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1.发明授权Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation 有权三环吡啶衍生物，含有此类化合物的药物，其用途及其制备方法公开(公告)号：US09029544B2
公开(公告)日：2015-05-12
申请号：US13029697
申请日：2011-02-17
申请人： Holger Wagner , Daniela Berta , Klaus Fuchs , Riccardo Giovannini , Dieter Wolfgang Hamprecht , Ingo Konetzki , Ruediger Streicher , Thomas Trieselmann
发明人： Holger Wagner , Daniela Berta , Klaus Fuchs , Riccardo Giovannini , Dieter Wolfgang Hamprecht , Ingo Konetzki , Ruediger Streicher , Thomas Trieselmann
IPC分类号： C07D491/20 , A61K31/506 , C07D491/048 , C07D491/04 , C07D215/56
CPC分类号： C07D491/04 , A61K31/506 , C07D215/56 , C07D491/20
摘要： The present invention relates to compounds defined by formula I wherein the variables R1-R8 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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2.发明申请公开(公告)号：US20130053404A1
公开(公告)日：2013-02-28
申请号：US13397855
申请日：2012-02-16
申请人： Holger Wagner , Daniela Berta , Klaus Fuchs , Riccardo Giovannini , Dieter Wolfgang Hamprecht , Ingo Konetzki , Ruediger Streicher , Thomas Trieselmann
发明人： Holger Wagner , Daniela Berta , Klaus Fuchs , Riccardo Giovannini , Dieter Wolfgang Hamprecht , Ingo Konetzki , Ruediger Streicher , Thomas Trieselmann
IPC分类号： C07D491/048 , A61K31/4747 , A61K31/506 , C07D491/20 , A61P9/10 , C07D221/20 , A61P9/00 , A61P3/00 , A61P3/06 , A61K31/4741 , C07D215/56
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 R1-R8 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.
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3.发明授权Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation 有权三环吡啶衍生物，含有此类化合物的药物，其用途及其制备方法公开(公告)号：US08703793B2
公开(公告)日：2014-04-22
申请号：US12920722
申请日：2009-03-02
申请人： Holger Wagner , Daniela Berta , Riccardo Giovannini , Alessandro Mazzacani , Ruediger Streicher , Klaus Fuchs
发明人： Holger Wagner , Daniela Berta , Riccardo Giovannini , Alessandro Mazzacani , Ruediger Streicher , Klaus Fuchs
IPC分类号： A61K31/4355 , C07D491/048
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.
摘要翻译： 式（I）的化合物，其中基团R 1至R 8具有说明书中所述的含义，互变异构体，立体异构体，其混合物及其盐具有有价值的药理学性质，使其可用于治疗心血管和相关疾病 。
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4.发明申请Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation 有权三环吡啶衍生物，含有此类化合物的药物，其用途及其制备方法公开(公告)号：US20110021550A1
公开(公告)日：2011-01-27
申请号：US12920722
申请日：2009-03-02
申请人： Holger Wagner , Daniela Berta , Riccardo Giovannini , Alessandro Mazzacani , Ruediger Streicher , Klaus Fuchs
发明人： Holger Wagner , Daniela Berta , Riccardo Giovannini , Alessandro Mazzacani , Ruediger Streicher , Klaus Fuchs
IPC分类号： A61K31/438 , C07D491/04 , C07D491/10 , A61K31/4355 , A61P9/10
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.
摘要翻译： 式（I）化合物，其中基团R 1至R 8具有说明书中所述的含义，互变异构体，立体异构体，其混合物及其盐具有有价值的药理学性质，使其可用于治疗心血管和相关疾病 。
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5.发明申请CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD 审中-公开CYPIC PYRIMIDIN-4-CARBOXAMIDES作为CCR2受体拮抗剂用于治疗炎症，哮喘和COPD公开(公告)号：US20120053164A1
公开(公告)日：2012-03-01
申请号：US13140591
申请日：2009-12-17
申请人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Thomas Trieselmann , Patrick Tielmann , Stefan Scheuerer , Silke Hobbie , Frank Buettner
发明人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Thomas Trieselmann , Patrick Tielmann , Stefan Scheuerer , Silke Hobbie , Frank Buettner
IPC分类号： A61K31/506 , C07D405/14 , C07D413/14 , A61K31/5377 , C07D403/14 , A61K31/55 , C07D401/06 , C07D471/10 , C07D417/14 , C07D471/04 , C07D498/10 , C07D451/02 , A61K31/553 , C07D403/06 , A61K31/551 , A61P29/00 , A61P11/00 , A61P11/06 , A61P25/00 , A61P37/00 , A61P9/00 , A61P13/12 , A61P3/10 , A61P9/10 , A61P25/04 , C07D401/14
CPC分类号： C07D498/10 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/10 , C07D491/052 , Y02A50/385 , Y02A50/409 , Y02A50/411
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. Formula (I), wherein A is selected from among a single bond, ═CH—, —CH2—, —O—, —S—, and —NH—; wherein n is 1, 2 or 3; wherein Z is C or N, the other variables are as defined in the claims, as well as in form of their acid addition salts with pharmacologically acceptable acids.
摘要翻译： 本发明涉及CCR2（CC趋化因子受体2）的新型拮抗剂及其用于治疗疾病，特别是肺疾病如哮喘和COPD的药物的用途。 式（I）其中A选自单键，-CH =，-CH 2 - ， - O - ， - S - 和-NH-; 其中n为1,2或3; 其中Z是C或N，其它变量如权利要求中所定义，以及其与药理学上可接受的酸的酸加成盐的形式。
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公开(公告)号：US20120004252A1
公开(公告)日：2012-01-05
申请号：US12969745
申请日：2010-12-16
申请人： Heiner Ebel , Sara Frattini , Kai Gerlach , Riccardo Giovannini , Christoph Hoenke , Rocco Mazzaferro , Marco Santagostino , Stefan Scheuerer , Christofer Tautermann , Thomas Trieselmann
发明人： Heiner Ebel , Sara Frattini , Kai Gerlach , Riccardo Giovannini , Christoph Hoenke , Rocco Mazzaferro , Marco Santagostino , Stefan Scheuerer , Christofer Tautermann , Thomas Trieselmann
IPC分类号： A61K31/506 , C07D405/14 , C07D491/107 , A61K31/4545 , A61P9/10 , A61P11/06 , A61P29/00 , A61P25/00 , A61P3/10 , C07D401/14 , A61P11/00
CPC分类号： C07D491/107 , C07D405/14
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
摘要翻译： 本发明涉及CCR2（CC趋化因子受体2）的新型拮抗剂及其用于治疗疾病，特别是肺疾病如哮喘和COPD的药物的用途。
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7.发明授权Cyclic pyrimidin-4-carboxamides as CCR2 receptor antagonists for treatment of inflammation, asthma and COPD 有权循环嘧啶-4-甲酰胺作为治疗炎症，哮喘和COPD的CCR2受体拮抗剂公开(公告)号：US08835440B2
公开(公告)日：2014-09-16
申请号：US13949696
申请日：2013-07-24
申请人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Thomas Trieselmann , Patrick Tielmann , Stefan Scheuerer , Silke Hobbie , Frank Buettner
发明人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Thomas Trieselmann , Patrick Tielmann , Stefan Scheuerer , Silke Hobbie , Frank Buettner
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04 , C07D498/10 , C07D403/06 , A61K31/55 , C07D491/052 , C07D401/06 , A61K31/553 , C07D405/14 , C07D471/10 , C07D407/14 , C07D417/14 , A61K31/5377 , A61K31/551 , C07D471/04 , C07D403/14 , C07D451/02 , C07D401/14 , A61K31/506 , C07D413/14
CPC分类号： C07D498/10 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/10 , C07D491/052 , Y02A50/385 , Y02A50/409 , Y02A50/411
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
摘要翻译： 本发明涉及CCR2（CC趋化因子受体2）的新型拮抗剂及其用于治疗疾病，特别是肺疾病如哮喘和COPD的药物的用途。
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公开(公告)号：US08765949B2
公开(公告)日：2014-07-01
申请号：US12969745
申请日：2010-12-16
申请人： Heiner Ebel , Sara Frattini , Kai Gerlach , Riccardo Giovannini , Christoph Hoenke , Rocco Mazzaferro , Marco Santagostino , Stefan Scheuerer , Christofer Tautermann , Thomas Trieselmann
发明人： Heiner Ebel , Sara Frattini , Kai Gerlach , Riccardo Giovannini , Christoph Hoenke , Rocco Mazzaferro , Marco Santagostino , Stefan Scheuerer , Christofer Tautermann , Thomas Trieselmann
IPC分类号： C07D239/02 , C07D211/68 , C07D211/80 , C07D211/60 , A01N43/54 , A01N43/40 , A61K31/445 , A01N43/16 , A61K31/35 , C07D405/14 , C07D491/107
CPC分类号： C07D491/107 , C07D405/14
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
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公开(公告)号：US20130143905A1
公开(公告)日：2013-06-06
申请号：US13515852
申请日：2010-12-13
申请人： Heiner Ebel , Sara Frattini , Kai Gerlach , Riccardo Giovannini , Christoph Hoenke , Marco Santagostino , Stefan Scheuerer , Thomas Trieselmann
发明人： Heiner Ebel , Sara Frattini , Kai Gerlach , Riccardo Giovannini , Christoph Hoenke , Marco Santagostino , Stefan Scheuerer , Thomas Trieselmann
IPC分类号： C07D401/14 , C07D405/14
CPC分类号： C07D401/14 , C07D405/14
摘要： The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
摘要翻译： 本发明涉及式（I）的CCR2（CC趋化因子受体2）的新型拮抗剂及其用于治疗疾病，特别是肺疾病如哮喘和COPD的药物的用途。
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公开(公告)号：US09067951B2
公开(公告)日：2015-06-30
申请号：US14445137
申请日：2014-07-29
申请人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Thomas Trieselmann , Patrick Tielmann
发明人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Thomas Trieselmann , Patrick Tielmann
IPC分类号： C07D498/10 , A61K31/506 , C07D401/06 , C07D401/14 , C07D403/06 , C07D407/14 , C07D413/14 , C07D471/10 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07D403/14 , C07D405/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D491/052
CPC分类号： C07D498/10 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/10 , C07D491/052 , Y02A50/385 , Y02A50/409 , Y02A50/411
摘要： The present invention relates to a process for the production of novel antagonists for CCR2 (CC chemokine receptor 2) and intermediates thereof.
摘要翻译： 本发明涉及生产CCR2（CC趋化因子受体2）的新型拮抗剂及其中间体的方法。
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