公开(公告)号：EP2661433B1

公开(公告)日：2017-08-16

申请号：EP12700094.1

申请日：2012-01-02

申请人： Novartis AG

发明人： ALTMANN, Eva ,  HOMMEL, Ulrich ,  LORTHIOIS, Edwige Liliane Jeanne ,  MAIBAUM, Juergen Klaus ,  OSTERMANN, Nils ,  QUANCARD, Jean ,  RANDL, Stefan Andreas ,  SIMIC, Oliver ,  VULPETTI, Anna ,  ROGEL, Olivier

IPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61K31/403 ,  A61K31/407 ,  A61K31/416 ,  A61P27/02

CPC分类号： C07D403/12 ,  A61K31/404 ,  A61K31/437 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

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.

公开(公告)号：EP2867222A1

公开(公告)日：2015-05-06

申请号：EP13765775.5

申请日：2013-06-27

申请人： Novartis AG

发明人： HOMMEL, Ulrich ,  LORTHIOIS, Edwige Liliane Jeanne ,  MAIBAUM, Juergen Klaus ,  OSTERMANN, Nils ,  RANDL, Stefan Andreas ,  VULPETTI, Anna

IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D471/04 ,  C07D417/14 ,  A61K31/444 ,  A61K31/4745 ,  A61K31/497 ,  A61K31/4439 ,  A61P27/00 ,  A61P9/00 ,  A61P11/00 ,  A61P19/00 ,  A61P37/00 ,  A61P3/00

CPC分类号： C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D417/14

摘要： The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as complement alternative inhibitors for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

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.

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.

公开(公告)号：EP2867225B1

公开(公告)日：2017-08-09

申请号：EP13762561.2

申请日：2013-06-27

申请人： Novartis AG

发明人： ALTMANN, Eva ,  HOMMEL, Ulrich ,  LORTHIOIS, Edwige, Liliane, Jeanne ,  MAIBAUM, Juergen, Klaus ,  OSTERMANN, Nils ,  QUANCARD, Jean ,  RANDL, Stefan, Andreas ,  VULPETTI, Anna

IPC分类号： C07D403/06 ,  C07D403/14 ,  C07D417/14 ,  C07D417/04 ,  A61K31/506 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/427 ,  A61P27/00 ,  A61P9/00 ,  A61P11/00 ,  A61P19/00 ,  A61P37/00 ,  A61P3/00

CPC分类号： A61K38/05 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D417/14 ,  C07D471/04 ,  C07K5/06026

公开(公告)号：EP2661433A1

公开(公告)日：2013-11-13

申请号：EP12700094.1

申请日：2012-01-02

申请人： Novartis AG

发明人： ALTMANN, Eva ,  HOMMEL, Ulrich ,  LORTHIOIS, Edwige Liliane Jeanne ,  MAIBAUM, Juergen Klaus ,  OSTERMANN, Nils ,  QUANCARD, Jean ,  RANDL, Stefan Andreas ,  SIMIC, Oliver ,  VULPETTI, Anna ,  ROGEL, Olivier

IPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61K31/403 ,  A61K31/407 ,  A61K31/416 ,  A61P27/02

CPC分类号： C07D403/12 ,  A61K31/404 ,  A61K31/437 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： The present invention provides a compound of formula (I): 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：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。

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.

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.

公开(公告)号：EP2872503A2

公开(公告)日：2015-05-20

申请号：EP13765778.9

申请日：2013-06-27

申请人： Novartis AG

发明人： HOMMEL, Ulrich ,  LORTHIOIS, Edwige Liliane Jeanne ,  MAIBAUM, Juergen Klaus ,  OSTERMANN, Nils ,  RANDL, Stefan Andreas ,  VULPETTI, Anna ,  ROGEL, Olivier

IPC分类号： C07D403/14 ,  A61K31/403 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4162 ,  A61P27/02

CPC分类号： C07D403/14 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/437 ,  A61K45/06 ,  C07D471/04 ,  A61K2300/00

摘要： The present invention provides a compound of formula I: 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： 本发明提供了式I化合物：制备本发明化合物的方法及其治疗用途。 本发明进一步提供药理活性剂和药物组合物的组合。