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![Substituted pyrido [3′, 2′: 4, 5] thieno [3, 2-D] pyrimidines and pyrido [3′, 2′: 4, 5] furo [3, 2-D] pyrimidines used as inhibitors of the PDE-4 and/or the release of TNF-ALPHA](/abs-image/US/2011/11/15/US08058285B2/abs.jpg.150x150.jpg)
1.发明授权Substituted pyrido [3′, 2′: 4, 5] thieno [3, 2-D] pyrimidines and pyrido [3′, 2′: 4, 5] furo [3, 2-D] pyrimidines used as inhibitors of the PDE-4 and/or the release of TNF-ALPHA 有权用作PDE抑制剂的取代的吡啶并[3'，2'：4,5]噻吩并[3,2-D]嘧啶和吡啶并[3'，2'：4,5]呋喃并[3,2-D]嘧啶 -4和/或TNF-ALPHA的释放公开(公告)号：US08058285B2
公开(公告)日：2011-11-15
申请号：US11625691
申请日：2007-01-22
申请人： Claudia Reichelt , Alexander Ludwig , Alexander Schulze , Mohammed Daghish , Siegfried Leistner , Andreas Krödel , Jochen Heinicke
发明人： Claudia Reichelt , Alexander Ludwig , Alexander Schulze , Mohammed Daghish , Siegfried Leistner , Andreas Krödel , Jochen Heinicke
IPC分类号： A61K31/505
CPC分类号： C07D491/14 , C07D495/14
摘要： The invention relates to compounds of general formula (I); 1a, 1 b, 1 c and 1 d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNFα-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes.
摘要翻译： 本发明涉及通式（I）的化合物; 1a，1b，1c和1d。 本发明还涉及其制备方法，含有可由其制备和/或溶剂合物的所述化合物和/或其生理相容性盐的药物制剂，以及所述化合物，其盐或溶剂合物作为抑制剂的药物用途 磷酸二酯酶4.该化合物包括用于治疗可通过抑制磷酸二酯酶4和/或TNFα释放的活性而具有阳性影响的疾病的活性成分，例如在淋巴细胞，嗜酸性粒细胞和嗜碱粒细胞，巨噬细胞和肥大细胞中。
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2.发明授权Polycyclic pyrimidine -2,4(1H,3H)-diones with functionalized alkyl residues at the 1- and/or 3-position(s); methods for their synthesis and pharmaceutical preparation 失效在1位和/或3位有官能化烷基残基的多环嘧啶-2,4（1H，3H） - 二酮; 其合成和药物制备方法公开(公告)号：US06872727B1
公开(公告)日：2005-03-29
申请号：US09830518
申请日：2000-08-21
IPC分类号： C07D239/96 , C07D495/04 , A61K31/517
CPC分类号： C07D495/04 , C07D239/96
摘要： Polycyclic pyrimidine-2,4(1H,3H)-diones with functionalized alkyl residues at the 1-, the 3-, or both position(s); methods for their synthesis, production, and pharmaceutical preparation. The invention concerns the synthesis of the above-described compounds, their chemical and structural characterization, and the analysis of their physiological/pharmacological activities in vitro and in vivo. These goals have been attained by the specification of routes of synthesis, methods for the production of the compounds, and the presentation of compound-specific characteristics. The substances encompassed by the present invention demonstrate pharmacologically significant collangenase/matrix metalloproteinase inhibitory activities. The specific example 1-(3-mercaptoprop-1-yl)-3-methyl-chinazolin-2,4(1H,3H)-dione will be presented in detail.
摘要翻译： 在1-，3-或两个位置具有官能化烷基残基的多环嘧啶-2,4（1H，3H） - 二酮; 其合成，生产和药物制备方法。 本发明涉及上述化合物的合成，其化学和结构表征以及其体外和体内其生理/药理学活性的分析。 这些目标已经通过合成路线的说明，化合物的制备方法和化合物特异性的表现来实现。 本发明包括的物质显示药理学上显着的胆碱酯酶/基质金属蛋白酶抑制活性。 将详细给出具体实施例1-（3-巯基丙-1-基）-3-甲基 - 唑烷-2,4（1H，3H） - 二酮。
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公开(公告)号：US5306721A
公开(公告)日：1994-04-26
申请号：US101269
申请日：1993-08-02
申请人： Siegfried Leistner , Michael Gutschow , Karl Drossler , Helmut Vieweg , Gunther Wagner , Thomas Strohscheidt , Dieter Lohmann , Gunter Laban , Herwart Ambrosius , Angela Siegling
发明人： Siegfried Leistner , Michael Gutschow , Karl Drossler , Helmut Vieweg , Gunther Wagner , Thomas Strohscheidt , Dieter Lohmann , Gunter Laban , Herwart Ambrosius , Angela Siegling
IPC分类号： C07D239/96 , A61K31/505
CPC分类号： C07D239/96
摘要： A compound or its tautomer of Formula I, ##STR1## wherein R.sup.1 is hydrogen, a 6-methyl, 6-fluoro, 6-chloro, 6-bromo, or 6,7-dimethoxy residue,R.sup.2 is hydrogen, or a methyl residue,and n is 1 or 2,and tautomers and their pharmaceutically acceptable alkali, or ammonium salts.
摘要翻译： 式I的化合物或其互变异构体，其中R 1是氢，6-甲基，6-氟，6-氯，6-溴或者6,7-二甲氧基残基，R 2是氢或 甲基残基，n为1或2，以及互变异构体及其药学上可接受的碱金属盐或铵盐。
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![SUBSTITUTED PYRIDO [3', 2': 4, 5] THIENO [3, 2-D] PYRIMIDINES AND PYRIDO [3', 2': 4, 5] FURO [3, 2-D] PYRIMIDINES USED AS INHIBITORS OF THE PDE-4 AND/OR THE RELEASE OF TNF-alpha](/abs-image/US/2012/04/19/US20120094987A1/abs.jpg.150x150.jpg)
4.发明申请SUBSTITUTED PYRIDO [3', 2': 4, 5] THIENO [3, 2-D] PYRIMIDINES AND PYRIDO [3', 2': 4, 5] FURO [3, 2-D] PYRIMIDINES USED AS INHIBITORS OF THE PDE-4 AND/OR THE RELEASE OF TNF-alpha 审中-公开取代的吡啶[3'，2'：4,5]噻吩[3,2-D]吡嗪并吡啶并[3'，2'：4,5]用作PDE的抑制剂的呋喃并[3,2-D] -4和/或释放TNF-α公开(公告)号：US20120094987A1
公开(公告)日：2012-04-19
申请号：US13251351
申请日：2011-10-03
申请人： Claudia Reichelt , Alexander Ludwig , Alexander Schulze , Mohammed Daghish , Siegfried Leistner , Andreas Krödel , Jochen Heinicke
发明人： Claudia Reichelt , Alexander Ludwig , Alexander Schulze , Mohammed Daghish , Siegfried Leistner , Andreas Krödel , Jochen Heinicke
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/519 , A61P11/06 , A61P11/00 , A61P19/02 , A61P1/00 , A61P17/00 , A61P37/08 , A61P3/10 , A61P25/28 , A61P25/16 , A61P9/00 , A61P9/10 , A61P35/00 , A61P31/12 , A61P35/02 , C07D495/14
CPC分类号： C07D491/14 , C07D495/14
摘要： The invention relates to compounds of general formula (I); 1a, 1b, 1c and 1d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNFα-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes.
摘要翻译： 本发明涉及通式（I）的化合物; 1a，1b，1c和1d。 本发明还涉及其制备方法，含有可由其制备和/或溶剂合物的所述化合物和/或其生理相容性盐的药物制剂以及所述化合物，其盐或溶剂合物作为抑制剂的药物用途 磷酸二酯酶4.该化合物包括用于治疗可通过抑制磷酸二酯酶4和/或TNFα释放的活性而具有阳性影响的疾病的活性成分，例如在淋巴细胞，嗜酸性粒细胞和嗜碱粒细胞，巨噬细胞和肥大细胞中。
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![SUBSTITUTED PYRIDO [3', 2': 4, 5] THIENO [3, 2-D] PYRIMIDINES AND PYRIDO [3', 2': 4, 5] FURO [3, 2-D] PYRIMIDINES USED AS INHIBITORS OF THE PDE-4 AND/OR THE RELEASE OF TNF-ALPHA](/abs-image/US/2008/07/03/US20080160028A1/abs.jpg.150x150.jpg)
5.发明申请SUBSTITUTED PYRIDO [3', 2': 4, 5] THIENO [3, 2-D] PYRIMIDINES AND PYRIDO [3', 2': 4, 5] FURO [3, 2-D] PYRIMIDINES USED AS INHIBITORS OF THE PDE-4 AND/OR THE RELEASE OF TNF-ALPHA 有权取代的吡啶[3'，2'：4,5]噻吩[3,2-D]吡嗪并吡啶并[3'，2'：4,5]用作PDE的抑制剂的呋喃并[3,2-D] -4和/或释放TNF-α公开(公告)号：US20080160028A1
公开(公告)日：2008-07-03
申请号：US11625691
申请日：2007-01-22
申请人： Claudia Reichelt , Alexander Ludwig , Alexander Schulze , Mohammed Daghish , Siegfried Leistner , Andreas Krodel , Jochen Heinicke
发明人： Claudia Reichelt , Alexander Ludwig , Alexander Schulze , Mohammed Daghish , Siegfried Leistner , Andreas Krodel , Jochen Heinicke
IPC分类号： A61K31/519 , C07D495/14 , A61K31/5377 , C07D495/22 , A61K31/541 , A61P11/00 , A61P17/00 , A61P25/00 , A61P9/00 , A61P31/12 , A61K39/395 , A61P35/02
CPC分类号： C07D491/14 , C07D495/14
摘要： The invention relates to compounds of general formula (I); 1a, 1 b, 1 c and 1 d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNFα-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes.
摘要翻译： 本发明涉及通式（I）的化合物; 1a，1b，1c和1d。 本发明还涉及其制备方法，含有可由其制备和/或溶剂合物的所述化合物和/或其生理相容性盐的药物制剂以及所述化合物，其盐或溶剂合物作为抑制剂的药物用途 磷酸二酯酶4.化合物包括用于治疗可以通过抑制磷酸二酯酶4和/或TNFα释放的活性而具有积极影响的疾病的活性成分，例如在淋巴细胞，嗜酸性粒细胞和嗜碱粒细胞，巨噬细胞和肥大细胞中。
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