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![5-oxo-2,3,4,5-tetrahydro-benzo[b]oxepine-4-carboxylic acid amides and 2,3-dihydro-benzo[b]oxepine-4-carboxylic acid amides for treatment and prevention of diabetes typ 1 and 2](/abs-image/US/2013/02/26/US08383838B2/abs.jpg.150x150.jpg)
1.发明授权5-oxo-2,3,4,5-tetrahydro-benzo[b]oxepine-4-carboxylic acid amides and 2,3-dihydro-benzo[b]oxepine-4-carboxylic acid amides for treatment and prevention of diabetes typ 1 and 2 有权5-氧代-2,3,4,5-四氢 - 苯并[b]氧杂七环素-4-羧酸酰胺和2,3-二氢 - 苯并[b]氧杂七环素-4-羧酸酰胺，用于治疗和预防糖尿病 1和2公开(公告)号：US08383838B2
公开(公告)日：2013-02-26
申请号：US12920362
申请日：2009-02-05
申请人： Christoph Saal , Lars Burgdorf , Ulrich Emde , Norbert Beier , Johannes Gleitz , Christine Charon
发明人： Christoph Saal , Lars Burgdorf , Ulrich Emde , Norbert Beier , Johannes Gleitz , Christine Charon
IPC分类号： C07D313/00
CPC分类号： C07D405/12 , C07D417/12
摘要： The present invention relates to novel compounds of general formula (I) and uses thereof.
摘要翻译： 本发明涉及通式（I）的新化合物及其用途。
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公开(公告)号：US08198452B2
公开(公告)日：2012-06-12
申请号：US12305524
申请日：2007-05-26
IPC分类号： C07D401/00 , A61K31/445
CPC分类号： C07D491/04
摘要： The invention relates to a process for the manufacture of enantiomerically enriched or pure compounds of formula I wherein R1, R2, R3, R6, R7 and Q are defined as in claim 1 as well as their crystalline forms for the treatment of proliferative diseases such as cancer.
摘要翻译： 本发明涉及制备对映体富集或纯化的式I化合物的方法，其中R 1，R 2，R 3，R 6，R 7和Q如权利要求1中所定义，以及它们用于治疗增殖性疾病如 癌症。
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公开(公告)号：US08383679B2
公开(公告)日：2013-02-26
申请号：US13120577
申请日：2009-08-25
申请人： Antje Ernst , Clemens Kuehn , Matthias Bartels , Christoph Saal , Nathalie Bosc
发明人： Antje Ernst , Clemens Kuehn , Matthias Bartels , Christoph Saal , Nathalie Bosc
IPC分类号： A01N37/00 , A61K31/185
CPC分类号： C07C309/15 , C07B2200/13
摘要： The present invention relates to a novel crystal form of calcium 3-acetylaminopropane-1-sulfonate, to a process for the preparation thereof, and to the use thereof in medicaments.
摘要翻译： 本发明涉及一种新型的3-乙酰氨基丙烷-1-磺酸钙结晶形式，其制备方法及其在药物中的应用。
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公开(公告)号：US20120065142A1
公开(公告)日：2012-03-15
申请号：US13321001
申请日：2010-05-20
申请人： Alfred Jonczyk , Clemens Kuehn , Kerstin Seemann , Christoph Saal , Gerald Scholz , Soenke Petersen , Harald Untenecker , Michael Lange
发明人： Alfred Jonczyk , Clemens Kuehn , Kerstin Seemann , Christoph Saal , Gerald Scholz , Soenke Petersen , Harald Untenecker , Michael Lange
摘要： The instant invention relates to novel solid materials of {[(2S,5R,8S,11S)-5-Benzyl-11-(3-guanidino-propyl)-8-isopropyl-7-methyl-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaaza-cyclopentadec-2-yl]-acetic acid}, methods for producing them, and the use of said solid materials in pharmaceuticals.
摘要翻译： 本发明涉及{[（2S，5R，8S，11S）-5-苄基-11-（3-胍基 - 丙基）-8-异丙基-7-甲基-3,6,9,12 ，15-五氧代-1,4,7,10,13-五氮杂 - 环戊烷-2-基] - 乙酸}，其制备方法和所述固体材料在药物中的用途。
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![Crystal form of (3-cyano-1H-Indo1-7-yl)-[4-(4-fluorophenethyl)piperazin-1-yl]methanone, hydrochloride](/abs-image/US/2011/07/19/US07981897B2/abs.jpg.150x150.jpg)
5.发明授权Crystal form of (3-cyano-1H-Indo1-7-yl)-[4-(4-fluorophenethyl)piperazin-1-yl]methanone, hydrochloride 失效（3-氰基-1H-吲哚-1-基） - [4-（4-氟苯乙基）哌嗪-1-基]甲酮，盐酸盐公开(公告)号：US07981897B2
公开(公告)日：2011-07-19
申请号：US11576086
申请日：2005-09-08
申请人： Andreas Bathe , Bernd Helfert , Ralf Knierieme , Christoph Saal , Ronald Keiner
发明人： Andreas Bathe , Bernd Helfert , Ralf Knierieme , Christoph Saal , Ronald Keiner
IPC分类号： A61K31/497 , C07D403/06
CPC分类号： C07D209/42
摘要： The present invention relates to a hitherto unknown crystal form B of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl)-piperazin-1-yl]methanone, hydrochloride, to a process for the preparation thereof, and to the use thereof for the preparation of a medicament.
摘要翻译： 本发明涉及迄今未知的（3-氰基-1H-吲哚-7-基） - [4-（4-氟苯乙基） - 哌嗪-1-基]甲酮盐酸盐的结晶形式B，用于 以及其用于制备药物的用途。
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![5-Oxo-2,3,4,5-tetrahydro-benzo[b]oxepine-4-carboxylic acid amides and 2,3-Dihydro-benzo[b]oxepine-4-carboxylic acid amides for treatment and prevention of Diabetes Typ 1 and 2](/abs-image/US/2011/01/13/US20110009455A1/abs.jpg.150x150.jpg)
6.发明申请5-Oxo-2,3,4,5-tetrahydro-benzo[b]oxepine-4-carboxylic acid amides and 2,3-Dihydro-benzo[b]oxepine-4-carboxylic acid amides for treatment and prevention of Diabetes Typ 1 and 2 有权5-氧代-2,3,4,5-四氢 - 苯并[b]氧杂七环素-4-羧酸酰胺和2,3-二氢 - 苯并[b]氧杂七环素-4-羧酸酰胺，用于治疗和预防糖尿病典型 1和2公开(公告)号：US20110009455A1
公开(公告)日：2011-01-13
申请号：US12920362
申请日：2009-02-05
申请人： Christoph Saal , Lars Burgdorf , Ulrich Emde , Norbert Beier , Johannes Gleitz , Christine Charon
发明人： Christoph Saal , Lars Burgdorf , Ulrich Emde , Norbert Beier , Johannes Gleitz , Christine Charon
IPC分类号： A61K31/4433 , C07D405/12 , C07D417/12 , A61K31/427 , A61P3/10 , A61P3/04 , A61P13/12
CPC分类号： C07D405/12 , C07D417/12
摘要： The present invention relates to novel compounds of general formula (I) and uses thereof.The present invention relates to novel compounds of general formula (I) for use as glucokinase activators in the treatment of diabetes and obesity.
摘要翻译： 本发明涉及通式（I）的新化合物及其用途。 本发明涉及用作糖尿病和肥胖症治疗中的葡糖激酶活化剂的通式（I）的新型化合物。
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公开(公告)号：US20110009437A1
公开(公告)日：2011-01-13
申请号：US12919627
申请日：2009-02-03
IPC分类号： A61K31/513 , C07D401/14 , C07D401/12 , C07D403/12 , C07D409/14 , A61K31/444 , A61K31/4439 , A61P3/10 , A61P3/04 , A61P13/12 , A61P25/00
CPC分类号： C07D401/12 , C07D401/14
摘要： Novel heterocyclic compounds of the formula I wherein D is wherein R1, R2, E′, E″, E′″, Y″, Y″, G′, G″, G′″ and G′″ have the meaning of claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.
摘要翻译： 式I的新型杂环化合物其中D是其中R 1，R 2，E'，E“，E”“，Y”，Y“，G'，G”，G“”和G'“具有权利要求1的含义 是葡萄糖激酶的活化剂，可用于预防和/或治疗1型和2型糖尿病，肥胖，神经病和/或肾病。
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![Polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof](/abs-image/US/2014/04/29/US08710058B2/abs.jpg.150x150.jpg)
8.发明授权Polymorphic forms of 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride salt and processes of manufacturing thereof 有权3-（1- {3- [5-（1-甲基 - 哌啶-4-基甲氧基） - 嘧啶-2-基] - 苄基} -6-氧代-1,6-二氢 - 哒嗪-3-基的多晶型形式 吡啶-3-基） - 苄腈盐酸盐及其制备方法公开(公告)号：US08710058B2
公开(公告)日：2014-04-29
申请号：US13143831
申请日：2009-12-04
申请人： Axel Becker , Clemens Kuehn , Christoph Saal , Oliver Schadt , Dieter Dorsch , Heinz Hermann Bokel , Frank Stieber , Cristina Donini
发明人： Axel Becker , Clemens Kuehn , Christoph Saal , Oliver Schadt , Dieter Dorsch , Heinz Hermann Bokel , Frank Stieber , Cristina Donini
IPC分类号： C07D401/14 , A61K31/501 , A61P35/00
CPC分类号： A61K31/506 , A61K31/517 , A61K45/06 , C07D401/14 , C07D403/10
摘要： Compounds of the present invention concern 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The compound, 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile, has the following structural formula: The hydrochloride solvates and crystalline modifications thereof according to the invention are useful for treatment of physiological and/or pathophysiological conditions, such as cancer, that are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, especially Met-kinase. The present invention further relates to processes of manufacturing these crystalline modifications.
摘要翻译： 本发明的化合物涉及3-（1- {3- [5-（1-甲基 - 哌啶-4-基甲氧基） - 嘧啶-2-基] - 苄基} -6-氧代-1,6-二氢 - 哒嗪 -3-基） - 苄腈盐酸盐溶剂合物及其结晶修饰物。 化合物3-（1- {3- [5-（1-甲基 - 哌啶-4-基甲氧基） - 嘧啶-2-基] - 苄基} -6-氧代-1,6-二氢 - 哒嗪-3-基] 基） - 苄腈具有以下结构式：根据本发明的盐酸盐溶剂合物及其结晶修饰物可用于治疗通过抑制引起，介导和/或增殖的生理和/或病理生理条件如癌症 ，调节和/或调节激酶的信号转导，特别是抑制酪氨酸激酶，特别是Met激酶。 本发明还涉及制造这些晶体改性的方法。
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9.发明申请Novel Polymorphic Forms of 3-(1--6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile Hydrochloride Salt and Processes of Manufacturing Thereof 有权3-（1-6-氧代-1,6-二氢 - 哒嗪-3-基） - 苄腈盐酸盐的新型多晶型及其制备方法公开(公告)号：US20110269767A1
公开(公告)日：2011-11-03
申请号：US13143831
申请日：2009-12-04
申请人： Axel Becker , Clemens Kuehn , Christoph Saal , Oliver Schadt , Dieter Dorsch , Heinz Hermann Bokel , Frank Stieber , Cristina Donini
发明人： Axel Becker , Clemens Kuehn , Christoph Saal , Oliver Schadt , Dieter Dorsch , Heinz Hermann Bokel , Frank Stieber , Cristina Donini
IPC分类号： A61K31/506 , A61P35/00 , A61P35/02 , C07D401/14
CPC分类号： A61K31/506 , A61K31/517 , A61K45/06 , C07D401/14 , C07D403/10
摘要： The present invention relates to 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile hydrochloride solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
摘要翻译： 本发明涉及3-（1- {3- [5-（1-甲基 - 哌啶-4-基甲氧基） - 嘧啶-2-基] - 苄基} -6-氧代-1,6-二氢 - 吡啶-3-基） - 苄腈盐酸盐溶剂合物及其结晶修饰物。 本发明进一步涉及制造这些结晶修饰的方法及其在治疗和/或预防生理和/或病理生理条件中的用途，其通过抑制，调节和/或调节引起，介导和/或传播 的激酶的信号转导，特别是通过抑制酪氨酸激酶，例如 病理生理条件如癌症。
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10.发明申请Novel Polymorphic Forms of 6-(1-methyl-1H-pyrazol-4-yl)-2--2H-pyridazin-3-one Dihydrogenphosphate and Processes of Manufacturing thereof 有权6-（1-甲基-1H-吡唑-4-基）-2-哒嗪-3-酮磷酸二氢盐的新型多晶型及其制造方法公开(公告)号：US20110257180A1
公开(公告)日：2011-10-20
申请号：US13141142
申请日：2009-11-24
申请人： Axel Becker , Clemens Kuehn , Christoph Saal , Oliver Schadt , Dieter Dorsch , Eva Kriegbaum , Frank Stieber , Cristina Donini
发明人： Axel Becker , Clemens Kuehn , Christoph Saal , Oliver Schadt , Dieter Dorsch , Eva Kriegbaum , Frank Stieber , Cristina Donini
IPC分类号： A61K31/5377 , A61P35/00 , C07D413/14
CPC分类号： C07D403/14
摘要： The present invention relates to 6-(1-methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one dihydrogenphosphate, its solvates and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
摘要翻译： 本发明涉及6-（1-甲基-1H-吡唑-4-基）-2- {3- [5-（2-吗啉-4-基 - 乙氧基） - 嘧啶-2-基] - 苄基} -2H-哒嗪-3-酮磷酸二氢盐，其溶剂合物及其结晶修饰物。 本发明进一步涉及制造这些结晶修饰的方法及其在治疗和/或预防生理和/或病理生理条件中的用途，其通过抑制，调节和/或调节引起，介导和/或传播 的激酶的信号转导，特别是通过抑制酪氨酸激酶，例如 病理生理条件如癌症。
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