公开(公告)号：US20140073641A1

公开(公告)日：2014-03-13

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： 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。

公开(公告)号：US20130040955A1

公开(公告)日：2013-02-14

申请号：US13369596

申请日：2012-02-09

申请人： Niklas HEINE ,  Riccardo GIOVANNINI

发明人： Niklas HEINE ,  Riccardo GIOVANNINI

IPC分类号： C07D487/04 ,  A61P25/00 ,  A61P25/28 ,  A61P25/16 ,  A61P25/18 ,  A61P15/08 ,  A61P25/14 ,  A61P3/04 ,  A61P3/00 ,  A61P3/10 ,  A61P3/06 ,  A61K31/519 ,  A61P25/08

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The invention relates to novel pyrazolopyrimidinones according to formula (I). wherein X is CRe or unsubstituted N, D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3- or 4-pyridyl, Ra, Rb, Rc, Rd, Re are either H or optional substituents, m=1 or 2 and n is 0, 1 or 2.The new compounds are for use as the active entity of medicaments or for the manufacture of medicaments respectively, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may for example be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds are also for example for the manufacture of medicaments and/or for use in the treatment of these diseases, in particular for cognitive impairment associated with such disease. The compounds of the invention show PDE9 inhibiting properties.

摘要翻译： 本发明涉及式（I）的新型吡唑并嘧啶酮。 其中X为CRe或未取代的N，D为任选取代的环戊基，环己基，四氢呋喃基，四氢吡喃基或2-，3-或4-吡啶基，Ra，Rb，Rc，Rd，Re为H或任选的取代基，m = 1或 2和n为0,1或2.新化合物分别用作药物的活性成分或用于制备药物，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。 这种情况可能例如与阿尔茨海默病，精神分裂症和其他疾病相关。 新化合物还例如用于制备药物和/或用于治疗这些疾病，特别是与这种疾病相关的认知障碍。 本发明化合物显示PDE9抑制性质。

公开(公告)号：US20140350025A1

公开(公告)日：2014-11-27

申请号：US14087035

申请日：2013-11-22

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： 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V-W- *，其中V和W彼此独立地可以是芳基或 彼此独立地可以任选地被取代的杂芳基。 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。

公开(公告)号：US20120329773A1

公开(公告)日：2012-12-27

申请号：US13324245

申请日：2011-12-13

申请人： Riccardo GIOVANNINI ,  Dieter HAMPRECHT ,  Barbara KISTLER ,  Iain LINGARD

发明人： Riccardo GIOVANNINI ,  Dieter HAMPRECHT ,  Barbara KISTLER ,  Iain LINGARD

IPC分类号： A61K31/438 ,  C07D487/04 ,  A61K31/4985 ,  C07D498/04 ,  A61K31/5383 ,  C07D513/10 ,  A61K31/547 ,  C07D491/107 ,  A61K31/397 ,  C07D221/20 ,  C07D498/14 ,  A61K31/407 ,  C07D471/04 ,  A61K31/437 ,  C07D498/20 ,  A61K31/5386 ,  C07D513/04 ,  A61P11/00 ,  A61P29/00 ,  A61P1/00 ,  A61P19/02 ,  A61P17/00 ,  A61P27/02 ,  A61P35/00 ,  A61P25/00 ,  A61P11/02 ,  A61P37/08 ,  A61P7/10 ,  A61P11/06 ,  A61P31/00 ,  C07D471/10

CPC分类号： C07D471/10 ,  C07D211/32 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D498/04 ,  C07D513/04

摘要： This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

摘要翻译： 本发明涉及通式1的双环体系取代的酰胺官能化酚，它们作为CXCR2活性抑制剂的用途，含有它们的药物组合物及其用途用于治疗和/或预防呼吸道或胃肠道疾病或 疾病，关节，皮肤或眼睛的炎性疾病，外周或中枢神经系统或癌症的疾病，以及含有这些化合物的药物组合物。