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1. 发明申请

WO2006114260A1 PHENYLACETYLENE DERIVATIVES HAVING MGLUR5 RECEPTOR AFFINITY 审中-公开
标题翻译：具有MGLUR5受体亲和力的苯乙烯衍生物
公开(公告)号：WO2006114260A1
公开(公告)日：2006-11-02
申请号：PCT/EP2006/003764
申请日：2006-04-24
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , GLATTHAR, Ralf , TROXLER, Thomas, J.
发明人： GLATTHAR, Ralf , TROXLER, Thomas, J.
IPC分类号： C07C211/52 , C07D277/42 , C07D231/38 , C07D213/74 , C07D241/42 , C07D241/44 , C07D215/40 , C07D487/04 , C07D231/56 , C07D285/14 , C07D405/04 , C07D239/12 , C07D241/20 , C07D233/54 , C07D235/06
CPC分类号： C07C215/44 , C07C49/747 , C07C2601/14 , C07D213/74 , C07D215/40 , C07D231/38 , C07D231/56 , C07D233/64 , C07D235/06 , C07D239/12 , C07D241/20 , C07D241/42 , C07D241/44 , C07D249/08 , C07D277/42 , C07D285/14 , C07D405/04 , C07D487/04
摘要： The invention provides compounds of formula (I) wherein the substituents are as defined in the specification, to processes for their preparation and corresponding intermediates, and their use as modulators of the mglu5 receptor.
摘要翻译：本发明提供式（I）化合物，其中取代基如说明书中所定义，其制备方法和相应的中间体及其作为mglu5受体调节剂的用途。

2. 发明申请

WO2005035535A1 CERTAIN SUBSTITUTED SPIROCYCLIC LACTAMS AND USE THEREOF AS PHARMACEUTICALS 审中-公开
标题翻译：某些替代的螺旋藻和其作为药物的用途
公开(公告)号：WO2005035535A1
公开(公告)日：2005-04-21
申请号：PCT/EP2004/011054
申请日：2004-10-04
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , GLATTHAR, Ralf , SALTER, RHYS , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina
发明人： AUBERSON, Yves , GLATTHAR, Ralf , SALTER, RHYS , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D487/10
CPC分类号： C07D487/10
摘要： The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4-4]non-7-yl)-propionam ides of the formula wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及下式的新的2-（6-氧代-1,7-二氮杂 - 螺[4-4]壬-7-基） - 丙酰胺其中R1，R2，R3，R4，R5，R6， m和p如说明书中所定义，它们的制备，用作药物和含有它们的药物组合物。

3. 发明申请

WO2005014517A2 NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF 审中-公开
标题翻译：新二苯并[B，F] OXEPINE-10-羧酰胺及其药物用途
公开(公告)号：WO2005014517A2
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008283
申请日：2004-07-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , BETSCHART, Claudia , FLOHR, Stefanie , GLATTHAR, Ralf , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VANGREVELINGHE, Eric , VEENSTRA, Siem, Jacob
发明人： AUBERSON, Yves , BETSCHART, Claudia , FLOHR, Stefanie , GLATTHAR, Ralf , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VANGREVELINGHE, Eric , VEENSTRA, Siem, Jacob
IPC分类号： C07C61/00
CPC分类号： C07D405/12 , C07C235/82 , C07C2603/32 , C07D313/14 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to compounds of formula (I) wherein X is O, NH, N(C 1-4 )alkyl, CO or CHOH, Y is CH or N, A and B are each hydrogen or together form a second bond between the carbon atoms to which they are attached, R 1 is hydrogen or (C 1-4 )alkyl, R 2 is optionally substituted (C 1-8 )alkyl, (C 3-7 )cycloalkyl, (C 3-7 )cycloalkyl(C 1-4 )alkyl, aryl or heteroaryl, R 3 is CH(R e )CONR a R b or (CH 2 ) n NR c ,R d , n is 0, 1 or 2, R a , R b , R c and R d , independently, are hydrogen or optionally substituted (C 1-8 )alkyl, (C 3-7 )cycloalkyl, (C 3-7 )cycloalkyl(C 1-4 )alkyl, (C 7-9 )bicycloalkyl, 1-aza-(C 7-9 )bicycloalkyl, aryl, aryl(C 1-4 )alkyl, heteroaryl, heteroaryl(C 1-4 )alkyl or heterocyclyl, or R a , R b , R c and R d , together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, R e is (C 1-8 )alkyl, (C 1-4 )alkoxy(C 1-4 )alkyl, (C 3-7 )cycloalkyl or (C 3-7 )cycloalkyl(C 1-4 )alkyl, and R 4 , R 5 , R 6 , R 7 , R 8 and R 9 , independently, are hydrogen, (C 1-4 )alkyl, (C 1-4 )alkoxy, (C 1-4 )alkyl-SO 2 , cyano, nitro or halogen; to a process for the preparation of such compounds of formula (I), their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物，其中X是O，NH，N（C 1-4）烷基，CO或CHOH，Y是CH或N，A和B各自是氢或一起形成第二键碳原子，R 1是氢或（C 1-4）烷基，R 2是任选取代的（C 1-8）烷基，（C 3-7）环烷基，（C 3-7）环烷基（C 1-4）烷基，芳基或杂芳基，R3是CH（Re）CONRaRb或（CH2）nNRc，Rd，n是0,1或2，Ra，Rb，Rc和Rd独立地是氢或任选取代的（C 1-8）烷基，（ C3-7）环烷基，（C3-7）环烷基（C1-4）烷基，（C7-9）双环烷基，1-氮杂 - （C7-9）双环烷基，芳基，芳基（C1-4）烷基，杂芳基，杂芳基（C 1-4）烷基或杂环基，或R a，R b，R c和R d与它们所连接的氮一起形成任选取代的吡咯烷基，哌啶子基，吗啉代或哌嗪基，Re是（C 1-8）烷基，（C 1-4）烷氧基（C 1-4）烷基，（C 3-7）环烷基或（C 3-7）环烷基（C 1-4）烷基，R 4，R 5，R 6，R 7，R 8和R 9独立地为氢，（C1-4 ）烷基，（C 1-4）烷氧基，（C 1-4）烷基-SO 2，氰基，硝基或卤素; 制备这种式（I）化合物的方法，它们作为药物的用途，特别是用于治疗与β-淀粉样蛋白生成和/或聚集相关的神经和血管疾病，以及包含这些化合物的药物组合物和组合的式（I）化合物。

4. 发明申请

WO2007071358A1 NICOTINIC ACID DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：作为代谢型谷氨酸受体调节剂的非酸性衍生物
公开(公告)号：WO2007071358A1
公开(公告)日：2007-06-28
申请号：PCT/EP2006/012181
申请日：2006-12-18
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , GLATTHAR, Ralf , ORAIN, David , SPANKA, Carsten
发明人： GLATTHAR, Ralf , ORAIN, David , SPANKA, Carsten
IPC分类号： C07D213/82 , C07D237/24 , C07D239/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08 , A61K31/4427 , A61K31/4545 , A61K31/465 , A61K31/4725
CPC分类号： C07D213/82 , C07D239/42 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14
摘要： The present invention relates to novel nicotinic acid derivatives, of formula (I), wherein the substituents are defined in the specification, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）的新型烟酸衍生物，其中取代基在说明书中定义，其制备方法，它们作为药物的用途和含有它们的药物组合物。

5. 发明申请

WO2006114262A1 ACETYLENE DERIVATIVES 审中-公开
标题翻译：乙烯衍生物
公开(公告)号：WO2006114262A1
公开(公告)日：2006-11-02
申请号：PCT/EP2006/003766
申请日：2006-04-24
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , GLATTHAR, Ralf , TROXLER, Thomas, J. , ZOLLER, Thomas , NOZULAK, Joachim
发明人： GLATTHAR, Ralf , TROXLER, Thomas, J. , ZOLLER, Thomas , NOZULAK, Joachim
IPC分类号： C07C233/74 , C07C233/23 , C07D307/68 , C07D233/90 , C07D249/10 , A61K31/166 , A61K31/165 , A61K31/341 , A61K31/4178 , A61P25/00
CPC分类号： C07C235/54 , C07C233/22 , C07C233/23 , C07C233/74 , C07C235/14 , C07C235/36 , C07C235/78 , C07C237/38 , C07C317/44 , C07D233/90 , C07D249/08 , C07D249/10 , C07D307/68
摘要： The invention provides compounds of formula (I) wherein R 1 represents hydrogen or alkyl; R 2 represents an unsubstituted or substituted heterocycle or R 2 represents an unsubstituted or substituted aryl; R 3 represents alkyl or halogen; X represents a single bond or an alkandiyl-group, optionally interrupted by one ore more oxygen atoms or carbonyl groups or carbonyloxy groups in free base or acid addition salt form, processes for their preparation and their use as pharmaceuticals.
摘要翻译：本发明提供式（I）化合物，其中R 1表示氢或烷基; R 2表示未取代或取代的杂环，或者R 2表示未取代或取代的芳基; R 3表示烷基或卤素; X表示单键或烷二基，任选地被一个或多个氧原子或羰基或羰基氧基以游离碱或酸加成盐形式中断，其制备方法和用作药物。

6. 发明申请

WO2006089700A1 PYRROLIDINE AND PIPERIDINE ACETYLENE DERIVATIVES FOR USE AS MGLUR5 ANTAGONISTS 审中-公开
标题翻译：吡咯啉和哌啶乙酰衍生物用作MGLUR5拮抗剂
公开(公告)号：WO2006089700A1
公开(公告)日：2006-08-31
申请号：PCT/EP2006/001505
申请日：2006-02-20
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , GLATTHAR, Ralf , TROXLER, Thomas, J. , ZOLLER, Thomas , NOZULAK, Joachim
发明人： GLATTHAR, Ralf , TROXLER, Thomas, J. , ZOLLER, Thomas , NOZULAK, Joachim
IPC分类号： C07D405/06 , C07D211/48 , C07D413/06 , C07D401/06 , C07D471/04 , C07D405/14 , C07D403/06 , A61K31/445 , A61K31/40 , A61P25/00 , A61P29/00
CPC分类号： C07D471/04 , C07D211/48 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/14 , C07D413/06
摘要： The invention provides Compounds of formula (I) wherein the substituents are as defined in the description, processes and intermediates for their preparation and their use as pharmaceuticals in the treatment of disorders mediated by mGluR5.
摘要翻译：本发明提供式（I）化合物，其中取代基如本说明书中所定义，其制备方法和中间体及其作为药物用于治疗由mGluR5介导的病症的用途。

7. 发明申请

WO2007113276A1 NOVEL BI-ARYL AMINES 审中-公开
标题翻译：新颖的双甲苯胺
公开(公告)号：WO2007113276A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053155
申请日：2007-04-02
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , GLATTHAR, Ralf , CARCACHE, David , SPANKA, Carsten , VRANESIC, Ivan-Toma , TROXLER, Thomas J.
发明人： GLATTHAR, Ralf , CARCACHE, David , SPANKA, Carsten , VRANESIC, Ivan-Toma , TROXLER, Thomas J.
IPC分类号： C07D401/04 , C07D471/04 , C07D487/04 , A61K31/55 , A61P25/00
CPC分类号： C07D401/04 , C07D471/04 , C07D487/04
摘要： The present invention relates to novel bi-aryl amines of formula (I) and to pharmaceutically acceptable prodrugs, salts, solvates, hydrates, and N-oxides thereof and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation.
摘要翻译：本发明涉及式（I）的新型双芳基胺及其药学上可接受的前药，盐，溶剂合物，水合物和N-氧化物以及包含它们的药物组合物，其使用方法及其制备方法。

8. 发明申请

WO2006114264A1 ACETYLENE DERIVATIVES 审中-公开
标题翻译：乙烯衍生物
公开(公告)号：WO2006114264A1
公开(公告)日：2006-11-02
申请号：PCT/EP2006/003768
申请日：2006-04-24
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , GLATTHAR, Ralf , TROXLER, Thomas, J.
发明人： GLATTHAR, Ralf , TROXLER, Thomas, J.
IPC分类号： C07C271/24 , C07D307/68 , C07D307/85 , C07D213/81 , C07D213/82 , C07D231/38 , C07D307/32 , C07D295/08 , C07D211/58 , C07C309/14 , C07D233/54 , A61P1/00 , A61P13/00 , A61P25/00 , A61K31/325
CPC分类号： C07C215/44 , C07C217/84 , C07C271/24 , C07C2601/14 , C07D211/58 , C07D213/81 , C07D213/82 , C07D231/38 , C07D233/64 , C07D295/096 , C07D307/33 , C07D307/68 , C07D307/85 , C07D453/02
摘要： The invention provides compounds of formula (I), wherein the substituents are as defined in the specification, to processes for their preparation and their use as pharmaceuticals.
摘要翻译：本发明提供式（I）化合物，其中取代基如说明书中所定义，其制备方法及其作为药物的用途。

9. 发明申请

WO2005049585A1 MACROCYCLIC LACTAMS AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：大肠杆菌及其药物用途
公开(公告)号：WO2005049585A1
公开(公告)日：2005-06-02
申请号：PCT/EP2004/012497
申请日：2004-11-04
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , BETSCHART, Claudia , GLATTHAR, Ralf , LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VEENSTRA, Siem, Jacob
发明人： AUBERSON, Yves , BETSCHART, Claudia , GLATTHAR, Ralf , LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VEENSTRA, Siem, Jacob
IPC分类号： C07D245/02
CPC分类号： C07D245/02 , C07D255/00 , C07D273/00 , C07D281/00 , C07D471/08 , C07D513/08
摘要： The present invention relates to novel macrocyclic compounds of the formula (I) wherein R 1 , R 2 , R 3 , U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的新的大环化合物，其中R 1，R 2，R 3，U，V，W，X，Y，Z和n如说明书中所定义，大环中包括的环原子数环为14,15,16或17，以游离碱形式或以酸加成盐形式，其制备用作药物和包含它们的药物组合物。

10. 发明公开

EP1877364A1 PHENYLACETYLENE DERIVATIVES HAVING MGLUR5 RECEPTOR AFFINITY 有权
标题翻译：苯甲酸乙酯麻醉剂
公开(公告)号：EP1877364A1
公开(公告)日：2008-01-16
申请号：EP06724538.1
申请日：2006-04-24
申请人： Novartis AG , Novartis Pharma GmbH
发明人： GLATTHAR, Ralf , TROXLER, Thomas, J.
IPC分类号： C07C211/52 , C07D277/42 , C07D231/38 , C07D213/74 , C07D241/42 , C07D241/44 , C07D215/40 , C07D487/04 , C07D231/56 , C07D285/14 , C07D405/04 , C07D239/12 , C07D241/20 , C07D233/54 , C07D235/06
CPC分类号： C07C215/44 , C07C49/747 , C07C2601/14 , C07D213/74 , C07D215/40 , C07D231/38 , C07D231/56 , C07D233/64 , C07D235/06 , C07D239/12 , C07D241/20 , C07D241/42 , C07D241/44 , C07D249/08 , C07D277/42 , C07D285/14 , C07D405/04 , C07D487/04
摘要： The invention provides compounds of formula (I) wherein the substituents are as defined in the specification, to processes for their preparation and corresponding intermediates, and their use as modulators of the mglu5 receptor.
摘要翻译：本发明提供式（I）化合物，其中取代基如说明书中所定义，其制备方法和相应的中间体及其作为药物的用途。

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