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1. 发明申请

WO2013192345A1 COMPLEMENT PATHWAY MODULATORS AND USES THEREOF 审中-公开
标题翻译：补充路径调制器及其用途
公开(公告)号：WO2013192345A1
公开(公告)日：2013-12-27
申请号：PCT/US2013/046644
申请日：2013-06-19
申请人： NOVARTIS AG , DECHANTSREITER, Michael A. , GROB, Jonathan E. , MAC SWEENEY, Aengus , MILTZ, Wolfgang , RANDL, Stefan , SEDRANI, Richard , SELLNER, Holger , SIROCKIN, Finton , VALEUR, Eric
发明人： DECHANTSREITER, Michael A. , GROB, Jonathan E. , MAC SWEENEY, Aengus , MILTZ, Wolfgang , RANDL, Stefan , SEDRANI, Richard , SELLNER, Holger , SIROCKIN, Finton , VALEUR, Eric
IPC分类号： C07D403/12 , C07D401/14 , C07D413/14 , C07D401/12 , C07D403/04 , C07D403/14 , C07D405/12 , C07D409/12 , C07D239/95 , A61K31/517 , A61P27/00 , A61P37/00
CPC分类号： C07D239/95 , A61K31/517 , A61K31/5377 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D413/14
摘要： The present invention provides a compound of formula I a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitor of the complement alternative pathway and particularly as inhibitor of Factor B for the treatment of e.g. age-related macular degeneration and diabetic retinopathy. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供了式I化合物，其制备本发明化合物的方法及其治疗用途作为补体替代途径的抑制剂，特别是作为因子B的抑制剂，用于治疗例如血液透析液。年龄相关性黄斑变性和糖尿病性视网膜病变。本发明还提供药理活性剂和药物组合物的组合。

2. 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。

3. 发明申请

WO2007071738A1 CONDENSED HETEROCYCLIC COMPOUNDS USEFUL AS DPP-IV INHIBITORS 审中-公开
标题翻译：浓缩的杂环化合物可用作DPP-IV抑制剂
公开(公告)号：WO2007071738A1
公开(公告)日：2007-06-28
申请号：PCT/EP2006/070029
申请日：2006-12-20
申请人： Novartis AG , Novartis Pharma GmbH , BAESCHLIN, Daniel Kaspar , CLARK, David Edward , DUNSDON, Stephen John , FENTON, Garry , FILLMORE, Amanda , HARRIS, Neil Victor , HIGGS, Christopher , HURLEY, Christopher Antony , KRINTEL, Sussie Lerche , MACKENZIE, Robert Edward , OSTERMANN, Nils , SIROCKIN, Finton , SUTTON, Jonathan Mark
发明人： BAESCHLIN, Daniel Kaspar , CLARK, David Edward , DUNSDON, Stephen John , FENTON, Garry , FILLMORE, Amanda , HARRIS, Neil Victor , HIGGS, Christopher , HURLEY, Christopher Antony , KRINTEL, Sussie Lerche , MACKENZIE, Robert Edward , OSTERMANN, Nils , SIROCKIN, Finton , SUTTON, Jonathan Mark
IPC分类号： C07D487/04 , A61K31/519 , A61P3/00 , A61P7/00 , A61P9/00 , A61P25/00
CPC分类号： C07D487/04
摘要： The invention provides novel deazaxanthine and deazahypoxanthine compounds, of formula (I), wherein X is -CH= and Y is =N-; or X is -C(O)- and Y is -N(R 3 )-; The compounds may be useful in the therapy of diseases and conditions in wich dipeptidylpeptidase-IV (DPP-IV) is implicated.
摘要翻译：本发明提供了式（I）的新型脱珠黄质和去偶氮黄嘌呤化合物，其中X为-CH =，Y为= N-; 或X是-C（O） - ，Y是-N（R 3））。该化合物可用于治疗涉及二肽基肽酶-IV（DPP-IV）的疾病和病症。

4. 发明申请

WO2008077597A1 1-AMINOMETHYL- L- PHENYL- CYCLOHEXANE DERIVATIVES AS DDP-IV INHIBITORS 审中-公开
标题翻译：作为DDP-IV抑制剂的1-氨基乙基-L-苯基环己烷衍生物
公开(公告)号：WO2008077597A1
公开(公告)日：2008-07-03
申请号：PCT/EP2007/011304
申请日：2007-12-20
申请人： NOVARTIS AG , BAESCHLIN, Daniel, Kaspar , SEDRANI, Richard , FLOHR, Stefanie , NAMOTO, Kenji , SIROCKIN, Finton , GESSIER, François , FENTON, Garry , BESWIK, Mandy, Christine , CLARK, David, Edward , WASZKOWYCZ, Bohdan
发明人： BAESCHLIN, Daniel, Kaspar , SEDRANI, Richard , FLOHR, Stefanie , NAMOTO, Kenji , SIROCKIN, Finton , GESSIER, François , FENTON, Garry , BESWIK, Mandy, Christine , CLARK, David, Edward , WASZKOWYCZ, Bohdan
IPC分类号： A61K31/137 , A61K31/4985 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/381 , A61K31/4015 , A61K31/4035 , A61K31/415 , A61K31/417 , A61K31/4172 , A61K31/42 , A61K31/429 , A61K31/433 , A61K31/437
CPC分类号： C07C215/42 , C07C211/29 , C07C211/31 , C07C211/40 , C07C215/14 , C07C217/16 , C07C217/52 , C07C229/16 , C07C233/41 , C07C237/10 , C07C237/24 , C07C237/36 , C07C255/24 , C07C271/20 , C07C311/07 , C07C311/08 , C07C311/20 , C07C311/29 , C07C317/32 , C07C317/44 , C07C2601/02 , C07C2601/14 , C07D207/404 , C07D211/14 , C07D211/60 , C07D213/64 , C07D213/81 , C07D213/82 , C07D233/36 , C07D237/14 , C07D237/24 , C07D239/10 , C07D239/90 , C07D263/20 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/14 , C07D409/04 , C07D471/04 , C07D487/04
摘要： Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R 3 , R 4 , R 5 , R 6 , R 7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.
摘要翻译：提供式（I）化合物：其中V，W，X，Y，Z，R 3，R 4，R 5， R 6，R 7和m如说明书中所定义; 及其药学上可接受的盐和前药。该化合物可用于治疗或预防涉及二肽基肽酶-IV（DPP-IV）的各种疾病和病症。

5. 发明申请

WO2007115821A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2007115821A2
公开(公告)日：2007-10-18
申请号：PCT/EP2007/003185
申请日：2007-04-10
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BAESCHLIN, Daniel, Kaspar , FENTON, Garry , NAMOTO, Kenji , OSTERMANN, Nils , SEDRANI, Richard , SIROCKIN, Finton
发明人： BAESCHLIN, Daniel, Kaspar , FENTON, Garry , NAMOTO, Kenji , OSTERMANN, Nils , SEDRANI, Richard , SIROCKIN, Finton
IPC分类号： C07D211/26 , C07D211/96 , C07D471/08 , A61K31/439 , A61P3/10
CPC分类号： C07D211/96 , C07D211/26 , C07D471/08
摘要： The present invention relates to compounds of the formula; and their use in therapy.
摘要翻译：本发明涉及下式的化合物：及其在治疗中的应用。

6. 发明申请

WO2007113226A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2007113226A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053064
申请日：2007-03-29
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BAESCHLIN, Daniel Kaspar , OSTERMANN, Nils , GESSIER, Francois , SIROCKIN, Finton , NAMOTO, Kenji
发明人： BAESCHLIN, Daniel Kaspar , OSTERMANN, Nils , GESSIER, Francois , SIROCKIN, Finton , NAMOTO, Kenji
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61K31/4985 , A61K31/5025 , A61P3/00
CPC分类号： C07D519/00 , C07D471/04
摘要： New compounds of the Formula (I) for the treatment of non-insulin-dependent diabetes mellitus.
摘要翻译：式（I）的新化合物用于治疗非胰岛素依赖性糖尿病。

7. 发明公开

EP2029544A1 PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS 审中-公开
标题翻译： AS BACE抑制剂SUITABLE吡咯烷
公开(公告)号：EP2029544A1
公开(公告)日：2009-03-04
申请号：EP07725827.5
申请日：2007-06-04
申请人： NOVARTIS AG
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.

8. 发明授权

EP2864322B1 COMPLEMENT PATHWAY MODULATORS AND USES THEREOF 有权
标题翻译：调制器和其用途的补
公开(公告)号：EP2864322B1
公开(公告)日：2016-04-27
申请号：EP13733200.3
申请日：2013-06-19
申请人： Novartis AG
发明人： GROB, Jonathan E. , MAC SWEENEY, Aengus , DECHANTSREITER, Michael A. , MILTZ, Wolfgang , RANDL, Stefan , SEDRANI, Richard , SELLNER, Holger , SIROCKIN, Finton , VALEUR, Eric
IPC分类号： C07D403/12 , C07D401/14 , C07D413/14 , C07D401/12 , C07D403/04 , C07D403/14 , C07D405/12 , C07D409/12 , C07D239/95 , A61K31/517 , A61P27/00 , A61P37/00
CPC分类号： C07D239/95 , A61K31/517 , A61K31/5377 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D413/14

9. 发明公开

EP2007723A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：EP2007723A2
公开(公告)日：2008-12-31
申请号：EP07724126.3
申请日：2007-04-10
申请人： NOVARTIS AG
发明人： BAESCHLIN, Daniel, Kaspar , FENTON, Garry , NAMOTO, Kenji , OSTERMANN, Nils , SEDRANI, Richard , SIROCKIN, Finton
IPC分类号： C07D211/26 , C07D211/96 , C07D471/08 , A61K31/439 , A61P3/10
CPC分类号： C07D211/96 , C07D211/26 , C07D471/08
摘要： The present invention relates to compounds of the formula; and their use in therapy.
摘要翻译：本发明涉及下式的化合物：和它们在治疗中的用途。

10. 发明公开

EP1966215A1 CONDENSED HETEROCYCLIC COMPOUNDS USEFUL AS DPP-IV INHIBITORS 审中-公开
标题翻译：简明杂环化合物AS DDP-IV抑制剂
公开(公告)号：EP1966215A1
公开(公告)日：2008-09-10
申请号：EP06848730.5
申请日：2006-12-20
申请人： Novartis AG
发明人： BAESCHLIN, Daniel Kaspar , CLARK, David Edward , DUNSDON, Stephen John , FENTON, Garry , FILLMORE, Amanda , HARRIS, Neil Victor , HIGGS, Christopher , HURLEY, Christopher Antony , KRINTEL, Sussie Lerche , MACKENZIE, Robert Edward , OSTERMANN, Nils , SIROCKIN, Finton , SUTTON, Jonathan Mark
IPC分类号： C07D487/04 , A61K31/519 , A61P3/00 , A61P7/00 , A61P9/00 , A61P25/00
CPC分类号： C07D487/04
摘要： The invention provides novel deazaxanthine and deazahypoxanthine compounds, of formula (I), wherein X is -CH= and Y is =N-; or X is -C(O)- and Y is -N(R3)-; The compounds may be useful in the therapy of diseases and conditions in wich dipeptidylpeptidase-IV (DPP-IV) is implicated.

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