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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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![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)
2.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)
3.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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![SUBSTITUTED 5H-PYRIMIDO[5,4-B]INDOLES, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF FOR TREATING NON-SOLID MALIGNANT TUMORS OF THE BLOOD-PRODUCING SYSTEM](/abs-image/US/2011/01/27/US20110021511A1/abs.jpg.150x150.jpg)
4.发明申请SUBSTITUTED 5H-PYRIMIDO[5,4-B]INDOLES, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF FOR TREATING NON-SOLID MALIGNANT TUMORS OF THE BLOOD-PRODUCING SYSTEM 失效取代的5H-吡啶并[5,4-B]吲哚，其生产方法及其用于治疗血液生成系统的非固体恶性肿瘤的用途公开(公告)号：US20110021511A1
公开(公告)日：2011-01-27
申请号：US12520480
申请日：2007-12-21
申请人： Claudia Reichelt , Alexander Schulze , Mohammed Daghish , Friedrich-Alexander Ludwig , Jochen Heinicke , Konrad Herrmann , Maj Schuster , Sven Letschert , Kenneth Mugridge , Joseph DeAngelo
发明人： Claudia Reichelt , Alexander Schulze , Mohammed Daghish , Friedrich-Alexander Ludwig , Jochen Heinicke , Konrad Herrmann , Maj Schuster , Sven Letschert , Kenneth Mugridge , Joseph DeAngelo
IPC分类号： C07D487/04 , A61P35/02 , A61K31/5377 , A61P35/04 , A61K31/496 , A61P35/00 , A61K31/541
CPC分类号： C07D487/04
摘要： The invention relates to compounds of general formula 1 to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts and/or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as inductors of apoptosis in the case of non-solid malignant tumors of the hematopoietic system, in particular in the case of leukemias and lymphomas, more particularly in the case of leukemic B lymphocytes.
摘要翻译： 本发明涉及通式1的化合物，其制备方法，含有所述化合物的药物制剂和/或可由其制备的生理上相容的盐和/或溶剂化物以及所述化合物的药物用途，所述盐 或在造血系统的非固体恶性肿瘤的情况下，特别是在白血病和淋巴瘤的情况下，更具体地在白血病B淋巴细胞的情况下，作为细胞凋亡的感应器。
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5.发明授权公开(公告)号：US08410310B2
公开(公告)日：2013-04-02
申请号：US13471007
申请日：2012-05-14
申请人： Torsten Steinmetzer , Andrea Schweinitz , Joerg Stuerzebecher , Peter Steinmetzer , Anett Soeffing , Andreas Van De Locht , Silke Nicklisch , Claudia Reichelt , Friedrich-Alexander Ludwig , Alexander Schulze , Mohammed Daghish , Jochen Heinicke
发明人： Torsten Steinmetzer , Andrea Schweinitz , Joerg Stuerzebecher , Peter Steinmetzer , Anett Soeffing , Andreas Van De Locht , Silke Nicklisch , Claudia Reichelt , Friedrich-Alexander Ludwig , Alexander Schulze , Mohammed Daghish , Jochen Heinicke
IPC分类号： C07D303/00
CPC分类号： C07D213/56 , C07D213/89 , C07D233/64 , C07K5/06078 , C07K5/06086
摘要： The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrein, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.
摘要翻译： 本发明涉及通式（I）的胰蛋白酶样丝氨酸蛋白酶的抑制剂，其中以及纤溶酶也抑制血浆激肽释放酶，以及它们作为药物的制备和用途，优选用于治疗失血，特别是在这种情况下 的超纤维蛋白溶解状态，在器官移植或心脏手术干预中，特别是与体外循环，或作为纤维蛋白粘合剂的组分。
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![Substituted 5H-pyrimido[5,4-B]indoles, method for the production thereof and use thereof for treating non-solid malignant tumors of the blood-producing system](/abs-image/US/2014/03/04/US08664233B2/abs.jpg.150x150.jpg)
6.发明授权Substituted 5H-pyrimido[5,4-B]indoles, method for the production thereof and use thereof for treating non-solid malignant tumors of the blood-producing system 失效取代的5H-嘧啶并[5,4-B]吲哚，其制备方法及其用于治疗产血系统的非固体恶性肿瘤公开(公告)号：US08664233B2
公开(公告)日：2014-03-04
申请号：US12520480
申请日：2007-12-21
申请人： Claudia Reichelt , Alexander Schulze , Mohammed Daghish , Friedrich-Alexander Ludwig , Jochen Heinicke , Konrad Herrmann , Maj Schuster , Sven Letschert , Kenneth Mugridge , Joseph DeAngelo
发明人： Claudia Reichelt , Alexander Schulze , Mohammed Daghish , Friedrich-Alexander Ludwig , Jochen Heinicke , Konrad Herrmann , Maj Schuster , Sven Letschert , Kenneth Mugridge , Joseph DeAngelo
IPC分类号： A01N43/54 , A61K31/505 , A01N43/38 , A61K31/40
CPC分类号： C07D487/04
摘要： The invention relates to compounds of general formula 1 to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts and/or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as inductors of apoptosis in the case of non-solid malignant tumors of the hematopoietic system, in particular in the case of leukemias and lymphomas, more particularly in the case of leukemic B lymphocytes.
摘要翻译： 本发明涉及通式1的化合物，其制备方法，含有所述化合物的药物制剂和/或可由其制备的生理上相容的盐和/或溶剂化物以及所述化合物的药物用途，所述盐 或在造血系统的非固体恶性肿瘤的情况下，特别是在白血病和淋巴瘤的情况下，更具体地在白血病B淋巴细胞的情况下，作为细胞凋亡的感应器。
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7.发明申请公开(公告)号：US20120225913A1
公开(公告)日：2012-09-06
申请号：US13471007
申请日：2012-05-14
申请人： Torsten STEINMETZER , Andrea Schweinitz , Joerg Stuerzebecher , Peter Steinmetzer , Anett Soeffing , Andreas Van De Locht , Silke Nicklisch , Claudia Reichelt , Friedrich-Alexander Ludwig , Alexander Schulze , Mohammed Daghisch , Jochen Heinicke
发明人： Torsten STEINMETZER , Andrea Schweinitz , Joerg Stuerzebecher , Peter Steinmetzer , Anett Soeffing , Andreas Van De Locht , Silke Nicklisch , Claudia Reichelt , Friedrich-Alexander Ludwig , Alexander Schulze , Mohammed Daghisch , Jochen Heinicke
IPC分类号： A61K31/195 , A61K31/196 , A61K31/4409 , A61P7/04 , A61K31/18 , A61K31/417
CPC分类号： C07D213/56 , C07D213/89 , C07D233/64 , C07K5/06078 , C07K5/06086
摘要： The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrein, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.
摘要翻译： 本发明涉及通式（I）的胰蛋白酶样丝氨酸蛋白酶的抑制剂，其中以及纤溶酶也抑制血浆激肽释放酶，以及它们作为药物的制备和用途，优选用于治疗失血，特别是在这种情况下 的超纤维蛋白溶解状态，在器官移植或心脏手术干预中，特别是与体外循环，或作为纤维蛋白粘合剂的组分。
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8.发明授权公开(公告)号：US08207378B2
公开(公告)日：2012-06-26
申请号：US12429766
申请日：2009-04-24
申请人： Torsten Steinmetzer , Andrea Schweinitz , Joerg Stuerzebecher , Peter Steinmetzer , Anett Soeffing , Andreas Van De Locht , Silke Nicklisch , Claudia Reichelt , Friedrich-Alexander Ludwig , Alexander Schulze , Mohammed Daghisch , Jochen Heinicke
发明人： Torsten Steinmetzer , Andrea Schweinitz , Joerg Stuerzebecher , Peter Steinmetzer , Anett Soeffing , Andreas Van De Locht , Silke Nicklisch , Claudia Reichelt , Friedrich-Alexander Ludwig , Alexander Schulze , Mohammed Daghisch , Jochen Heinicke
IPC分类号： C07C303/00
CPC分类号： C07D213/56 , C07D213/89 , C07D233/64 , C07K5/06078 , C07K5/06086
摘要： The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrien, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.
摘要翻译： 本发明涉及通式（I）的胰蛋白酶样丝氨酸蛋白酶的抑制剂，其中以及纤溶酶也抑制血浆激蛋白，以及它们作为药物的制备和用途，优选用于治疗失血，特别是在这种情况下 的超纤维蛋白溶解状态，在器官移植或心脏手术干预中，特别是与体外循环，或作为纤维蛋白粘合剂的组分。
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9.发明申请公开(公告)号：US20100022781A1
公开(公告)日：2010-01-28
申请号：US12429766
申请日：2009-04-24
申请人： Torsten Steinmetzer , Andrea Schweinitz , Joerg Stuerzebecher , Peter Steinmetzer , Anett Soffing , Andreas Van De Locht , Silke Nicklisch , Claudia Reichelt , Friedrich-Alexander Ludwig , Alexander Schulze , Mohammed Daghisch , Jochen Heinicke
发明人： Torsten Steinmetzer , Andrea Schweinitz , Joerg Stuerzebecher , Peter Steinmetzer , Anett Soffing , Andreas Van De Locht , Silke Nicklisch , Claudia Reichelt , Friedrich-Alexander Ludwig , Alexander Schulze , Mohammed Daghisch , Jochen Heinicke
IPC分类号： C07C311/13 , C07D233/64
CPC分类号： C07D213/56 , C07D213/89 , C07D233/64 , C07K5/06078 , C07K5/06086
摘要： The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrien, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.
摘要翻译： 本发明涉及通式（I）的胰蛋白酶样丝氨酸蛋白酶的抑制剂，其中以及纤溶酶也抑制血浆激蛋白，以及它们作为药物的制备和用途，优选用于治疗失血，特别是在这种情况下 的超纤维蛋白溶解状态，在器官移植或心脏手术干预中，特别是与体外循环，或作为纤维蛋白粘合剂的组分。
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