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1. 发明申请

WO2005039591A1 BENZAZEPINE DERIVATIVES AS MAO-B INHIBITORS 审中-公开
标题翻译：苯并噻吩衍生物作为MAO-B抑制剂
公开(公告)号：WO2005039591A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011541
申请日：2004-10-14
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , RODRIGUEZ SARMIENTO, Rosa Maria , THOMAS, Andrew, William , WOSTL, Wolfgang , WYLER, Rene
发明人： JOLIDON, Synese , RODRIGUEZ SARMIENTO, Rosa Maria , THOMAS, Andrew, William , WOSTL, Wolfgang , WYLER, Rene
IPC分类号： A61K31/55
CPC分类号： C07D223/16
摘要： The present invention relates to novel benzazepine derivatives of the following formula: (I) wherein R 1 , R 2 , R 3 , R 4 and R 5 , 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的苯并氮杂衍生物：其中R 1，R 2，R 3，R 4和R 5，X，X'，Y和Y '如在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的疾病的药物的用途牵连。

2. 发明申请

WO2004014856A1 2,3-DIHYDRO-ISOINDOL-1-ONES WITH MAO-B INHIBITING ACTIVITY 审中-公开
标题翻译： 2,3-DIHYDRO-ISOINDOL-1-ONES与MAO-B抑制活性
公开(公告)号：WO2004014856A1
公开(公告)日：2004-02-19
申请号：PCT/EP2003/008456
申请日：2003-07-31
申请人： F. HOFFMANN-LA ROCHE AG
发明人： JOLIDON, Synese , RODRIGUEZ-SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WYLER, Rene
IPC分类号： C07D209/46
CPC分类号： C07D471/04 , C07D209/46
摘要： 2,3 Dihydro-isoindol-1-one derivatives, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them, for the prevention and treatment of diseases which are mediated by monoamine oxidase B inhibitors.
摘要翻译： 2,3二氢 - 异吲哚-1-酮衍生物，其制备方法，它们作为药物的用途和包含它们的药物组合物，用于预防和治疗由单胺氧化酶B抑制剂介导的疾病。

3. 发明申请

WO2004026826A1 4-PYRROLIDINO-PHENYL-BENZYL ETHER DERIVATIVES 审中-公开
标题翻译： 4-吡咯烷基 - 苯基 - 苯甲醚衍生物
公开(公告)号：WO2004026826A1
公开(公告)日：2004-04-01
申请号：PCT/EP2003/010383
申请日：2003-09-18
申请人： F. HOFFMANN-LA ROCHE AG
发明人： JOLIDON, Synese , RODRIGUEZ-SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WOSTL, Wolfgang , WYLER, Rene
IPC分类号： C07D207/26
CPC分类号： C07D207/273 , C07D207/277
摘要： Racemic or enantiomerically pure 4-pyrrolidino derivatives of formula (I), 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：式（I）的外消旋或对映异构体纯的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。

4. 发明申请

WO2003080573A1 PHTHALIMIDO DERIVATIVES AS INHIBITORS OF MONOAMINE OXIDASE B 审中-公开
标题翻译：作为单胺氧化酶B的抑制剂的邻苯二甲酰亚胺衍生物
公开(公告)号：WO2003080573A1
公开(公告)日：2003-10-02
申请号：PCT/EP2003/002931
申请日：2003-03-20
申请人： F. HOFFMANN-LA ROCHE AG
发明人： CESURA, Andrea , RODRIGUEZ SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WYLER, Rene
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , C07D401/04 , C07D413/04 , C07D471/04
摘要： This invention realtes to phthalimido derivatives of the general formula (I), wherein X is -N= or -CH, and R 1 to R 4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of dieases in which MAO-B inhibitors might be beneficial.
摘要翻译：本发明涉及通式（I）的邻苯二甲酰亚氨基衍生物，其中X为-N =或-CH，R 1至R 4和m如说明书中所定义，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，其制备方法及其制备用于治疗或预防MAO-B抑制剂可能有益的预防药物的用途。

5. 发明申请

WO2004054985A1 3H-QUINAZOLIN-4-ONE DERIVATIVES 审中-公开
标题翻译： 3H-喹唑啉-4-酮衍生物
公开(公告)号：WO2004054985A1
公开(公告)日：2004-07-01
申请号：PCT/EP2003/013888
申请日：2003-12-08
申请人： F. HOFFMANN-LA ROCHE AG
发明人： RODRIGUEZ SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WYLER, Rene
IPC分类号： C07D239/00
CPC分类号： C07D239/90
摘要： This invention relates to 3H-quinazolin-4-one derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as selective monoamine oxidase B inhibitors.
摘要翻译：本发明涉及如说明书和权利要求书中定义的3H-喹唑啉-4-酮衍生物及其制备方法，包含它们的药物组合物及其作为选择性单胺氧化酶B抑制剂的用途。

6. 发明申请

WO2002060877A1 IMIDAZOLE DERIVATIVES 审中-公开
标题翻译：咪唑衍生物
公开(公告)号：WO2002060877A1
公开(公告)日：2002-08-08
申请号：PCT/EP2002/000552
申请日：2002-01-21
申请人： F. HOFFMANN-LA ROCHE AG
发明人： ALANINE, Alexander , BUETTELMANN, Bernd , HEITZ NEIDHART, Marie-Paule , JAESCHKE, Georg , PINARD, Emmanuel , WYLER, Rene
IPC分类号： C07D233/54
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D233/84 , C07D249/08
摘要： The invention related to compounds of the general formula (I), wherein the substituents are defined in claim 1. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are therefore suitable in the control or treatment of diseases, related to this receptor.
摘要翻译：本发明涉及通式（I）的化合物，其中取代基如权利要求1中所定义。这些化合物对NMDA（N-甲基-D-天冬氨酸） - 受体亚型选择性阻断剂具有良好的亲和力，其具有关键在调节神经元活动和可塑性方面起作用，这使他们成为介导中枢神经系统发育过程以及学习和记忆形成的关键因素。因此，这些化合物适用于与该受体相关的疾病的控制或治疗。

7. 发明申请

WO2006000324A3 NEW MAO-B INHIBITORS 审中-公开
公开(公告)号：WO2006000324A3
公开(公告)日：2006-01-05
申请号：PCT/EP2005/006398
申请日：2005-06-15
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , RODRIGUEZ-SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WOSTL, Wolfgang , WYLER, Rene
发明人： JOLIDON, Synese , RODRIGUEZ-SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WOSTL, Wolfgang , WYLER, Rene
IPC分类号： C07C235/34 , C07C271/12 , A61K31/165 , A61K31/27 , A61P25/28
摘要： The invention relates to compounds of the general formula (I), wherein R 1 , R 2 are independently from each other hydrogen or C l -C 6 -alkyl; R 3 , R 4 are independently from each other hydrogen or C 1 -C 6 -alkyl; R 5 is halogen, CN, (C 1 -C 6 )-alkyl or (C 1 -C 6 )-alkoxy; n, m or o is 0, 1 or 2; as well as to their pharmaceutically acceptable salts. The compounds may be used for the treatment and prevention of Alzheimer's disease or senile dementia.

8. 发明申请

WO2003099763A1 N-ACYLAMINOBENZENE DERVATIVES AS SELECTIVE MONOAMINE OXIDASE B INHIBITORS 审中-公开
标题翻译：作为选择性单胺氧化酶B抑制剂的N-亚氨基苯甲酸衍生物
公开(公告)号：WO2003099763A1
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005297
申请日：2003-05-21
申请人： F. HOFFMANN-LA ROCHE AG
发明人： JOLIDON, Synese , RODRIGUEZ SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WYLER, Rene
IPC分类号： C07C233/25
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 general formula (I), wherein R 1 is halogen, halogen-(C 1 -C 6 )-alkyl, cyano, C 1 -C 6 -alkoxy or halogen-(C 1 -C 6 )-alkoxy; R 21 , R 22 , R 23 and R 24 independently from each other are selected from the group consisting of hydrogen, (C 1 -C 6 )-alkyl, halogen, halogen-(C 1 -C 6 )-alkyl, hydroxy, C 1 -C 6 -alkoxy or -CHO; R 3 is hydrogen or C 1 -C 3 -alkyl; R 4 , R 5 independently from each other are selected from the group consisting of hydrogen, C 1- C 6 -alkyl, C 1 -C 6 -alkoxy or -COO(C 1 -C 6 )alkyl; or R 4 and R 5 form together with the C-atom to which they are attach a C 3 -C 7 -cycloalkyl ring; R 6 is -CO-NR 7 R 8 ; -COO(C 1 -C 6 )-alkyl, -CN, -NR 2 or -NHC(O)R; R 7 and R 8 independently from each other are selected from the group consisting of hydrogen, C 1- C 6 -alkyl, NH 2 or hydroxy; R is hydrogen or C 1 -C 6 -alkyl; n is 0, 1, 2 or 3. X is -CHRO, -OCHR, -CH 2 S-, -SCH 2 -, -CH 2 CH 2 -, -CH=CH- or -C≡C-; and to pharmaceutically active acid addition salts thereof. It has been found that the compounds of general formula (I) are selective monoamine oxidase B inhibitors and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B inhibitors, for example for the treatment of Alzheimer’s disease or senile dementia.
摘要翻译：本发明涉及通式（I）的N-酰基氨基芳基衍生物，其中R 1是卤素，卤素 - （C 1 -C 6） - 烷基，氰基，C 1 -C 6 - 烷氧基或卤素 - （C 1 -C 6）烷氧基; R 21，R 22，R 23和R 24彼此独立地选自氢，（C 1 -C 6） - 烷基，卤素，卤素 - （C 1 -C 6） - 烷基，羟基，C 1 -C 6 - 烷氧基或-CHO; R 3是氢或C 1 -C 3 - 烷基; R 4，R 5彼此独立地选自氢，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基或-COO（C 1 -C 6）烷基; 或R 4和R 5与它们所连接的C-C原子一起形成C 3 -C 7 - 环烷基环; R 6是-CO-NR 7 R 8; -COO（C 1 -C 6） - 烷基，-CN，-NR 2或-NHC（O）R; R 7和R 8彼此独立地选自氢，C 1 -C 6 - 烷基，NH 2或羟基; R是氢或C 1 -C 6 - 烷基; n是0,1,2或3.X是-CHRO，-OCHR，-CH 2 S - ， - CH 2 - ， - CH 2 CH 2 - ， - CH = CH-或-C = C-; 及其药物活性的酸加成盐。已经发现通式（I）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抑制剂介导的疾病，例如用于治疗阿尔茨海默氏病或老年痴呆症。

9. 发明申请

WO2003091219A1 ISOQUINOLINE DERIVATIVES 审中-公开
标题翻译：异喹啉衍生物
公开(公告)号：WO2003091219A1
公开(公告)日：2003-11-06
申请号：PCT/EP2003/003845
申请日：2003-04-14
申请人： F. HOFFMANN-LA ROCHE AG
发明人： CESURA, Andrea , RODRIGUEZ SARMIENTO, Rosa Maria , SCALONE, Michelangelo , THOMAS, Andrew, William , WYLER, Rene
IPC分类号： C07D217/24
CPC分类号： C07D217/24
摘要： This invention relates to isoquinolino derivatives of the general Formula (I) wherein Y is >C=O or CH 2 -, Z is >C=O or CH 2 -, and R 1 , R 2 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.
摘要翻译：本发明涉及通式（I）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如说明书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，其制备方法及其制备用于治疗或预防MAO-B抑制剂可能有益的疾病的药物的用途。

10. 发明申请

WO2004026827A1 PYRROLIDONE DERIVATIVES AS MAOB INHIBITORS 审中-公开
标题翻译：吡咯烷酮衍生物作为MAOB抑制剂
公开(公告)号：WO2004026827A1
公开(公告)日：2004-04-01
申请号：PCT/EP2003/010384
申请日：2003-09-18
申请人： F. HOFFMANN-LA ROCHE AG
发明人： IDING, Hans , JOLIDON, Synese , KRUMMENACHER, Daniela , RODRIGUEZ SARMIENTO, Rosa, Maria , THOMAS, Andrew, William , WIRZ, Beat , WOSTL, Wolfgang , WYLER, Rene
IPC分类号： C07D207/26
CPC分类号： C07D207/273 , C07D207/277
摘要： Racemic enantiomerically pure 4- pyrrolidino derivatives of formula (I), 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：式（I）的外消旋对映体纯的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，特别是阿尔茨海默病或老年痴呆症。

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