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1. 发明授权

US08853193B2 Thienopyrimidines containing a substituted alkyl group for pharmaceutical compositions 有权
标题翻译：含有用于药物组合物的取代烷基的噻吩并嘧啶
公开(公告)号：US08853193B2
公开(公告)日：2014-10-07
申请号：US13035023
申请日：2011-02-25
申请人： Armin Heckel , Frank Himmelsbach , Joerg Kley , Thorsten Lehmann-Lintz , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Phillip Black , Wesley Blackaby , Ian Linney , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter
发明人： Armin Heckel , Frank Himmelsbach , Joerg Kley , Thorsten Lehmann-Lintz , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Phillip Black , Wesley Blackaby , Ian Linney , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter
IPC分类号： C07D495/04 , A61K31/519 , A61K31/5377 , A61K31/56 , A61P29/00 , A61P35/00 , A61P25/28 , A61P13/12 , A61K31/395
CPC分类号： C07D495/04
摘要： The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要翻译：本发明涉及包含这些化合物的通式药物组合物的新型噻吩并嘧啶化合物及其用于预防和/或治疗可受到抑制Mnk1和/或Mnk2（Mnk2a或Mnk2b的激酶活性）的疾病的治疗用途）和/或其变体。

2. 发明授权

US08754079B2 Cycloalkyl containing thienopyrimidines for pharmaceutical compositions 有权
标题翻译：含有用于药物组合物的噻吩并嘧啶的环烷基
公开(公告)号：US08754079B2
公开(公告)日：2014-06-17
申请号：US13034855
申请日：2011-02-25
申请人： Thorsten Lehmann-Lintz , Armin Heckel , Joerg Kley , Elke Langkopf , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter , Phillip Black , Wesley Blackaby , Ian Linney
发明人： Thorsten Lehmann-Lintz , Armin Heckel , Joerg Kley , Elke Langkopf , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter , Phillip Black , Wesley Blackaby , Ian Linney
IPC分类号： C07D495/04 , A61K31/519 , A61K31/496 , A61K31/5355 , C07D413/12 , A61P25/28 , A61P29/00 , A61P35/00
CPC分类号： C07D495/04
摘要： The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要翻译：本发明涉及包含这些化合物的通式药物组合物的新型噻吩并嘧啶化合物及其用于预防和/或治疗可受到抑制Mnk1和/或Mnk2（Mnk2a或Mnk2b的激酶活性）的疾病的治疗用途）和/或其变体。

3. 发明授权

US08648068B2 Heterocycloalkyl-containing thienopyrimidines for pharmaceutical compositions 有权
标题翻译：用于药物组合物的含杂环烷基的噻吩并嘧啶
公开(公告)号：US08648068B2
公开(公告)日：2014-02-11
申请号：US13034913
申请日：2011-02-25
申请人： Thorsten Lehmann-Lintz , Joerg Kley , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter , Phillip Black , Wesley Blackaby , Ian Linney
发明人： Thorsten Lehmann-Lintz , Joerg Kley , Norbert Redemann , Achim Sauer , Leo Thomas , Dieter Wiedenmayer , Matthias Austen , John Danilewicz , Martin Schneider , Kay Schreiter , Phillip Black , Wesley Blackaby , Ian Linney
IPC分类号： C07D495/04 , A61K31/519 , A61K31/5355 , A61P35/00 , A61P25/28 , A61P3/10
CPC分类号： C07D495/04 , C07D519/00
摘要： The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要翻译：本发明涉及包含噻吩并嘧啶化合物的新型药物组合物。此外，本发明涉及本发明的噻吩并嘧啶化合物用于生产药物组合物用于预防和/或治疗可受到抑制Mnk1和/或Mnk2（Mnk2a）激酶活性的疾病的用途或Mnk2b）和/或其变体。

4. 发明授权

US08901138B2 Sulfoximine substituted quinazolines for pharmaceutical compositions 有权
标题翻译：用于药物组合物的磺酰亚胺取代喹唑啉
公开(公告)号：US08901138B2
公开(公告)日：2014-12-02
申请号：US14073907
申请日：2013-11-07
申请人： Andreas Blum , Dirk Gottschling , Armin Heckel , Joerg Hehn , Thorsten Lehmann-Lintz , Dieter Wiedenmayer
发明人： Andreas Blum , Dirk Gottschling , Armin Heckel , Joerg Hehn , Thorsten Lehmann-Lintz , Dieter Wiedenmayer
IPC分类号： C07D411/14 , C07D239/94 , A61K31/47 , A61P35/00 , A61K31/541 , A61K31/517 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D493/04
CPC分类号： A61K31/541 , A61K31/517 , A61K45/06 , C07D239/94 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D411/14 , C07D417/12 , C07D493/04
摘要： This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined herein, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.
摘要翻译：本发明涉及式I的新型磺酰亚胺取代喹唑啉衍生物，其中Ar，R 1和R 2如本文所定义，以及它们作为MNK1（MNK1a或MNK1b）和/或MNK2（MNK2a或MNK2b）激酶抑制剂的用途，含有它们的药物组合物以及使用其作为治疗或改善MNK1（MNK1a或MNK1b）和/或MNK2（MNK2a或MNK2b）介导的病症的药剂的方法。

5. 发明授权

US08637550B2 Heteroaryl diamide compounds useful as MMP-13 inhibitors 有权
标题翻译：可用作MMP-13抑制剂的杂芳基二酰胺化合物
公开(公告)号：US08637550B2
公开(公告)日：2014-01-28
申请号：US13127256
申请日：2009-11-05
申请人： Neil Alexander Farrow , Donghong Amy Gao , Alexander Heim-Riether , Sabine Schlyer , Lana Louise Smith Keenan , Steven John Taylor , Bernd Wellenzohn , Dieter Wiedenmayer , Zhaoming Xiong , Qiang Zhang
发明人： Neil Alexander Farrow , Donghong Amy Gao , Alexander Heim-Riether , Sabine Schlyer , Lana Louise Smith Keenan , Steven John Taylor , Bernd Wellenzohn , Dieter Wiedenmayer , Zhaoming Xiong , Qiang Zhang
IPC分类号： A61K31/443 , C07D405/12 , C07D405/10
CPC分类号： C07D407/10 , C07D231/14 , C07D263/16 , C07D277/56 , C07D307/68 , C07D401/04 , C07D407/14 , C07D411/12 , C07D471/04
摘要： Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).
摘要翻译：公开了作为MMP-13抑制剂的如本文所述的式（I）的化合物和组合物。还公开了使用和制备式（I）化合物的方法。

6. 发明申请

US20070066609A1 Long acting beta-2-agonists and their use as medicaments 有权
公开(公告)号：US20070066609A1
公开(公告)日：2007-03-22
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 Hoenike , Klaus Rudolf
发明人： Thierry Bouyssou , Ingo Konetzki , Philipp Lustenberger , Juergen Mack , Andreas Schnapp , Dieter Wiedenmayer , Christoph Hoenike , Klaus Rudolf
IPC分类号： A61K31/538 , C07D413/02
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.

7. 发明授权

US07160882B2 Long acting β-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：US07160882B2
公开(公告)日：2007-01-09
申请号：US11029451
申请日：2005-01-05
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： The present invention relates to compounds of formula 1 wherein the groups X, Ra, Rb, R1, R1′, R2, R2′, R2″, R2′″, V and n 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的化合物，其中基团X，R a，R b，R 1，R 1， R 2，R 2，R 2，R“2”，R“2”，R“2” ，V和n可以具有权利要求书和说明书中给出的含义，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。

8. 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。

9. 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.

10. 发明授权

US09139577B2 Sulfoximine substituted quinazolines for pharmaceutical compositions 有权
标题翻译：用于药物组合物的磺酰亚胺取代喹唑啉
公开(公告)号：US09139577B2
公开(公告)日：2015-09-22
申请号：US14315399
申请日：2014-06-26
申请人： Andreas Blum , Dirk Gottschling , Armin Heckel , Joerg P. Hehn , Bernhard Schmid , Dieter Wiedenmayer
发明人： Andreas Blum , Dirk Gottschling , Armin Heckel , Joerg P. Hehn , Bernhard Schmid , Dieter Wiedenmayer
IPC分类号： C07D413/14 , C07D239/94 , A61K31/517 , C07D409/12 , C07D401/12 , C07D413/12 , C07D411/12 , C07D409/14 , C07D495/10 , C07D403/12 , A61K45/06 , A61K31/541 , C07D401/14 , C07D405/12 , C07D417/04 , C07D417/14
CPC分类号： C07D239/94 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D495/10
摘要： This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.
摘要翻译：本发明涉及式I的新型磺酰亚胺取代的喹唑啉衍生物，其中Ar，R 1和R 2如说明书和权利要求中所定义，以及它们作为MNK1（MNK1a或MNK1b）和/或MNK2（MNK2a或MNK2b）激酶抑制剂，药物含有该化合物的组合物，以及使用其作为治疗或改善MNK1（MNK1a或MNK1b）和/或MNK2（MNK2a或MNK2b）介导的病症的药剂的方法。

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