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公开(公告)号:US20110028441A1
公开(公告)日:2011-02-03
申请号:US12738412
申请日:2008-10-13
申请人: Pascale Pouzet , Christoph Hoenke , Peter Nickolaus , Rolf Goeggel , Thomas Fox , Dennis Fiegen , Klaus Klinder
发明人: Pascale Pouzet , Christoph Hoenke , Peter Nickolaus , Rolf Goeggel , Thomas Fox , Dennis Fiegen , Klaus Klinder
IPC分类号: A61K31/573 , C07D495/04 , A61K31/519 , A61P1/04 , A61P11/06 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28
CPC分类号: A61K31/519 , C07D495/04
摘要: The invention relates to novel dihydrothienopyrimidines of the formula 1, and to pharmacologically acceptable salts thereof, formula (1) in which X is SO or SO2, but preferably SO, and either R3 is a monosubstituted phenyl ring in the ortho position or in the meta position, or R3 is a phenyl ring bisubstituted in any positions, and pharmaceutical compositions which comprise these compounds. These novel dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal symptoms or disorders, inflammatory disorders of the joints, of the skin or of the eyes, disorders of the peripheral or central nervous system or cancers.
摘要翻译: 本发明涉及式1的新型二氢噻吩并嘧啶及其药学上可接受的盐,其中X为SO或SO 2,但优选为SO的式(1),R3为邻位或元环中的单取代苯环 位置,或R3是在任何位置双取代的苯环,以及包含这些化合物的药物组合物。 这些新型二氢噻吩并嘧啶适用于治疗呼吸系统或胃肠道症状,疾病,关节炎,皮肤或眼睛的炎症,外周或中枢神经系统或癌症的疾病。
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公开(公告)号:US08754073B2
公开(公告)日:2014-06-17
申请号:US12738344
申请日:2008-10-16
申请人: Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
发明人: Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
IPC分类号: C07D495/04 , A61K31/519 , A61P29/00 , A61P11/06 , A61P25/28
CPC分类号: C07D495/04 , C07D519/00
摘要: Piperidinodihydrothienopyrimidines of formula 1 wherein X is SO or SO2 (preferably SO), and R1, R2, R3, and R4 may have the meanings given in the disclosure and claims, pharmacologically acceptable salts thereof, and pharmaceutical compositions containing these compounds. These piperidinodihydrothienopyrimidines 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.
摘要翻译: 其中X为SO或SO 2(优选为SO)的R1为吡啶并二氢噻吩并嘧啶,R1,R2,R3和R4可具有本公开和权利要求书中给出的含义,其药理学上可接受的盐,以及含有这些化合物的药物组合物。 这些哌啶二氢噻吩并嘧啶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,外周或中枢神经系统疾病或癌症。
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公开(公告)号:US08486948B2
公开(公告)日:2013-07-16
申请号:US12738425
申请日:2008-10-16
申请人: Pascale Pouzet , Christoph Hoenke , Peter Nickolaus , Rolf Goeggel , Thomas Fox , Dennis Fiegen , Klaus Klinder
发明人: Pascale Pouzet , Christoph Hoenke , Peter Nickolaus , Rolf Goeggel , Thomas Fox , Dennis Fiegen , Klaus Klinder
IPC分类号: C07D495/04 , A61K31/519 , A61P25/28 , A61P25/24 , A61P25/22 , A61P29/00 , A61P11/06
CPC分类号: C07D495/04 , C07D519/00 , A61K31/519 , A61K2300/00
摘要: The invention relates to the novel dihydrothienopyrimidine sulfoxides of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO2, preferably however SO, and wherein R3, R4, R4′, R5, R6 and R7 are defined as in claim 1. The invention also relates to pharmaceutical compositions containing said compounds. The novel dihydrothienopyrimidine sulfoxides are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers.
摘要翻译: 本发明涉及式(I)的新型二氢噻吩并嘧啶亚砜及其药学上可接受的盐,其中X表示SO或SO 2,优选SO,其中R 3,R 4,R 4',R 5,R 6和R 7定义如 本发明还涉及含有所述化合物的药物组合物。 新型二氢噻吩并嘧啶亚砜适用于治疗呼吸道或胃肠疾病或疾病,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。
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公开(公告)号:US20110046096A1
公开(公告)日:2011-02-24
申请号:US12738425
申请日:2008-10-16
申请人: Pascale Pouzet , Christoph Hoenke , Peter Nickolaus , Rolf Goeggel , Thomas Fox , Dennis Fiegen , Klaus Klinder
发明人: Pascale Pouzet , Christoph Hoenke , Peter Nickolaus , Rolf Goeggel , Thomas Fox , Dennis Fiegen , Klaus Klinder
IPC分类号: A61K31/573 , C07D495/04 , A61K31/519 , C07D413/14 , A61K31/5377 , A61P25/00 , A61P29/00 , A61P1/00
CPC分类号: C07D495/04 , C07D519/00 , A61K31/519 , A61K2300/00
摘要: The invention relates to the novel dihydrothienopyrimidine sulfoxides of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO2, preferably however SO, and wherein R3, R4, R4′, R5, R6 and R7 are defined as in claim 1. The invention also relates to pharmaceutical compositions containing said compounds. The novel dihydrothienopyrimidine sulfoxides are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers.
摘要翻译: 本发明涉及式(I)的新型二氢噻吩并嘧啶亚砜及其药学上可接受的盐,其中X表示SO或SO 2,优选SO,其中R 3,R 4,R 4',R 5,R 6和R 7定义如 本发明还涉及含有所述化合物的药物组合物。 新型二氢噻吩并嘧啶亚砜适用于治疗呼吸道或胃肠疾病或疾病,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。
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公开(公告)号:US09115142B2
公开(公告)日:2015-08-25
申请号:US14134367
申请日:2013-12-19
申请人: Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
发明人: Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
IPC分类号: C07D495/04 , A61K31/519 , C07D519/00
CPC分类号: C07D495/04 , A61K31/519 , A61K2300/00
摘要: Dihydrothienopyrimidinesulphoxides of formula 1 wherein X is SO or SO2, R1 is H or C1-6-alkyl, R2 is H or an organic group as disclosed herein, and R3 is an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl, and the pharmacologically acceptable salts thereof, as well as pharmaceutical compositions which contain these compounds. These dihydrothienopyrimidinesulphoxides 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.
摘要翻译: 式1的二氢噻吩并嘧啶亚砜,其中X是SO或SO 2,R 1是H或C 1-6 - 烷基,R 2是H或如本文所公开的有机基团,并且R 3是任选取代的单或双环不饱和的,部分饱和的或饱和的 杂环或任选取代的单环或双环杂芳基及其药理学上可接受的盐,以及含有这些化合物的药物组合物。 这些二氢噻吩并嘧啶亚砜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,外周或中枢神经系统疾病或癌症。
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公开(公告)号:US09090626B2
公开(公告)日:2015-07-28
申请号:US13911712
申请日:2013-06-06
申请人: Pascale Pouzet , Christoph Hoenke , Peter Nickolaus , Rolf Goeggel , Thomas Fox , Dennis Fiegen , Klaus Klinder
发明人: Pascale Pouzet , Christoph Hoenke , Peter Nickolaus , Rolf Goeggel , Thomas Fox , Dennis Fiegen , Klaus Klinder
IPC分类号: C07D495/04 , A61K31/519 , C07D519/00
CPC分类号: C07D495/04 , C07D519/00 , A61K31/519 , A61K2300/00
摘要: A method for treating diseases associated with the inhibition of phosphodiesterase 4 (PDE4) enzyme in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a dihydrothienopyrimidinesulphoxide of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof
摘要翻译: 一种用于治疗与患者中磷酸二酯酶4(PDE4)酶的抑制有关的疾病的方法,包括向有需要的患者施用治疗有效量的式1的二氢噻吩并嘧啶亚砜,以及药理学上可接受的盐,非对映异构体,对映异构体,外消旋体 ,水合物或溶剂化物
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公开(公告)号:US08637519B2
公开(公告)日:2014-01-28
申请号:US12738429
申请日:2008-10-16
申请人: Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
发明人: Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
IPC分类号: C07D495/04 , A61K31/519 , A61P11/06 , A61P25/28 , A61P25/24 , A61P25/22 , A61P25/18 , A61P35/00
CPC分类号: C07D495/04 , A61K31/519 , A61K2300/00
摘要: Dihydrothienopyrimidinesulphoxides of formula 1 wherein X is SO or SO2, R1 is H or C1-6-alkyl, R2 is H or an organic group as disclosed herein, and R3 is an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl, and the pharmacologically acceptable salts thereof, as well as pharmaceutical compositions which contain these compounds. These dihydrothienopyrimidinesulphoxides 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.
摘要翻译: 式1的二氢噻吩并嘧啶亚砜,其中X是SO或SO 2,R 1是H或C 1-6 - 烷基,R 2是H或如本文所公开的有机基团,并且R 3是任选取代的单或双环不饱和的,部分饱和的或饱和的 杂环或任选取代的单环或双环杂芳基及其药理学上可接受的盐,以及含有这些化合物的药物组合物。 这些二氢噻吩并嘧啶亚砜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,外周或中枢神经系统疾病或癌症。
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公开(公告)号:US20110021501A1
公开(公告)日:2011-01-27
申请号:US12738344
申请日:2008-10-16
申请人: Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
发明人: Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
IPC分类号: A61K31/519 , C07D495/04 , A61K31/527 , A61K31/55 , A61K31/5377 , C07D498/10 , A61K31/5386 , A61P29/00 , A61P25/28 , A61P25/18 , A61P25/00
CPC分类号: C07D495/04 , C07D519/00
摘要: The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 may have the meanings given in claim 1, as well as pharmaceutical compositions which contain these compounds.These new piperidino-dihydrothienopyrimidines 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.
摘要翻译: 本发明涉及式1的新的哌啶子基 - 二氢噻吩并嘧啶,以及其药学上可接受的盐,其中X是SO或SO 2,但优选为SO,其中R 1,R 2,R 3和R 4可以具有权利要求1中给出的含义, 以及含有这些化合物的药物组合物。 这些新的哌啶子基 - 二氢噻吩并嘧啶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,外周或中枢神经系统或癌症的疾病。
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公开(公告)号:US20100305102A1
公开(公告)日:2010-12-02
申请号:US12738429
申请日:2008-10-16
申请人: Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
发明人: Pascale Pouzet , Ralf Anderskewitz , Horst Dollinger , Dennis Fiegen , Thomas Fox , Rolf Goeggel , Christoph Hoenke , Domnic Martyres , Peter Nickolaus , Klaus Klinder
IPC分类号: A61K31/519 , C07D495/04 , A61K31/55 , A61P29/00 , A61P25/00 , A61P25/28 , A61P25/16 , A61P25/22 , A61P25/24 , A61P1/00 , A61P7/00
CPC分类号: C07D495/04 , A61K31/519 , A61K2300/00
摘要: The invention relates to new dihydrothienopyrimidinesulphoxides of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl and wherein R1 and R2 have the meanings stated in claim 1, as well as pharmaceutical compositions which contain these compounds. These new dihydrothienopyrimidinesulphoxides 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.
摘要翻译: 本发明涉及式1的新的二氢噻吩并嘧啶亚砜,以及其药学上可接受的盐,其中X是SO或SO 2,但优选为SO,其中R 3表示任选取代的单或双环不饱和,部分饱和或饱和的杂环或 任选取代的单环或双环杂芳基,其中R1和R2具有权利要求1所述的含义,以及含有这些化合物的药物组合物。 这些新的二氢噻吩并嘧啶亚砜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,外周或中枢神经系统或癌症的疾病。
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10.
公开(公告)号:US20080096882A1
公开(公告)日:2008-04-24
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: A61K31/496 , A61K31/5377 , A61P11/00 , A61P25/00 , A61P29/00 , C07D413/14 , C07D495/04
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,水合物或溶剂合物,其中X是SO或SO 2,但优选SO,其中R R 1,R 2和R 3具有说明书中给出的含义,适用于治疗呼吸道或胃肠道疾病或疾病 ,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。
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