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1.发明授权1-HETEROCYCLYL-1,5-DIHYDRO-PYRAZOLO[3,4-D]PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MODULATORS 有权1 - 杂环基-1,5-二氢 - 吡唑并[3,4-d]嘧啶-4- ON DERIVATIE及其作为调节剂的PDE9A
公开(公告)号：EP2300478B1
公开(公告)日：2016-03-23
申请号：EP09727328.8
申请日：2009-04-01
发明人： GIOVANNINI, Riccardo , DORNER-CIOSSEK, Cornelia , EICKMEIER, Christian , FIEGEN, Dennis , FOX, Thomas , FUCHS, Klaus , HEINE, Niklas , ROSENBROCK, Holger , SCHAENZLE, Gerhard
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28
CPC分类号： C07D487/04 , A61K31/519
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公开(公告)号：EP2566864B1
公开(公告)日：2014-09-03
申请号：EP11718989.4
申请日：2011-05-06
发明人： GRAUERT, Matthias , BAKKER, Remko , BREITFELDER, Steffen , BUETTNER, Frank , EICKELMANN, Peter , FOX, Thomas , GRUNDL, Marc , LEHMANN-LINTZ, Thorsten , RIST, Wolfgang
IPC分类号： C07D413/04 , C07D413/14 , A61K31/501 , A61P3/00
CPC分类号： C07D413/10 , C07D413/04 , C07D413/14 , C07D417/14 , C07D453/02 , C07D498/04
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公开(公告)号：EP2215093A1
公开(公告)日：2010-08-11
申请号：EP08840365.4
申请日：2008-10-16
发明人： POUZET, Pascale , HOENKE, Christoph , NICKOLAUS, Peter , GOEGGEL, Rolf , FOX, Thomas , FIEGEN, Dennis , KLINDER, Klaus
IPC分类号： C07D495/04 , C07D519/00 , A61K31/519 , A61P11/00
CPC分类号： C07D495/04 , C07D519/00 , A61K31/519 , A61K2300/00
摘要： The invention relates to the novel dihydrothienopyrimidine sulfoxides of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO2, preferably however SO, and wherein R3, R4, R4', R5, R6 and R7 are defined as in claim 1. The invention also relates to pharmaceutical compositions containing said compounds. The novel dihydrothienopyrimidine sulfoxides are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers.
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公开(公告)号：EP2214673B1
公开(公告)日：2012-05-30
申请号：EP08841954.4
申请日：2008-10-13
发明人： POUZET, Pascale , HOENKE, Christoph , NICKOLAUS, Peter , GOEGGEL, Rolf , FOX, Thomas , FIEGEN, Dennis , KLINDER, Klaus
IPC分类号： A61K31/519 , C07D495/04 , A61P11/00 , A61P29/00 , A61P1/00
CPC分类号： A61K31/519 , C07D495/04
摘要： The invention relates to novel dihydrothienopyrimidines of the formula 1, and to pharmacologically acceptable salts thereof, formula (1) in which X is SO or SO2, but preferably SO, and either R3 is a monosubstituted phenyl ring in the ortho position or in the meta position, or R3 is a phenyl ring bisubstituted in any positions, and pharmaceutical compositions which comprise these compounds. These novel dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal symptoms or disorders, inflammatory disorders of the joints, of the skin or of the eyes, disorders of the peripheral or central nervous system or cancers.
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公开(公告)号：EP2215092A1
公开(公告)日：2010-08-11
申请号：EP08839793.0
申请日：2008-10-16
发明人： POUZET, Pascale , ANDERSKEWITZ, Ralf , DOLLINGER, Horst , FIEGEN, Dennis , FOX, Thomas , GOEGGEL, Rolf , HOENKE, Christoph , MARTYRES, Domnic , NICKOLAUS, Peter , KLINDER, Klaus
IPC分类号： C07D495/04 , C07D519/00 , A61K31/519 , A61P11/00
CPC分类号： C07D495/04 , C07D519/00
摘要： The invention relates to the novel piperidino-dihydrothienopyrimidines of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO2, preferably however SO, and wherein R1, R2, R3 and R4 are defined as in claim 1. The invention also relates to pharmaceutical compositions containing said compounds. The novel piperidino-dihydrothienopyrimidines are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers.
摘要翻译： 本发明涉及式（I）的新的哌啶子基 - 二氢噻吩并嘧啶及其药理学可接受的盐，其中X代表SO或SO 2，然而优选SO，并且其中R 1，R 2，R 3和R 4如权利要求1中所定义。 本发明还涉及含有所述化合物的药物组合物。 新的哌啶子基 - 二氢噻吩并嘧啶适用于治疗呼吸系统或胃肠疾病或疾病，关节炎症，皮肤或眼睛，外周或中枢神经系统疾病或癌症。
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6.发明公开
公开(公告)号：EP2205609A2
公开(公告)日：2010-07-14
申请号：EP08840075.9
申请日：2008-10-16
发明人： POUZET, Pascale , ANDERSKEWITZ, Ralf , DOLLINGER, Horst , FIEGEN, Dennis , FOX, Thomas , GOEGGEL, Rolf , HOENKE, Christoph , MARTYRES, Domnic , NICKOLAUS, Peter , KLINDER, Klaus
IPC分类号： C07D495/04 , C07D519/00 , A61K31/519 , A61P1/00 , A61P11/00 , A61P25/00
CPC分类号： C07D495/04 , A61K31/519 , A61K2300/00
摘要： The invention relates to the novel dihydrothienopyrimidine sulfoxides of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO2, preferably however SO, and wherein R3 represents an optionally substituted, monocyclic or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, monocyclic or bicyclic heteroaryl, and wherein R1 and R2 are defined as in claim 1. The invention also relates to pharmaceutical compositions containing said compounds. The novel dihydrothienopyrimidine sulfoxides are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers.
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公开(公告)号：EP2217602B1
公开(公告)日：2018-08-29
申请号：EP08855654.3
申请日：2008-11-27
发明人： EICKMEIER, Christian , DORNER-CIOSSEK,Cornelia , FIEGEN, Dennis , FOX, Thomas , FUCHS, Klaus , GIOVANNINI, Riccardo , HEINE, Niklas , HENDRIX, Martin , ROSENBROCK, Holger , SCHAENZLE, Gerhard
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterized by general Formula (I): with R1 being phenyl or pyridyl, any of which is substituted with 1 to 4, preferably 1 to 3 substituents X; X independently of each other being selected from C2-C6-alky1 or Ci-C6-alkoxy, where C2-C6-alkyl and C1-C6-alkoxy are at least dihalogenated up to perhalogenated. preferably with 2 to 6 halogen substituents, and the halogen atoms being selected from the group of fluoro, chloro and bromo, preferably fluoro; R2 being phenyl or heteroaryl, where phenyl is substituted by 1 to 3 radicals and heteroaryl is optionally substituted by 1 to 3 radicals in each case independently of one another selected from the group of C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, cyano, trifluoromethyl, amino, nitro, hydroxy, C1-C6-alkylamino, halogen, C6-C10-arylcarbonylamino, C1-C6-alkylcarbonylamino, C1-C6-alkylaminocarbonyl. C1-C6-alkoxycarbonyl, C6-C10-arylaminocarbonyl, heteroarylaminocarbonyl. heteroarylcarbonylamino, C1-C6-alkylsulphonyl-amino, C1-C6-alkylsulphonyl and C1-C6-alkylthio; The new compounds shall be used for the manufacture of medicaments, in particular medicaments for improving, perception, concentration, learning and/or memory in patients in need thereof.
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公开(公告)号：EP2566864A2
公开(公告)日：2013-03-13
申请号：EP11718989.4
申请日：2011-05-06
发明人： GRAUERT, Matthias , BAKKER, Remko , BREITFELDER, Steffen , BUETTNER, Frank , EICKELMANN, Peter , FOX, Thomas , GRUNDL, Marc , LEHMANN-LINTZ, Thorsten , RIST, Wolfgang
IPC分类号： C07D413/04 , C07D413/14 , A61K31/501 , A61P3/00
CPC分类号： C07D413/10 , C07D413/04 , C07D413/14 , C07D417/14 , C07D453/02 , C07D498/04
摘要： The present invention relates to pyridazinone derivatives of general formula (I), wherein the groups A, G and R
1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.-
9.发明授权
公开(公告)号：EP2334684B1
公开(公告)日：2017-08-02
申请号：EP09782607.7
申请日：2009-09-04
发明人： FUCHS, Klaus , DORNER-CIOSSEK, Cornelia , EICKMEIER, Christian , FIEGEN, Dennis , FOX, Thomas , GIOVANNINI, Riccardo , HEINE, Niklas , HENDRIX, Martin , ROSENBROCK, Holger , SCHAENZLE, Gerhard
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00 , A61P3/00
CPC分类号： C07D487/04
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公开(公告)号：EP2205609B1
公开(公告)日：2017-03-29
申请号：EP08840075.9
申请日：2008-10-16
发明人： POUZET, Pascale , ANDERSKEWITZ, Ralf , DOLLINGER, Horst , FIEGEN, Dennis , FOX, Thomas , GOEGGEL, Rolf , HOENKE, Christoph , MARTYRES, Domnic , NICKOLAUS, Peter , KLINDER, Klaus
IPC分类号： C07D495/04 , C07D519/00 , A61K31/519 , A61P1/00 , A61P11/00 , A61P25/00
CPC分类号： C07D495/04 , A61K31/519 , A61K2300/00
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