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公开(公告)号:US20080249135A1
公开(公告)日:2008-10-09
申请号:US11696526
申请日:2007-04-04
申请人: Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
发明人: Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
IPC分类号: A61K31/44 , A61K31/404 , A61P25/28 , C07D257/04 , C07D401/00 , C07D209/04 , A61K31/41
CPC分类号: C07D209/60 , A61K31/403 , C07D209/08 , C07D209/10 , C07D209/14 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D491/10 , C07F7/1804
摘要: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(═O)OH, -L-CH═CHC(═O)OH, -L-C(═O)NH2, -L-C(═O)NH(C1-3 alkyl), -L-C(═O)N(C1-3 alkyl)2, -L-S(═O)2(C1-3alkyl), -L-S(═O)2NH2, -L-S(═O)2N(C1-3 alkyl)2, -L-S(═O)2NH(C1-3 alkyl), -L-C(═O)NHOH, -L-C(═O)CH2NH2, -L-C(═O)CH2OH, -L-C(═O)CH2SH, -L-C(═O)NHCN, -L-NHC(═O)ORo, -L-C(═O)NHRo, -L-NH(C═O)NHRo, -L-C(═O)N(Ro)2, -L-NH(C═O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
摘要翻译: 本发明提供了可用于治疗包括阿尔茨海默病和痴呆的神经变性疾病的新化合物。 化合物具有选自-LC(-O)OH,-L-CH-CHC(-O)OH,-LC(-O)NH 2,-LC(-O)NH (C 1-3烷基),-LC(-O)N(C 1-3烷基)亚磺酰基,-LS(-O )2(C 1-3烷基),-LS(-O)2 NH 2,-LS (-O)2 N(C 1-3烷基)2,-LS(-O)2 NH(C 1-3烷基),-LC(-O)NHOH,-LC(-O)CH 2 NH 2 - , - LC(-O)CH 2 OH,-LC(-O)CH 2 SH,-LC(-O)NHCN,-L-NHC(-O)OR -OC(-O)NHR o,-L-NH(CO)NHR o,-LC(-O)N( 2-N,R-NH(CO)N(R 0)2 - , - 磺基,-L-(2,6-二氟苯酚),-L-膦酰基和-L-四唑基,其中L是连接体。
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公开(公告)号:US09034871B2
公开(公告)日:2015-05-19
申请号:US13447115
申请日:2012-04-13
申请人: Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
发明人: Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
IPC分类号: A61K31/404 , A61K31/403 , A61K31/405 , C07D209/10 , C07D209/60 , C07D209/08 , C07D209/14 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D491/10 , C07F7/18
CPC分类号: C07D209/60 , A61K31/403 , C07D209/08 , C07D209/10 , C07D209/14 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D491/10 , C07F7/1804
摘要: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(═O)OH, -L-CH═CHC(═O)OH, -L-C(═O)NH2, -L-C(═O)NH(C1-3 alkyl), -L-C(═O)N(C1-3 alkyl)2, -L-S(═O)2(C1-3alkyl), -L-S(═O)2NH2, -L-S(═O)2N(C1-3 alkyl)2, -L-S(═O)2NH(C1-3 alkyl), -L-C(═O)NHOH, -L-C(═O)CH2NH2, -L-C(═O)CH2OH, -L-C(═O)CH2SH, -L-C(═O)NHCN, -L-NHC(═O)ORo, -L-C(═O)NHRo, -L-NH(C═O)NHRo, -L-C(═O)N(Ro)2, -L-NH(C═O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
摘要翻译: 本发明提供了可用于治疗包括阿尔茨海默病和痴呆的神经变性疾病的新化合物。 化合物具有选自-LC(= O)OH,-L-CH = CHC(= O)OH,-LC(= O)NH 2,-LC(= O)NH(C 1-3烷基), - LC(= O)N(C 1-3烷基)2,-LS(= O)2(C 1-3烷基),-LS(= O)2 NH 2,-LS(= -LS(= O)2 NH(C 1-3烷基),-LC(= O)NHOH,-LC(= O)CH 2 NH 2,-LC(= O)CH 2 OH,-LC(= O)CH 2 SH,-LC(= O)NHCN,-L-NHC(= O)OR o,-LC(= O)NHRo,-L-NH(C = O)NHRo,-LC(= O)N(Ro)2,-L-NH C = O)N(R o)2,-L-磺基,-L-(2,6-二氟苯酚),-L-膦酰基和-L-四唑基,其中L为连接基。
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公开(公告)号:US20120225873A1
公开(公告)日:2012-09-06
申请号:US13447115
申请日:2012-04-13
申请人: Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
发明人: Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
IPC分类号: A61K31/5377 , A61K31/4985 , A61K31/437 , A61K31/4439 , C07D413/14 , A61K31/422 , A61K31/403 , C07D403/10 , C07D209/18 , C07D413/10 , A61K31/501 , C07D471/06 , C07D401/04 , C07D417/04 , C07D413/04 , C07D491/10 , C07D209/90 , A61K31/404 , C07D209/12 , C07D413/08 , C07D401/14 , C07D405/14 , A61P25/28 , A61K31/5025
CPC分类号: C07D209/60 , A61K31/403 , C07D209/08 , C07D209/10 , C07D209/14 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D491/10 , C07F7/1804
摘要: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(═O)OH, -L-CH═CHC(═O)OH, -L-C(═O)NH2, -L-C(═O)NH(C1-3 alkyl), -L-C(═O)N(C1-3 alkyl)2, -L-S(═O)2(C1-3alkyl), -L-S(═O)2NH2, -L-S(═O)2N(C1-3 alkyl)2, -L-S(═O)2NH(C1-3 alkyl), -L-C(═O)NHOH, -L-C(═O)CH2NH2, -L-C(═O)CH2OH, -L-C(═O)CH2SH, -L-C(═O)NHCN, -L-NHC(═O)ORo, -L-C(═O)NHRo, -L-NH(C═O)NHRo, -L-C(═O)N(Ro)2, -L-NH(C═O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
摘要翻译: 本发明提供了可用于治疗包括阿尔茨海默病和痴呆的神经变性疾病的新化合物。 化合物具有选自-LC(= O)OH,-L-CH = CHC(= O)OH,-LC(= O)NH 2,-LC(= O)NH(C 1-3烷基), - LC(= O)N(C 1-3烷基)2,-LS(= O)2(C 1-3烷基),-LS(= O)2 NH 2,-LS(= -LS(= O)2 NH(C 1-3烷基),-LC(= O)NHOH,-LC(= O)CH 2 NH 2,-LC(= O)CH 2 OH,-LC(= O)CH 2 SH,-LC(= O)NHCN,-L-NHC(= O)OR o,-LC(= O)NHRo,-L-NH(C = O)NHRo,-LC(= O)N(Ro)2,-L-NH C = O)N(R o)2,-L-磺基,-L-(2,6-二氟苯酚),-L-膦酰基和-L-四唑基,其中L为连接基。
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公开(公告)号:US20100184975A1
公开(公告)日:2010-07-22
申请号:US12719672
申请日:2010-03-08
申请人: Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
发明人: Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
IPC分类号: C07D413/10 , C07D209/60 , C07D209/08 , C07D403/10 , C07D401/04 , C07D403/04
CPC分类号: C07D209/60 , A61K31/403 , C07D209/08 , C07D209/10 , C07D209/14 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D491/10 , C07F7/1804
摘要: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(═O)OH, -L-CH═CHC(═O)OH, -L-C(═O)NH2, -L-C(═0)NH(C1-3alkyl), -L-C(═O)N(C1-3alkyl)2, -L-S(═O)2(C1-3alkyl), -L-S(═O)2NH2, -L-S(═O)2N(C1-3alkyl)2, -L-S(═O)2NH(C1-3alkyl), -L-C(═O)NHOH, -L-C(═O)CH2NH2, -L-C(═O)CH2OH, -L-C(═O)CH2SH, -L-C(═O)NHCN, -L-NHC(═O)ORo, -L-C(═O)NHRo, -L-NH(C═O)NHRo, -L-C(═O)N(Ro)2, -L-NH(C═O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
摘要翻译: 本发明提供了可用于治疗包括阿尔茨海默病和痴呆的神经变性疾病的新化合物。 这些化合物具有选自-LC(= O)OH,-L-CH = CHC(= O)OH,-LC(= O)NH 2,-LC(= O)NH(C 1-3烷基),-LC (= O)N(C 1-3烷基)2,-LS(= O)2(C 1-3烷基),-LS(= O)2 NH 2,-LS(= O)2 N(C 1-3烷基)2,-LS( (= O)CH 2 OH,-LC(= O)CH 2 OH,-LC(= O)CH 2 SH,-LC(= O)NHCN, -L-NHC(= O)OR o,-LC(= O)NHRo,-L-NH(C = O)NHRo,-LC(= O)N(Ro)2,-L-NH(C = O) N(Ro)2,-L-磺基,-L-(2,6-二氟苯酚),-L-膦酰基和-L-四唑基,其中L是连接基。
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公开(公告)号:US07678823B2
公开(公告)日:2010-03-16
申请号:US11696526
申请日:2007-04-04
申请人: Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
发明人: Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
IPC分类号: A61K31/416 , C07D209/04
CPC分类号: C07D209/60 , A61K31/403 , C07D209/08 , C07D209/10 , C07D209/14 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D491/10 , C07F7/1804
摘要: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(═O)OH, -L-CH═CHC(═O)OH, -L-C(═O)NH2, -L-C(═O)NH(C1-3 alkyl), -L-C(═O)N(C1-3 alkyl)2, -L-S(═O)2(C1-3alkyl), -L-S(═O)2NH2, -L-S(═O)2N(C1-3 alkyl)2, -L-S(═O)2NH(C1-3 alkyl), -L-C(═O)NHOH, -L-C(═O)CH2NH2, -L-C(═O)CH2OH, -L-C(═O)CH2SH, -L-C(═O)NHCN, -L-NHC(═O)ORo, -L-C(═O)NHRo, -L-NH(C═O)NHRo, -L-C(═O)N(Ro)2, -L-NH(C═O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
摘要翻译: 本发明提供了可用于治疗包括阿尔茨海默病和痴呆的神经变性疾病的新化合物。 化合物具有选自-LC(= O)OH,-L-CH = CHC(= O)OH,-LC(= O)NH 2,-LC(= O)NH(C 1-3烷基), - LC(= O)N(C 1-3烷基)2,-LS(= O)2(C 1-3烷基),-LS(= O)2 NH 2,-LS(= -LS(= O)2 NH(C 1-3烷基),-LC(= O)NHOH,-LC(= O)CH 2 NH 2,-LC(= O)CH 2 OH,-LC(= O)CH 2 SH,-LC(= O)NHCN,-L-NHC(= O)OR o,-LC(= O)NHRo,-L-NH(C = O)NHRo,-LC(= O)N(Ro)2,-L-NH C = O)N(R o)2,-L-磺基,-L-(2,6-二氟苯酚),-L-膦酰基和-L-四唑基,其中L为连接基。
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公开(公告)号:US20100216862A1
公开(公告)日:2010-08-26
申请号:US12775253
申请日:2010-05-06
IPC分类号: A61K31/402 , C07D207/327 , A61P25/28 , C12N5/071
CPC分类号: C07D207/327 , C07D207/325 , C07D207/33 , C07D207/34
摘要: Novel pyrrole derivatives are disclosed as Aβ42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the Aβ42 peptide.
摘要翻译: 公开了新颖的吡咯衍生物作为治疗和预防神经变性疾病的42降低剂,其特征在于包含Aβ42肽的淀粉样蛋白斑的形成或积累。
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公开(公告)号:US07714022B2
公开(公告)日:2010-05-11
申请号:US12057140
申请日:2008-03-27
IPC分类号: A61K31/40 , C07D207/30
CPC分类号: C07D207/327 , C07D207/325 , C07D207/33 , C07D207/34
摘要: Novel pyrrole derivatives are disclosed as Aβ42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the Aβ42 peptide.
摘要翻译: 公开了新颖的吡咯衍生物作为治疗和预防神经变性疾病的42降低剂,其特征在于包含Aβ42肽的淀粉样蛋白斑的形成或积累。
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公开(公告)号:US20080249158A1
公开(公告)日:2008-10-09
申请号:US12057140
申请日:2008-03-27
IPC分类号: A61K31/40 , C07D207/32 , A61P25/28
CPC分类号: C07D207/327 , C07D207/325 , C07D207/33 , C07D207/34
摘要: Novel pyrrole derivatives are disclosed as Aβ42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the Aβ42 peptide.
摘要翻译: 公开了新颖的吡咯衍生物作为用于治疗和预防特征在于包含AβAβ42肽的淀粉样蛋白斑的形成或积累的神经退行性病症的抗Aβ药物。
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公开(公告)号:US08217073B2
公开(公告)日:2012-07-10
申请号:US12775253
申请日:2010-05-06
IPC分类号: A61K31/40 , C07D207/30
CPC分类号: C07D207/327 , C07D207/325 , C07D207/33 , C07D207/34
摘要: Novel pyrrole derivatives are disclosed as Aβ42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the Aβ42 peptide.
摘要翻译: 公开了新颖的吡咯衍生物作为治疗和预防神经变性疾病的42降低剂,其特征在于包含Aβ42肽的淀粉样蛋白斑的形成或积累。
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