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公开(公告)号：EP1833816B1
公开(公告)日：2009-11-11
申请号：EP05820552.7
申请日：2005-12-28
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BREITENSTEIN, Werner , EHARA, Takeru Novartis Pharma K.K. , EHRHARDT, Claus , GROSCHE, Philipp , HITOMI, Yuko Novartis Pharma K.K. , IWAKI, Yuki Novartis Pharma K.K. , KANAZAWA, Takanori Novartis Pharma K.K. , KONISHI, Kazuhide Novartis Pharma K.K. , MAIBAUM, Juergen, Klaus , MASUYA, Keiichi , NIHONYANAGI, Atsuko Novartis Pharma K.K. , OSTERMANN, Nils , SUZUKI, Masaki Novartis Pharma K.K. , TOYAO, Atsushi Novartis Pharma K.K. , YOKOKAWA, Fumiaki Novartis Pharma K.K.
IPC分类号： C07D401/10 , C07D401/12 , C07D413/12 , C07D413/04 , C07D409/12 , C07D405/12 , C07D409/10 , C07D401/14 , C07D417/12 , C07D413/14 , C07D471/04 , A61K31/4545 , A61P9/00
CPC分类号： C07D471/04 , C07D211/60 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/10 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12
摘要： 3,4-substituted piperidine 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 activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.
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2.发明授权4-PHENYLPIPERIDINE DERIVATIVES AS RENIN INHIBITORS 有权4- PHENYLPIPERIDINDERIVATE ALS RENININHIBITOREN
公开(公告)号：EP1689712B1
公开(公告)日：2009-08-19
申请号：EP04798086.7
申请日：2004-11-25
申请人： NOVARTIS AG , NOVARTIS-PHARMA GMBH
发明人： SEDRANI, Richard , MAIBAUM, Jürgen, Klaus , BREITENSTEIN, Werner , SELLNER, Holger , EHRHARDT, Claus , OSTERMANN, Nils
IPC分类号： C07D211/42 , C07D405/04 , C07D401/10 , C07D409/10 , A61K31/4418 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444
CPC分类号： C07D401/10 , C07D211/42 , C07D405/04 , C07D409/10
摘要： Compounds of the present invention having the formula (I) exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
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3.发明公开AMINO-PROPANOL DERIVATIVES AS SPHINGOSINE-1-PHOSPHATE RECEPTOR MODULATOR 有权AMINO-PROPANOLDERIVATIVE AS鞘氨醇-1-磷酸受体的调节剂
公开(公告)号：EP1636171A2
公开(公告)日：2006-03-22
申请号：EP04739810.2
申请日：2004-06-11
申请人： Novartis AG , Novartis Pharma GmbH
发明人： EHRHARDT, Claus , HINTERDING, Klaus
IPC分类号： C07C217/72 , C07F9/09 , A61K31/137 , A61K31/661 , A61P31/00 , A61P37/02
CPC分类号： C07F9/094 , C07C217/72 , C07F9/65744
摘要： Compounds of formula (I) wherein A, R1, R2, R3, R4 and R5 as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
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4.发明公开
公开(公告)号：EP1337527A1
公开(公告)日：2003-08-27
申请号：EP01993604.6
申请日：2001-11-05
申请人： Novartis AG , Novartis Pharma GmbH
发明人： ALBERT, Rainer , COOKE, Nigel, Graham , COTTENS, Sylvain , EHRHARDT, Claus , EVENOU, Jean-Pierre , SEDRANI, Richard , VON MATT, Peter , WAGNER, Jürgen , ZENKE, Gerhard
IPC分类号： C07D403/04 , C07D403/14 , A61K31/404 , A61P29/00 , A61P37/06
CPC分类号： C07D403/14 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D471/10
摘要： Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.
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公开(公告)号：EP2007788A2
公开(公告)日：2008-12-31
申请号：EP07781535.5
申请日：2007-04-09
申请人： NOVARTIS AG , Novartis Pharma GmbH
发明人： COTTENS, Sylvain , EHRHARDT, Claus , FU, Jiping , PARKER, David Thomas , PATANE, Michael , RADETICH, Branko , RAMAN, Prakash , RANDL, Stefan Andreas , RIGOLLIER, Pascal , SEEPERSAUD, Mohindra , SIMIC, Oliver , WAN, Dongpeng
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/06078 , C07K5/06165 , C07K5/0808 , C07K5/1016
摘要： The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
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6.发明公开
公开(公告)号：EP1836163A2
公开(公告)日：2007-09-26
申请号：EP05825434.3
申请日：2005-12-21
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BREITENSTEIN, Werner , COTTENS, Sylvain , EHRHARDT, Claus , JACOBY, Edgar , LORTHIOIS, Edwige, Liliane, Jeanne , MAIBAUM, Juergen, Klaus , OSTERMANN, Nils , SELLNER, Holger , SIMIC, Oliver
IPC分类号： C07D207/09 , C07D207/14 , C07D401/12 , C07D405/12 , C07D403/12 , C07D409/12 , C07D207/08 , C07D413/12 , C07D417/12 , C07D491/10 , A61K31/40 , A61K31/41 , A61K31/435 , A61K31/54 , A61P9/00
CPC分类号： C07D207/08 , C07D207/09 , C07D207/14 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/10
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 inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula (I), wherein the substituents are as described in the specificacion.
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公开(公告)号：EP1833816A1
公开(公告)日：2007-09-19
申请号：EP05820552.7
申请日：2005-12-28
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BREITENSTEIN, Werner , EHARA, Takeru Novartis Pharma K.K. , EHRHARDT, Claus , GROSCHE, Philipp , HITOMI, Yuko Novartis Pharma K.K. , IWAKI, Yuki Novartis Pharma K.K. , KANAZAWA, Takanori Novartis Pharma K.K. , KONISHI, Kazuhide Novartis Pharma K.K. , MAIBAUM, Juergen, Klaus , MASUYA, Keiichi , NIHONYANAGI, Atsuko Novartis Pharma K.K. , OSTERMANN, Nils , SUZUKI, Masaki Novartis Pharma K.K. , TOYAO, Atsushi Novartis Pharma K.K. , YOKOKAWA, Fumiaki Novartis Pharma K.K.
IPC分类号： C07D401/10 , C07D401/12 , C07D413/12 , C07D413/04 , C07D409/12 , C07D405/12 , C07D409/10 , C07D401/14 , C07D417/12 , C07D413/14 , C07D471/04 , A61K31/4545 , A61P9/00
CPC分类号： C07D471/04 , C07D211/60 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/10 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12
摘要： 3,4-substituted piperidine 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 activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.
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公开(公告)号：EP1154988B1
公开(公告)日：2004-08-11
申请号：EP00916832.9
申请日：2000-02-14
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BAENTELI, Rolf , BAUER, Wilfried , COTTENS, Sylvain , EHRHARDT, Claus , HOMMEL, Ulrich , KALLEN, Jörg , MEINGASSNER, Josef, Gottfried , NUNINGER, François , WEITZ-SCHMIDT, Gabriele
IPC分类号： C07C235/26 , C07C237/18 , C07C235/30 , C07C237/20 , C07D211/76 , C07D265/24 , C07D401/06 , A61K31/4402 , A61K31/45 , A61K31/4545 , A61K31/535 , A61P9/10 , A61P3/06 , A61P29/00 , A61P37/00
CPC分类号： C07C271/12 , C07C235/26 , C07C235/30 , C07C237/18 , C07C2602/28 , C07D211/76 , C07D265/10
摘要： Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.
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9.发明公开
公开(公告)号：EP1863477A1
公开(公告)日：2007-12-12
申请号：EP06707621.6
申请日：2006-03-21
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： SELLNER, Holger , OSTERMANN, Nils , MAIBAUM, Juergen, Klaus , LORTHIOIS, Edwige, Liliane, Jeanne , IRIE, Osamu NOvartis Pharma K.K. , EHRHARDT, Claus
IPC分类号： A61K31/4025 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/4035 , A61K31/404 , A61K31/416 , A61K31/422 , A61K31/4409 , A61K31/454 , A61K31/4704 , A61K31/506 , A61K31/5355 , A61K31/5377
CPC分类号： C07D207/27 , A61K31/341 , A61K31/351 , A61K31/352 , A61K31/357 , A61K31/4025 , A61K31/4035 , A61K31/404 , A61K31/416 , A61K31/422 , A61K31/423 , A61K31/4409 , A61K31/454 , A61K31/4704 , A61K31/506 , A61K31/5355 , A61K31/5377 , C07D207/09 , C07D207/16 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine 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 activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The substituted pyrrolidine compounds are of the formula (I), wherein R1, R2, R3, R4, R5 and T are defined as in the specification.
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公开(公告)号：EP1220852B1
公开(公告)日：2006-01-18
申请号：EP00969490.2
申请日：2000-10-11
申请人： Novartis AG , Novartis Pharma GmbH
发明人： ALBERT, Rainer , EHRHARDT, Claus , HOMMEL, Ulrich , KALLEN, Jörg , MEINGASSNER, Josef, Gottfried , ROCHE, Didier , WATTANASIN, Sompong , WEITZ-SCHMIDT, Gabriele , WELZENBACH, Karl
IPC分类号： C07D401/06 , C07D243/08 , A61K31/4709 , A61K31/551
CPC分类号： C07K5/06139 , A61K38/05 , A61K31/00 , A61K2300/00
摘要： The invention provides novel diazepanes having interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1, -ICAM-2 or -ICAM-3 interactions.
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