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21. 发明授权

US08278302B2 Substituted piperidines as CCR3 antagonists 有权
标题翻译：取代的哌啶作为CCR3拮抗剂
公开(公告)号：US08278302B2
公开(公告)日：2012-10-02
申请号：US12727318
申请日：2010-03-19
申请人： Marc Grundl , Horst Dollinger , Riccardo Giovannini , Christoph Hoenke , Matthias Hoffmann , Jan Kriegl , Domnic Martyres , Georg Rast , Peter Seither
发明人： Marc Grundl , Horst Dollinger , Riccardo Giovannini , Christoph Hoenke , Matthias Hoffmann , Jan Kriegl , Domnic Martyres , Georg Rast , Peter Seither
IPC分类号： A61K31/535 , A61K31/445 , C07D413/04 , C07D413/14 , C07D401/04 , C07D401/14
CPC分类号： C07D401/04 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/5355 , A61K31/56 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/14
摘要： Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明的目的是新的取代的式1化合物，其中A，R 1，R 2，R 3和R 4如描述中所定义。本发明的另一个目的是提供CCR3的拮抗剂，更具体地说是提供包含药用载体和治疗有效量的至少一种本发明化合物或其药学上可接受的盐的药物组合物。

22. 发明授权

US08114878B2 6,7-dihydrothieno[3,2-d]pyrimidine for the treatment of inflammatory diseases 有权
标题翻译： 6,7-二氢噻吩并[3,2-d]嘧啶，用于治疗炎性疾病
公开(公告)号：US08114878B2
公开(公告)日：2012-02-14
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： C07D495/04 , A61K31/519 , A61K31/497 , A61P37/06
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。

23. 发明授权

US07786111B2 Medicaments for the treatment of chronic obstructive pulmonary disease 有权
公开(公告)号：US07786111B2
公开(公告)日：2010-08-31
申请号：US12258830
申请日：2008-10-27
申请人： Ingo Konetzki , Kurt Schromm , Hermann Schollenberger , Sabine Pestel , Andreas Schnapp , Thierry Bouyssou , Frank Buettner , Claudia Heine , Klaus Rudolf , Philipp Lustenberger , Christoph Hoenke
发明人： Ingo Konetzki , Kurt Schromm , Hermann Schollenberger , Sabine Pestel , Andreas Schnapp , Thierry Bouyssou , Frank Buettner , Claudia Heine , Klaus Rudolf , Philipp Lustenberger , Christoph Hoenke
IPC分类号： C07D265/36 , A61K31/538
CPC分类号： A61K31/535 , A61K31/538 , C07D265/36
摘要： A pharmaceutical composition comprising a compound of formula 1 wherein: n is 1 or 2; R1 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R2 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R3 is hydrogen, C1-C4-alkyl, OH, halogen, —O—C1-C4-alkyl, —O—C1-C4-alkylene-COOH, or —O—C1-C4-alkylene-CO—O—C1-C4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid, or a solvate or hydrate thereof; and a pharmaceutically acceptable excipient or carrier, and methods for using the pharmaceutical formulation in the treatment of chronic obstructive pulmonary disease (COPD).

24. 发明授权

US07632834B2 Long acting beta-2-agonists and their use as medicaments 有权
标题翻译：长效β-2-激动剂及其用作药物
公开(公告)号：US07632834B2
公开(公告)日：2009-12-15
申请号：US12101462
申请日：2008-04-11
申请人： Thierry Bouyssou , Ingo Konetzki , Philipp Lustenberger , Juergen Mack , Andreas Schnapp , Dieter Wiedenmayer , Christoph Hoenke , Klaus Rudolf
发明人： Thierry Bouyssou , Ingo Konetzki , Philipp Lustenberger , Juergen Mack , Andreas Schnapp , Dieter Wiedenmayer , Christoph Hoenke , Klaus Rudolf
IPC分类号： A61K31/538 , A61K31/536 , C07D413/12 , C07D413/14
CPC分类号： C07D265/36 , C07D413/12
摘要： A compound of formula 1′″ wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1′ are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1′ together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2′, R2″, and R2′″ are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, or a corresponding acid addition salt thereof with a pharmacologically acceptable acid, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.
摘要翻译：式1“'的化合物，其中：V是-CH 2 - ， - NH-或-O-; R a和R b各自独立地为氢，C 1-4 - 烷基或卤素-C 1-4 - 烷基，或者R a和R b一起是C 2-5亚烷基桥，其中一个或多个氢原子任选被卤素取代; R 1和R 1'各自独立地为氢，C 1-6 - 烷基，C 3-6 - 环烷基，卤素-C 1-6 - 烷基，卤素-C 3-6环烷基或C 1-6亚烷基-C 3-6环烷基，或者R1和R1'一起是C2-5亚烷基桥，其中一个或多个氢原子任选地被卤素取代; R 2，R 2'，R 2“和R 2”各自独立地为氢，C 1-6 - 烷基，卤素-C 1-6亚烷基，OH，HO-C 1-6 - 亚烷基，-O-C 1-6 - 烷基，C 6-10 - 芳基，C 6-10 - 芳基-C 1-4 - 亚烷基，C 6-10 - 芳基-C 1-6 - 亚烷基-O，COOH，COOC 1-6 - 烷基，O-C 1-6亚烷基 - COOH，O-C 1-6亚烷基-COOC 1-6 - 烷基，NHSO 2 -C 1-6 - 烷基，CN，NH 2，NH-C 1-6 - 烷基，N（C 1-6 - 烷基）2，NO 2， C 1-6 - 烷基，SO 2 -C 1-6 - 烷基，SO-C 1-6 - 烷基，O（CO）C 1-6 - 烷基，CO C 1-6 - 烷基，NHCOC 1-6 - 烷基或卤素; 和n为0,1或2，或其光学异构体或其与药理学上可接受的酸的相应的酸加成盐，以及其作为药物组合物的用途，特别是用于治疗炎性和阻塞性呼吸道疾病。

25. 发明授权

US07563806B2 Substituted cycloalkyl derivatives, process for the manufacture thereof and use thereof as medicament 有权
标题翻译：取代的环烷基衍生物，其制备方法及其作为药物的用途
公开(公告)号：US07563806B2
公开(公告)日：2009-07-21
申请号：US12034409
申请日：2008-02-20
申请人： Ingo Konetzki , Thierry Bouyssou , Phillip Lustenberger , Andreas Schnapp , Christoph Hoenke , Klaus Rudolf , Marco Santagostino
发明人： Ingo Konetzki , Thierry Bouyssou , Phillip Lustenberger , Andreas Schnapp , Christoph Hoenke , Klaus Rudolf , Marco Santagostino
IPC分类号： C07D215/58 , A61K31/47
CPC分类号： C07D265/36 , C07C215/60 , C07C215/68 , C07C217/74 , C07C311/08 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D215/227
摘要： The present invention relates to compounds of formula 1 wherein the groups R1, R2, R3, R4, R5, R6, R7, R8, n, m and X may have the meanings given in the claims and in the specification, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.
摘要翻译：本发明涉及式1化合物，其中基团R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，n，m和X可以具有权利要求书和说明书中给出的含义及其用途作为药物组合物，特别是用于治疗炎性和阻塞性呼吸道疾病。

26. 发明授权

US07511045B2 Compounds for the treatment of inflammatory diseases 有权
标题翻译：用于治疗炎性疾病的化合物
公开(公告)号：US07511045B2
公开(公告)日：2009-03-31
申请号：US11408122
申请日：2006-04-20
申请人： Christoph Hoenke , Birgit Jung , Domnic Martyres , Peter Nickolaus , Pascale Pouzet
发明人： Christoph Hoenke , Birgit Jung , Domnic Martyres , Peter Nickolaus , Pascale Pouzet
IPC分类号： C07D413/02 , C07D417/04 , A61K31/4365 , A61K31/4355
CPC分类号： C07D521/00 , C07D495/04 , C07D519/00
摘要： Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, 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：式1的二氢噻吩并嘧啶及其药理学上可接受的盐，对映异构体，外消旋体，水合物或溶剂合物，其适用于治疗呼吸道或胃肠道疾病，关节，皮肤或眼睛的炎性疾病，外周疾病或中枢神经系统或癌症，以及含有这些化合物的药物组合物。

27. 发明授权

US07375104B2 Long acting beta-2-agonists and their use as medicaments 有权
公开(公告)号：US07375104B2
公开(公告)日：2008-05-20
申请号：US11600417
申请日：2006-11-15
申请人： Thierry Bouyssou , Ingo Konetzki , Philipp Lustenberger , Juergen Mack , Andreas Schnapp , Dieter Wiedenmayer , Christoph Hoenke , Klaus Rudolf
发明人： Thierry Bouyssou , Ingo Konetzki , Philipp Lustenberger , Juergen Mack , Andreas Schnapp , Dieter Wiedenmayer , Christoph Hoenke , Klaus Rudolf
IPC分类号： C07D413/12 , C07D413/14 , A61K31/538 , A61K31/536
CPC分类号： C07D265/36 , C07D413/12
摘要： A compound of formula 1′ wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1′ are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1′ together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2′, R2″, and R′″ are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, or a corresponding acid addition salt thereof with a pharmacologically acceptable acid, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.

28. 发明授权

US09206164B2 Pyrazole compounds as CRTH2 antagonists 有权
标题翻译：吡唑化合物作为CRTH2拮抗剂
公开(公告)号：US09206164B2
公开(公告)日：2015-12-08
申请号：US14006170
申请日：2012-03-15
申请人： Domnic Martyres , Ralf Anderskewitz , Christoph Hoenke , Jan Kriegl , Thorsten Oost , Wolfgang Rist , Peter Seither
发明人： Domnic Martyres , Ralf Anderskewitz , Christoph Hoenke , Jan Kriegl , Thorsten Oost , Wolfgang Rist , Peter Seither
IPC分类号： A61K31/335 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4164 , A61K31/421 , A61K31/426 , C07D403/10 , C07D471/04 , C07D487/04 , A61K31/4155 , A61K31/4184 , A61K31/437 , A61K31/52 , A61K45/06 , C07D473/00
CPC分类号： C07D403/10 , A61K31/335 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4184 , A61K31/421 , A61K31/437 , A61K31/52 , A61K45/06 , C07D471/04 , C07D473/00 , C07D487/04
摘要： The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2 antagonistic activity, wherein L, Y1, Y2, Y3, Y4, Y5, Z, R1, R2, R3 and n have one of the meanings as indicated in the specification and claims, to their use as medicaments, to pharmaceutical compositions containing said compounds and to pharmaceutical compositions containing said compounds in combination with one or more active substances.
摘要翻译：本发明涉及具有CRTH2拮抗活性的式（I）的吡唑化合物及其药学上可接受的盐，其中L，Y1，Y2，Y3，Y4，Y5，Z，R1，R2，R3和n具有以下含义之一：在说明书和权利要求书中指出其作为药物的用途，含有所述化合物的药物组合物和含有所述化合物与一种或多种活性物质组合的药物组合物。

29. 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。

30. 发明授权

US08946218B2 CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments 有权
标题翻译： CCR2受体拮抗剂，其制备方法及其作为药物的用途
公开(公告)号：US08946218B2
公开(公告)日：2015-02-03
申请号：US13696860
申请日：2011-05-10
申请人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Rocco Mazzaferro , Stefan Scheuerer
发明人： Heiner Ebel , Sara Frattini , Riccardo Giovannini , Christoph Hoenke , Rocco Mazzaferro , Stefan Scheuerer
IPC分类号： C07D401/14 , A61K31/506 , C07D413/14 , C07D401/06 , C07D405/14
CPC分类号： C07D413/14 , C07D401/06 , C07D401/14 , 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 and pain diseases.
摘要翻译：本发明涉及用于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以及疼痛疾病的药物的用途。

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