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1. 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。

2. 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。

3. 发明申请

WO2015177646A1 CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：羧酰胺衍生物
公开(公告)号：WO2015177646A1
公开(公告)日：2015-11-26
申请号：PCT/IB2015/001539
申请日：2015-05-14
申请人： NOVARTIS AG , D'SOUZA, Ann-Marie , AHMED, Mahbub , PULZ, Robert, Alexander , ROONEY, Lisa, Ann , SMITH, Nichola , TROXLER, Thomas, J.
发明人： D'SOUZA, Ann-Marie , AHMED, Mahbub , PULZ, Robert, Alexander , ROONEY, Lisa, Ann , SMITH, Nichola , TROXLER, Thomas, J.
IPC分类号： C07D403/12 , A61K31/4192 , A61P9/12 , A61P19/02 , A61P19/04 , A61P19/08 , C07D487/04
CPC分类号： A61K31/4192 , A61K31/55 , C07D403/12 , C07D413/12 , C07D413/14 , C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or co-crystal thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐或共结晶; 制备本发明化合物的方法及其治疗用途。本发明还提供药理活性剂和药物组合物的组合。

4. 发明申请

WO2003042234A2 NON-PEPTIDE SOMATOSTATIN RECEPTOR LIGANDS 审中-公开
标题翻译：非肽SOMATOSTATIN受体配体
公开(公告)号：WO2003042234A2
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： C07K
CPC分类号： C07D403/06 , C07D405/14
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.
摘要翻译：本发明提供式（I）化合物，其中X，Y，R 1，R 2，R 3和R 4如说明书中所定义，及其制备。该化合物与生长抑素受体结合，并且可用作药物制剂。

5. 发明申请

WO2015173656A1 CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：羧酰胺衍生物
公开(公告)号：WO2015173656A1
公开(公告)日：2015-11-19
申请号：PCT/IB2015/001498
申请日：2015-05-14
申请人： NOVARTIS AG , ARISTA, Luca , COTESTA, Simona , D'ALESSANDRO, Pier , D'SOUZA, Anne-marie , LATTMANN, Rene , LIZOS, Dimitrios , PULZ, Robert, Alexander , ROONEY, Lisa, Ann , SMITH, Nichola , TAYLOR, Jessica, Louise , TROXLER, Thomas, J.
发明人： ARISTA, Luca , COTESTA, Simona , D'ALESSANDRO, Pier , D'SOUZA, Anne-marie , LATTMANN, Rene , LIZOS, Dimitrios , PULZ, Robert, Alexander , ROONEY, Lisa, Ann , SMITH, Nichola , TAYLOR, Jessica, Louise , TROXLER, Thomas, J.
IPC分类号： C07D403/12 , A61K31/4192 , A61P9/12 , A61P19/02 , A61P19/04 , A61P19/08 , C07D413/14 , C07D413/12
CPC分类号： C07D413/12 , A61K31/422 , C07D403/12 , C07D413/14
摘要： The present invention provides a compound of formula (I) and/or a pharmaceutically acceptable salt thereof. The compounds of formula (I) (and/or their pharmaceutically acceptable salts) demonstrate properties as Smurf-1 inhibitors and are thus useful in the treatment of a range of disorders, such as, for example, pulmonary arterial hypertension, fibrosis, rheumatoid arthritis, fracture healing, glaucoma, hereditary hemorrhagic telangiectasia (HHT), proteinuria, wound healing, COPD, and/or asthma.
摘要翻译：本发明提供式（I）化合物和/或其药学上可接受的盐。式（I）化合物（和/或其药学上可接受的盐）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，例如肺动脉高压，纤维化，类风湿性关节炎，骨折愈合，青光眼，遗传性出血性毛细血管扩张症（HHT），蛋白尿，伤口愈合，COPD和/或哮喘。

6. 发明申请

WO2007009662A1 SUBSTITUTED PIPERIDINE DERIVATIVES AS SOMATOSTATIN SST1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：取代的哌啶衍生物作为SOMATOSTATIN SST1受体拮抗剂
公开(公告)号：WO2007009662A1
公开(公告)日：2007-01-25
申请号：PCT/EP2006/006867
申请日：2006-07-13
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , HOYER, Daniel , HURTH, Konstanze , TROXLER, Thomas, J.
发明人： HOYER, Daniel , HURTH, Konstanze , TROXLER, Thomas, J.
IPC分类号： A61K31/496 , C07D407/06 , C07D407/14 , C07D409/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , A61P25/00
CPC分类号： C07D405/06 , C07D405/14 , C07D409/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Compound of the formula (I) wherein R 1 , R 2 , n and m are as defined in the specification. The compounds of formula (I) are somatostatin sst1 receptor antagonists.
摘要翻译：其中R 1，R 2，n和m的式（I）化合物如说明书中所定义。式（I）化合物是生长抑素sst1受体拮抗剂。

7. 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。

8. 发明申请

WO2006005608A1 3-(HETEROARYL-OXY)-2-ALKYL-1-AZA-BICYCLOALKYL DERIVATIVES AS ALPHA.7-NACHR LIGANDS FOR THE TREATMENT OF CNS DISEASES 审中-公开
标题翻译： 3-（异环氧）-2-烷基-1-氮杂双环烷基衍生物作为用于治疗CNS疾病的ALPHA.7-NACHR配体
公开(公告)号：WO2006005608A1
公开(公告)日：2006-01-19
申请号：PCT/EP2005/007630
申请日：2005-07-13
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FEUERBACH, Dominik , ROY, Bernard, Lucien , TROXLER, Thomas, J. , HURTH, Konstanze
发明人： FEUERBACH, Dominik , ROY, Bernard, Lucien , TROXLER, Thomas, J. , HURTH, Konstanze
IPC分类号： C07D453/02
CPC分类号： C07D453/02 , C07D487/08
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 in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acelylcholine receptors (NACHR) ligands.
摘要翻译：本发明涉及式（I）的1-氮杂 - 双环烷基衍生物，其中取代基如说明书中所定义，其制备方法，它们作为药物用于预防和治疗精神病和神经变性疾病。所要求的化合物作为烟碱乙酰胆碱受体（NACHR）配体。

9. 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。

10. 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。

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