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1. 发明申请

WO2005003106A1 MACROCYCLIC COMPOUNDS HAVING ASPARTIC PROTEASE INHIBITING ACTIVITY AND PHARMACEUTICAL USES THEREOF 审中-公开
标题翻译：具有ASPARTIC PROTEASE抑制活性的药物化合物及其药物用途
公开(公告)号：WO2005003106A1
公开(公告)日：2005-01-13
申请号：PCT/EP2004/007247
申请日：2004-07-02
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BETSCHART, Claudia , TINTELNOT-BLOMLEY, Marina
发明人： BETSCHART, Claudia , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D273/02
CPC分类号： C07D285/00 , A61K31/33 , C07D273/02 , C07D291/08
摘要： The present invention relates to macrocyclic compounds of formula (I), wherein R 1 , is (C 1-8 )alkyl, (C 1-4 )alkoxy(C 1-4 )alkyl, hydroxy(C 1-6 )alkyl, (C 1-4 )alkylthio(C 1-4 )alkyl, (C 1-6 )alkenyl, (C 3-7 )cycloalkyl, (C 3-7 )cycloalkyl(C 1-4 )alkyl, piperidinyl or pyrrolidinyl, R 2 and R 4 , independently, are hydrogen or optionally substituted (C 1-8 )alkyl, (C 3-7 ) cycloalkyl, (C 3-7 )cycloalkyl(C 1-4 )alkyl, aryl, aryl(C 1-4 )alkyl, heteroaryl or heteroaryl(C 1-4 ) alkyl, or R 2 and R 4 , together with the nitrogen to which they are attached, form an optionally substituted piperidino, pyrrolidinyl, morpholino or piperazinyl group, R 3 is hydrogen or (C 1-4 )alkyl, X 1 is CH 2 , X 2 is CH 2 , O, S, CO, COO, OCO, NHCO, CONH, or NR, R being hydrogen or (C 1-4 )alkyl, Y is (C 1-8 )alkylen or (C 1-8 )alkylenoxy(C 1-6 )alkylen, (C 1-8 )alkenylen or (C 1-8 )alkenylenoxy(C 1-6 )alkylen, Ar is a phenyl ring optionally mono- di or trisubstituted by, independently, hydroxy or halogen, whereby X 1 , and X 2 are in meta or para position to each other, and either Z is CO, AA is a natural or unnatural alpha-amino-acid, and n is 0 or 1, or Z is S0 2 , AA is an optionally substituted ethylencarbonyl group (derived from a natural or unnatural alpha-amino acid by replacement of the nitrogen by a methylen group), and n is 1; processes for the preparation of these compounds; pharmaceutical compositions and combinations comprising the same; and their use in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation.
摘要翻译：本发明涉及式（I）的大环化合物，其中R1是（C1-8）烷基，（C1-4）烷氧基（C1-4）烷基，羟基（C1-6）烷基，（C1-4）烷硫基（C 1-4）烷基，（C 1-6）烯基，（C 3-7）环烷基，（C 3-7）环烷基（C 1-4）烷基，哌啶基或吡咯烷基，R 2和R 4独立地为氢或任选取代（C 1-8）烷基，（C 3-7）环烷基，（C 3-7）环烷基（C 1-4）烷基，芳基，芳基（C 1-4）烷基，杂芳基或杂芳基 R4与其连接的氮一起形成任选取代的哌啶子基，吡咯烷基，吗啉代或哌嗪基，R 3是氢或（C 1-4）烷基，X 1是CH 2，X 2是CH 2，O，S，CO， CO，OCO，NHCO，CONH或NR，R为氢或（C1-4）烷基，Y为（C1-8）亚烷基或（C1-8）亚烷基氧基（C1-6）亚烷基，（C1-8）或（C 1-8）亚烯基氧基（C 1-6）亚烷基，Ar是任选被羟基或卤素单独二或三取代的苯环，其中X 1和X 2在每个ot 而且Z为CO，AA为天然或非天然的α-氨基酸，n为0或1，或Z为SO 2，AA为任选取代的亚乙基羰基（衍生自天然或非天然的α-氨基酸通过亚甲基取代氮），n为1; 制备这些化合物的方法; 药物组合物及其组合物; 以及它们用于治疗与β-淀粉样蛋白生成和/或聚集相关的神经和血管疾病的用途。

2. 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。

3. 发明申请

WO2008009750A2 MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：大环化合物可用作BACE抑制剂
公开(公告)号：WO2008009750A2
公开(公告)日：2008-01-24
申请号：PCT/EP2007/057540
申请日：2007-07-20
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem Jacob
发明人： LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem Jacob
IPC分类号： C07D245/06 , C07D401/12 , C07D413/14 , C07D413/12 , C07D273/02 , C07D273/00 , A61K31/395 , A61K31/4427 , A61P25/00
CPC分类号： C07D273/00 , C07D245/06 , C07D273/02 , C07D401/12 , C07D413/12 , C07D413/14
摘要： The invention relates to novel macrocyclic compounds of the Formula (I) in which all of the variables are as defined in the specification, in free base form or in acid addition 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）的新型大环化合物，其中所有变量如本说明书中所定义，游离碱形式或酸加成盐形式，其制备方法，用作药物和药物，其包含他们。

4. 发明申请

WO2007093621A1 CYCLIC SULFONES USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：循环硫磺有效用作BACE抑制剂
公开(公告)号：WO2007093621A1
公开(公告)日：2007-08-23
申请号：PCT/EP2007/051454
申请日：2007-02-14
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , RUEEGER, Heinrich , MCCARTHY, Clive , MOEBITZ, Henrik , RONDEAU, Jean-Michel , TINTELNOT-BLOMLEY, Marina
发明人： RUEEGER, Heinrich , MCCARTHY, Clive , MOEBITZ, Henrik , RONDEAU, Jean-Michel , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D335/02
CPC分类号： C07D335/02 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12
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 base form or in acid addition 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，其中所有变量如本说明书中所定义，游离碱形式或酸加成盐形式，其制备方法，用作药物和药物包括他们。

5. 发明申请

WO2007077004A1 MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：大环化合物可用作BACE抑制剂
公开(公告)号：WO2007077004A1
公开(公告)日：2007-07-12
申请号：PCT/EP2006/012569
申请日：2006-12-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BETSCHART, Claudia , KOLLER, Manuel , LAUMEN, Kurt , LERCHNER, Andreas , MACHAUER, Rainer , MCCARTHY, Clive , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem, Jacob
发明人： BETSCHART, Claudia , KOLLER, Manuel , LAUMEN, Kurt , LERCHNER, Andreas , MACHAUER, Rainer , MCCARTHY, Clive , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem, Jacob
IPC分类号： C07D245/04 , A61P25/00 , A61K31/33
CPC分类号： C07D245/04 , C07D273/00
摘要： The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free base form or in acid addition 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）的新型大环化合物，其中所有变量如说明书中所定义，游离碱形式或酸加成盐形式，其制备方法，用作药物和药物包括他们。

6. 发明申请

WO2006074950A1 MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：大环化合物可用作BACE抑制剂
公开(公告)号：WO2006074950A1
公开(公告)日：2006-07-20
申请号：PCT/EP2006/000280
申请日：2006-01-13
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BETSCHART, Claudia , LERCHNER, Andreas , MACHAUER, Rainer , RÜEGER, Heinrich , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem, Jacob
发明人： BETSCHART, Claudia , LERCHNER, Andreas , MACHAUER, Rainer , RÜEGER, Heinrich , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem, Jacob
CPC分类号： C07D273/00 , C07D245/04 , C07D273/02 , C07D413/04 , C07D413/12 , C07D413/14 , C07D471/08
摘要： The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables 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 medicaments and to medicaments comprising them.
摘要翻译：本发明涉及式（I）的新型大环化合物，其中所有变量如说明书中所定义，大环中包括的环原子数为14,15,16或17，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。

7. 发明申请

WO2007140980A1 PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：吡咯烷衍生物有效用作BACE抑制剂
公开(公告)号：WO2007140980A1
公开(公告)日：2007-12-13
申请号：PCT/EP2007/004959
申请日：2007-06-04
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , ROGEL, Olivier , RONDEAU, Jean-Michel , RUEEGER, Heinrich , SIMIC, Oliver , SIROCKIN, Finton , TINTELNOT-BLOMLEY, Marina
发明人： ROGEL, Olivier , RONDEAU, Jean-Michel , RUEEGER, Heinrich , SIMIC, Oliver , SIROCKIN, Finton , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D215/48 , A61K31/47 , A61P25/28
CPC分类号： C07D215/48
摘要： Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class in the treatment of a disease that depends on the activity of beta- secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound. The substituted pyrrolidine compounds are especially of the formula (I), wherein the substituents are as defined in the specification.
摘要翻译：新型3-单，3,4-二和3,4,4-三取代的吡咯烷化合物，用于诊断和治疗温血动物，特别是用于治疗疾病的化合物（=无序），其取决于β-分泌酶的活性和/或β-淀粉样蛋白的产生，并随后聚集成低聚物和原纤维; 使用该类化合物来制备用于治疗依赖于β-分泌酶的活性和/或产生β-淀粉样蛋白的疾病的药物制剂并随后聚集成低聚物和原纤维; 使用该类化合物治疗依赖于β-分泌酶活性和/或产生β-淀粉样蛋白的疾病，随后聚集成低聚物和原纤维; 包含所述取代的吡咯烷化合物的药物制剂和/或包括施用所述取代的吡咯烷化合物的治疗方法。取代的吡咯烷化合物特别是式（I），其中取代基如说明书中所定义。

8. 发明申请

WO2006074940A3 MACROCYCLIC COMPOUNDS AND COMPOSITIONS USEFUL AS BACE INHIBITORS 审中-公开
公开(公告)号：WO2006074940A3
公开(公告)日：2006-07-20
申请号：PCT/EP2006/000265
申请日：2006-01-13
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , LERCHNER, Andreas , MACHAUER, Rainer , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina
发明人： LERCHNER, Andreas , MACHAUER, Rainer , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D245/06 , C07D281/00 , A61P25/28 , A61K31/395
摘要： The invention relates to novel macrocyclic compounds of the formula in which R 1 , R 3 , V 1 , V 2 , X 1 , X 2 , Y, Z, Ar, AA and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16, 17 or 18, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

9. 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。

10. 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。

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