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81.发明授权Glucopyranosyl-substituted benzene derivatives, medicaments containing such compounds, their use and process for their manufacture 有权吡喃葡萄糖基取代的苯衍生物，含有这些化合物的药物，它们的用途和制备方法公开(公告)号：US07687469B2
公开(公告)日：2010-03-30
申请号：US11304284
申请日：2005-12-15
IPC分类号： A61K31/7004 , C07H7/04
CPC分类号： C07H7/04
摘要： Glucopyranosyl-substituted benzene derivatives defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.
摘要翻译： 根据权利要求1所述的吡喃葡萄糖基取代的苯衍生物，包括互变异构体，其立体异构体，其混合物及其盐。 根据本发明的化合物适用于治疗代谢性疾病。
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82.发明授权Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions 有权咪唑并哒嗪酮和咪唑并吡酮衍生物，其制备及其作为药物组合物的用途公开(公告)号：US07566707B2
公开(公告)日：2009-07-28
申请号：US10865719
申请日：2004-06-10
申请人： Matthias Eckhardt , Norbert Hauel , Elke Langkopf , Frank Himmelsbach , Iris Kauffmann-Hefner , Mohammad Tadayyon , Michael Mark
发明人： Matthias Eckhardt , Norbert Hauel , Elke Langkopf , Frank Himmelsbach , Iris Kauffmann-Hefner , Mohammad Tadayyon , Michael Mark
IPC分类号： A61P7/12 , A61P3/04 , A61P19/00 , A61K31/55 , A61K31/553 , A61K31/554 , A61K31/54 , A61K31/535 , A61K31/495 , A61K31/50 , C07D223/00 , C07D273/00 , C07D285/00 , C07D243/00 , C07D267/00 , C07D281/00 , C07D291/00 , C07D498/00 , C07D513/00 , C07D515/00 , C07D487/00 , C07D491/00 , C07D279/00 , C07D265/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的取代的咪唑并 - 吡啶酮和咪唑并哒嗪酮，其中Y和R 1至R 4如权利要求1所定义，互变异构体，对映异构体，非对映异构体，其混合物及其盐具有有价值的药理学性质， 特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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83.发明授权8-(3-amino-piperidin-1-yl)-7-(but-2-ynyl)-xanthines, the preparation thereof and their use as pharmaceutical compositions 有权8-（3-氨基 - 哌啶-1-基）-7-（丁-2-炔基） - 黄嘌呤，其制备及其作为药物组合物的用途公开(公告)号：US07495003B2
公开(公告)日：2009-02-24
申请号：US11218057
申请日：2005-09-01
IPC分类号： C07D473/06 , C07D519/00 , C07D473/04 , A61K31/522 , A61P3/10
CPC分类号： C07D473/06 , C07D473/04
摘要： The application relates to new substituted xanthines of general formula wherein R1 and R2 are defined as in claims 1 to 11, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本申请涉及通式的新的取代黄嘌呤，其中R 1和R 2如权利要求1至11中所定义，互变异构体，对映异构体，非对映异构体，其混合物及其盐具有有价值的药理学性质，特别是抑制作用 关于酶二肽肽酶-IV（DPP-IV）的活性。
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84.发明申请Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them 有权双环杂环化合物，含有这些化合物的药物组合物，它们的用途和制备方法公开(公告)号：US20090036676A1
公开(公告)日：2009-02-05
申请号：US12072510
申请日：2008-02-26
申请人： Frank Himmelsbach , Birgit Jung , Flavio Solca
发明人： Frank Himmelsbach , Birgit Jung , Flavio Solca
IPC分类号： C07D413/14 , C07D239/72 , C07D401/02 , C07D413/02
CPC分类号： C07D401/12 , C07D239/94 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D491/08
摘要： The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula wherein said substituents are as defined herein.
摘要翻译： 本发明涉及用于治疗选自良性或恶性肿瘤，气道和肺疾病，胃肠道疾病，胆管和胆囊中的疾病的方法，通过给予有需要的患者 治疗有效量的通式的双环杂环基团，其中所述取代基如本文所定义。
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85.发明申请PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF RESPIRATORY AND GASTROINTESTINAL DISORDERS 审中-公开用于治疗呼吸道感染和胃肠疾病的药物组合物公开(公告)号：US20090017036A1
公开(公告)日：2009-01-15
申请号：US12202784
申请日：2008-09-02
申请人： Birgit Jung , Frank Himmelsbach
发明人： Birgit Jung , Frank Himmelsbach
IPC分类号： A61K39/395 , A61K31/4375 , A61K31/56 , A61P11/08 , A61P1/06 , A61P11/06 , A61K31/5377
CPC分类号： A61K31/47 , A61K31/4709 , A61K31/517 , A61K31/519 , A61K39/395 , A61K45/06 , A61K2300/00
摘要： The present invention relates to novel pharmaceutical compositions comprising at least one EGFR kinase inhibitor and at least one additional active compound selected from beta-2 mimetics, steroids, PDE-IV inhibitors, p38 MAP kinase inhibitors, NK1 antagonists and endothelin-antagonists, processes for preparing the compositions and the use thereof as medicament in the treatment of respiratory or gastrointestinal complaints, as well as inflammatory diseases of the joints, the skin or the eyes.
摘要翻译： 本发明涉及包含至少一种EGFR激酶抑制剂和至少一种选自β-2模拟物，类固醇，PDE-IV抑制剂，p38 MAP激酶抑制剂，NK1拮抗剂和内皮素 - 拮抗剂的其它活性化合物的新型药物组合物， 制备组合物及其用作治疗呼吸道或胃肠道疾病以及关节，皮肤或眼睛的炎性疾病的药物。
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![8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2008/08/05/US07407955B2/abs.jpg.150x150.jpg)
86.发明授权8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions 有权8- [3-氨基 - 哌啶-1-基] - 黄嘌呤，其制备及其作为药物组合物的用途公开(公告)号：US07407955B2
公开(公告)日：2008-08-05
申请号：US10639036
申请日：2003-08-12
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf R. H. Lotz , Mohammad Tadayyon
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf R. H. Lotz , Mohammad Tadayyon
IPC分类号： C07D473/06 , A61K31/52 , A61P3/10 , A61P19/02 , A61P3/04 , C07D519/00
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08 , C07D519/00
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及以下通式的取代黄嘌呤：其中R 1至R 3定义如权利要求1至16中所定义，互变异构体，立体异构体，混合物，前体药物 其具有有价值的药理学特性的盐，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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87.发明授权Imidazopyridazinediones, their preparation and their use as pharmaceutical compositions 有权咪唑并哒嗪酮，其制备及其作为药物组合物的用途公开(公告)号：US07393847B2
公开(公告)日：2008-07-01
申请号：US11075791
申请日：2005-03-09
申请人： Matthias Eckhardt , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
发明人： Matthias Eckhardt , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
IPC分类号： C07D487/04 , C07D471/04 , A61K31/5025
CPC分类号： C07D487/04
摘要： The invention relates to substituted imidazopyridazinediones of general formula wherein R1 and R4 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的取代咪唑并哒嗪酮，其中R 1和R 4定义如权利要求1，互变异构体，对映异构体，非对映异构体，其混合物和 其具有有价值的药理学性质，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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88.发明授权D-xylopyranosyl-substituted phenyl derivatives, medicaments containing such compounds, their use and process for their manufacture 有权D-吡喃木糖基取代的苯基衍生物，含有这些化合物的药物，它们的用途和制备方法公开(公告)号：US07393836B2
公开(公告)日：2008-07-01
申请号：US11168905
申请日：2005-06-28
摘要： A D-Xylopyranosyl-substituted phenyl compound of general formula I wherein the groups R1 to R5, X, Z and R7a, R7b, R7c are defined as in claim 1, have an inhibiting effect on the sodium-dependent glucose cotransporter SGLT. The present invention also relates to pharmaceutical compositions for the treatment of metabolic disorders.
摘要翻译： 通式I的D-吡喃葡萄糖基取代的苯基化合物，其中基团R 1至R 5，X，Z和R 7a，R 如权利要求1中所定义，R 7，R 7c对钠依赖性葡萄糖转运蛋白SGLT具有抑制作用。 本发明还涉及用于治疗代谢紊乱的药物组合物。
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89.发明申请Imidazopyridazinediones, Their Preparation And Their Use As Pharmaceutical Compositions 有权咪唑并哒嗪酮，其制备及其作为药物组合物的用途公开(公告)号：US20070142383A1
公开(公告)日：2007-06-21
申请号：US11676019
申请日：2007-02-16
申请人： Matthias Eckhardt , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
发明人： Matthias Eckhardt , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
IPC分类号： A61K31/503 , C07D487/02
CPC分类号： C07D487/04
摘要： The invention relates to substituted imidazopyridazinediones of general formula wherein R1 to R4 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的取代的咪唑并哒嗪酮，其中R 1至R 4定义如权利要求1，互变异构体，对映异构体，非对映异构体，其混合物和 其具有有价值的药理学性质，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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90.发明授权Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them 有权双环杂环，含有这些化合物的药物组合物，它们的用途和制备方法公开(公告)号：US07196091B2
公开(公告)日：2007-03-27
申请号：US10860453
申请日：2004-06-03
申请人： Frank Himmelsbach , Rainer Soyka , Birgit Jung
发明人： Frank Himmelsbach , Rainer Soyka , Birgit Jung
IPC分类号： A61K31/517 , C07D239/78
CPC分类号： C07D413/12 , C07D239/94
摘要： The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb, Rc, Rd, X and n are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibiting effect on the signal transduction mediated by tyrosine kinases, their use in treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract and the preparation thereof.
摘要翻译： 本发明涉及通式的双环杂环
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