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11. 发明授权

US06903095B2 Phthalimido derivatives and a process for their preparation 失效
标题翻译：邻苯二甲酰亚胺衍生物及其制备方法
公开(公告)号：US06903095B2
公开(公告)日：2005-06-07
申请号：US10657857
申请日：2003-09-09
申请人： Andrea Cesura , Rosa Maria Rodriguez Sarmiento , Andrew William Thomas , Rene Wyler
发明人： Andrea Cesura , Rosa Maria Rodriguez Sarmiento , Andrew William Thomas , Rene Wyler
IPC分类号： A61K31/4035 , A61K31/42 , A61K31/437 , A61K31/454 , A61K31/5377 , A61P25/28 , A61P43/00 , C07D209/48 , C07D401/04 , C07D405/06 , C07D407/06 , C07D409/06 , C07D413/04 , C07D413/06 , C07D471/04 , A61K31/535 , C07D413/00
CPC分类号： C07D209/48 , C07D401/04 , C07D413/04 , C07D471/04
摘要： This invention relates to phthalimido derivatives of the formula wherein X is —N═ or —CH═, and R1 to R4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to pharmaceutical compositions containing these compounds, a method of treating a disease by administering a therapeutically effective amount of at least one of these compounds, and a process for their preparation for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.
摘要翻译：本发明涉及下式的邻苯二甲酰亚氨基衍生物其中X是-N-或-CH-，R 1至R 4和m如说明书中所定义，如以及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，通过施用治疗有效量的这些化合物中的至少一种来治疗疾病的方法及其制备治疗或预防MAO-B抑制剂可能是有益的

12. 发明授权

US06642247B2 Di-or triaza-spiro [4,5] decane derivatives 失效
标题翻译：二 - 或三氮杂螺[4,5]癸烷衍生物
公开(公告)号：US06642247B2
公开(公告)日：2003-11-04
申请号：US09330724
申请日：1999-06-11
申请人： Geo Adam , Andrea Cesura , François Jenck , Sabine Kolczewski , Stephan Röver , Jürgen Wichmann
发明人： Geo Adam , Andrea Cesura , François Jenck , Sabine Kolczewski , Stephan Röver , Jürgen Wichmann
IPC分类号： A61K31438
CPC分类号： C07D471/10 , C07D513/10
摘要： The present invention relates to compounds of the general formula wherein R1 is C6-10-cycloalkyl, optionally substituted by lower alkyl or —C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl or octahydro-inden-2-yl; R2 is hydrogen; lower alkyl; ═O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; X is —CH(OH)—; —C(O)—; —CHR3—; —CR3═; —O—; —S—; —CH(COOR4)— or C(COOR4)═; Y is —CH2—; —CH═; —CH(COOR4)—, —C(COOR4)═; or —C(CN)—; R3 is hydrogen or lower alkoxy; R4 is lower alkyl, cycloalkyl, phenyl, or benzyl and either a or b is optionally an additional bond, and to pharmaceutically acceptable acid addition salts thereof. The compounds are agonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.
摘要翻译：本发明涉及通式化合物R 1的化合物是任选被低级烷基或-C（O）O-低级烷基取代的C 6-10 - 环烷基; 十氢萘-1-基; 十氢萘-2-基; 茚满-1-基或茚满-2-基，任选被低级烷基取代; 十氢 - 薁-2-基; 双环[6.2.0]癸-9-基; 苊-1-基; 2,3-二氢-1H-苯并芬-1-基; 2,3,3a，4,5,6-六氢-1H-吩酚-1-基或八氢 - 茚-2-基; R 2是氢; 低级烷基任选被低级烷基，卤素或烷氧基取代的O或苯基;是任选被低级烷基，卤素或烷氧基取代的环己基或苯基; X是-CH（OH） - ; -C（O） - ; -CHR 3 - ; -CR 3 = -O-; -S-; -CH（COOR 4） - 或C（COOR 4）=; Y是-CH 2 - ; -CH =; -CH（COOR 4） - ， - C（COOR 4）=; 或-C（CN） - ; R 3是氢或低级烷氧基; R 4是低级烷基，环烷基，苯基或苄基，a或b任选是另外的键，以及其药学上可接受的酸加成盐该化合物是孤儿素FQ（QFQ）受体的激动剂，因此可用于治疗与该受体有关的疾病。

13. 发明申请

US20060252822A1 Mitochrondrial permeability transition pore affinity labels and modulators 失效
标题翻译：线粒体通透性转移孔亲和标记和调节剂
公开(公告)号：US20060252822A1
公开(公告)日：2006-11-09
申请号：US11487119
申请日：2006-07-14
申请人： Andrea Cesura , Emmanuel Pinard
发明人： Andrea Cesura , Emmanuel Pinard
IPC分类号： A61K31/353 , G01N33/53
CPC分类号： C07C255/47 , A61K31/12 , A61K31/35 , C07C49/665 , C07C49/683 , C07C2601/10 , C07C2603/32 , C07C2603/98 , C07D311/22
摘要： Methods of utilizing compounds of general formulas I and II as modulators and affinity labels of the MPTP complex are elucidated. Furthermore, methods for modulating the activity of the MPTP complex, methods for determining the presence of a component of the MPTP complex, and methods for identifying an active agent that modulates the activity of the MPTP complex, specifically methods for identifying an active agent that modulates the activity of the MPTP complex by interacting with the VDAC1 component are identified. Moreover, novel compounds of general formulas I and II are disclosed.
摘要翻译：阐述了将通式I和II的化合物用作MPTP复合物的调节剂和亲和标记物的方法。此外，用于调节MPTP复合物的活性的方法，用于确定MPTP复合物的组分的存在的方法，以及用于鉴定调节MPTP复合物的活性的活性剂的方法，具体地说，用于鉴定调节的活性剂的方法识别通过与VDAC1组分相互作用的MPTP复合物的活性。此外，公开了通式I和II的新化合物。

14. 发明授权

US07101917B2 Mitochrondrial permeability transition pore affinity labels and modulators 失效
公开(公告)号：US07101917B2
公开(公告)日：2006-09-05
申请号：US10817975
申请日：2004-04-05
申请人： Andrea Cesura , Emmanuel Pinard
发明人： Andrea Cesura , Emmanuel Pinard
IPC分类号： A61K31/12
CPC分类号： C07C255/47 , A61K31/12 , A61K31/35 , C07C49/665 , C07C49/683 , C07C2601/10 , C07C2603/32 , C07C2603/98 , C07D311/22
摘要： Methods of utilizing compounds of general formulas I and II as modulators and affinity labels of the MPTP complex are elucidated. Furthermore, methods for modulating the activity of the MPTP complex, methods for determining the presence of a component of the MPTP complex, and methods for identifying an active agent that modulates the activity of the MPTP complex, specifically methods for identifying an active agent that modulates the activity of the MPTP complex by interacting with the VDAC1 component are identified. Moreover, novel compounds of general formulas I and II are disclosed.

15. 发明授权

US06818774B2 Isoquinoline derivatives 失效
标题翻译：异喹啉衍生物
公开(公告)号：US06818774B2
公开(公告)日：2004-11-16
申请号：US10417378
申请日：2003-04-16
申请人： Andrea Cesura , Rosa Maria Rodriguez Sarmiento , Michelangelo Scalone , Andrew William Thomas , Rene Wyler
发明人： Andrea Cesura , Rosa Maria Rodriguez Sarmiento , Michelangelo Scalone , Andrew William Thomas , Rene Wyler
IPC分类号： C07D21722
CPC分类号： C07D217/24
摘要： Disclosed are isoquinolino derivatives of the formula wherein Y is >C═O or —CH2—, Z is >C═O or —CH2—, and R1, R2 and m are as defined herein as well as the pharmaceutically acceptable salts thereof. These compounds are MAO-B selective inhibitors useful, inter alia, in the treatment of Alzheimer's disease and/or senile dementia.
摘要翻译：公开了式Ⅳ所示的异喹啉衍生物，其中Y为> C = O或-CH 2 - ，Z为> C = O或-CH 2 - ，R 1，R 2和m如本文所定义，其可接受的盐。这些化合物是尤其用于治疗阿尔茨海默病和/或老年痴呆的MAO-B选择性抑制剂。

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