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1.发明授权Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease 有权苄醚和苄氨基β-分泌酶抑制剂用于治疗阿尔茨海默病公开(公告)号：US07829597B2
公开(公告)日：2010-11-09
申请号：US10573232
申请日：2004-09-29
IPC分类号： C07C15/12 , C07C13/48 , A61K31/135
CPC分类号： C07D213/81 , C07C255/57 , C07C311/08 , C07C2601/02 , C07D207/06 , C07D207/08 , C07D213/76 , C07D295/192 , C07D333/20 , C07D405/04
摘要： The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂的式（I）化合物，其可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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2.发明申请BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权用于治疗阿尔茨海默病的苯甲醚和苯甲酰胺抑制剂公开(公告)号：US20100210693A1
公开(公告)日：2010-08-19
申请号：US12772711
申请日：2010-05-03
IPC分类号： A61K31/18 , C07C311/01 , C07D333/24 , C07D405/04 , C07D207/09 , C07D213/72 , A61K31/381 , A61K31/4025 , A61K31/40 , A61K31/44 , A61P25/28
CPC分类号： C07D213/81 , C07C255/57 , C07C311/08 , C07C2601/02 , C07D207/06 , C07D207/08 , C07D213/76 , C07D295/192 , C07D333/20 , C07D405/04
摘要： The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病如阿尔茨海默氏病的化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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3.发明授权Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease 有权苄醚和苄氨基β-分泌酶抑制剂用于治疗阿尔茨海默病公开(公告)号：US08008315B2
公开(公告)日：2011-08-30
申请号：US12772711
申请日：2010-05-03
IPC分类号： A01N43/40 , A61K43/42 , C07D295/00
CPC分类号： C07D213/81 , C07C255/57 , C07C311/08 , C07C2601/02 , C07D207/06 , C07D207/08 , C07D213/76 , C07D295/192 , C07D333/20 , C07D405/04
摘要： The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病如阿尔茨海默氏病的化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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4.发明授权Phenylcarboxylate beta-secretase inhibitors for the treatment of alzheimer's disease 失效用于治疗阿尔茨海默病的苯基羧酸β-分泌酶抑制剂公开(公告)号：US07348448B2
公开(公告)日：2008-03-25
申请号：US10562470
申请日：2004-06-25
IPC分类号： C07C313/00 , C07C255/00
CPC分类号： C07D207/08 , C07C233/66 , C07C255/57 , C07C311/08 , C07C2601/02 , C07D207/06 , C07D295/192 , C07D401/04
摘要： The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病如阿尔茨海默氏病的化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及β-分泌酶的疾病中的用途。
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5.发明申请Macrocyclic Tertiary Amine Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease 有权用于治疗阿尔茨海默病的大环叔胺β-分泌酶抑制剂公开(公告)号：US20080269302A1
公开(公告)日：2008-10-30
申请号：US11667913
申请日：2005-11-14
申请人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Stacey Lindsley , Keith P. Moore , Shawn J. Stachel
发明人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Stacey Lindsley , Keith P. Moore , Shawn J. Stachel
IPC分类号： A61K31/365 , C07D267/00 , C07D313/00 , A61K31/395 , A61P25/28 , C07D498/00 , C07D321/00
CPC分类号： C07D273/01 , C07D267/00 , C07D313/00 , C07D321/00 , C07D323/00 , C07D413/04 , C07D498/08
摘要： The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及由通式（I）表示的大环叔胺化合物，其为β-分泌酶的抑制剂，可用于治疗其中涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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6.发明申请Aminomethyl Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease 有权氨基甲基β-分泌酶抑制剂治疗阿尔茨海默病公开(公告)号：US20080153846A1
公开(公告)日：2008-06-26
申请号：US11795283
申请日：2006-01-13
申请人： Craig A. Coburn , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer
发明人： Craig A. Coburn , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer
IPC分类号： A61K31/496 , C07C211/00 , A61K31/13 , A61K31/4245 , A61P25/28 , C07D271/06 , C07D413/06
CPC分类号： C07D413/06 , C07D271/10
摘要： The present invention is directed to aminomethyl compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗涉及β-分泌酶的疾病如阿尔茨海默氏病的氨基甲基化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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公开(公告)号：US07084134B2
公开(公告)日：2006-08-01
申请号：US10427435
申请日：2003-05-01
IPC分类号： A61K38/00
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof.
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8.发明授权2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease 有权用作治疗阿尔茨海默氏病的β-分泌酶抑制剂的2,3,4,6-取代的吡啶衍生物化合物公开(公告)号：US08394837B2
公开(公告)日：2013-03-12
申请号：US11791204
申请日：2005-11-18
申请人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , James C. Barrow , Shaun R. Stauffer , Joseph P. Vacca , Keith P. Moore , Shawn J. Stachel , Mattahew G. Stanton
发明人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , James C. Barrow , Shaun R. Stauffer , Joseph P. Vacca , Keith P. Moore , Shawn J. Stachel , Mattahew G. Stanton
IPC分类号： A61K31/4439 , C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is directed to 2,3,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及2,3,4,6-取代的吡啶基衍生物化合物，其是β-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默病 。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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公开(公告)号：US07144899B2
公开(公告)日：2006-12-05
申请号：US10467439
申请日：2002-02-05
申请人： Harold G. Selnick , Mary Beth Young , Philippe G. Nantermet , James C. Barrow , Peter D. Williams , Terry A. Lyle , Donnette D. Staas , Kenneth J. Stauffer , Philip E. Sanderson
发明人： Harold G. Selnick , Mary Beth Young , Philippe G. Nantermet , James C. Barrow , Peter D. Williams , Terry A. Lyle , Donnette D. Staas , Kenneth J. Stauffer , Philip E. Sanderson
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： C07D257/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D417/12
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)—N(R25)CH(R30)— wherein the nitrogen atom is attached to R1, and R25 and R30 are independently selected from the group consisting of hydrogen, C3-6cycloalkyl, and C1-6alkyl, or 2) wherein the nitrogen atom is attached to R1, and m is 0, 1, or 2
摘要翻译： 本发明的化合物可用于抑制具有以下结构式（I）的凝血酶和相关的血栓闭塞：其中u是CH或N; Q是1）-N（R 25）CH（R 30） - 其中氮原子连接到R 1， SUP> 25和R 30独立地选自氢，C 3-6环烷基和C 1-6烷基， 或者2）其中氮原子连接到R 1，m是0,1或2
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公开(公告)号：US06515011B2
公开(公告)日：2003-02-04
申请号：US10023776
申请日：2001-12-18
申请人： Harold G. Selnick , James C. Barrow , Philippe G. Nantermet , Peter D. Williams , Kenneth J. Stauffer , Philip E. Sanderson , Kenneth E. Rittle , Matthew M. Morrissette , Catherine M. Wiscount , Lekhanh O. Tran , Terry A. Lyle , Donnette D. Staas
发明人： Harold G. Selnick , James C. Barrow , Philippe G. Nantermet , Peter D. Williams , Kenneth J. Stauffer , Philip E. Sanderson , Kenneth E. Rittle , Matthew M. Morrissette , Catherine M. Wiscount , Lekhanh O. Tran , Terry A. Lyle , Donnette D. Staas
IPC分类号： A61K3140
CPC分类号： C07D401/06 , A61K38/00 , C07D205/04 , C07D207/16 , C07D403/12 , C07K5/06 , C07K5/06034 , C07K5/06078 , C07K5/06139 , C07K5/06191
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. where R3 is —CH2NH2, —CH2CH2NH2, or —CH2NHC(O)OC(CH3)3.
摘要翻译： 本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓闭塞：或其药学上可接受的盐，例如， 其中R 3是-CH 2 NH 2，-CH 2 CH 2 NH 2或-CH 2 NHC（O）OC（CH 3）3。
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