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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
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.
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2.发明公开N-ARYL(THIO)ANTHRANILIC ACID AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS VEGF RECEPTOR TYROSINE KINASE INHIBITORS 审中-公开N-芳基（硫代）邻氨基苯甲酸酰胺衍生物，其制备及其作为VEGF受体酪氨酸激酶INHIBITORS-
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.
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3.发明公开
公开(公告)号：EP0876357A1
公开(公告)日：1998-11-11
申请号：EP96946000.0
申请日：1996-11-15
发明人： HUTH, Andreas , KRÜGER, Martin , OTTOW, Eckhard , SEIDELMANN, Dieter , NEUHAUS, Roland , SCHNEIDER, Herbert , TURSKI, Lechoslaw
CPC分类号： C07D241/44 , C07F9/650994
摘要： New quinoxalindone derivatives are disclosed having formula (I), in which R?1, R5, R6 and R7¿ have the meanings given in the description, as well as their preparation and use in medicaments.
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4.发明授权
公开(公告)号：EP1280799B1
公开(公告)日：2004-01-21
申请号：EP01940416.9
申请日：2001-05-08
发明人： KRÜGER, Martin , HUTH, Andreas , PETROV, Orlin , SEIDELMANN, Dieter , THIERAUCH, Karl-Heinz , HABEREY, Martin , MENRAD, Andreas , ERNST, Alexander
IPC分类号： C07D405/12 , C07D401/12 , C07D213/38 , A61K31/44 , A61P35/00
CPC分类号： C07D213/38
摘要： The invention relates to ortho-substituted anthranilic acid amides and to their use as medicaments for treating medical disorders, which are triggered by persistent angiogenesis.
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5.发明公开
公开(公告)号：EP1280799A1
公开(公告)日：2003-02-05
申请号：EP01940416.9
申请日：2001-05-08
发明人： KRÜGER, Martin , HUTH, Andreas , PETROV, Orlin , SEIDELMANN, Dieter , THIERAUCH, Karl-Heinz , HABEREY, Martin , MENRAD, Andreas , ERNST, Alexander
IPC分类号： C07D405/12 , C07D401/12 , C07D213/38 , A61K31/44 , A61P35/00
CPC分类号： C07D213/38
摘要： The invention relates to ortho-substituted anthranilic acid amides and to their use as medicaments for treating medical disorders, which are triggered by persistent angiogenesis.
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公开(公告)号：EP0993461A1
公开(公告)日：2000-04-19
申请号：EP98942480.9
申请日：1998-06-26
IPC分类号： C07D413/04 , C07D417/04 , A61K31/495
CPC分类号： C07D241/44
摘要： The invention relates to compounds of formula (I), the production thereof and the use of the same in medicaments.
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公开(公告)号：EP0633779A1
公开(公告)日：1995-01-18
申请号：EP93908924.0
申请日：1993-04-06
发明人： HUTH, Andreas , KRÜGER, Martin , RAHTZ, Dieter , SEIDELMANN, Dieter , TURSKI, Lechoslaw , LÖSCHMANN, Peter-Andreas , STEPHENS, David-Norman , SCHNEIDER, Herbert
CPC分类号： C07D471/04 , A61K31/44 , A61K31/445 , A61K31/495
摘要： The invention concerns the use of compounds of formula (I), in which R?3, R4, R9 and RA¿ are as defined in the description, as non-competitive glutamate antagonists in the preparation of a drug for the treatment of neurological and psychiatric disorders. The invention also concerns drugs containing these compounds, as well as the new compounds of formula (Ia) and a method of preparing them.
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8.发明公开$g(b)-CARBOLIN-3-HYDROXYALKYLCARBONSÄUREESTERDERIVATE, VERFAHREN ZU DEREN HERSTELLUNG UND DEREN VERWENDUNG IN ARZNEIMITTELN 失效-g（B）咔啉-3-HYDROXYALKYLCARBONSÄUREESTERDERIVATE，其制备方法及其用途毒品。
公开(公告)号：EP0536361A1
公开(公告)日：1993-04-14
申请号：EP92908837.0
申请日：1992-04-15
发明人： HUTH, Andreas , KRÜGER, Martin , SEIDELMANN, Dieter , SCHMIECHEN, Ralph , KRAUSE, Werner , SCHNEIDER, Herbert , TURSKI, Lechoslaw
CPC分类号： C07D471/04
摘要： Il est décrit des dérivés d'esters d'acide beta-carboline-3-hydroxyalkylcarboxylique ayant la formule (I): dans laquelle RA, R4 et R3 ont les notations spécifiées dans la description, ainsi que leur procédé de fabrication et leur utilisation dans des médicaments.
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公开(公告)号：EP0282502A1
公开(公告)日：1988-09-21
申请号：EP87904844.0
申请日：1987-07-30
发明人： BIERE, Helmut , HUTH, Andreas , RAHTZ, Dieter , SCHMIECHEN, Ralph , SEIDELMANN, Dieter , SCHNEIDER, Herbert, Hans , STEPHENS, David, Norman
CPC分类号： C07D413/04 , C07D233/90
摘要： Dérivés d'imidazole de formule générale (I), où R1 est hydrogène ou halogène en position o, m ou p, l'halogène pouvant intervenir une seule fois ou plusieurs fois au niveau du résidu phényle, R4 est -COOR6, (II), -CN, (III) or (IV), R6 et R9 représentant de l'hydrogène ou un groupe alkyle droit ou ramifié avec 1 à 6 atomes de carbone, R7 et R8 sont identiques ou différents et représentent de l'hydrogène ou un groupe alkyle droit ou ramifié avec 1 à 6 atomes de carbone, ou bien R7 et R8 représentent conjointement avec l'atome d'azote un noyau pentagonal ou hexagonal hétérocyclique saturé contenant éventuellement un hétéroatome supplémentaire, et R5 est hydrogène, un groupe alkyle avec 1 à 6 atomes de carbone ou un groupe alkoxyalkyl avec 1 à 6 atomes de carbone. Ces dérivés conviennent en tant que médicaments psychotropes.
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10.发明授权
公开(公告)号：EP1387838B1
公开(公告)日：2006-04-19
申请号：EP02748691.9
申请日：2002-05-03
发明人： ERNST, Alexander , HUTH, Andreas , KRÜGER, Martin , THIERAUCH, Karl-Heinz , MENRAD, Andreas , HABEREY, Martin
IPC分类号： C07D401/12 , C07D401/14 , C07D405/12 , A61K31/44 , A61P19/02 , A61P33/00
CPC分类号： C04B35/632 , C07D401/12
摘要： The invention relates to substituted cyanoanthranilamide derivatives, to the production and use thereof as medicaments for the treatment of diseases triggered by persistent angiogenesis. The inventive compounds can be used, for instance in psoriasis, Kaposis sarcoma, restenosis, e.g. stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia, arthritis, e.g. rheumatoid arthritis, hemangioma, angiofribroma, eye diseases, e.g. diabetic retinopathy, neovascular glaucoma, kidney diseases, e.g. glomerulonephritis, diabetic nephropathy, malign nephrosclerosis, thrombotic microangiopatic syndrome, transplantation rejections and glomerulopathy, fibrotic diseases such as liver cirrhosis, mesangial cell proliferative diseases, arteriosclerosis, injuries of nerve tissue and inhibition of reocclusion of blood vessels after balloon catheter treatment, in vascular prosthetics or after implantation of mechanical devices for keeping blood vessels open, e.g. stents, as immunosuppressants, as aid in scarless wound healing, age spots and contact dermatitis. The inventive compounds can also be used as VEGFR-3 inhibitors in lymphangiogenesis. The invention further relates to compounds of general formula (I), wherein A represents group -N(R7)-; Y1 to Y5 represent a nitrogen atom or group -CY6; Y6 represents cyano, halogen, C¿1?-C6-alkyl, C1-C6-alkoxy, amino or hydroxy, wherein at least one nitrogen atom is contained in the ring and at least one cyano radical is contained in the ring.
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