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公开(公告)号：US20060128715A1
公开(公告)日：2006-06-15
申请号：US11177348
申请日：2005-07-11
申请人： Jennifer Sealy , Roy Hom , Varghese John , Gary Probst , Jay Tung
发明人： Jennifer Sealy , Roy Hom , Varghese John , Gary Probst , Jay Tung
IPC分类号： A61K31/4965 , A61K31/513 , A61K31/50 , A61K31/381 , A61K31/416 , A61K31/4015 , A61K31/44 , A61K31/165
CPC分类号： C07D239/74 , C07C233/36 , C07C237/18 , C07C251/44 , C07C251/54 , C07C251/58 , C07C251/84 , C07C255/31 , C07C255/61 , C07C2601/14 , C07D207/335 , C07D213/40 , C07D213/53 , C07D231/12 , C07D231/56 , C07D239/18 , C07D239/26 , C07D261/20 , C07D307/52 , C07D317/72 , C07D333/22 , C07D403/10 , C07D405/10 , C07D409/04 , C07D409/10
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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2.发明申请Methods of treatment of amyloidosis using spirocyclohexane aspartyl-protease inhibitors 审中-公开使用螺环己烷天冬氨酰蛋白酶抑制剂治疗淀粉样变性的方法公开(公告)号：US20060014790A1
公开(公告)日：2006-01-19
申请号：US11038790
申请日：2005-01-21
申请人： Varghese John , Roy Hom , Jennifer Sealy , Jose Aquino , Gary Probst , Jay Tung , Lawrence Fang
发明人： Varghese John , Roy Hom , Jennifer Sealy , Jose Aquino , Gary Probst , Jay Tung , Lawrence Fang
IPC分类号： A61K31/445 , A61K31/38 , A61K31/165 , A61K31/381
CPC分类号： A61K31/38 , A61K31/165 , A61K31/381 , A61K31/445
摘要： The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in 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： 本发明涉及可用于治疗与淀粉样变性相关的疾病，病症和病症的乙酰基2-羟基-1,3-二氨基螺环己烷及其衍生物。 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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5.发明申请Methods of treatment of amyloidosis using bi-aryl aspartyl protease inhibitors 审中-公开使用双芳基天冬氨酰蛋白酶抑制剂治疗淀粉样变性的方法公开(公告)号：US20060014737A1
公开(公告)日：2006-01-19
申请号：US11075445
申请日：2005-03-09
申请人： Varghese John , Roy Hom , Jennifer Sealy , John Tucker
发明人： Varghese John , Roy Hom , Jennifer Sealy , John Tucker
IPC分类号： A61K31/54 , A61K31/5377 , A61K31/495 , A61K31/138 , A61K31/445
CPC分类号： A61K31/138 , A61K31/445 , A61K31/495 , A61K31/5377 , A61K31/54
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：US06737420B2
公开(公告)日：2004-05-18
申请号：US09815960
申请日：2001-03-23
申请人： Roy Hom , Shumeye S. Mamo , Jay Tung , Andrea Gailunas , Varghese John , Lawrence Y. Fang
发明人： Roy Hom , Shumeye S. Mamo , Jay Tung , Andrea Gailunas , Varghese John , Lawrence Y. Fang
IPC分类号： A01N5502
CPC分类号： C07C237/22 , A61K38/00 , C07B2200/07 , C07C271/14 , C07C271/18 , C07C271/22 , C07C2601/14 , C07C2603/74 , C07D261/20 , C07D295/13 , C07D295/185 , C07D307/14 , C07D307/33 , C07D307/52 , C07K5/0207 , C07K7/02
摘要： The present invention is directed toward substituted hydroxyethylene compounds of formula (XII): useful in treating Alzheimer's disease and other similar diseases.
摘要翻译： 本发明涉及式（XII）的取代羟基亚乙基化合物：可用于治疗阿尔茨海默氏病和其它类似疾病。
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公开(公告)号：US06864240B1
公开(公告)日：2005-03-08
申请号：US09594978
申请日：2000-06-15
申请人： Varghese John , Jay Tung , Roy Hom , Ashley Guinn , Lawrence Fang , Andrea Gailunas , Shumeye S. Mamo
发明人： Varghese John , Jay Tung , Roy Hom , Ashley Guinn , Lawrence Fang , Andrea Gailunas , Shumeye S. Mamo
CPC分类号： C07K5/101 , C07K5/0205
摘要： Dipeptide derived inhibitors of the β-secretase enzyme are provided which are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of Aβ peptide in a mammal. The compounds of the invention provide useful methods of treatment by administration of these inhibitors to reduce Aβ peptide formation and in pharmaceutical compositions.
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公开(公告)号：US07276484B2
公开(公告)日：2007-10-02
申请号：US11075232
申请日：2005-03-08
申请人： Varghese John , Jay Tung , Roy Hom , Ashley Guinn , Lawrence Fang , Andrea Gailunas , Shumeye S. Mamo
发明人： Varghese John , Jay Tung , Roy Hom , Ashley Guinn , Lawrence Fang , Andrea Gailunas , Shumeye S. Mamo
IPC分类号： C07K5/06
CPC分类号： C07K5/101 , C07K5/0205
摘要： Dipeptide derived inhibitors of the β-secretase enzyme are provided which are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of Aβ peptide in a mammal. The compounds of the invention provide useful methods of treatment by administration of these inhibitors to reduce Aβ peptide formation and in pharmaceutical compositions.
摘要翻译： 提供了二肽衍生的β-分泌酶的抑制剂，其可用于治疗阿尔茨海默病和以哺乳动物中Abeta肽沉积为特征的其它疾病。 本发明的化合物提供了通过施用这些抑制剂以减少Aβ肽形成和药物组合物治疗的有用方法。
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公开(公告)号：US06992081B2
公开(公告)日：2006-01-31
申请号：US09960634
申请日：2001-09-21
申请人： Roy Hom , Shumeye Mamo , Jay Tung , Andrea Gailunas , Varghese John , Lawrence Fang
发明人： Roy Hom , Shumeye Mamo , Jay Tung , Andrea Gailunas , Varghese John , Lawrence Fang
IPC分类号： A01N43/46 , A01N43/58 , A61K31/55 , A61K31/54 , A61K31/535
CPC分类号： C07D295/185 , A61K38/00 , C07B2200/07 , C07C237/22 , C07C271/14 , C07C271/18 , C07C271/22 , C07C2601/14 , C07C2603/74 , C07D261/20 , C07D295/13 , C07D307/14 , C07D307/33 , C07D307/52 , C07D403/02 , C07D413/02 , C07D417/02 , C07K5/0207 , C07K7/02
摘要： The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.
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10.发明申请Substituted urea and carbamate, phenacyl-2-hydroxy-3-diaminoalkane, and benzamide-2-hydroxy-3-diaminoalkane aspartyl-protease inhibitors 审中-公开取代的脲和氨基甲酸酯，苯甲酰甲基-2-羟基-3-二氨基烷烃和苯甲酰胺-2-羟基-3-二氨基烷烃天冬氨酰蛋白酶抑制剂公开(公告)号：US20050261273A1
公开(公告)日：2005-11-24
申请号：US11075292
申请日：2005-03-09
申请人： Varghese John , Michel Maillard , John Tucker , Jose Aquino , Roy Hom , Jay Tung , Darren Dressen , Neerav Shah , R. Neitz
发明人： Varghese John , Michel Maillard , John Tucker , Jose Aquino , Roy Hom , Jay Tung , Darren Dressen , Neerav Shah , R. Neitz
IPC分类号： A61K31/16 , A61K31/40 , A61K31/445 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/553 , C07C215/28 , C07C229/42 , C07C229/60 , C07C233/40 , C07C235/10 , C07C235/42 , C07C235/74 , C07C235/82 , C07C237/14 , C07C237/30 , C07C239/16 , C07C255/34 , C07C275/06 , C07C275/14 , C07C275/26 , C07C275/28 , C07C311/03 , C07C311/05 , C07C311/07 , C07C311/08 , C07C323/30 , C07C323/59 , C07C327/46 , C07D205/04 , C07D207/16 , C07D207/28 , C07D209/12 , C07D209/18 , C07D211/56 , C07D211/58 , C07D211/94 , C07D213/56 , C07D213/81 , C07D213/82 , C07D231/14 , C07D233/30 , C07D233/46 , C07D233/54 , C07D233/76 , C07D233/90 , C07D239/26 , C07D241/24 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/14 , C07D261/18 , C07D277/14 , C07D277/28 , C07D277/56 , C07D307/00 , C07D307/24 , C07D307/54 , C07D307/68 , C07D309/14 , C07D311/96 , C07D317/72 , C07D333/20 , C07D333/24 , C07D333/28 , C07D333/38 , C07D335/06 , C07D405/10 , C07D407/12 , C07F9/40
CPC分类号： C07D335/06 , A61K31/16 , C07C215/28 , C07C229/42 , C07C229/60 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/74 , C07C235/82 , C07C237/30 , C07C239/16 , C07C255/34 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/26 , C07C311/03 , C07C311/05 , C07C311/07 , C07C311/08 , C07C323/30 , C07C323/59 , C07C327/46 , C07C2601/02 , C07C2601/10 , C07C2601/14 , C07C2602/10 , C07C2603/74 , C07D205/04 , C07D207/16 , C07D207/28 , C07D209/12 , C07D209/18 , C07D209/42 , C07D211/56 , C07D211/58 , C07D211/94 , C07D213/56 , C07D213/81 , C07D213/82 , C07D231/14 , C07D233/30 , C07D233/46 , C07D233/58 , C07D233/64 , C07D233/76 , C07D233/90 , C07D239/26 , C07D241/24 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/14 , C07D261/18 , C07D277/14 , C07D277/24 , C07D277/28 , C07D277/56 , C07D307/00 , C07D307/24 , C07D307/54 , C07D307/68 , C07D309/14 , C07D311/96 , C07D317/72 , C07D333/18 , C07D333/20 , C07D333/24 , C07D333/28 , C07D333/38 , C07D405/10 , C07D407/12 , C07F9/4006
摘要： The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating at least one disease, disorder, and condition associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and condition associated with abnormal deposition of A-beta protein.
摘要翻译： 本发明涉及可用于治疗与淀粉样变性相关的至少一种疾病，病症和状况的乙酰基2-羟基-1,3-二氨基螺环己烷及其衍生物。 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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