公开(公告)号：EP1129075A1

公开(公告)日：2001-09-05

申请号：EP99971802.6

申请日：1999-11-08

申请人： Novartis AG ,  Novartis-Erfindungen Verwaltungsgesellschaft m.b.H. ,  SCHERING AKTIENGESELLSCHAFT

发明人： ALTMANN, Karl-Heinz ,  BOLD, Guido ,  FURET, Pascal ,  MANLEY, Paul, William ,  WOOD, Jeanette, Marjorie ,  FERRARI, Stefano ,  HOFMANN, Francesco ,  MESTAN, Jürgen ,  HUTH, Andreas ,  KRÜGER, Martin ,  SEIDELMANN, Dieter ,  MENRAD, Andreas ,  HABEREY, Martin ,  THIERAUCH, Karl-Heinz

IPC分类号： C07D213/38 ,  A61K31/44 ,  C07D215/12 ,  A61K31/47 ,  C07D213/64 ,  C07D233/54 ,  A61K31/415 ,  C07D213/89 ,  C07D405/12 ,  A61P35/00

CPC分类号： A61K31/415 ,  A61K31/44 ,  A61K31/47 ,  C07D213/38 ,  C07D213/56 ,  C07D213/64 ,  C07D213/89 ,  C07D215/12 ,  C07D233/54 ,  C07D405/12

摘要： Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10-(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y = SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.

公开(公告)号：EP1129074A2

公开(公告)日：2001-09-05

申请号：EP99953967.9

申请日：1999-11-09

申请人： SCHERING AKTIENGESELLSCHAFT ,  Novartis AG

发明人： HUTH, Andreas ,  SEIDELMANN, Dieter ,  THIERAUCH, Karl-Heinz ,  BOLD, Guido ,  MANLEY, Paul, William ,  FURET, Pascal ,  WOOD, Jeanette, Marjorie ,  MESTAN, Jürgen ,  BRÜGGEN, Jose ,  FERRARI, Stefano ,  KRÜGER, Martin ,  OTTOW, Eckhard ,  MENRAD, Andreas ,  SCHIRNER, Michael

IPC分类号： C07D213/38

CPC分类号： C07C237/32

摘要： The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.

公开(公告)号：EP1418917A1

公开(公告)日：2004-05-19

申请号：EP02794592.2

申请日：2002-08-09

申请人： Novartis AG ,  GSF - National Research Institute for Environment and Health, GmbH ,  GSF - Forschungszentrum für Umwelt und Gesundheit GmbH ,  BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

发明人： DONATO, Nicholas, J. ,  FABBRO, Doriano ,  MANLEY, Paul, William ,  MESTAN, Jürgen ,  WARMUTH, Markus ,  HALLEK, Michael ,  TALPAZ, Moshe ,  WU, Ji

IPC分类号： A61K31/506 ,  A61K31/519 ,  A61P35/02

CPC分类号： A61K35/02 ,  A61K31/506 ,  A61K31/519

摘要： The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine.

公开(公告)号：EP1879585A1

公开(公告)日：2008-01-23

申请号：EP06751956.1

申请日：2006-05-01

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： ALLAND, Leila ,  FABBRO, Doriano ,  MESTAN, Jürgen ,  MANLEY, Paul, W.

IPC分类号： A61K31/506 ,  A61P7/00 ,  A61P37/00 ,  A61P35/00

CPC分类号： A61K31/506

摘要： The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of systemic mastocytosis.

公开(公告)号：EP1879584B1

公开(公告)日：2016-06-22

申请号：EP06724677.7

申请日：2006-05-02

申请人： Novartis AG

发明人： MANLEY, Paul, W. ,  MESTAN, Jürgen ,  FABBRO, Doriano

IPC分类号： A61K31/506 ,  A61P7/00 ,  A61P35/02

CPC分类号： A61K31/506

公开(公告)号：EP1879585B1

公开(公告)日：2013-04-17

申请号：EP06751956.1

申请日：2006-05-01

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： ALLAND, Leila ,  FABBRO, Doriano ,  MESTAN, Jürgen ,  MANLEY, Paul, W.

IPC分类号： A61K31/506 ,  A61P7/00 ,  A61P37/00 ,  A61P35/00

CPC分类号： A61K31/506

公开(公告)号：EP1879584A1

公开(公告)日：2008-01-23

申请号：EP06724677.7

申请日：2006-05-02

申请人： Novartis AG ,  NOVARTIS-PHARMA GMBH

发明人： MANLEY, Paul, W. ,  MESTAN, Jürgen ,  FABBRO, Doriano

IPC分类号： A61K31/506 ,  A61P7/00 ,  A61P35/02

CPC分类号： A61K31/506

摘要： The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of FIP1L1-PDGFRα-induced or TEL-PDGFRβ-induced myeloproliferative diseases, especially for the curative and/or prophylactic treatment of hypereosinophilic syndrome and hypereosinophilc syndrome with resistance to imatinib, and to a method of treating hypereosinophilic syndrome, chronic eosinophilic leukemia and hypereosinophilic syndrome with resistance to imatinib, or other diseases associated with FIP1L1-PDGFRα, TEL-PDGFRβ or similar mutations that activate PDGFR.