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1. 发明授权

US08772305B2 Substituted pyridinyl-pyrimidines and their use as medicaments 有权
标题翻译：取代的吡啶基嘧啶及其作为药物的用途
公开(公告)号：US08772305B2
公开(公告)日：2014-07-08
申请号：US13357734
申请日：2012-01-25
申请人： Georg Dahmann , Dennis Fiegen , Martin Fleck , Matthias Hoffmann , Jasna Klicic , Stephen Peter East , Spencer Charles R. Napier , John Scott
发明人： Georg Dahmann , Dennis Fiegen , Martin Fleck , Matthias Hoffmann , Jasna Klicic , Stephen Peter East , Spencer Charles R. Napier , John Scott
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/10
摘要： The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
摘要翻译：本发明涉及式1的新的取代的吡啶基 - 嘧啶，其中环A是五元饱和或不饱和碳环，任选地包含一个，两个或三个彼此独立地选自N，S和O的杂原子，其中 R 1，R 2，R 4，R 3，R 5和R 6如权利要求1中所定义，并且其中环A进一步任选被一个或两个其它取代基取代，并且上述化合物的药学上可接受的盐，非对映异构体，对映异构体，外消旋物，水合物和溶剂合物。

2. 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。

3. 发明申请

US20110212960A1 NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDER 审中-公开
标题翻译：用于治疗CNS病症的新化合物
公开(公告)号：US20110212960A1
公开(公告)日：2011-09-01
申请号：US12855129
申请日：2010-08-12
申请人： Niklas HEINE , Cornelia DORNER-CIOSSEK , Christian EICKMEIER , Dennis FIEGEN , Thomas FOX , Klaus FUCHS , Riccardo GIOVANNINI , Holger ROSENBROCK , Gerhard SCHAENZLE , Lars BAERFACKER
发明人： Niklas HEINE , Cornelia DORNER-CIOSSEK , Christian EICKMEIER , Dennis FIEGEN , Thomas FOX , Klaus FUCHS , Riccardo GIOVANNINI , Holger ROSENBROCK , Gerhard SCHAENZLE , Lars BAERFACKER
IPC分类号： C07D487/04 , A61K31/5377 , A61K31/519 , A61P25/28 , A61P25/00 , A61P25/18 , A61P3/10 , A61P3/06 , A61P3/00 , A61P1/00 , A61P9/00 , A61P11/00
CPC分类号： C07D487/04
摘要： The invention relates to novel pyrazolopyrimidinones according to formula (I). The new compounds shall be used 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. Further aspects of the present invention refer to a process for the manufacture of the compounds and their use for producing medicaments.
摘要翻译：本发明涉及式（I）的新型吡唑并嘧啶酮。新化合物应用于制造药物，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。本发明的其它方面是指化合物的制造方法及其制备药物的用途。

4. 发明授权

US09102679B2 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：US09102679B2
公开(公告)日：2015-08-11
申请号：US14087035
申请日：2013-11-22
申请人： Riccardo Giovannini , Cornelia Dornier-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Niklas Heine , Holger Rosenbrock , Gerhard Schaenzle
发明人： Riccardo Giovannini , Cornelia Dornier-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Niklas Heine , Holger Rosenbrock , Gerhard Schaenzle
IPC分类号： C07D487/04 , A61K31/519
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。

5. 发明申请

US20140057926A1 SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY 审中-公开
公开(公告)号：US20140057926A1
公开(公告)日：2014-02-27
申请号：US13971378
申请日：2013-08-20
申请人： Thorsten OOST , Dennis FIEGEN , Christian GNAMM
发明人： Thorsten OOST , Dennis FIEGEN , Christian GNAMM
IPC分类号： C07D213/82 , C07D417/04 , C07D405/04 , C07D401/04 , C07D413/04
CPC分类号： C07D417/04 , C07D213/82 , C07D401/04 , C07D405/04 , C07D413/04
摘要： This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.

6. 发明申请

US20130274264A1 PIPERAZINO-DIHYDROTHIENOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译：哌嗪 - 二氢吲哚二酮衍生物
公开(公告)号：US20130274264A1
公开(公告)日：2013-10-17
申请号：US13911712
申请日：2013-06-06
申请人： Pascale POUZET , Christoph HOENKE , Peter NICKOLAUS , Rolf GOEGGEL , Thomas FOX , Dennis FIEGEN , Klaus KLINDER
发明人： Pascale POUZET , Christoph HOENKE , Peter NICKOLAUS , Rolf GOEGGEL , Thomas FOX , Dennis FIEGEN , Klaus KLINDER
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , C07D519/00 , A61K31/519 , A61K2300/00
摘要： A method for treating diseases associated with the inhibition of phosphodiesterase 4 (PDE4) enzyme in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a dihydrothienopyrimidinesulphoxide of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof
摘要翻译：一种用于治疗与患者中磷酸二酯酶4（PDE4）酶的抑制有关的疾病的方法，包括向有需要的患者施用治疗有效量的式1的二氢噻吩并嘧啶亚砜，以及药理学上可接受的盐，非对映异构体，对映异构体，外消旋体，水合物或溶剂化物

7. 发明申请

US20120108534A1 Dihydrothienopyrimidines for the treatment of inflammatory Diseases 有权
标题翻译：用于治疗炎性疾病的二氢噻吩并嘧啶
公开(公告)号：US20120108534A1
公开(公告)日：2012-05-03
申请号：US13343391
申请日：2012-01-04
申请人： Pascale POUZET , Christoph HOENKE , Rolf GOEGGEL , Birgit JUNG , Peter NICKOLAUS , Dennis FIEGEN , Thomas FOX
发明人： Pascale POUZET , Christoph HOENKE , Rolf GOEGGEL , Birgit JUNG , Peter NICKOLAUS , Dennis FIEGEN , Thomas FOX
IPC分类号： A61K31/7064 , A61K31/496 , A61P29/00 , A61P17/00 , A61P11/00 , A61P35/00 , A61P25/00 , A61P37/08 , A61P11/06 , A61P1/00 , A61K31/5377 , A61P27/02
CPC分类号： A61K31/5377 , A61K31/519 , A61K45/06 , C07D495/04 , C07D519/00
摘要： The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2 and R3 have the meanings given in the description,and which are suitable for the treatment 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：本发明涉及式1的新的二氢噻吩并嘧啶，以及其药学上可接受的盐，非对映异构体，对映异构体，外消旋物，水合物或溶剂化物，其中X是SO或SO 2，但优选为SO，并且其中R1，R2和R3具有给定的含义并且适用于治疗呼吸系统或胃肠道疾病，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。

8. 发明申请

US20110082137A1 NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS 有权
标题翻译：用于治疗CNS病症的新化合物
公开(公告)号：US20110082137A1
公开(公告)日：2011-04-07
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 , A61K31/5377 , A61P25/00 , A61P25/28 , A61P25/18 , A61P25/08
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。

9. 发明申请

US20110028441A1 NOVEL PHENYL-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES 审中-公开
标题翻译：新戊烯取代的哌嗪二氢吲哚
公开(公告)号：US20110028441A1
公开(公告)日：2011-02-03
申请号：US12738412
申请日：2008-10-13
申请人： Pascale Pouzet , Christoph Hoenke , Peter Nickolaus , Rolf Goeggel , Thomas Fox , Dennis Fiegen , Klaus Klinder
发明人： Pascale Pouzet , Christoph Hoenke , Peter Nickolaus , Rolf Goeggel , Thomas Fox , Dennis Fiegen , Klaus Klinder
IPC分类号： A61K31/573 , C07D495/04 , A61K31/519 , A61P1/04 , A61P11/06 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28
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.
摘要翻译：本发明涉及式1的新型二氢噻吩并嘧啶及其药学上可接受的盐，其中X为SO或SO 2，但优选为SO的式（1），R3为邻位或元环中的单取代苯环位置，或R3是在任何位置双取代的苯环，以及包含这些化合物的药物组合物。这些新型二氢噻吩并嘧啶适用于治疗呼吸系统或胃肠道症状，疾病，关节炎，皮肤或眼睛的炎症，外周或中枢神经系统或癌症的疾病。

10. 发明申请

US20080096882A1 Dihydrothienopyrimidines for the Treatment of Inflammatory Diseases 有权
标题翻译：用于治疗炎症疾病的二氢噻吩并嘧啶
公开(公告)号：US20080096882A1
公开(公告)日：2008-04-24
申请号：US11736703
申请日：2007-04-18
申请人： Pascale Pouzet , Christoph Hoenke , Rolf Goeggel , Birgit Jung , Peter Nickolaus , Dennis Fiegen , Thomas Fox
发明人： Pascale Pouzet , Christoph Hoenke , Rolf Goeggel , Birgit Jung , Peter Nickolaus , Dennis Fiegen , Thomas Fox
IPC分类号： A61K31/496 , A61K31/5377 , A61P11/00 , A61P25/00 , A61P29/00 , C07D413/14 , C07D495/04
CPC分类号： A61K31/5377 , A61K31/519 , A61K45/06 , C07D495/04 , C07D519/00
摘要： The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2 and R3 have the meanings given in the description, and which are suitable for the treatment 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：本发明涉及式1的新的二氢噻吩并嘧啶，以及其药学上可接受的盐，非对映异构体，对映异构体，外消旋物，水合物或溶剂合物，其中X是SO或SO 2，但优选SO，其中R R 1，R 2和R 3具有说明书中给出的含义，适用于治疗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。

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