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1. 发明授权

EP1828199B1 THIENO-PYRIDINE DERIVATIVES AS GABA-B ALLOSTERIC ENHANCERS 有权
标题翻译：噻吩并吡啶衍生物ALS变构GABA-B增强剂
公开(公告)号：EP1828199B1
公开(公告)日：2009-05-06
申请号：EP05815262.0
申请日：2005-12-09
申请人： F. Hoffmann-La Roche AG
发明人： MALHERBE, Parichehr , MASCIADRI, Raffaello , NORCROSS, Roger, David , RATNI, Hasane , THOMAS, Andrew, William
IPC分类号： C07D495/04 , A61K31/435 , A61P25/00 , C07D495/14
CPC分类号： C07D495/04 , C07D495/14
摘要： The present invention relates to compounds of formula (I), Wherein R1 to R5 are as defined in the specification which compounds are active on the GABAB receptor and can be used for the manufacture of medicaments useful for treating CNS disorders.

2. 发明授权

EP1572666B1 3H-QUINAZOLIN-4-ONE DERIVATIVES 有权
标题翻译： 3H-CHINAZOLINE -4-ON DERIVATEN
公开(公告)号：EP1572666B1
公开(公告)日：2006-08-09
申请号：EP03789170.2
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 , C07D239/90 , A61K31/517 , A61P25/28
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.

3. 发明授权

EP1337535B1 BENZODIAZEPINE DERIVATIVES AS GABA A RECEPTOR MODULATORS 有权
标题翻译：苯并二氮杂衍生物作为GABA-A受体调节剂
公开(公告)号：EP1337535B1
公开(公告)日：2004-06-09
申请号：EP01996541.7
申请日：2001-11-08
申请人： F. HOFFMANN-LA ROCHE AG
发明人： MASCIADRI, Raffaello , THOMAS, Andrew, William , WICHMANN, Juergen
IPC分类号： C07D487/14 , A61K31/55 , A61P25/00
CPC分类号： C07D487/14

4. 发明授权

EP1501804B1 ISOQUINOLINE DERIVATIVES MAO-B INHIBITORS 有权
标题翻译：异喹啉THAN MAO-B抑制剂的
公开(公告)号：EP1501804B1
公开(公告)日：2009-08-26
申请号：EP03725018.0
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 , A61K31/472 , A61P25/16
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 CH2-, Z is >C=O or CH2-, and R1, R2 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.

5. 发明授权

EP1523469B1 CINNAMIDE DERIVATIVES 有权
标题翻译： ZIMTSÄUREAMIDDERIVATE
公开(公告)号：EP1523469B1
公开(公告)日：2008-10-08
申请号：EP03740425.8
申请日：2003-07-07
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： C07C235/34 , C07C255/54 , A61K31/165 , A61K31/275 , A61P25/28
CPC分类号： C07C255/54 , C07C235/34
摘要： 3-Phenyl-propionamido, 3-phenyl-acrylamido and 3-phenyl-propynamido derivatives, processes for their preparation, compositions containing them and the use of said derivatives as MAO-B inhibitors.

6. 发明公开

EP1680127A1 BENZAZEPINE DERIVATIVES AS MAO-B INHIBITORS 有权
标题翻译：苯并吖庚因衍生物作为MAO-B抑制剂的
公开(公告)号：EP1680127A1
公开(公告)日：2006-07-19
申请号：EP04790400.8
申请日：2004-10-14
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： A61K31/55 , C07D223/16 , A61P25/00
CPC分类号： C07D223/16
摘要： The present invention relates to novel benzazepine derivatives of the following formula: (I) 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.

7. 发明公开

EP1572666A1 3H-QUINAZOLIN-4-ONE DERIVATIVES 有权
标题翻译： 3H-喹唑啉-4酮衍生物
公开(公告)号：EP1572666A1
公开(公告)日：2005-09-14
申请号：EP03789170.2
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 , C07D239/90 , A61K31/517 , A61P25/28
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.

8. 发明授权

EP1680127B1 BENZAZEPINE DERIVATIVES AS MAO-B INHIBITORS 有权
标题翻译：苯并吖庚因衍生物作为MAO-B抑制剂的
公开(公告)号：EP1680127B1
公开(公告)日：2008-10-15
申请号：EP04790400.8
申请日：2004-10-14
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： A61K31/55 , C07D223/16 , A61P25/00
CPC分类号： C07D223/16
摘要： The present invention relates to novel benzazepine derivatives of the following formula: (I) 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.

9. 发明授权

EP1828194B1 TETRACYCLIC IMIDAZO-BENZODIAZEPINES AS GABA RECEPTORS MODULATORS 有权
标题翻译： TETRA CYCLICAL imidazobenzodiazepines AS GABA受体调节剂
公开(公告)号：EP1828194B1
公开(公告)日：2008-05-28
申请号：EP05825935.9
申请日：2005-12-05
申请人： F. Hoffmann-La Roche AG
发明人： BUETTELMANN, Bernd , KNUST, Henner , THOMAS, Andrew, William
IPC分类号： C07D487/14 , A61K31/5517
CPC分类号： C07D487/14
摘要： The present invention is concerned with substituted imidazo [1,5-a] [1,2,4] triazolo [1,5-d] [1,4]benzodiazepine derivatives of the following formula (I) wherein R' is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, -O(CH2)mO(CH2)mOH or -C≡C-R'; R2 is hydrogen or methyl; R3 is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, -(CH2)n-cycloalkyl, -(CR'R')m CH3, or is phenyl, unsubstituted or substituted by halogen, or is pyridinyl or thienyl, unsubstituted or substituted by lower alkyl, or is -(CH2)n-NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR'R')mOH, or is lower alkynyl-phenyl, wherein the phenyl ring is unsubstituited or substituted by halogen, CF3, lower alkyl or lower alkoxy; R' is hydrogen or lower alkyl; R' is hydrogen, hydroxy or lower alkyl; n is 0, 1 or 2; m is 1, 2 or 3; o is 1 or 2; and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA A α 5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

10. 发明公开

EP1539694A1 2,3-DIHYDRO-ISOINDOL-1-ONES WITH MAO-B INHIBITING ACTIVITY 审中-公开
标题翻译： 2,3-二氢-1-酮与MAO-B的抑制活性
公开(公告)号：EP1539694A1
公开(公告)日：2005-06-15
申请号：EP03784117.8
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 , C07D471/04 , A61K31/405 , A61P25/28
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.

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