 , C07D239/28 , C07D239/42 , C07D239/48 , C07D241/20 , C07D241/24 , C07D241/44 , C07D243/08 , C07D249/06 , C07D249/10 , C07D251/46 , C07D251/54 , C07D257/04 , C07D257/06 , C07D261/08 , C07D261/14 , C07D261/18 , C07D263/34 , C07D263/48 , C07D263/54 , C07D263/58 , C07D265/36 , C07D271/08 , C07D271/12 , C07D275/06 , C07D277/30 , C07D277/36 , C07D277/56 , C07D277/68 , C07D277/82 , C07D279/16 , C07D285/06 , C07D285/10 , C07D285/135 , C07D295/155 , C07D295/185 , C07D295/192 , C07D295/26 , C07D307/20 , C07D307/46 , C07D307/68 , C07D307/84 , C07D307/86 , C07D307/91 , C07D311/04 , C07D333/22 , C07D333/32 , C07D333/34 , C07D333/38 , C07D333/62 , C07D333/68 , C07D335/06 , C07D401/04 , C07D405/12 , C07D409/04 , C07D411/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/06 , C07D473/08 , C07D473/16 , C07D487/04 , C07D495/04
摘要： Disclosed are compounds of the formula wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of beta-secretase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.
摘要翻译： 公开了下式的化合物，其中R 1，R 2，R 1，R 2，R 2，R 2， ＆lt; 2＆gt;和＆lt; 3＆gt;如本文所定义。 这些化合物具有作为β-分泌酶抑制剂的活性，因此可用于治疗诸如阿尔茨海默氏病之类的各种紊乱。
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公开(公告)号：US07176242B2
公开(公告)日：2007-02-13
申请号：US10291318
申请日：2002-11-08
申请人： Varghese John , Michel Maillard , Barbara Jagodzinska , James Beck , Andrea Gailunas , John Freskos , John Mickelson , Lakshman Samala , Jennifer Sealy , Ruth TenBrink , Lawrence Fang , Roy Hom
发明人： Varghese John , Michel Maillard , Barbara Jagodzinska , James Beck , Andrea Gailunas , John Freskos , John Mickelson , Lakshman Samala , Jennifer Sealy , Ruth TenBrink , Lawrence Fang , Roy Hom
IPC分类号： A61K31/133 , C07C217/00
CPC分类号： C07D263/32 , C07C233/36 , C07C233/40 , C07C233/58 , C07C233/78 , C07C235/20 , C07C235/50 , C07C235/74 , C07C237/04 , C07C237/06 , C07C237/08 , C07C237/22 , C07C237/42 , C07C251/38 , C07C255/58 , C07C271/28 , C07C271/44 , C07C311/08 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/37 , C07C317/46 , C07C317/50 , C07C323/60 , C07C323/62 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/267 , C07D207/27 , C07D209/42 , C07D211/58 , C07D211/60 , C07D211/96 , C07D213/71 , C07D213/80 , C07D213/82 , C07D213/85 , C07D215/36 , C07D215/42 , C07D215/48 , C07D215/56 , C07D217/22 , C07D231/14 , C07D231/38 , C07D233/84 , C07D233/90 , C07D237/14 , C07D239/28 , C07D239/42 , C07D239/48 , C07D241/20 , C07D241/24 , C07D241/44 , C07D243/08 , C07D249/06 , C07D249/10 , C07D251/46 , C07D251/54 , C07D257/04 , C07D257/06 , C07D261/08 , C07D261/14 , C07D261/18 , C07D263/34 , C07D263/48 , C07D263/54 , C07D263/58 , C07D265/36 , C07D271/08 , C07D271/12 , C07D275/06 , C07D277/30 , C07D277/36 , C07D277/56 , C07D277/68 , C07D277/82 , C07D279/16 , C07D285/06 , C07D285/10 , C07D285/135 , C07D295/155 , C07D295/185 , C07D295/192 , C07D295/26 , C07D307/20 , C07D307/46 , C07D307/68 , C07D307/84 , C07D307/86 , C07D307/91 , C07D311/04 , C07D333/22 , C07D333/32 , C07D333/34 , C07D333/38 , C07D333/62 , C07D333/68 , C07D335/06 , C07D401/04 , C07D405/12 , C07D409/04 , C07D411/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/06 , C07D473/08 , C07D473/16 , C07D487/04 , C07D495/04
摘要： Disclosed are compounds of the formula wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of beta-secretase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.
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公开(公告)号：US07727997B2
公开(公告)日：2010-06-01
申请号：US11636903
申请日：2006-12-11
申请人： Varghese John , Michel Maillard , Barbara Jagodzinska , James Beck , Andrea Gailunas , John Freskos , John Mickelson , Lakshman Samala , Jennifer Sealey , Ruth Tenbrink , Larry Fang , Roy Hom
发明人： Varghese John , Michel Maillard , Barbara Jagodzinska , James Beck , Andrea Gailunas , John Freskos , John Mickelson , Lakshman Samala , Jennifer Sealey , Ruth Tenbrink , Larry Fang , Roy Hom
IPC分类号： A61K31/133 , C07D217/00
CPC分类号： C07D263/32 , C07C233/36 , C07C233/40 , C07C233/58 , C07C233/78 , C07C235/20 , C07C235/50 , C07C235/74 , C07C237/04 , C07C237/06 , C07C237/08 , C07C237/22 , C07C237/42 , C07C251/38 , C07C255/58 , C07C271/28 , C07C271/44 , C07C311/08 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/37 , C07C317/46 , C07C317/50 , C07C323/60 , C07C323/62 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/267 , C07D207/27 , C07D209/42 , C07D211/58 , C07D211/60 , C07D211/96 , C07D213/71 , C07D213/80 , C07D213/82 , C07D213/85 , C07D215/36 , C07D215/42 , C07D215/48 , C07D215/56 , C07D217/22 , C07D231/14 , C07D231/38 , C07D233/84 , C07D233/90 , C07D237/14 , C07D239/28 , C07D239/42 , C07D239/48 , C07D241/20 , C07D241/24 , C07D241/44 , C07D243/08 , C07D249/06 , C07D249/10 , C07D251/46 , C07D251/54 , C07D257/04 , C07D257/06 , C07D261/08 , C07D261/14 , C07D261/18 , C07D263/34 , C07D263/48 , C07D263/54 , C07D263/58 , C07D265/36 , C07D271/08 , C07D271/12 , C07D275/06 , C07D277/30 , C07D277/36 , C07D277/56 , C07D277/68 , C07D277/82 , C07D279/16 , C07D285/06 , C07D285/10 , C07D285/135 , C07D295/155 , C07D295/185 , C07D295/192 , C07D295/26 , C07D307/20 , C07D307/46 , C07D307/68 , C07D307/84 , C07D307/86 , C07D307/91 , C07D311/04 , C07D333/22 , C07D333/32 , C07D333/34 , C07D333/38 , C07D333/62 , C07D333/68 , C07D335/06 , C07D401/04 , C07D405/12 , C07D409/04 , C07D411/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/06 , C07D473/08 , C07D473/16 , C07D487/04 , C07D495/04
摘要： Disclosed are compounds of the formula wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of beta-secretase and are therefore useful in treating a variety of disorders such as Alzheimer's Disease.
摘要翻译： 公开了下式的化合物，其中变量RN，RC，R1，R25，R2和R3如本文所定义。 这些化合物具有作为β-分泌酶抑制剂的活性，因此可用于治疗多种疾病如阿尔茨海默病。
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