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1. 发明申请

WO2011018495A1 NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS 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：WO2011018495A1
公开(公告)日：2011-02-17
申请号：PCT/EP2010/061735
申请日：2010-08-12
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , HEINE, Niklas , DORNER-CIOSSEK, Cornelia , EICKMEIER, Christian , FIEGEN, Dennis , FOX, Thomas , FUCHS, Klaus , GIOVANNINI, Riccardo , ROSENBROCK, Holger , SCHAENZLE, Gerhard , BAERFACKER, Lars
发明人： HEINE, Niklas , DORNER-CIOSSEK, Cornelia , EICKMEIER, Christian , FIEGEN, Dennis , FOX, Thomas , FUCHS, Klaus , GIOVANNINI, Riccardo , ROSENBROCK, Holger , SCHAENZLE, Gerhard , BAERFACKER, Lars
IPC分类号： C07D487/04 , A61K31/522 , A61P25/28
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造用药物的用途。

2. 发明申请

WO2010112437A1 1-HETEROCYCLYL-1, 5-DIHYDRO-PYRAZOLO [3, 4-D] PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MODULATORS 审中-公开
标题翻译： 1-环己基-1,5-二氢吡喃并[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：WO2010112437A1
公开(公告)日：2010-10-07
申请号：PCT/EP2010/054050
申请日：2010-03-26
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , GIOVANNINI, Riccardo , DORNER-CIOSSEK, Cornelia , EICKMEIER, Christian , FIEGEN, Dennis , FOX, Thomas , FUCHS, Klaus , HEINE, Niklas , ROSENBROCK, Holger , SCHAENZLE, Gerhard
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
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 R 1 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。

3. 发明申请

WO2010026214A1 PYRAZOLOPYRIMIDINES AND THEIR USE FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：吡唑并嘧啶及其用于治疗CNS病症的用途
公开(公告)号：WO2010026214A1
公开(公告)日：2010-03-11
申请号：PCT/EP2009/061455
申请日：2009-09-04
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , FUCHS, Klaus , DORNER-CIOSSEK, Cornelia , EICKMEIER, Christian , FIEGEN, Dennis , FOX, Thomas , GIOVANNINI, Riccardo , HEINE, Niklas , HENDRIX, Martin , ROSENBROCK, Holger , SCHAENZLE, Gerhard
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
摘要： The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I), wherein A is selected from the group A 1 consisting of a C 3 -C 8 -cycloalkyl group or a C 4 -C 8 - cycloalkenyl group, whereby the members of C 3 -C 8 -cycloalkyl group being selected from the group of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptanyl and cyclooctanyl; and the members of the C 4 -C 8 -cycloalkenyl group, being selected from cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, cyclopentadienyl, cyclohexadienyl, cycloheptadienyl, cyclooctadienyl, cycloheptatrienyl, cyclooctathenyl, cyclooctatetraenyl. 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. Chemically, the compounds are characterised as pyrazolopyrimidinones with a cycloalkyl-moiety directly bound to the 1 position of the pyrazolopyrimidinone and a second substituent in the 6 position which is bound via an optionally substituted methylene-bridge. 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）的新的环烷基 - 或环烯基取代的吡唑并嘧啶酮，其中A选自由C 3 -C 8 - 环烷基或C 4 -C 8 - 环烯基组成的组A1，其中C3- 环烷基选自环丙基，环丁基，环戊基，环己基，环庚烷基和环辛基; 选自环丁烯基，环戊烯基，环己烯基，环庚烯基，环辛烯基，环戊二烯基，环己二烯基，环庚二烯基，环辛二烯基，环庚三烯基，环辛烯基，环辛烯四烯基的C4-C8-环烯基的成员。新化合物应用于制造药物，特别是用于改善有需要的患者的感知，集中，学习和/或记忆的药物。在化学上，化合物的特征在于吡唑并嘧啶酮，其中环烷基部分直接键合在吡唑并嘧啶酮的1位上，而6位上的第二个取代基通过任意取代的亚甲基桥结合。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. 发明申请

WO2009121919A1 1-HETEROCYCLYL-1,5-DIHYDRO-PYRAZOLO[3,4-D] PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MODULATORS 审中-公开
标题翻译： 1-环己基-1,5-二氢吡喃并[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：WO2009121919A1
公开(公告)日：2009-10-08
申请号：PCT/EP2009/053907
申请日：2009-04-01
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , GIOVANNINI, Riccardo , DOERNER-CIOSSEK, Cornelia , EICKMEIER, Christian , FIEGEN, Dennis , FOX, Thomas , FUCHS, Klaus , HEINE, Niklas , ROSENBROCK, Holger , SCHAENZLE, Gerhard
发明人： GIOVANNINI, Riccardo , DOERNER-CIOSSEK, Cornelia , EICKMEIER, Christian , FIEGEN, Dennis , FOX, Thomas , FUCHS, Klaus , HEINE, Niklas , ROSENBROCK, Holger , SCHAENZLE, Gerhard
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, Formula (I) with Hc is a mono-, bi- or tricyclic heterocyclyl group, the ring members of which are carbon atoms and at least 1, preferably 1, 2 or 3, heteroatom(s), which are selected from the group of nitrogen, oxygen and sulphur, which is in the form of -S(O) r - with r being 0, 1 or 2, and - said heterocyclyl group is or comprises 1 non-aromatic, saturated, or partly unsaturated monocyclic ring which comprises at least 1 heteroatom as ring member and - said heterocyclyl group is bound to the scaffold by said 1 non- aromatic, saturated, or partly unsaturated monocyclic ring which comprises at least 1 heteroatom as ring member. 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：本发明涉及新的1,6-二取代的吡唑并嘧啶酮，其中Hc的式（I）是单 - ，二 - 或三环杂环基，其环成员是碳原子，至少1个，优选1,2或3个，选自氮，氧和硫的杂原子，其为-S（O）r - ，其中r为0,1或2，并且所述杂环基为或包含1个芳族，饱和或部分不饱和的单环，其包含至少1个杂原子作为环成员，并且所述杂环基通过所述1个非芳族，饱和或部分不饱和的单环与支架结合，所述单环包含至少1个杂原子环成员。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。

5. 发明申请

WO2009068617A1 1, 5-DIHYDRO-PYRAZOLO (3, 4-D) PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MODULATORS FOR THE TEATMENT OF CNS DISORDERS 审中-公开
标题翻译： 1,5-二羟基吡唑并（3,4-D）嘧啶-4-酮衍生物及其作为PDE9A调节剂用于中枢神经系统疾病
公开(公告)号：WO2009068617A1
公开(公告)日：2009-06-04
申请号：PCT/EP2008/066350
申请日：2008-11-27
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , EICKMEIER, Christian , DOERNER-CIOSSEK, Cornelia , FIEGEN, Dennis , FOX, Thomas , FUCHS, Klaus , GIOVANNINI, Riccardo , HEINE, Niklas , HENDRIX, Martin , ROSENBROCK, Holger , SCHAENZLE, Gerhard
发明人： EICKMEIER, Christian , DOERNER-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 characterised by general Formula (I): with R 1 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 C 2 -C 6 -alky 1 or Ci-C 6 -alkoxy, where C 2 -C 6 -alkyl and C 1 -C 6 -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; R 2 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 C 1 -C 6 -alkyI, C 1 -C 6 - alkoxy, hydroxycarbonyl, cyano, trifluoromethyl, amino, nitro, hydroxy, C 1 -C 6 - alkylamino, halogen, C 6 -C 10 -arylcarbonylamino, C 1 -C 6 -alkylcarbonylamino, C 1 - C 6 -alkylaminocarbonyl. C 1 -C 6 -alkoxycarbonyl, C 6 -C 10 -arylaminocarbonyl, heteroarylaminocarbonyl. heteroarylcarbonylamino, C 1 -C 6 -alkylsulphonyl- amino, C 1 -C 6 -alkylsulphonyl and C 1 -C 6 -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为苯基或杂芳基，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。

6. 发明申请

WO2012020022A1 6-CYCLOALKYL-1, 5-DIHYDRO-PYRAZOLO [3, 4-D] PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A INHIBITORS 审中-公开
标题翻译： 6-环丙基-1,5-二氢吡喃并[3,4-D]嘧啶-4-酮衍生物及其作为PDE9A抑制剂的用途
公开(公告)号：WO2012020022A1
公开(公告)日：2012-02-16
申请号：PCT/EP2011/063705
申请日：2011-08-09
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , HEINE, Niklas , EICKMEIER, Christian , FERRARA, Marco , GIOVANNINI, Riccardo , ROSENBROCK, Holger , SCHAENZLE, Gerhard
发明人： HEINE, Niklas , EICKMEIER, Christian , FERRARA, Marco , GIOVANNINI, Riccardo , ROSENBROCK, Holger , SCHAENZLE, Gerhard
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I) wherein R 1 is a 5 or 6 membered aromatic heteroaryl-group, R 2 is an optional substituent, D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3- or 4-pyridyl, 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 Alzheimers 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）的新的6-环烷基 - 吡唑并嘧啶酮，其中R 1为5或6元芳族杂芳基，R 2为任选的取代基，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，m = 1或2，n为0,1或2.这些新化合物分别用作药物活性物质或用于制备药物，特别是用于治疗有关感知，集中，学习或记忆的缺陷。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有关。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。

7. 发明申请

WO2013017657A1 PHENYL-3-AZA-BICYCLO[3.1.0]HEX-3-YL-METHANONES AND THE USE THEREOF AS MEDICAMENT 审中-公开
标题翻译：苯基-3-氮杂双环[3.1.0] HEX-3-YL-甲烷及其作为药物的用途
公开(公告)号：WO2013017657A1
公开(公告)日：2013-02-07
申请号：PCT/EP2012/065140
申请日：2012-08-02
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , GIOVANNINI, Riccardo , BERTANI, Barbara , FERRARA, Marco , LINGARD, Iain , MAZZAFERRO, Rocco , ROSENBROCK, Holger
发明人： GIOVANNINI, Riccardo , BERTANI, Barbara , FERRARA, Marco , LINGARD, Iain , MAZZAFERRO, Rocco , ROSENBROCK, Holger
IPC分类号： C07D401/04 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , A61K31/421 , A61K31/427 , A61K31/437 , A61K31/4439 , A61P25/18 , A61P25/28
CPC分类号： C07D413/04 , C07D209/52 , C07D401/04 , C07D403/04 , C07D413/14 , C07D417/04 , C07D471/04
摘要： The present inventions relates to substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl- methanones of general formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as herein described or salts thereof, preferably pharmaceutically acceptable salts thereof. The invention further relates to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various conditions such as conditions concerning positive and negative symptoms of schizophrenia as well as cognitive impairments associated with schizophrenia, Alzheimers Disease and other neurological and psychiatric disorders. The compounds of the invention show glycine transporter-1 (GlyT1) inhibiting properties.
摘要翻译：本发明涉及通式（I）的取代的苯基-3-氮杂 - 双环[3.1.0]己-3-基 - 甲酮，其中R 1，R 2，R 3，R 4，R 5和R 6如本文所述或其盐，优选其药学上可接受的盐。本发明进一步涉及所述化合物的制造，包含根据通式（I）的化合物的药物组合物，以及所述化合物用于治疗各种病症的用途，例如关于精神分裂症的正和负症状的症状以及认知与精神分裂症，阿尔茨海默病和其他神经和精神疾病有关的损伤。本发明化合物显示甘氨酸转运体-1（GlyT1）抑制性质。

8. 发明申请

WO2012110440A9 6 - CYCLOBUTYL - 1, 5 - DIHYDRO - PYRAZOLO [3, 4-D] PYRIMIDIN- 4 - ONE DERIVATIVES THEIR USE AS PDE9A INHIBITORS 审中-公开
公开(公告)号：WO2012110440A9
公开(公告)日：2012-08-23
申请号：PCT/EP2012/052378
申请日：2012-02-13
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , HEINE, Niklas , GIOVANNINI, Riccardo , FERRARA, Marco
发明人： HEINE, Niklas , GIOVANNINI, Riccardo , FERRARA, Marco
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28
摘要： The invention relates to novel pyrazolopyrimidinones according to formula (I), wherein R 1 is a pyridyl or pyrimidinyl group and D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3-or 4-pyridyl. 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.

9. 发明申请

WO2012110441A1 6-CYCLOALKYL-PYRAZOLOPYRIMIDINONES FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS疾病的6-环丙基 - 吡唑并嘧啶酮
公开(公告)号：WO2012110441A1
公开(公告)日：2012-08-23
申请号：PCT/EP2012/052379
申请日：2012-02-13
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , HEINE, Niklas , GIOVANNINI, Riccardo
发明人： HEINE, Niklas , GIOVANNINI, Riccardo
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention relates to novel pyrazolopyrimidinones according to formula (I), wherein X is CR e or unsubstituted N, D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3- or 4-pyridyl, R a , R b , R c , R d , R e 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，n为0,1或2.新化合物分别用作药物的活性成分或药物的制备，特别是用于治疗关于感知，集中，学习或记忆缺陷的情况。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。

10. 发明申请

WO2012110599A1 TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：三环吡啶衍生物，含有这些化合物的药物，其使用及其制备方法
公开(公告)号：WO2012110599A1
公开(公告)日：2012-08-23
申请号：PCT/EP2012/052687
申请日：2012-02-16
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , WAGNER, Holger , BERTA, Daniela , FUCHS, Klaus , GIOVANNINI, Riccardo , HAMPRECHT, Wolfgang , KONETZKI, Ingo , STREICHER, Ruediger , TRIESELMANN, Thomas
发明人： WAGNER, Holger , BERTA, Daniela , FUCHS, Klaus , GIOVANNINI, Riccardo , HAMPRECHT, Wolfgang , KONETZKI, Ingo , STREICHER, Ruediger , TRIESELMANN, Thomas
IPC分类号： C07D491/04 , A61P3/06 , A61P9/00 , A61K31/4741
CPC分类号： C07D491/048 , C07D491/107 , C07D491/18
摘要： The present invention relates to compounds defined by formula (I), wherein the variables R 1 -R 8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
摘要翻译：本发明涉及由式（I）定义的化合物，其中变量R1-R8如描述中所定义，具有有价值的药理学活性。特别地，化合物是胆固醇酯转移蛋白（CETP）的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病。

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