公开(公告)号：EP2085379A1

公开(公告)日：2009-08-05

申请号：EP09157663.7

申请日：2000-08-07

申请人： NOVARTIS AG ,  Novartis Pharma GmbH

发明人： BREITENSTEIN, Werner ,  HAYAKAWA, Kenji ,  IWASAKI, Genji ,  KANAZAWA, Takanori ,  KASAOKA, Tatsuhiko ,  KOIZUMI, Shinichi ,  MATSUNAGA, Shinichiro ,  NAKAJIMA, Motowo ,  SAKAKI, Junichi

IPC分类号： C07C311/29 ,  C07D295/12 ,  C07D405/12 ,  C07D213/42 ,  C07D211/58 ,  C07D257/04 ,  C07D207/32 ,  A61K31/18 ,  A61K31/33

CPC分类号： C07D207/32 ,  C07C311/29 ,  C07D213/42 ,  C07D215/12 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/06 ,  C07D249/08 ,  C07D257/04 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D307/52 ,  C07D333/20

摘要： α-Amino hydroxamic acid derivative of the formula I,

in which R is C 2 -C 7 -alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C 3 -C 5 -cycloalkyl or unsubstituted or substituted C 3 -C 6 -heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C 3 -C 7 -alkenyl or C 3 -C 7 -alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C 3 -C 5 -cydoalkyl or unsubstituted or substituted C 3 -C 6 -heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N;
and the other symbols are as defined in claim 1,
are described.
These compounds are MMP and in particular MMP2 inhibitors and can be used for treatment of MMP dependent diseases, in particular inflammation conditions, rheumatoid arthritis, osteoarthritis, tumors (tumor growth, metastasis, progression or invasion) and pulmonary disorders (e.g. emphysema, COPD).

摘要翻译： 其中R是C 2 -C 7 - 烷基，其是被卤素，硝基，低级酰氧基，三氟甲氧基，氰基，C 3 -C 5 - 烷基单，二或三取代的式I的氨基异羟肟酸衍生物， 环烷基或未取代或取代的C 3 -C 6 - 杂芳基，其包含一个或两个选自O，S和N的杂原子; 或C 3 -C 7 - 烯基或C 3 -C 7 - 炔基，其在每种情况下是未取代的或被卤素，硝基，低级酰氧基，三氟甲氧基，氰基，C 3 -C 5 - 或包含一个或两个选自O，S和N的杂原子的未取代或取代的C 3 -C 6 - 杂芳基; 并且其它符号如权利要求1中所定义。 这些化合物是MMP，特别是MMP2抑制剂，可用于治疗MMP依赖性疾病，特别是炎症病症，类风湿性关节炎，骨关节炎，肿瘤（肿瘤生长，转移，进展或侵袭）和肺部疾病（例如肺气肿，COPD） 。

公开(公告)号：EP1532138B1

公开(公告)日：2008-11-19

申请号：EP03762632.2

申请日：2003-07-04

申请人： NOVARTIS AG ,  Novartis Pharma GmbH

发明人： BREITENSTEIN, Werner ,  FURET, Pascal ,  JACOB, Sandra ,  MANLEY, Paul, William

IPC分类号： C07D401/14

CPC分类号： C07D401/14 ,  C07D405/14

摘要： The invention relates to compounds of formula (I) Wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such disease.

公开(公告)号：EP1879882A1

公开(公告)日：2008-01-23

申请号：EP06742763.3

申请日：2006-05-02

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： BAESCHLIN, Daniel, Kaspar ,  BREITENSTEIN, Werner ,  EHRHARDT, Claus ,  MAIBAUM, Juergen, Klaus ,  OSTERMANN, Nils ,  ZIMMERMANN, Juerg ,  RÜDISSER, Simon ,  VANGREVELINGHE. Eric ,  YOKOKAWA, Fumiaki

IPC分类号： C07D405/12 ,  C07D211/60 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D409/14 ,  A61K31/453 ,  A61K31/445 ,  A61K31/55 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/4535 ,  A61K31/4525 ,  A61P9/00

CPC分类号： C07D405/14 ,  C07D211/60 ,  C07D401/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The invention relates to 3,5-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 3,5- piperidine compound, and/or a method of treatment comprising administering a 3,5- piperidine compound, a method for the manufacture of a 3,5-piperidine compound, and novel intermediates and partial steps for their synthesis. Especially, the 3,5-piperidine compounds have the formula I, wherein the symbols have the meanings described in the specification.

公开(公告)号：EP1532138A1

公开(公告)日：2005-05-25

申请号：EP03762632.2

申请日：2003-07-04

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： BREITENSTEIN, Werner ,  FURET, Pascal ,  JACOB, Sandra ,  MANLEY, Paul, William

IPC分类号： C07D401/14

CPC分类号： C07D401/14 ,  C07D405/14

摘要： The invention relates to compounds of formula (I) Wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such disease.

公开(公告)号：EP1761505A1

公开(公告)日：2007-03-14

申请号：EP05756693.7

申请日：2005-06-23

申请人： Novartis AG ,  NOVARTIS-PHARMA GMBH ,  IRM LLC

发明人： DING, Qiang ,  GRAY, Nathanael, Schiander ,  LI, Bing ,  LIU, Yi ,  SIM, Taebo ,  UNO, Tetsuo ,  ZHANG, Guobao ,  PISSOT SOLDERMANN, Carole ,  BREITENSTEIN, Werner ,  BOLD, Guido ,  CARAVATTI, Giorgio ,  FURET, Pascal ,  GUAGNANO, Vito ,  LANG, Marc ,  MANLEY, Paul, W. ,  SCHOEPFER, Joseph ,  SPANKA, Carsten

IPC分类号： C07D239/48 ,  C07D409/12 ,  C07D401/12 ,  C07D405/12 ,  C07D403/12 ,  A61K31/505 ,  A61K31/506 ,  C07D251/48 ,  A61P35/00

CPC分类号： C07D239/48 ,  C07D251/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.

公开(公告)号：EP1689712A1

公开(公告)日：2006-08-16

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：EP1322634B1

公开(公告)日：2009-12-16

申请号：EP01984640.1

申请日：2001-09-11

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： BUERGER, Hans, Michael ,  CARAVATTI, Giorgio ,  ZIMMERMANN, Juerg ,  MANLEY, Paul, William ,  BREITENSTEIN, Werner ,  CUDD, Margaret, Amelia

IPC分类号： C07D401/04 ,  A61K31/506 ,  C07D401/14

CPC分类号： C07D401/04 ,  A61K31/506

摘要： The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula (I) wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to medicaments comprising those compounds, and the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.

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：EP1546127A1

公开(公告)日：2005-06-29

申请号：EP03750639.1

申请日：2003-09-26

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： MANLEY, Paul, William ,  BREITENSTEIN, Werner ,  JACOB, Sandra ,  FURET, Pascal

IPC分类号： C07D401/04 ,  A61K31/506 ,  A61P35/00

CPC分类号： C07D401/04

摘要： The invention relates to novel substituted N-(3-benzoylaminophenyl)-4-pyridyl-2-pyrimidinarnine derivatives, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, and a method for the treatment of such a disease.