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11. 发明申请

US20100144681A1 COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的化合物
公开(公告)号：US20100144681A1
公开(公告)日：2010-06-10
申请号：US12063356
申请日：2006-08-08
申请人： Klaus Fuchs , Christian Eickmeier , Niklas Heine , Stefan Peters , Cornelia Dorner-Ciossek , Sandra Handschuh , Herbert Nar , Klaus Klinder
发明人： Klaus Fuchs , Christian Eickmeier , Niklas Heine , Stefan Peters , Cornelia Dorner-Ciossek , Sandra Handschuh , Herbert Nar , Klaus Klinder
IPC分类号： A61K31/18 , C07C311/02 , C07D333/22 , C07D277/30 , C07D211/70 , C07D285/16 , A61K31/381 , A61K31/426 , A61K31/4402 , A61K31/54 , A61K31/355 , A61K31/445 , A61K31/473 , A61K31/55 , A61K31/44 , A61K31/65 , A61P25/28
CPC分类号： C07C311/08 , C07C307/10 , C07C311/21 , C07C2601/02 , C07C2601/04 , C07D213/40 , C07D231/12 , C07D265/10 , C07D277/28 , C07D285/16 , C07D333/20 , C07D417/12
摘要： The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.
摘要翻译：本发明涉及通式（I）的取代的1,2-乙二胺，其中基团R 1 -R 13，A，B，L和i如说明书和权利要求中所定义。本发明还涉及其用于治疗阿尔茨海默病（AD）和类似疾病的用途。

12. 发明申请

US20100298278A1 INHIBITORS OF BETA-SECRETASE FOR THE TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的β-分泌酶的抑制剂
公开(公告)号：US20100298278A1
公开(公告)日：2010-11-25
申请号：US12063270
申请日：2006-08-08
申请人： Christian Eickmeier , Klaus Fuchs , Niklas Heine , Stefan Peters , Cornelia Dorner-Ciossek , Sandra Handschuh , Herbert Nar , Klaus Klinder
发明人： Christian Eickmeier , Klaus Fuchs , Niklas Heine , Stefan Peters , Cornelia Dorner-Ciossek , Sandra Handschuh , Herbert Nar , Klaus Klinder
IPC分类号： A61K31/549 , C07D417/12 , C07D285/16 , C07D277/28 , C07D211/96 , C07D295/26 , C07D265/10 , C07D413/12 , A61K31/426 , A61K31/4453 , A61K31/5375 , A61K31/535 , A61K31/445 , A61K31/473 , A61K31/55 , A61K31/439 , A61K31/437 , A61K31/65 , A61K31/496 , A61P25/28 , A61P3/10 , A61P9/10 , A61P1/18 , A61P25/00
CPC分类号： C07C307/10 , C07C2601/02 , C07D213/40 , C07D265/10 , C07D277/28 , C07D285/16 , C07D295/26 , C07D417/12
摘要： The invention relates to the substituted 1,2-ethylenediamines of general formula (I), wherein the groups R1 to R13, A, B, L and i are defined as in the description and the claims. The invention also relates to the use thereof in the treatment of Alzheimer's disease (AD) and similar diseases.
摘要翻译：本发明涉及通式（I）的取代的1,2-乙二胺，其中基团R 1至R 13，A，B，L和i如在说明书和权利要求书中所定义。本发明还涉及其在治疗阿尔茨海默病（AD）和类似疾病中的用途。

13. 发明授权

US08222264B2 Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture 有权
标题翻译：取代的氨基 - 喹唑啉酮，包含所述化合物的药物，其用途及其制备方法
公开(公告)号：US08222264B2
公开(公告)日：2012-07-17
申请号：US12667907
申请日：2008-07-03
申请人： Klaus Fuchs , Niklas Heine , Christian Eickmeier , Sandra Handschuh , Cornelia Dorner-Ciossek , Stefan Hoerer
发明人： Klaus Fuchs , Niklas Heine , Christian Eickmeier , Sandra Handschuh , Cornelia Dorner-Ciossek , Stefan Hoerer
IPC分类号： A61K31/517
CPC分类号： C07D239/95
摘要： The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
摘要翻译：本发明涉及通式（I）的取代氨基 - 喹唑啉酮，其中基团R 1至R 14和A如说明书和权利要求中所定义，以及其用于治疗阿尔茨海默病（AD）和类似疾病的用途。

14. 发明申请

US20100249158A1 SUBSTITUTED AMINO-QUINAZOLINONES, MEDICAMENTS COMPRISING SAID COMPOUND, THEIR USE AND THEIR METHOD OF MANUFACTURE 有权
标题翻译：取代的氨基喹唑啉酮，包含化合物的药物，其使用及其制备方法
公开(公告)号：US20100249158A1
公开(公告)日：2010-09-30
申请号：US12667907
申请日：2008-07-03
申请人： Klaus Fuchs , Niklas Heine , Christian Eickmeier , Sandra Handschuh , Cornelia Dorner-Ciossek , Stefan Hoerer
发明人： Klaus Fuchs , Niklas Heine , Christian Eickmeier , Sandra Handschuh , Cornelia Dorner-Ciossek , Stefan Hoerer
IPC分类号： A61K31/517 , C07D239/88 , A61P25/28
CPC分类号： C07D239/95
摘要： The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
摘要翻译：本发明涉及通式（I）的取代氨基 - 喹唑啉酮，其中基团R 1至R 14和A如说明书和权利要求中所定义，以及其用于治疗阿尔茨海默病（AD）和类似疾病的用途。

15. 发明授权

US08664388B2 Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture 有权
标题翻译：取代的氨基 - 喹唑啉酮，包含所述化合物的药物，其用途及其制备方法
公开(公告)号：US08664388B2
公开(公告)日：2014-03-04
申请号：US13523144
申请日：2012-06-14
申请人： Klaus Fuchs , Niklas Heine , Christian Eickmeier , Sandra Handschuh , Cornelia Dorner-Ciossek , Stefan Hoerer
发明人： Klaus Fuchs , Niklas Heine , Christian Eickmeier , Sandra Handschuh , Cornelia Dorner-Ciossek , Stefan Hoerer
IPC分类号： C07D239/95
CPC分类号： C07D239/95
摘要： The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
摘要翻译：本发明涉及通式（I）的取代氨基 - 喹唑啉酮，其中基团R 1至R 14和A如说明书和权利要求中所定义，以及其用于治疗阿尔茨海默病（AD）和类似疾病的用途。

16. 发明申请

US20110015193A1 1, 5-DIHYDRO-PYRAZOLO (3, 4-D) PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MUDULATORS FOR THE TREATMENT OF CNS DISORDERS 有权
标题翻译： 1,5-二羟基吡唑并（3,4-D）嘧啶-4-酮衍生物及其用作治疗CNS疾病的PDE9A制剂
公开(公告)号：US20110015193A1
公开(公告)日：2011-01-20
申请号：US12744750
申请日：2008-11-27
申请人： Christian Eickmeier , Cornelia Dorner-Ciossek , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Riccardo Giovannini , Niklas Heine , Martin Hendrix , Holger Rosenbrock , Gerhard Schaenzle
发明人： Christian Eickmeier , Cornelia Dorner-Ciossek , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Riccardo Giovannini , Niklas Heine , Martin Hendrix , Holger Rosenbrock , Gerhard Schaenzle
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/519 , C07D413/14 , A61P25/00
CPC分类号： C07D487/04
摘要： The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterised 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-alkyI, 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.
摘要翻译：本发明涉及新的取代吡唑并嘧啶。在化学上，化合物的特征在于通式（I）：其中R 1为苯基或吡啶基，其中任何一个被1至4个，优选1至3个取代基X取代; X独立地选自C 2 -C 6 - 烷基或C 1 -C 6 - 烷氧基，其中C 2 -C 6 - 烷基和C 1 -C 6 - 烷氧基至少被二卤代化为全卤代。优选具有2至6个卤素取代基，并且卤素原子选自氟，氯和溴，优选氟; R 2是苯基或杂芳基，其中苯基被1至3个基团取代，杂芳基任选被1至3个基团取代，各自独立地选自C1-C6-烷基，C1-C6-烷氧基，羟基羰基氰基，三氟甲基，氨基，硝基，羟基，C 1 -C 6烷基氨基，卤素，C 6 -C 10 - 芳基羰基氨基，C 1 -C 6烷基羰基氨基，C 1 -C 6烷基氨基羰基。 C 1 -C 6 - 烷氧基羰基，C 6 -C 10 - 芳基氨基羰基，杂芳基氨基羰基。杂芳基羰基氨基，C 1 -C 6烷基磺酰基 - 氨基，C 1 -C 6 - 烷基磺酰基和C 1 -C 6烷硫基; 新化合物应用于制造药物，特别是用于改善，感知，集中，学习和/或记忆有需要的患者的药物。

17. 发明授权

US09079905B2 Compounds for the treatment of CNS disorders 有权
标题翻译：用于治疗CNS疾病的化合物
公开(公告)号：US09079905B2
公开(公告)日：2015-07-14
申请号：US13062625
申请日：2009-09-04
申请人： Klaus Fuchs , Cornelia Dorner-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Riccardo Giovannini , Niklas Heine , Martin Hendrix , Holger Rosenbrock , Gerhard Schaenzle
发明人： Klaus Fuchs , Cornelia Dorner-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Riccardo Giovannini , Niklas Heine , Martin Hendrix , Holger Rosenbrock , Gerhard Schaenzle
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I). wherein A, R1-R5 and x are as defined herein, and their use as medicaments for improving perception, concentration, learning and/or memory in patients in need thereof.
摘要翻译：本发明涉及式（I）的新型环烷基 - 或环烯基取代的吡唑并嘧啶酮。其中A，R1-R5和x如本文所定义，并且它们作为用于改善有需要的患者的感知，浓度，学习和/或记忆的药物的用途。

18. 发明授权

US08623901B2 Compounds for the treatment of CNS disorders 有权
标题翻译：用于治疗CNS疾病的化合物
公开(公告)号：US08623901B2
公开(公告)日：2014-01-07
申请号：US12749904
申请日：2010-03-30
申请人： Riccardo Giovannini , Cornelia Dorner-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Niklas Heine , Holger Rosenbrock , Gerhard Schaenzle
发明人： Riccardo Giovannini , Cornelia Dorner-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Niklas Heine , Holger Rosenbrock , Gerhard Schaenzle
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and R1 is the group V−W−*, whereby V and W independently of each other may be an aryl group or an heteroaryl group, which independently of each other may optionally be substituted. According to one aspect of the invention the new compounds are for use as medicaments or for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments and/or for use in the treatment of e.g. Alzheimer's disease, in particular for cognitive impairment associated with Alzheimer's disease.
摘要翻译：本发明涉及式（I）的新颖的1,6-二取代吡唑并嘧啶酮，其中Hc是四氢吡喃基，R1是VW- *基团，其中V和W彼此独立地可以是芳基或杂芳基基团彼此独立地可以任选地被取代。根据本发明的一个方面，新化合物用作药物或用于制备药物，特别是用于治疗有关感知，集中，学习或记忆缺陷的病症的药物。新化合物也用于制备药物和/或用于治疗例如药物。阿尔茨海默病，特别是与阿尔茨海默病相关的认知障碍。

19. 发明授权

US08648085B2 1, 5-dihydro-pyrazolo (3, 4-D) pyrimidin-4-one derivatives and their use as PDE9A mudulators for the treatment of CNS disorders 有权
标题翻译： 1,5-二氢 - 吡唑并（3,4-D）嘧啶-4-酮衍生物及其用作治疗CNS紊乱的PDE9A混悬剂
公开(公告)号：US08648085B2
公开(公告)日：2014-02-11
申请号：US12744750
申请日：2008-11-27
申请人： Christian Eickmeier , Cornelia Dorner-Ciossek , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Riccardo Giovannini , Niklas Heine , Martin Hendrix , Holger Rosenbrock , Gerhard Schaenzle
发明人： Christian Eickmeier , Cornelia Dorner-Ciossek , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Riccardo Giovannini , Niklas Heine , Martin Hendrix , Holger Rosenbrock , Gerhard Schaenzle
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28 , A61P3/04 , A61P3/10 , A61P25/16
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.
摘要翻译：本发明涉及新的取代吡唑并嘧啶。在化学上，化合物的特征在于通式（I）：其中R 1为苯基或吡啶基，其中任何一个被1至4个，优选1至3个取代基X取代; X独立地选自C 2 -C 6 - 烷基或C 1 -C 6 - 烷氧基，其中C 2 -C 6 - 烷基和C 1 -C 6 - 烷氧基至少被二卤代化为全卤代。优选具有2至6个卤素取代基，并且卤素原子选自氟，氯和溴，优选氟; R 2是苯基或杂芳基，其中苯基被1至3个基团取代，杂芳基任选被1至3个基团取代，各自独立地选自C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，羟基羰基氰基，三氟甲基，氨基，硝基，羟基，C 1 -C 6烷基氨基，卤素，C 6 -C 10 - 芳基羰基氨基，C 1 -C 6烷基羰基氨基，C 1 -C 6烷基氨基羰基。 C 1 -C 6 - 烷氧基羰基，C 6 -C 10 - 芳基氨基羰基，杂芳基氨基羰基。杂芳基羰基氨基，C 1 -C 6烷基磺酰基 - 氨基，C 1 -C 6 - 烷基磺酰基和C 1 -C 6烷硫基; 新化合物应用于制造药物，特别是用于改善，感知，集中，学习和/或记忆有需要的患者的药物。

20. 发明授权

US09096603B2 1-heterocyclyl-1,5-dihydro-pyrazolo[3,4-D] pyrimidin-4-one derivatives and their use as PDE9A modulators 有权
标题翻译： 1-杂环基-1,5-二氢 - 吡唑并[3,4-D]嘧啶-4-酮衍生物及其作为PDE9A调节剂的用途
公开(公告)号：US09096603B2
公开(公告)日：2015-08-04
申请号：US14077534
申请日：2013-11-12
申请人： Riccardo Giovannini , Cornelia Dorner-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Niklas Heine , Holger Rosenbrock , Gerhard Schaenzle
发明人： Riccardo Giovannini , Cornelia Dorner-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Niklas Heine , Holger Rosenbrock , Gerhard Schaenzle
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones, wherein i.) the nitrogen atom of the pyrazolo-group that is next to the pyrimidino-group is attached to a non-aromatic, organic heterocycle having at least one ring hetero atom selected from O, N and S and ii.) to the C-atom between the two nitrogen atoms of the pyrimidinone-ring a second substituent is bound via an optionally substituted methylene-bridge. According to one aspect of the invention the new compounds are for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及新颖的1,6-二取代的吡唑并嘧啶酮，其中i）除了嘧啶基之外的吡唑并氮的氮原子连接到具有至少一个环杂原子的非芳族有机杂环上，从O，N和S和ii。）到嘧啶酮环的两个氮原子之间的C原子，第二取代基通过任选取代的亚甲基桥连接。根据本发明的一个方面，新化合物用于制造药物，特别是用于治疗有关感知，集中，学习或记忆缺陷的病症的药物。新化合物也用于制备用于治疗阿尔茨海默氏病的药物。

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