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11. 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。

12. 发明申请

WO2003042234A3 NON-PEPTIDE SOMATOSTATIN RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2003042234A3
公开(公告)日：2003-05-22
申请号：PCT/US2002/036827
申请日：2002-11-14
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN , BERNEY, Daniel , BRECKENRIDGE, Robin , NEUMANN, Peter , SHAPIRO, Gideon , SEILER, Peter, Max , TROXLER, Thomas, J.
发明人： BERNEY, Daniel , BRECKENRIDGE, Robin , NEUMANN, Peter , SHAPIRO, Gideon , SEILER, Peter, Max , TROXLER, Thomas, J.
IPC分类号： A61K31/4178
摘要： The present invention provides compounds of formula (I), wherein X, Y, R1, R2, R3, and R4 are as defined in the description, and the preparation thereof. The compounds of the formula bind to somatostatin receptiors and are useful as pharamaceuticals.

13. 发明申请

WO2003040125A1 PIPERAZINE DERIVATIVES HAVING SST1 ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有SST1拮抗活性的哌嗪衍生物
公开(公告)号：WO2003040125A1
公开(公告)日：2003-05-15
申请号：PCT/EP2002/012514
申请日：2002-11-08
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , TROXLER, Thomas, J. , HOYER, Daniel
发明人： TROXLER, Thomas, J. , HOYER, Daniel
IPC分类号： C07D311/90
CPC分类号： C07D213/74 , C07D295/185 , C07D311/90 , C07D335/20 , C07D405/12 , C07D487/04
摘要： The invention provides compounds of formula (I), wherein X, R 1 and R 2 are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals.
摘要翻译：本发明提供式（I）化合物，其中X，R 1和R 2如说明书中所定义，及其制备。式（I）的化合物可用作药物。

14. 发明申请

WO2014013469A1 CARBAMATE/UREA DERIVATIVES 审中-公开
标题翻译：碳酸盐/尿素衍生物
公开(公告)号：WO2014013469A1
公开(公告)日：2014-01-23
申请号：PCT/IB2013/055916
申请日：2013-07-18
申请人： NOVARTIS AG , AUBERSON, Yves , BOCK, Mark Gary , BRAGA, Dario , CURZI, Marco , DODD, Stephanie Kay , GIAFFREDA, Stefano Luca , JIANG, Haiyang , KARPINSKI, Piotr , TROXLER, Thomas J. , WANG, Tielin , WANG, Xiaoyang , ZHANG, Xuechun
发明人： AUBERSON, Yves , BOCK, Mark Gary , BRAGA, Dario , CURZI, Marco , DODD, Stephanie Kay , GIAFFREDA, Stefano Luca , JIANG, Haiyang , KARPINSKI, Piotr , TROXLER, Thomas J. , WANG, Tielin , WANG, Xiaoyang , ZHANG, Xuechun
IPC分类号： C07D401/14 , C07D401/04 , A61K31/4545 , A61P25/00
CPC分类号： C07D401/04 , A61K31/496 , A61K31/501 , C07B2200/13 , C07C57/15 , C07C59/265 , C07D403/04
摘要： The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译：本发明涉及式（I）化合物或其盐，其中取代基如说明书中所定义; 作为其制备，用作药物和包含它的药物。

15. 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。

16. 发明申请

WO2015173659A2 CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：羧酰胺衍生物
公开(公告)号：WO2015173659A2
公开(公告)日：2015-11-19
申请号：PCT/IB2015/001513
申请日：2015-05-14
申请人： NOVARTIS AG , ARISTA, Luca , BEERLI, Rene , COTESTA, Simona , D'ALESSANDRO, Pier, Luca , LATTMANN, Rene , PULZ, Robert, Alexander , TROXLER, Thomas, J.
发明人： ARISTA, Luca , BEERLI, Rene , COTESTA, Simona , D'ALESSANDRO, Pier, Luca , LATTMANN, Rene , PULZ, Robert, Alexander , TROXLER, Thomas, J.
IPC分类号： C07D413/12
CPC分类号： C07D413/12 , A61K31/423 , A61K31/424 , C07D498/04
摘要： The present invention provides a compound of formula (I). The compounds of formula (I) demonstrate properties as Smurf-1 inhibitors and are thus useful in the treatment of a range of disorders, particularly pulmonary arterial hypertension.
摘要翻译：本发明提供式（I）的化合物。式（I）化合物表现出作为Smurf-1抑制剂的性质，因此可用于治疗一系列病症，特别是肺动脉高压。

17. 发明申请

WO2009030270A1 DIHYDROINDOLE DERIVATIVES USEFUL IN PARKINSON'S DISEASE 审中-公开
标题翻译：用于PARKINSON疾病的DIHYDROINDOLE DERIVATIVES
公开(公告)号：WO2009030270A1
公开(公告)日：2009-03-12
申请号：PCT/EP2007/059194
申请日：2007-09-03
申请人： NOVARTIS AG , BOUWMEESTER, Tewis , GREENIDGE, Paulette , RICK, Jens, M. , ROVELLI, Giorgio , TROXLER, Thomas, J. , ZIMMERMANN, Kaspar
发明人： BOUWMEESTER, Tewis , GREENIDGE, Paulette , RICK, Jens, M. , ROVELLI, Giorgio , TROXLER, Thomas, J. , ZIMMERMANN, Kaspar
IPC分类号： C07D209/34 , C07D403/06 , A61K31/404 , A61P25/00
CPC分类号： C07D209/34 , C07D403/06
摘要： The invention relates to novel heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及式（I）的新型杂环化合物，其中所有变量如说明书中所定义，以游离形式或盐形式，其制备方式，其用作药物和包含它们的药物。

18. 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。

19. 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。

20. 发明申请

WO2005123732A1 1-AZA-BICYCLO[3.3.1]NONANES 审中-公开
标题翻译： 1-氮杂 - 二环[3.3.1]壬烷
公开(公告)号：WO2005123732A1
公开(公告)日：2005-12-29
申请号：PCT/EP2005/006566
申请日：2005-06-17
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FEUERBACH, Dominik , MÜLLER, Werner , ROY, Bernard, Lucien , TROXLER, Thomas, J. , HURTH, Konstanze , FREDERIKSEN, Mathias
发明人： FEUERBACH, Dominik , MÜLLER, Werner , ROY, Bernard, Lucien , TROXLER, Thomas, J. , HURTH, Konstanze , FREDERIKSEN, Mathias
IPC分类号： C07D471/04
CPC分类号： C07D471/08
摘要： The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R 1 ); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C 5 - C 10aryl , substituted or unsubstituted hetero-C 5 -C 10 aryl, a group N(R 1 )(R 4 ), or a group N(R 2 )(CHP 3 R 4 ); R represent a hydrogen, C 1 -C 4 alkyl, or CF 3 ; R 2 represents hydrogen, C 1 -C 4 alkyl, or CF 3 ; R 3 represents hydrogen, C 1 -C 4 alkyl, or CF 3 ; R 4 represents a substituted or unsubstituted C 5 -C 10 aryl or a substituted or unsubstituted C 5 -C 10 heteroaryl; in free base or acid addition salt form.
摘要翻译：本发明涉及式（I）的1-氮杂 - 双环烷基衍生物; 其中取代基如本说明书中所定义，其制备方法，它们作为药物的用途以及包含它们的药物组合物。式（I）其中A表示O或N（R 1）; Y表示一组式，或其中左键连接至A基团，右键连接至R基团; R表示取代或未取代的C 5 -C 10芳基，取代或未取代的杂-C 5 -C 10芳基，N（R 1）（R 4），或> N（R 2）（CH 2） 3> [R <4>）; R代表氢，C1-C4烷基或CF3; R 2表示氢，C 1 -C 4烷基或CF 3; R 3表示氢，C 1 -C 4烷基或CF 3; R 4表示取代或未取代的C 5 -C 10芳基或取代或未取代的C 5 -C 10杂芳基; 在游离碱或酸加成盐形式。

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