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公开(公告)号:US07763646B2
公开(公告)日:2010-07-27
申请号:US10529504
申请日:2003-09-26
申请人: Roy Hom , Varghese John
发明人: Roy Hom , Varghese John
IPC分类号: A61K31/382 , C07D335/06
CPC分类号: C07C233/78 , C07C311/18 , C07D335/06
摘要: The invention relates to compounds of formula (I). Useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
摘要翻译: 本发明涉及式(I)化合物。 用于治疗阿尔茨海默病和其他类似疾病。 这些化合物包括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Aβ肽沉积为特征的其它疾病。 本发明的化合物可用于降低Aβ肽形成的药物组合物和治疗方法。
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公开(公告)号:US20090074746A1
公开(公告)日:2009-03-19
申请号:US12074696
申请日:2004-09-24
申请人: Lawrence Y. Fang , Roy Hom , Varghese John , Michel Maillard
发明人: Lawrence Y. Fang , Roy Hom , Varghese John , Michel Maillard
IPC分类号: A61K31/166 , C07C233/64 , A61P25/00 , C12N9/50 , A61K39/395 , A61K38/00 , C12N9/99 , A61P25/28
CPC分类号: C07D295/13 , C07C215/28 , C07C233/78 , C07C235/84 , C07C239/20 , C07C243/22 , C07C243/28 , C07C271/16 , C07C271/18 , C07C275/24 , C07C311/03 , C07C311/08 , C07C311/13 , C07C311/16 , C07C311/37 , C07C317/44 , C07C323/60 , C07D211/60 , C07D215/12 , C07D277/04 , C07D303/36 , C07D307/52 , C07D307/54 , C07D333/24
摘要: The present invention is substituted amines of formula (X) useful in treating Alzheimer's disease and other similar diseases.
摘要翻译: 本发明是用于治疗阿尔茨海默病和其他类似疾病的式(X)的取代胺。
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公开(公告)号:US07214715B2
公开(公告)日:2007-05-08
申请号:US09896139
申请日:2001-06-29
申请人: James P. Beck , Lawrence Y. Fang , John N. Freskos , Andrea Gailunas , Roy Hom , Barbara Jagodzinska , Varghese John , Michel Maillard , Shon R. Pulley , Ruth E. TenBrink
发明人: James P. Beck , Lawrence Y. Fang , John N. Freskos , Andrea Gailunas , Roy Hom , Barbara Jagodzinska , Varghese John , Michel Maillard , Shon R. Pulley , Ruth E. TenBrink
IPC分类号: A61K31/166 , C07D233/78
CPC分类号: C07D295/26 , C07C215/28 , C07C233/78 , C07C235/84 , C07C239/20 , C07C243/22 , C07C243/28 , C07C271/16 , C07C271/18 , C07C275/24 , C07C311/03 , C07C311/08 , C07C311/13 , C07C311/16 , C07C311/37 , C07C317/44 , C07C323/60 , C07D211/60 , C07D215/12 , C07D277/04 , C07D295/13 , C07D303/36 , C07D307/52 , C07D307/54 , C07D333/24 , Y02P20/55 , Y02P20/582
摘要: The present invention is substituted amines of formula (X) and of the formula (X′) useful in treating Alzheimer's disease and other similar diseases.
摘要翻译: 本发明是用于治疗阿尔茨海默病和其他类似疾病的式(X)和式(X')的取代胺。
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公开(公告)号:US20050203096A1
公开(公告)日:2005-09-15
申请号:US11042695
申请日:2005-01-25
申请人: James Beck , Andrea Gailunas , Roy Hom , Barbara Jagodzinska , Varghese John , Michel Maillard
发明人: James Beck , Andrea Gailunas , Roy Hom , Barbara Jagodzinska , Varghese John , Michel Maillard
IPC分类号: A61P25/28 , C07C215/28 , C07C233/78 , C07C235/84 , C07C239/20 , C07C243/22 , C07C243/28 , C07C271/16 , C07C271/18 , C07C275/24 , C07C311/03 , C07C311/08 , C07C311/13 , C07C311/16 , C07C311/37 , C07C317/44 , C07C323/60 , C07D211/60 , C07D215/12 , C07D223/10 , C07D277/04 , C07D295/13 , C07D303/36 , C07D307/52 , C07D307/54 , C07D333/24 , A61K31/522 , A61K31/454 , A61K31/496 , A61K31/501
CPC分类号: C07D295/13 , C07C215/28 , C07C233/78 , C07C235/84 , C07C239/20 , C07C243/22 , C07C243/28 , C07C271/16 , C07C271/18 , C07C275/24 , C07C311/03 , C07C311/08 , C07C311/13 , C07C311/16 , C07C311/37 , C07C317/44 , C07C323/60 , C07D211/60 , C07D215/12 , C07D223/10 , C07D277/04 , C07D303/36 , C07D307/52 , C07D307/54 , C07D333/24
摘要: The present invention is disubstituted amines of formula (I) and disubstituted amines of formula (II) useful in treating Alzheimer's disease and other similar diseases.
摘要翻译: 本发明是式(I)的二取代胺和式(II)的二取代的胺,其可用于治疗阿尔茨海默病和其它类似疾病。
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公开(公告)号:US07262043B2
公开(公告)日:2007-08-28
申请号:US11090399
申请日:2005-03-25
申请人: John P. Anderson , Guriqbal Basi , Minh Tam Doan , Normand Frigon , Varghese John , Michael Power , Sukanto Sinha , Gwen Tatsuno , Jay Tung , Shuwen Wang , Lisa McConlogue
发明人: John P. Anderson , Guriqbal Basi , Minh Tam Doan , Normand Frigon , Varghese John , Michael Power , Sukanto Sinha , Gwen Tatsuno , Jay Tung , Shuwen Wang , Lisa McConlogue
CPC分类号: C12N9/6478 , A01K2217/075 , A61K38/00 , H01Q1/364 , H01Q1/38 , H01Q3/44 , H01Q9/0407 , H01Q9/0442 , H01Q15/02
摘要: Disclosed are various forms of an active, isolated β-secretase enzyme in purified and recombinant form. This enzyme is implicated in the production of amyloid plaque components which accumulate in the brains of individuals afflicted with Alzheimer's disease. Recombinant cells that produce this enzyme either alone or in combination with some of its natural substrates (β-APPwt and β-APPsw) are also disclosed, as are antibodies directed to such proteins. These compositions are useful for use in methods of selecting compounds that modulate β-secretase. Inhibitors of β-secretase are implicated as therapeutics in the treatment of neurodegenerative diseases, such as Alzheimer's disease.
摘要翻译: 公开了各种形式的纯化和重组形式的活性,分离的β-分泌酶。 这种酶涉及积聚在患有阿尔茨海默病的个体的脑中的淀粉样蛋白斑块成分的产生。 产生该酶的重组细胞单独或与其一些天然底物(β-APPwt和β-APPsw)组合也被公开,以及针对这种蛋白质的抗体。 这些组合物可用于选择调节β-分泌酶的化合物的方法。 β-分泌酶的抑制剂涉及作为治疗神经变性疾病如阿尔茨海默病的治疗剂。
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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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公开(公告)号:US20090144840A1
公开(公告)日:2009-06-04
申请号:US12191950
申请日:2008-08-14
申请人: John P. Anderson , Guriqbal Basi , Minh Tam Doan , Normand Frigon , Varghese John , Michael Power , Sukanto Sinha , Gwen Tatsuno , Jay Tung , Shuwen Wang , Lisa McConlogue
发明人: John P. Anderson , Guriqbal Basi , Minh Tam Doan , Normand Frigon , Varghese John , Michael Power , Sukanto Sinha , Gwen Tatsuno , Jay Tung , Shuwen Wang , Lisa McConlogue
IPC分类号: G01N33/573 , A01K67/027
CPC分类号: C12N9/6478 , A01K2217/075 , A61K38/00 , H01Q1/364 , H01Q1/38 , H01Q3/44 , H01Q9/0407 , H01Q9/0442 , H01Q15/02
摘要: Disclosed are various forms of an active, isolated β-secretase enzyme in purified and recombinant form. This enzyme is implicated in the production of amyloid plaque components which accumulate in the brains of individuals afflicted with Alzheimer's disease. Recombinant cells that produce this enzyme either alone or in combination with some of its natural substrates (β-APPwt and β-APPsw) are also disclosed, as are antibodies directed to such proteins. These compositions are useful for use in methods of selecting compounds that modulate β-secretase. Inhibitors of β-secretase are implicated as therapeutics in the treatment of neurodegenerative diseases, such as Alzheimer's disease.
摘要翻译: 公开了各种形式的纯化和重组形式的活性,分离的β-分泌酶。 这种酶涉及积聚在患有阿尔茨海默病的个体的脑中的淀粉样蛋白斑块成分的产生。 产生该酶的重组细胞单独或与其一些天然底物(β-APPwt和β-APPsw)组合也被公开,以及针对这种蛋白质的抗体。 这些组合物可用于选择调节β-分泌酶的化合物的方法。 β-分泌酶的抑制剂涉及作为治疗神经变性疾病如阿尔茨海默病的治疗剂。
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公开(公告)号:US07252963B2
公开(公告)日:2007-08-07
申请号:US11090866
申请日:2005-03-25
申请人: John P. Anderson , Guriqbal Basi , Minh Tam Doan , Normand Frigon , Varghese John , Michael Power , Sukanto Sinha , Gwen Tatsuno , Jay Tung , Shuwen Wang , Lisa McConlogue
发明人: John P. Anderson , Guriqbal Basi , Minh Tam Doan , Normand Frigon , Varghese John , Michael Power , Sukanto Sinha , Gwen Tatsuno , Jay Tung , Shuwen Wang , Lisa McConlogue
CPC分类号: C12N9/6478 , A01K2217/075 , A61K38/00 , H01Q1/364 , H01Q1/38 , H01Q3/44 , H01Q9/0407 , H01Q9/0442 , H01Q15/02
摘要: Disclosed are various forms of an active, isolated β-secretase enzyme in purified and recombinant form. This enzyme is implicated in the production of amyloid plaque components which accumulate in the brains of individuals afflicted with Alzheimer's disease. Recombinant cells that produce this enzyme either alone or in combination with some of its natural substrates (β-APPwt and β-APPsw) are also disclosed, as are antibodies directed to such proteins. These compositions are useful for use in methods of selecting compounds that modulate β-secretase. Inhibitors of β-secretase are implicated as therapeutics in the treatment of neurodegenerative diseases, such as Alzheimer's disease.
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公开(公告)号:US07109017B1
公开(公告)日:2006-09-19
申请号:US09724569
申请日:2000-11-28
申请人: John P. Anderson , Guriqbal Basi , Minh Tam Doan , Normand Frigon , Varghese John , Michael Power , Sukanto Sinha , Gwen Tatsuno , Jay Tung , Shuwen Wang , Lisa McConlogue
发明人: John P. Anderson , Guriqbal Basi , Minh Tam Doan , Normand Frigon , Varghese John , Michael Power , Sukanto Sinha , Gwen Tatsuno , Jay Tung , Shuwen Wang , Lisa McConlogue
CPC分类号: C12N9/6478 , A01K2217/075 , A61K38/00
摘要: Disclosed are various forms of an active, isolated β-secretase enzyme in purified and recombinant form. This enzyme is implicated in the production of amyloid plaque components which accumulate in the brains of individuals afflicted with Alzheimer's disease. Recombinant cells that produce this enzyme either alone or in combination with some of its natural substrates (β-APPwt and β-APPsw) are also disclosed, as are antibodies directed to such proteins. These compositions are useful for use in methods of selecting compounds that modulate β-secretase. Inhibitors of β-secretase are implicated as therapeutics in the treatment of neurodegenerative diseases, such as Alzheimer's disease.
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公开(公告)号:US20050261495A1
公开(公告)日:2005-11-24
申请号:US10416771
申请日:2001-11-05
申请人: James Audia , Varghese John , Lee Latimer , Stacey McDaniel , Jeffrey Nissen , Eugene Thorsett , Jay Tung
发明人: James Audia , Varghese John , Lee Latimer , Stacey McDaniel , Jeffrey Nissen , Eugene Thorsett , Jay Tung
IPC分类号: C07D223/16 , A61K31/55 , A61K38/00 , A61P25/28 , C07D487/02 , C07K5/06
CPC分类号: C07D223/16 , A61K38/00 , C07K5/06026
摘要: The present invention provides the compound (N)-((S)-2-hydroxy-3-methyl-butyryl)-1-(L-alaninyl)-(S)-1-amino-3-methyl-4,5,6,7-tetrahydro-2H-3-benzazepin-2-one, compositions thereof, and methods for using the same.
摘要翻译: 本发明提供了化合物(N) - ((S)-2-羟基-3-甲基 - 丁酰基)-1-(L-丙氨酰) - (S)-1-氨基-3-甲基-4,5,5- 6,7-四氢-2H-苯并吖庚因-2-酮及其组合物及其使用方法。
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