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公开(公告)号：US08486967B2
公开(公告)日：2013-07-16
申请号：US13023563
申请日：2011-02-09
申请人： Karlheinz Baumann , Alexander Flohr , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
发明人： Karlheinz Baumann , Alexander Flohr , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
IPC分类号： A01N43/42 , A61K31/44 , C07D513/02 , C07D515/02
CPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04
摘要： The invention relates to compounds of formula where hetaryl I, hetaryl II, R1, R2, R3, R4, m, n, and o are as defined in the specification or to pharmaceutically active acid addition salts thereof. The compounds of formula I are modulators for amyloid beta and thus may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
摘要翻译： 本发明涉及下式的化合物，其中杂芳基I，杂芳基II，R 1，R 2，R 3，R 4，m，n和o如说明书中所定义或其药学活性的酸加成盐。 式I化合物是淀粉样蛋白β的调节剂，因此可用于治疗或预防与脑中β-淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默氏病和其他疾病如脑淀粉样血管病，遗传性 脑出血伴淀粉样变性，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合征。
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公开(公告)号：US20120225884A1
公开(公告)日：2012-09-06
申请号：US13405404
申请日：2012-02-27
申请人： Karlheinz Baumann , Luke Green , Anja Limberg , Thomas Luebbers , Andrew Thomas
发明人： Karlheinz Baumann , Luke Green , Anja Limberg , Thomas Luebbers , Andrew Thomas
IPC分类号： A61K31/4985 , C07D451/04 , C07D487/04 , A61P25/00 , A61K31/437 , A61K31/506 , A61K31/519 , A61P25/28 , C07D471/04 , A61K31/444
CPC分类号： C07D451/04
摘要： The present invention relates to compounds of formula I hetaryl I, hetaryl II, R1, R2, R3, Y, m, and o or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
摘要翻译： 本发明涉及式I化合物，杂芳基I，杂芳基II，R 1，R 2，R 3，Y，m和o的化合物或其药物活性酸加成盐。 本发明式I化合物是淀粉样蛋白β的调节剂，因此它们可用于治疗或预防与脑中淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默氏病和其他疾病如脑 淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合征。
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公开(公告)号：US20110201605A1
公开(公告)日：2011-08-18
申请号：US13023563
申请日：2011-02-09
申请人： Karlheinz Baumann , Alexander Flohr , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
发明人： Karlheinz Baumann , Alexander Flohr , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
IPC分类号： A61K31/5365 , C07D471/04 , A61K31/437 , C07D401/14 , A61K31/454 , C07D403/14 , A61K31/506 , C07D413/14 , A61K31/5377 , C07D498/04 , A61P25/28
CPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04
摘要： The invention relates to compounds of formula where hetaryl I, hetaryl II, R1, R2, R3, R4, m, n, and o are as defined in the specification or to pharmaceutically active acid addition salts thereof. The compounds of formula I are modulators for amyloid beta and thus may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
摘要翻译： 本发明涉及下式的化合物，其中杂芳基I，杂芳基II，R 1，R 2，R 3，R 4，m，n和o如说明书中所定义或其药学活性的酸加成盐。 式I的化合物是淀粉样蛋白β的调节剂，因此可用于治疗或预防与脑中淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默病和其它疾病如脑淀粉样血管病， 遗传性脑出血伴淀粉样变性，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合症。
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公开(公告)号：US20110190269A1
公开(公告)日：2011-08-04
申请号：US13011951
申请日：2011-01-24
申请人： Karlheinz Baumann , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
发明人： Karlheinz Baumann , Erwin Goetschi , Luke Green , Synese Jolidon , Henner Knust , Anja Limberg , Thomas Luebbers , Andrew Thomas
IPC分类号： A61K31/55 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61K31/4985 , A61K31/5377 , A61K31/5025 , A61K31/538
CPC分类号： C07D471/04 , C07D487/04 , C07D498/04
摘要： The invention relates to compounds of formula wherein R1, R1′, R2, R3, n, A, and hetaryl are defined herein or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
摘要翻译： 本发明涉及下式的化合物，其中R 1，R 1'，R 2，R 3，n，A和杂芳基在本文中定义或其药学活性的酸加成盐。 本发明式I化合物是淀粉样蛋白β的调节剂，因此它们可用于治疗或预防与脑中淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默氏病和其他疾病如脑 淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合征。
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公开(公告)号：US08703763B2
公开(公告)日：2014-04-22
申请号：US13405404
申请日：2012-02-27
申请人： Karlheinz Baumann , Luke Green , Anja Limberg , Thomas Luebbers , Andrew Thomas
发明人： Karlheinz Baumann , Luke Green , Anja Limberg , Thomas Luebbers , Andrew Thomas
IPC分类号： A01N43/00 , A61K31/55 , C07D413/00 , C07D415/00 , C07D417/00 , C07D419/00
CPC分类号： C07D451/04
摘要： The present invention relates to compounds of formula I hetaryl I, hetaryl II, R1, R2, R3, Y, m, and o or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
摘要翻译： 本发明涉及式I化合物，杂芳基I，杂芳基II，R 1，R 2，R 3，Y，m和o的化合物或其药物活性酸加成盐。 本发明式I化合物是淀粉样蛋白β的调节剂，因此它们可用于治疗或预防与脑中淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默氏病和其他疾病如脑 淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合征。
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公开(公告)号：US08288403B2
公开(公告)日：2012-10-16
申请号：US12612002
申请日：2009-11-04
IPC分类号： A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4439 , A61K31/506 , C07D401/02 , C07D403/02 , C07D413/02 , C07D417/02
CPC分类号： C07D417/12 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.
摘要翻译： 本发明涉及治疗阿尔茨海默病，脑淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗塞性痴呆，痴呆症和唐氏综合征的方法，其包括给予治疗有效量的 其中R 1，R 2，R 3，V，W，Y和Z如本文所定义的式I化合物或这些化合物的药学活性的酸加成盐。 本发明还涉及这些化合物的亚属和含有它们的药物组合物，以及它们的制备方法。
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公开(公告)号：US20100120874A1
公开(公告)日：2010-05-13
申请号：US12612002
申请日：2009-11-04
IPC分类号： A61K31/4245 , A61K31/4196 , C07D249/08 , A61K31/4164 , C07D233/54 , A61K31/41 , C07D257/04 , C07D271/06 , A61K31/433 , C07D285/08 , A61K31/426 , C07D277/20 , A61P25/28
CPC分类号： C07D417/12 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.
摘要翻译： 本发明涉及治疗阿尔茨海默病，脑淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗塞性痴呆，痴呆症和唐氏综合征的方法，其包括给予治疗有效量的 其中R 1，R 2，R 3，V，W，Y和Z如本文所定义的式I化合物或这些化合物的药学活性的酸加成盐。 本发明还涉及这些化合物的亚属和含有它们的药物组合物，以及它们的制备方法。
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公开(公告)号：US20120208803A1
公开(公告)日：2012-08-16
申请号：US13452981
申请日：2012-04-23
申请人： Caterina Bissantz , Philippe Jablonski , Henner Knust , Andreas Koblet , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
发明人： Caterina Bissantz , Philippe Jablonski , Henner Knust , Andreas Koblet , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
IPC分类号： A61K31/496 , C07D403/14 , C07D405/14 , A61K31/498 , A61P25/24 , A61K31/541 , C07D413/06 , A61K31/5377 , A61P25/22 , C07D403/06 , C07D417/06
CPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, Ar and n are as defined herein and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds can be used for the treatment of depression, anxiety or schizophrenia.
摘要翻译： 本发明涉及其中R 1，R 2，R 3，Ar和n如本文所定义的药物活性盐，外消旋混合物，对映异构体，旋光异构体或其互变异构形式的式I化合物。 该化合物可用于治疗抑郁，焦虑或精神分裂症。
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公开(公告)号：US20090306043A1
公开(公告)日：2009-12-10
申请号：US12476267
申请日：2009-06-02
申请人： Philippe Jablonski , Kenichi Kawasaki , Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
发明人： Philippe Jablonski , Kenichi Kawasaki , Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer
IPC分类号： A61K31/4545 , C07D401/14 , A61K31/4439
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, R′, Ar, m, n, and o are as defined herein. The invention also relates to pharmaceutical compositions containing compounds of formula I and methods for the manufacture of such compounds and compositions. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译： 本发明涉及式I化合物，其中R 1，R 2，R 3，R'，Ar，m，n和o如本文所定义。 本发明还涉及含有式I化合物的药物组合物和制备这些化合物和组合物的方法。 本发明化合物是用于治疗抑郁，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜在NK-3受体拮抗剂。
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公开(公告)号：US07462639B2
公开(公告)日：2008-12-09
申请号：US11384052
申请日：2006-03-17
申请人： Guy Georges , Bernhard Goller , Klaus-Peter Kuenkele , Aude Lemarchand , Anja Limberg , Ulrike Reiff , Petra Rueger , Matthias Rueth
发明人： Guy Georges , Bernhard Goller , Klaus-Peter Kuenkele , Aude Lemarchand , Anja Limberg , Ulrike Reiff , Petra Rueger , Matthias Rueth
IPC分类号： A61K31/4155 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.
摘要翻译： 本发明涉及式I化合物：其药学上可接受的盐或酯，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物组合物及其制备，以及这些化合物的用途 控制或预防癌症等疾病。
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