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1. 发明申请

US20120053164A1 CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD 审中-公开
标题翻译： 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。

2. 发明授权

US08835440B2 Cyclic pyrimidin-4-carboxamides as CCR2 receptor antagonists for treatment of inflammation, asthma and COPD 有权
标题翻译：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。

3. 发明授权

US09067951B2 Process and intermediates for the production of CCR2 antagonists 有权
标题翻译：用于生产CCR2拮抗剂的方法和中间体
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。

4. 发明申请

US20100197908A1 Pyridazine Derivatives with MCH Antagonistic Activity and Medicaments Comprising These Compounds 审中-公开
标题翻译：具有MCH拮抗活性的哒嗪衍生物和包含这些化合物的药物
公开(公告)号：US20100197908A1
公开(公告)日：2010-08-05
申请号：US12518321
申请日：2007-12-10
申请人： Thorsten Lehmann-Lintz , Dirk Stenkamp , Gerald Juergen Roth , Stephan Georg Mueller , Joerg Kley , Armin Heckel , Klaus Rudolf , Marcus Schindler , Ralf Lotz , Patrick Tielmann
发明人： Thorsten Lehmann-Lintz , Dirk Stenkamp , Gerald Juergen Roth , Stephan Georg Mueller , Joerg Kley , Armin Heckel , Klaus Rudolf , Marcus Schindler , Ralf Lotz , Patrick Tielmann
IPC分类号： C07D403/10 , C07D413/10 , C07D401/10 , C07D403/14 , C07D401/14
CPC分类号： C07D237/14 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D417/10 , C07D471/04
摘要： The present invention relates to compounds of general formula I wherein the groups and radicals B, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
摘要翻译：本发明涉及通式I的化合物，其中基团B，W，X，Y，Z，R 1，R 2具有权利要求1中给出的含义。此外，本发明涉及含有至少一种化合物涉及本发明。由于它们的MCH受体拮抗活性，本发明的药物组合物适用于治疗代谢紊乱和/或进食障碍，特别是肥胖症，食欲过剩，厌食症，食欲过盛和糖尿病。

5. 发明申请

US20050153358A1 High-throughput screening method for determining the enantioselectivity of catalysts, biocatalysts, and agents 审中-公开
标题翻译：用于确定催化剂，生物催化剂和试剂的对映体选择性的高通量筛选方法
公开(公告)号：US20050153358A1
公开(公告)日：2005-07-14
申请号：US10506144
申请日：2003-02-22
申请人： Manfred Reetz , Patrick Tielmann , Andreas Eipper , Richard Mynott
发明人： Manfred Reetz , Patrick Tielmann , Andreas Eipper , Richard Mynott
IPC分类号： G01N24/08 , C07C27/02 , C07C31/12 , C07C33/20 , C07C69/013 , C07C69/145 , G01N37/00 , G01R33/30 , G01R33/46 , G01N33/53 , G01N33/543
CPC分类号： G01R33/46
摘要： The invention relates to a high-throughput screening method based on NMR spectroscopy for determining the enantioselectivity of reactions which show an asymmetric course. The reactions can be caused by chiral catalysts, agents, or biocatalysts such that said products can be evaluated regarding the enantioselectivity thereof. In one embodiment, isotope-marked pseudo-enantiomers or pseudo-prochiral substrates are used such that the enantioselectivity can be quantified by integrating the NMR signals of the respective substrates and/or products. The use of an automated setup of devices, including microtiter plates, robots, and high-throughput NMR devices, is decisive for the high-throughput process. In a second embodiment of the invention, the automated setup of devices is used to detect in a quantitative manner the products and/or educts that have been derivatized with enantiomer-pure agents in the form of diastereomers. At least 1000 ee determinations can be done per day with accuracy of at least ±5 percent in both embodiments.
摘要翻译：本发明涉及一种基于NMR光谱的高通量筛选方法，用于测定显示非对称过程的反应的对映体选择性。反应可以由手性催化剂，试剂或生物催化剂引起，使得可以评价所述产物的对映体选择性。在一个实施方案中，使用同位素标记的假对映异构体或假前手性底物，使得对映体选择性可以通过对各个底物和/或产物的NMR信号进行积分来定量。使用自动设置装置，包括微量滴定板，机器人和高通量NMR装置对于高通量过程是决定性的。在本发明的第二个实施方案中，设备的自动设置用于以定量方式检测已经以非对映异构体形式的对映异构体纯试剂衍生化的产物和/或离子。在两个实施方案中，至少可以进行1000次ee测定，其准确度至少为±5％。

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