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公开(公告)号：EP2822930B1
公开(公告)日：2016-01-20
申请号：EP13710937.7
申请日：2013-03-04
发明人： BUKHTIYAROV, Yuri , CACATIAN, Salvacion , DILLARD, Lawrence, Wayne , DORNER-CIOSSEK, Cornelia , FUCHS, Klaus , JIA, Lanqi , LALA, Deepak, S. , MORALES-RAMOS, Angel , RAST, Georg , REEVES, Jonathan , SINGH, Suresh, B. , VENKATRAMAN, Shankar , XU, Zhenrong , YUAN, Jing , ZHAO, Yi , ZHENG, Yajun
IPC分类号： C07D235/02 , C07D403/06 , C07D407/06 , C07C49/323 , A61K31/4184 , A61P25/28 , A61K31/506 , C07C255/47 , C07C313/06 , C07D405/06 , C07C229/50 , C07C331/14
CPC分类号： A61K31/506 , A61K31/4184 , C07C49/697 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/47 , C07C313/06 , C07C331/14 , C07D235/02 , C07D403/06 , C07D405/06 , C07D407/06
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公开(公告)号：EP2822930A1
公开(公告)日：2015-01-14
申请号：EP13710937.7
申请日：2013-03-04
发明人： BUKHTIYAROV, Yuri , CACATIAN, Salvacion , DILLARD, Lawrence, Wayne , DORNER-CIOSSEK, Cornelia , FUCHS, Klaus , JIA, Lanqi , LALA, Deepak, S. , MORALES-RAMOS, Angel , RAST, Georg , REEVES, Jonathan , SINGH, Suresh, B. , VENKATRAMAN, Shankar , XU, Zhenrong , YUAN, Jing , ZHAO, Yi , ZHENG, Yajun
IPC分类号： C07D235/02 , C07D403/06 , C07D407/06 , C07C49/323 , A61K31/4184 , A61P25/28
CPC分类号： A61K31/506 , A61K31/4184 , C07C49/697 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/47 , C07C313/06 , C07C331/14 , C07D235/02 , C07D403/06 , C07D405/06 , C07D407/06
摘要： The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACEl) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.
摘要翻译： 本发明涉及螺环酰基胍及其作为β-分泌酶（BACE1）活性抑制剂的用途，含有该化合物的药物组合物，以及使用该化合物作为治疗剂治疗神经变性疾病，以认知衰退为特征的疾病的方法 ，认知障碍，痴呆和特征在于产生β-淀粉样蛋白聚集体的疾病。
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公开(公告)号：EP2406240A2
公开(公告)日：2012-01-18
申请号：EP10708684.5
申请日：2010-03-12
发明人： CACATIAN, Salvacion , CLAREMON, David, A. , DILLARD, Lawrence, W. , FUCHS, Klaus , HEINE, Niklas , JIA, Lanqi , LEFTHERIS, Katerina , MCKEEVER, Brian , MORALES-RAMOS, Angel , SINGH, Suresh , VENKATRAMAN, Shankar , WU, Guosheng , WU, Zhongren , XU, Zhenrong , YUAN, Jing , ZHENG, Yajun
IPC分类号： C07D277/60 , C07D271/12 , C07D235/02 , C07D239/70 , C07D491/10 , C07D487/10 , C07D403/06 , C07D405/12 , C07D498/10 , A61K31/4245 , A61K31/4184 , A61K31/4188 , A61K31/517 , A61K31/519 , A61K31/428
CPC分类号： C07D271/12 , C07D233/46 , C07D235/02 , C07D239/70 , C07D277/60 , C07D279/08 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/10 , C07D487/10 , C07D491/10 , C07D493/20 , C07D495/10 , C07D498/10 , C07D513/10
摘要： The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
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公开(公告)号：EP2406240B1
公开(公告)日：2015-12-23
申请号：EP10708684.5
申请日：2010-03-12
发明人： CACATIAN, Salvacion , CLAREMON, David, A. , DILLARD, Lawrence, W. , FUCHS, Klaus , HEINE, Niklas , JIA, Lanqi , LEFTHERIS, Katerina , MCKEEVER, Brian , MORALES-RAMOS, Angel , SINGH, Suresh , VENKATRAMAN, Shankar , WU, Guosheng , WU, Zhongren , XU, Zhenrong , YUAN, Jing , ZHENG, Yajun
IPC分类号： C07D233/46 , C07D235/02
CPC分类号： C07D271/12 , C07D233/46 , C07D235/02 , C07D239/70 , C07D277/60 , C07D279/08 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/10 , C07D487/10 , C07D491/10 , C07D493/20 , C07D495/10 , C07D498/10 , C07D513/10
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公开(公告)号：EP2888236A1
公开(公告)日：2015-07-01
申请号：EP13760166.2
申请日：2013-08-26
发明人： BUKHTIYAROV, Yuri , CACATIAN, Salvacion , DILLARD, Lawrence, Wayne , DORNER-CIOSSEK, Cornelia , FUCHS, Klaus , GROSS, Ulrike , HEINE, Niklas , JIA, Lanqi , LALA, Deepak, S. , MORALES-RAMOS, Angel , SINGH, Suresh, B. , SAUER, Achim , VENKATRAMAN, Shankar , XU, Zhenrong , YUAN, Jing , ZHAO, Yi , ZHENG, Yajun
IPC分类号： C07D235/02 , C07D401/06 , C07D403/04 , A61K31/4184 , A61P25/28
CPC分类号： C07D235/02 , A61K31/4184 , A61K31/4439 , A61K31/506 , C07C49/747 , C07C49/755 , C07C229/50 , C07C255/59 , C07C313/06 , C07C331/26 , C07C2603/94 , C07C2603/97 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06
摘要： The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β- secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.
摘要翻译： 本发明涉及螺环酰基胍和它们作为β-分泌酶（BACE1）活性抑制剂的用途，含有该化合物的药物组合物，以及使用它们作为治疗剂治疗神经变性疾病，以认知衰退为特征的疾病的方法 ，认知障碍，痴呆和特征在于产生β-淀粉样蛋白聚集体的疾病。
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公开(公告)号：EP1915352A1
公开(公告)日：2008-04-30
申请号：EP06778201.1
申请日：2006-08-08
发明人： FUCHS, Klaus , EICKMEIER, Christian , HEINE, Niklas , PETERS, Stefan , DORNER-CIOSSEK, Cornelia , HANDSCHUH, Sandra , NAR, Herbert , KLINDER, Klaus
IPC分类号： C07D277/28 , C07D231/12 , C07D333/20 , C07D213/40 , C07D417/12 , C07D417/14 , A61K31/549 , A61K31/4439 , A61K31/4406 , A61K31/426 , A61K31/415 , A61K31/381 , A61P25/00
CPC分类号： C07D277/28 , C07D213/40 , C07D231/12 , C07D333/20 , C07D417/12 , C07D417/14
摘要： The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1 to R13, A, B, L, and i are defined as indicated in the description and the claims, as well as the use thereof for treating Alzheimer's disease (AD) and similar diseases.
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7.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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8.发明公开TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION 有权三环吡啶衍生物，这种含药物，用途和方法FOR THEIR
公开(公告)号：EP2268644A1
公开(公告)日：2011-01-05
申请号：EP09716535.1
申请日：2009-03-02
发明人： WAGNER, Holger , BERTA, Daniela , GIOVANNINI, Riccardo , MAZZACANI, Alessandro , STREICHER, Ruediger , FUCHS, Klaus
IPC分类号： C07D493/04 , C07D493/10 , A61K31/4355 , A61P9/00
CPC分类号： C07D493/04 , C07D493/10
摘要： Compounds of formula (I) wherein the groups R1 to R8 have the meanings indicated in the description, the tautomers.the stereoisomers.the mixtures thereof and the salts thereof have valuable pharmacological properties.which make them useful for the treatment of cardiovascular and related disorders.
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9.发明公开
公开(公告)号：EP1915353A2
公开(公告)日：2008-04-30
申请号：EP06792736.8
申请日：2006-08-08
发明人： HEINE, Niklas , FUCHS, Klaus , EICKMEIER, Christian , PETERS, Stefan , DORNER-CIOSSEK, Cornelia , HANDSCHUH, Sandra , NAR, Herbert , KLINDER, Klaus
IPC分类号： C07D277/28
CPC分类号： C07D417/12 , C07D213/40 , C07D277/28 , C07D333/20 , C07D409/12 , C07D417/14
摘要： The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the groups R1 - R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.
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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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