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公开(公告)号:EP2061779B1
公开(公告)日:2013-11-06
申请号:EP07788420.3
申请日:2007-08-14
发明人: KAUFFMANN-HEFNER, Iris , HAUEL, Norbert , WALTER, Rainer , EBEL, Heiner , DOODS, Henri , CECI, Angelo , SCHULER-METZ, Annette , KONETZKI, Ingo
IPC分类号: C07D401/02 , C07D311/16 , C07D205/04 , C07D207/06 , C07D223/04 , C07D403/04 , C07D403/06
CPC分类号: C07D401/02 , C07C311/29 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/06 , C07D223/04 , C07D403/04 , C07D403/06
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公开(公告)号:EP2061779A1
公开(公告)日:2009-05-27
申请号:EP07788420.3
申请日:2007-08-14
发明人: KAUFFMANN-HEFNER, Iris , HAUEL, Norbert , WALTER, Rainer , EBEL, Heiner , DOODS, Henri , CECI, Angelo , SCHULER-METZ, Annette , KONETZKI, Ingo
IPC分类号: C07D401/02 , C07D311/16 , C07D205/04 , C07D207/06 , C07D223/04 , C07D403/04 , C07D403/06
CPC分类号: C07D401/02 , C07C311/29 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/06 , C07D223/04 , C07D403/04 , C07D403/06
摘要: The invention relates to compounds of the general formula (I) in which A, B, D, Y, R1, R2, R3, R4 and R5 are defined as per claim 1, to their enantiomers, their diastereomers, their mixtures and their salts, especially their physiologically compatible salts with organic or inorganic acids or bases, which have valuable properties, to their preparation, to medicaments comprising the pharmacologically effective compounds, their preparation and their use.
摘要翻译: 吡啶 - 哌嗪 - 苯基衍生物(I)或其对映体,非对映体或盐,优选与有机或无机酸或碱的盐是新的。 式(R 5→-AR 4→-B 1→-R 3)-ADY 1> -N(R 2)-SO 2 -R 1)的吡啶 - 哌嗪 - 苯基衍生物(I))或其对映异构体, 非对映异构体或盐,优选与有机或无机酸或碱的盐是新的。 A:键或1-4C亚烷基; B 1>:键,1-3C亚烷基,-O-或-C(O) - ; D:式(-N(R 2)-C(O) - )或(-C(O)-N(R 2)) - 的胺基; Y 1>:任选被R 2'取代的1-4C-亚烷基,其中亚甲基可以另外被Y 2>取代; (O) - , - (R 2) - , - (R 2) - C(O) - , - C(O) R 2 - ) - , - C(O) - , - CH(芳基) - 或-S(O) R 1>:3-7C-环烷基 - 或芳基 - ,杂芳基 - 或芳基 - 1-3C-烷基 - (全部被1-4个R 1a取代); R 2>:H或1-3C-烷基,其中每个亚甲基被至多两个F取代,并且每个甲基被最多3F替代; R 3>:亚芳基,杂亚芳基,饱和4-7元杂环,不饱和5-7元杂环(全部被1或2个R 3a取代)或1-6C-亚烷基; R 4>:亚芳基,亚杂芳基,饱和4-7元杂环,不饱和5-7元杂环(全部被1或2个R 4a取代),-O - , - C(O) )NR 2 - , - NR 2 - , - NR 2 - ,-NR 2 - , - 37C-亚环烷基 - 或 - C 1-6 - 亚烷基 - R 5>:杂芳基,4-7元饱和杂环(均被1或2个R 5a取代),H,1-8C烷基,3-7C-环烷基(任选被1-3C烷基取代),H 2 N - , - -4C-烷基-NH-,(1-4C-烷基)2N-或H 2N-C(O) - ; 和R1a,R3a,R4a,R5a:H,F,Cl,Br,I,1-3C-烷基 - ,HO-,1-3C-烷基-O-或1-3C-烷基-O-2-4C- 亚烷基-O-。 对于无机或有机酸或碱,包括吡啶 - 哌嗪 - 苯基盐的独立权利要求。 活性:止痛; 偏头痛; 神经保护; 皮肤; 脑保护; Vasotropic; 抗过敏; 免疫抑制; 胃肠道根; 呼吸根; 平喘; 抗炎; 抗关节炎; 骨科。 行动机制:无给予。
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公开(公告)号:EP2155689B1
公开(公告)日:2015-07-08
申请号:EP08760165.4
申请日:2008-05-29
发明人: EBEL, Heiner , PETERS, Stefan , HOBBIE, Silke
IPC分类号: C07D231/38 , C07D401/04 , C07D401/14 , C07D413/12 , A61K31/415 , A61P11/06
CPC分类号: C07D231/38 , C07D401/04 , C07D401/14 , C07D413/12
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公开(公告)号:EP2513093B1
公开(公告)日:2014-08-27
申请号:EP10796336.5
申请日:2010-12-13
发明人: EBEL, Heiner , FRATTINI, Sara , GERLACH, Kai , GIOVANNINI, Riccardo , HOENKE, Christoph , MAZZAFERRO, Rocco , SANTAGOSTINO, Marco , SCHEUERER, Stefan , TAUTERMANN, Christofer , TRIESELMANN, Thomas
IPC分类号: C07D491/107 , C07D405/14 , A61K31/506 , A61P29/00
CPC分类号: C07D491/107 , C07D405/14
摘要: The present invention relates to a process for the production of novel antagonists for CCR2 (CC chemokine receptor 2) and intermediates thereof.
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5.NOVEL CCR2 RECEPTOR ANTAGONISTS, METHOD FOR PRODUCING THE SAME, AND USE THEREOF AS MEDICAMENTS 有权
标题翻译: 新型CCR2受体拮抗剂,其制备方法及其用作药物的用途公开(公告)号:EP2569298A1
公开(公告)日:2013-03-20
申请号:EP11719249.2
申请日:2011-05-10
发明人: EBEL, Heiner , FRATTINI, Sara , GIOVANNINI, Riccardo , HOENKE, Christoph , MAZZAFERRO, Rocco , SCHEUERER, Stefan
IPC分类号: C07D401/14 , C07D405/14 , C07D413/14 , C07D487/04 , C07D491/10 , C07D495/04 , C07D471/04 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61P37/00 , A61P9/00 , A61P25/00
CPC分类号: C07D405/14 , C07D401/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/10 , C07D491/107 , C07D495/04
摘要: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) 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: 本发明涉及式(I)的CCR2(CC趋化因子受体2)的新拮抗剂,其中HET是选自式(IIa)(IIb)(IIc)(IId)的基团及其用于提供用于治疗病症 和疾病,特别是肺部疾病如哮喘和COPD以及疼痛疾病。
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公开(公告)号:EP2576538B1
公开(公告)日:2015-10-28
申请号:EP11723037.5
申请日:2011-05-26
IPC分类号: C07D401/06 , C07D405/14 , A61P35/00 , A61P25/00 , A61P29/00 , A61P9/00 , A61K31/435
CPC分类号: C07D405/14 , C07D401/06 , C07D401/14
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7.CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD 有权
标题翻译: CYCLIC嘧啶-4-羧酸酰胺AS CCR2受体为炎症,哮喘和COPD于治疗拮抗剂公开(公告)号:EP2379525B1
公开(公告)日:2015-07-29
申请号:EP09775212.5
申请日:2009-12-17
发明人: EBEL, Heiner , FRATTINI, Sara , GIOVANNINI, Riccardo , HOENKE, Christoph , TRIESELMANN, Thomas , TIELMANN, Patrick , SCHEUERER, Stefan , HOBBIE, Silke (Marie Katrin) , BUETTNER, Frank
IPC分类号: C07D405/14 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07D417/14 , C07D451/02 , C07D471/04 , C07D491/052 , C07D498/10 , C07D401/14 , C07D413/14 , A61K31/506 , C07D401/06 , C07D403/06 , C07D403/14 , C07D407/14 , C07D471/10
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) of formula (I) from 6-Chloro-pyrimidine-methanone intermediates. Formula (I): Specifically claimed 6-chloropyrimidine-methanone intermediates are:
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公开(公告)号:EP2576542A1
公开(公告)日:2013-04-10
申请号:EP11721302.5
申请日:2011-05-23
IPC分类号: C07D405/14 , A61K31/501 , A61P11/00 , A61P25/00 , A61P13/12
CPC分类号: C07D405/14 , C07D401/14
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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9.NEW CCR2 RECEPTOR ANTAGONISTS, METHOD FOR PRODUCING THE SAME, AND USE THEREOF AS MEDICAMENTS 有权
标题翻译: 新的CCR2受体拮抗剂,其制备方法及其用作药物的用途公开(公告)号:EP2569295A1
公开(公告)日:2013-03-20
申请号:EP11721268.8
申请日:2011-05-10
发明人: EBEL, Heiner , FRATTINI, Sara , GIOVANNINI, Riccardo , HOENKE, Christoph , MAZZAFERRO, Rocco , SCHEUERER, Stefan
IPC分类号: C07D401/06 , C07D401/14 , C07D405/14 , A61P29/00
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提供用于治疗病症和疾病,特别是肺部疾病如哮喘和COPD和疼痛疾病的药物的用途。
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公开(公告)号:EP2513086A1
公开(公告)日:2012-10-24
申请号:EP10796008.0
申请日:2010-12-13
发明人: EBEL, Heiner , FRATTINI, Sara , GERLACH, Kai , GIOVANNINI, Riccardo , HOENKE, Christoph , SANTAGOSTINO, Marco , SCHEUERER, Stefan , TRIESELMANN, Thomas
IPC分类号: C07D401/14 , C07D405/14 , A61K31/506 , A61P29/00
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.
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