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1. 发明授权

EP1877365B1 ACETYLENE DERIVATIVES 有权
标题翻译： ACETYLENDERIVATE
公开(公告)号：EP1877365B1
公开(公告)日：2010-11-10
申请号：EP06724539.9
申请日：2006-04-24
申请人： Novartis AG
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 R1 represents hydrogen or alkyl; R2 represents an unsubstituted or substituted heterocycle or R2 represents an unsubstituted or substituted aryl; R3 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.

2. 发明授权

EP1877364B1 PHENYLACETYLENE DERIVATIVES HAVING MGLUR5 RECEPTOR AFFINITY 有权
标题翻译：具有MGLUR5受体亲和力的苯乙炔衍生物
公开(公告)号：EP1877364B1
公开(公告)日：2009-04-08
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：本发明提供了其中取代基如说明书中所定义的式（I）化合物，它们的制备方法和相应的中间体，以及它们作为mglu5受体的调节剂的用途。

3. 发明公开

EP1877367A1 ACETYLENE DERIVATIVES 有权
标题翻译：乙炔
公开(公告)号：EP1877367A1
公开(公告)日：2008-01-16
申请号：EP06724540.7
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： 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.

4. 发明授权

EP1377578B1 BETA-CARBOLINE DERIVATIVES AND ITS PHARMACEUTICAL USE AGAINST DEPRESSION AND ANXIETY 有权
标题翻译： β-咔啉衍生物和它们的药物来对付抑郁和焦虑
公开(公告)号：EP1377578B1
公开(公告)日：2011-07-20
申请号：EP02745204.4
申请日：2002-04-02
申请人： Novartis AG , Novartis Pharma GmbH
发明人： TROXLER, Thomas, J. , HURTH, Konstanze , HOYER, Daniel
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention provides compounds of formula (I) wherein R1 to R5 are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals.

5. 发明授权

EP1761533B1 1-AZA-BICYCLO[3.3.1]NONANES 失效转让
标题翻译： 1-氮杂 - 二环[3.3.1]壬烷
公开(公告)号：EP1761533B1
公开(公告)日：2011-04-20
申请号：EP05771214.3
申请日：2005-06-17
申请人： Novartis AG
发明人： FEUERBACH, Dominik , MÜLLER, Werner , ROY, Bernard, Lucien , TROXLER, Thomas, J. , HURTH, Konstanze , FREDERIKSEN, Mathias
IPC分类号： C07D471/04 , A61K31/439 , A61P25/00
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(R1); 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 C5- C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
摘要翻译：本发明涉及式（I）的1-氮杂 - 二环烷基衍生物; 其中取代基如说明书中所定义，涉及其制备方法，其作为药物的用途以及包含它们的药物组合物。式（I），其中A代表O或N（R1）; Y代表式的基团，或者其中左键连接至A基团并且右键连接至R基团; R代表取代或未取代的C 5 -C 10芳基，取代或未取代的杂-C 5 -C 10芳基，基团N（R 1）（R 4）或基团N（R 2）（CHP 3 R 4）。 R代表氢，C 1 -C 4烷基或CF 3; R2代表氢，C1-C4烷基或CF3; R3代表氢，C1-C4烷基或CF3; R4代表取代或未取代的C5-C10芳基或取代或未取代的C5-C10杂芳基; 以游离碱或酸加成盐形式。

6. 发明公开

EP1446399A1 PIPERAZINE DERIVATIVES HAVING SST1 ANTAGONISTIC ACTIVITY 有权
标题翻译： WITH的SCom1拮抗作用哌嗪衍生物
公开(公告)号：EP1446399A1
公开(公告)日：2004-08-18
申请号：EP02787612.7
申请日：2002-11-08
申请人： Novartis AG , Novartis Pharma GmbH
发明人： TROXLER, Thomas, J. , HOYER, Daniel
IPC分类号： C07D311/90 , C07D213/74 , C07D335/20 , C07D295/18 , C07D405/12 , C07D487/04 , A61K31/352 , A61K31/382 , A61P25/24
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, R1 and R2 are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals.

7. 发明公开

EP1377578A1 BETA-CARBOLINE DERIVATIVES AND ITS PHARMACEUTICAL USE AGAINST DEPRESSION AND ANXIETY 有权
标题翻译： β-咔啉衍生物和它们的药物来对付抑郁和焦虑
公开(公告)号：EP1377578A1
公开(公告)日：2004-01-07
申请号：EP02745204.4
申请日：2002-04-02
申请人： Novartis AG , Novartis Pharma GmbH
发明人： TROXLER, Thomas, J. , HURTH, Konstanze , HOYER, Daniel
IPC分类号： C07D471/04 , C07D519/00 , A61K31/44
CPC分类号： C07D471/04
摘要： The invention provides compounds of formula (I) wherein R1 to R5 are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals.

8. 发明授权

EP3143014B1 CARBOXAMIDE DERIVATIVES 有权
公开(公告)号：EP3143014B1
公开(公告)日：2018-10-24
申请号：EP15774680.1
申请日：2015-05-14
申请人： Novartis AG
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.

9. 发明授权

EP1877367B1 ACETYLENE DERIVATIVES 有权
标题翻译： ACETYLENDERIVATE
公开(公告)号：EP1877367B1
公开(公告)日：2009-10-14
申请号：EP06724540.7
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： 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. 发明授权

EP1651592B1 NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF 有权
标题翻译： NEW二苯并[b，f]恶-10-羧酸酰胺和它们的药物应用
公开(公告)号：EP1651592B1
公开(公告)日：2009-04-29
申请号：EP04763454.8
申请日：2004-07-23
申请人： NOVARTIS AG , Novartis Pharma GmbH
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： C07C235/40 , C07D313/14 , C07D267/20 , A61K31/335 , A61K31/395 , A61K31/165 , A61P25/28
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(C1-4)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, R1 is hydrogen or (C1-4)alkyl, R2 is optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl or heteroaryl, R3 is CH(Re)CONRaRb or (CH2)nNRc,Rd, n is 0, 1 or 2, Ra, Rb, Rc and Rd, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, (C7-9)bicycloalkyl, 1-aza-(C7-9)bicycloalkyl, aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl or heterocyclyl, or Ra, Rb, Rc and Rd, together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, Re is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, (C3-7)cycloalkyl or (C3-7)cycloalkyl(C1-4)alkyl, and R4, R5, R6, R7, R8 and R9, independently, are hydrogen, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkyl-SO2, 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).

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