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公开(公告)号：US20050154000A1
公开(公告)日：2005-07-14
申请号：US11028125
申请日：2005-01-03
申请人： Synese Jolidon , Emmanuel Pinard , Andrew Thomas
发明人： Synese Jolidon , Emmanuel Pinard , Andrew Thomas
IPC分类号： A61K31/435 , C07D471/10 , A61K31/4747
CPC分类号： C07D471/10
摘要： The present invention relates to compounds of formula wherein A—B, R1, R2, R3, R4, and n are as defined herein; and to pharmaceutically acceptable salts thereof. The compounds of formula I may be used in the treatment of neurological and neuropsychiatric disorders.
摘要翻译： 本发明涉及下式的化合物，其中AB，R 1，R 2，R 3，R 4， ，和n如本文所定义; 和其药学上可接受的盐。 式I化合物可用于治疗神经和神经精神障碍。
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公开(公告)号：US20050154001A1
公开(公告)日：2005-07-14
申请号：US11028281
申请日：2005-01-03
IPC分类号： C07D471/10 , A61K31/4747
CPC分类号： C07D471/10
摘要： The present invention relates to compounds of formula wherein A-B is —CH2—CH2—, —CH2—O— or —O—CH2—; X is hydrogen or hydroxy; R1 is aryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, cyano, CF3, —OCF3, lower alkoxy, —SO2-lower alkyl and heteroaryl; R2 is aryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, CF3, and lower alkoxy; R3 is hydrogen or lower alkyl; n is 0, 1 or 2; or a pharmaceutically active salt thereof. The compounds of the invention may be used in the treatment of neurological and neuropsychiatric disorders.
摘要翻译： 本发明涉及下式的化合物其中AB是-CH 2 -CH 2 - ， - CH 2 -O - 或-O- CH 2 - ; X是氢或羟基; R 1是芳基，任选被一个或两个选自卤素，低级烷基，氰基，CF 3，-OCF 3， 低级烷氧基，-SO 2 - 低级烷基和杂芳基; R 2是任选被一个或两个选自卤素，低级烷基，CF 3 N 3和低级烷氧基的取代基取代的芳基; R 3是氢或低级烷基; n为0,1或2; 或其药物活性盐。 本发明的化合物可用于治疗神经和神经精神障碍。
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公开(公告)号：US20060122235A1
公开(公告)日：2006-06-08
申请号：US11325747
申请日：2006-01-05
申请人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Rodriguez-Sarmiento , Andrew Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
发明人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Rodriguez-Sarmiento , Andrew Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
IPC分类号： A61K31/4439 , C07D403/04
CPC分类号： C07D207/273 , C07D207/277
摘要： The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.
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公开(公告)号：US20050288367A1
公开(公告)日：2005-12-29
申请号：US11156417
申请日：2005-06-20
IPC分类号： A61K31/165 , A61K31/277 , C07C235/20 , C07C255/54
CPC分类号： C07C255/54 , C07C235/20
摘要： The invention relates to compounds of the formula and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, n, m, and o are as defined in the specification. The compounds are selective monoamine oxidase β inhibitors and are useful for the treatment and prevention of Alzheimer's disease and senile dementia, as well as other CNS disorders. The invention also relates to processes for preparing such compounds and pharmaceutical compositions containing them.
摘要翻译： 本发明涉及下式的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4， / SUP>，R 5，n，m和o如说明书中所定义。 这些化合物是选择性单胺氧化酶β抑制剂，并且可用于治疗和预防阿尔茨海默氏病和老年痴呆以及其它CNS疾病。 本发明还涉及制备这些化合物的方法和含有它们的药物组合物。
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公开(公告)号：US20050107360A1
公开(公告)日：2005-05-19
申请号：US10967567
申请日：2004-10-18
IPC分类号： C07D223/16 , A61K31/55
CPC分类号： C07D223/16
摘要： The present invention relates to novel benzazepine derivatives of the following formula: wherein R1, R2, R3, R4 and R5, X, X′, Y and Y′ are as defined in the description and claims, processes for their preparation, pharmaceutical compositions containing said derivatives and their use for the preparation of medicaments useful for the prevention and treatment of diseases in which selective inhibition of monoamine oxidase B activity plays a role or is implicated.
摘要翻译： 本发明涉及下式的新型苯并氮杂衍生物：其中R 1，R 2，R 3，R 4， / SUP>和R 5，X，X'，Y和Y'如说明书和权利要求书中所定义，其制备方法，含有所述衍生物的药物组合物及其用于制备药物的用途 可用于预防和治疗单胺氧化酶B活性的选择性抑制发挥作用或牵连的疾病。
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公开(公告)号：US20070117791A1
公开(公告)日：2007-05-24
申请号：US11652970
申请日：2007-01-12
IPC分类号： A61K31/55
CPC分类号： C07D223/16
摘要： The present invention relates to methods for making and using novel benzazepine derivatives of the following formula: wherein R1, R2, R3, R4 and R5, X, X′, Y and Y′ are as defined in the description and claims, processes for their preparation, pharmaceutical compositions containing said derivatives and their use for the preparation of medicaments useful for the prevention and treatment of diseases in which selective inhibition of monoamine oxidase B activity plays a role or is implicated.
摘要翻译： 本发明涉及制备和使用下式的新型苯并氮杂衍生物的方法：其中R 1，R 2，R 3，R 3， 其中，X，X'，Y和Y'如说明书和权利要求书中所定义，其制备方法，含有所述衍生物的药物组合物及其用途 用于制备可用于预防和治疗单胺氧化酶B活性的选择性抑制发挥作用或牵连的疾病的药物。
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公开(公告)号：US20050283019A1
公开(公告)日：2005-12-22
申请号：US11213052
申请日：2005-08-26
IPC分类号： A61P3/00 , A61K31/15 , A61K31/167 , A61K31/216 , A61K31/275 , A61P3/04 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P29/00 , A61P43/00 , C07C231/02 , C07C233/15 , C07C233/25 , C07C233/33 , C07C233/60 , C07C235/16 , C07C237/04 , C07C237/22 , C07C243/14 , C07C243/28 , C07C255/19 , C07C255/23 , C07C255/25 , C07C255/58 , C07C259/06 , C07C323/41
CPC分类号： C07C259/06 , C07C233/15 , C07C233/25 , C07C233/33 , C07C233/60 , C07C235/16 , C07C237/04 , C07C237/22 , C07C243/14 , C07C243/28 , C07C255/19 , C07C255/23 , C07C255/25 , C07C323/41 , C07C2601/02
摘要： This invention relates to N-acylamino aryl derivatives of the formula where R1R21, R22, R23, R24, R3, R4, R5, R6, R7, R8, R, and n are as defined herein and where X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH═CH— or —C≡C—. The compounds of the invention are selective monoamine oxidase B inhibitors, and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B, for example, for the treatment of Alzheimer's disease or senile dementia.
摘要翻译： 本发明涉及下式的N-酰基氨基芳基衍生物：其中R 1，R 2，R 22，R 23， >，R 24，R 3，R 4，R 5，R 6， R 7，R 8，R 8和n如本文所定义，并且其中X是-CHRO，-OCHR - ， - CH 2 ，-SCH 2 - ， - CH 2 CH 2 - ， - CH-CH-或-C≡C-。 本发明的化合物是选择性单胺氧化酶B抑制剂，因此它们可用于治疗由单胺氧化酶B介导的疾病，例如用于治疗阿尔茨海默氏病或老年痴呆症。
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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：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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