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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：US07122562B2
公开(公告)日：2006-10-17
申请号：US11325747
申请日：2006-01-05
申请人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
发明人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
IPC分类号： A61K31/4439 , C07D401/04
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.
摘要翻译： 本发明涉及外消旋或对映体纯的4-吡咯烷子基衍生物，其制备方法，包含所述衍生物的药物组合物及其在预防和治疗疾病中的用途，特别是其由单胺氧化酶B抑制剂介导的，特别是阿尔茨海默氏病 或老年痴呆症。
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公开(公告)号：US07037935B2
公开(公告)日：2006-05-02
申请号：US10667088
申请日：2003-09-18
申请人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
发明人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
IPC分类号： A61K31/402 , C07D209/34
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.
摘要翻译： 本发明涉及外消旋或对映体纯的4-吡咯烷子基衍生物，其制备方法，包含所述衍生物的药物组合物及其在预防和治疗疾病中的用途，特别是其由单胺氧化酶B抑制剂介导的，特别是阿尔茨海默氏病 或老年痴呆症。
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公开(公告)号：US07151111B2
公开(公告)日：2006-12-19
申请号：US10667087
申请日：2003-09-18
申请人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
发明人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
IPC分类号： A61K31/44 , A61K31/40 , C07D401/06 , C07D207/06
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 a disease which is mediated by a monoamine oxidase B inhibitor, in particular Alzheimer's disease and senile dementia.
摘要翻译： 本发明涉及外消旋或对映体纯的4-吡咯烷子基衍生物，其制备方法，包含所述衍生物的药物组合物及其在预防和治疗由单胺氧化酶B抑制剂，特别是阿尔茨海默氏病介导的疾病中的用途，以及 老年性痴呆。
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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：US07173023B2
公开(公告)日：2007-02-06
申请号：US10967567
申请日：2004-10-18
申请人： Synese Jolidon , Rosa Maria Rodriguez Sarmiento , Andrew William Thomas , Wolfgang Wostl , Rene Wyler
发明人： Synese Jolidon , Rosa Maria Rodriguez Sarmiento , Andrew William Thomas , Wolfgang Wostl , Rene Wyler
IPC分类号： A61K31/55 , C07D223/16 , C07D487/02
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：US07235581B2
公开(公告)日：2007-06-26
申请号：US10666594
申请日：2003-09-18
申请人： Synese Jolidon , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Wolfgang Wostl , Rene Wyler
发明人： Synese Jolidon , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Wolfgang Wostl , Rene Wyler
IPC分类号： A61K31/4015 , C07D207/04
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, e.g. which are mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.
摘要翻译： 本发明涉及外消旋或对映体纯的4-吡咯烷子基衍生物，其制备方法，包含所述衍生物的药物组合物及其在预防和治疗疾病中的用途。 其由单胺氧化酶B抑制剂介导，特别是阿尔茨海默病或老年痴呆。
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