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31.发明申请Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein 有权制备吡喃葡萄糖基取代的苄基苯衍生物及其中间体的方法公开(公告)号：US20060258749A1
公开(公告)日：2006-11-16
申请号：US11416683
申请日：2006-05-03
申请人： Matthias Eckhardt , Frank Himmelsbach , Xiao-jun Wang , Wenjun Tang , Xiufeng Sun , Li Zhang , Dhileepkumar Krishnamurthy , Christopher Senanayake , Zhengxu Han
发明人： Matthias Eckhardt , Frank Himmelsbach , Xiao-jun Wang , Wenjun Tang , Xiufeng Sun , Li Zhang , Dhileepkumar Krishnamurthy , Christopher Senanayake , Zhengxu Han
IPC分类号： A61K31/135
CPC分类号： C07D407/12 , C07D309/10 , C07F1/02 , C07F3/02 , C07H15/04 , C07H15/203 , C07H19/01
摘要： The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1 and R3 are defined according to claim 1. Furthermore this inventions relates to intermediates obtained in these processes.
摘要翻译： 本发明涉及制备通式I化合物的方法，其中R 1和R 3基团根据权利要求1定义。此外，本发明涉及中间体 在这些过程中获得。
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公开(公告)号：US07119084B2
公开(公告)日：2006-10-10
申请号：US11083247
申请日：2005-03-17
申请人： Frank Himmelsbach , Birgit Jung , Flavio Solca
发明人： Frank Himmelsbach , Birgit Jung , Flavio Solca
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.
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33.发明申请Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions 审中-公开黄嘌呤衍生物，其制备及其作为药物组合物的用途公开(公告)号：US20060205711A1
公开(公告)日：2006-09-14
申请号：US11419756
申请日：2006-05-22
申请人： Frank Himmelsbach , Michael Mark , Matthias Eckhardt , Elke Langkopf , Roland Maier , Ralf Lotz
发明人： Frank Himmelsbach , Michael Mark , Matthias Eckhardt , Elke Langkopf , Roland Maier , Ralf Lotz
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/522 , C07D473/02
CPC分类号： C07D473/08 , C07D473/04 , C07D473/06 , C07D473/10 , C07D473/12
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs 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 4定义如权利要求1，互变异构体及其立体异构体，其混合物，前药和 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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34.发明申请D-xylopyranosyl-phenyl-substituted cycles, medicaments containing such compounds, their use and process for their manufacture 审中-公开D-吡喃木糖基 - 苯基取代的周期，含有这些化合物的药物，它们的用途和制造方法公开(公告)号：US20060035841A1
公开(公告)日：2006-02-16
申请号：US11199962
申请日：2005-08-09
IPC分类号： C07H5/04 , A61K31/7052
CPC分类号： C07H7/04 , C07D309/10 , C07D405/12 , C07D407/10
摘要： A D-Xylopyranosyl-phenyl-substituted cycle compound of general formula I wherein the groups R1 to R6, Z, X, Cy and R7a, R7b and 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 - 苯基取代的环状化合物，其中基团R 1至R 6，Z，X，Cy和R 7a， 如权利要求1中所定义，R＆gt;和＆lt; 7＆gt; 7c＆gt;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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35.发明授权4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transduction mediated by tyrosine kinases 有权对酪氨酸激酶介导的信号转导具有抑制作用的4-氨基 - 喹唑啉和喹啉衍生物公开(公告)号：US06972288B1
公开(公告)日：2005-12-06
申请号：US09914323
申请日：2000-02-24
申请人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Thomas Metz , Flavio Solca , Stefan Blech
发明人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Thomas Metz , Flavio Solca , Stefan Blech
IPC分类号： A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/517 , A61P35/00 , C07D215/42 , C07D215/54 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12
CPC分类号： C07D401/12 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/517 , C07D215/54 , C07D239/94 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rd, A to G and X are defined as in claim 1, the tautomers, the steroisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, their use for treating diseases, particularly tumoral diseases, 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，其中R a至R d，A至G和X如权利要求1所定义，互变异构体，立体异构体和 其盐，特别是其具有有价值的药理学性质的无机或有机酸或碱的生理上可接受的盐，特别是对由酪氨酸激酶介导的信号转导的抑制作用，其用于治疗疾病，特别是肿瘤疾病，肺和呼吸道疾病 道及其制备。
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![8-[3-Amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical composition](/abs-image/US/2005/08/25/US20050187227A1/abs.jpg.150x150.jpg)
36.发明申请8-[3-Amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical composition 有权8- [3-氨基 - 哌啶-1-基] - 黄嘌呤，它们的制备及其作为药物组合物的用途公开(公告)号：US20050187227A1
公开(公告)日：2005-08-25
申请号：US11062518
申请日：2005-02-22
IPC分类号： A61K31/522 , C07D473/04 , C07D473/06
CPC分类号： C07D473/06
摘要： The present invention relates to substituted xanthines of general formula wherein R1 and R2 are defined as in the claims, the tautomers, the stereoisomers, 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： 本发明涉及以下通式的取代黄嘌呤：其中R 1和R 2如权利要求中所定义，互变异构体，立体异构体，其混合物和盐 其具有有价值的药理学特性，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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![8-(piperazin-1yl)- and 8-([1,4]diazepan-1yl)-xanthines, the preparation thereof and their use as pharmaceutical composition](/abs-image/US/2005/06/16/US20050130985A1/abs.jpg.150x150.jpg)
37.发明申请8-(piperazin-1yl)- and 8-([1,4]diazepan-1yl)-xanthines, the preparation thereof and their use as pharmaceutical composition 有权8-（哌嗪-1-基） - 和8 - （[1,4]二氮杂环庚烷-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：US20050130985A1
公开(公告)日：2005-06-16
申请号：US10979468
申请日：2004-11-02
IPC分类号： A61K31/522 , C07D473/04 , C07D519/00
CPC分类号： C07D519/00 , C07D473/04
摘要： The present invention relates to substituted xanthines of the general formula in which R1 to R3 and n are as defined in claims 1 to 8, their tautomers, their enantiomers, their diastereomers, their mixtures, their prodrugs and their salts, which have valuable pharmacological properties, in particular an inhibitory action on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的取代黄嘌呤，其中R 1至R 3和n如权利要求1至8中所定义，其互变异构体，其对映异构体，它们的对映异构体 非对映异构体，它们的混合物，它们的前药和它们的盐，其具有有价值的药理学特性，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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38.发明申请New imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions 有权新的咪唑并哒嗪酮和咪唑并吡喃酮衍生物，其制备及其作为药物组合物的用途公开(公告)号：US20050026921A1
公开(公告)日：2005-02-03
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： C07D471/04 , C07D487/04 , C07D519/00 , C07D471/02 , A61K31/4745 , C07D487/02
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， 其具有有价值的药理特性，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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公开(公告)号：US06617329B2
公开(公告)日：2003-09-09
申请号：US09938314
申请日：2001-08-23
申请人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
发明人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
IPC分类号： C07D23994
CPC分类号： C07D405/12 , A61K31/505 , A61K31/517 , C07D405/14 , C07D413/12 , C07D413/14
摘要： Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof.
摘要翻译： 该化合物对由酪氨酸激酶介导的信号转导具有抑制作用，其用于治疗疾病，特别是肿瘤疾病以及肺和空气疾病以及其制备。
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40.发明授权Amidine derivatives, the preparation and use thereof as medicaments with Itb4 antagonistic effect 有权脒衍生物，其制备和用途为具有Itb4拮抗作用的药物公开(公告)号：US06489365B1
公开(公告)日：2002-12-03
申请号：US09484073
申请日：2000-01-18
申请人： Ralf Anderskewitz , Kurt Schromm , Ernst-Otto Renth , Frank Himmelsbach , Franz Birke , Armin Fugner
发明人： Ralf Anderskewitz , Kurt Schromm , Ernst-Otto Renth , Frank Himmelsbach , Franz Birke , Armin Fugner
IPC分类号： A61K3124
CPC分类号： C07D213/78 , C07C257/18 , C07C317/18 , C07C317/22 , C07C317/44 , C07C323/20 , C07C323/62 , C07D307/79 , C07D311/22
摘要： Compounds of the formula which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.
摘要翻译： 在说明书中更全面地解释的制剂的化合物可以通过常规方法制备并在常规的盖伦制剂中治疗地使用。
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