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71.发明授权Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions 有权二氢蝶啶酮，其制备方法及其作为药物组合物的用途公开(公告)号：US07371753B2
公开(公告)日：2008-05-13
申请号：US11211783
申请日：2005-08-25
申请人： Heinz Stadtmueller , Harald Engelhardt , Andreas Schoop , Martin Steegmaier , Matthias Hoffmann , Matthias Grauert
发明人： Heinz Stadtmueller , Harald Engelhardt , Andreas Schoop , Martin Steegmaier , Matthias Hoffmann , Matthias Grauert
IPC分类号： A61K31/5025 , A61K31/496 , A61K31/551 , A61K31/5355 , C07D237/20 , C07D237/22 , C07D239/10 , C07D241/18 , C07D243/08 , C07D413/12 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D211/74 , C07D211/72 , C07D211/84 , C07D211/86 , C07D213/73 , C07D213/76 , C07D213/22
CPC分类号： C07D475/04
摘要： Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.
摘要翻译： 公开了通式（I）的新的二氢蝶啶酮，其中基团R 1至R 5，R a至R c， SUP，W，Q 1和Q 2具有权利要求书和说明书中给出的含义，其异构体及其用于制备治疗药物组合物的用途 以细胞增殖过度或异常为特征的疾病。
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公开(公告)号：US20070238730A1
公开(公告)日：2007-10-11
申请号：US11690356
申请日：2007-03-23
申请人： Steffen Breitfelder , Udo Maier , Christoph Hoenke , Anne Joergensen , Alexander Pautsch , Trixi Brandl , Matthias Grauert , Matthias Hoffmann , Stefan Scheuerer , Klaus Erb , Michael Pieper , Ingo Pragst
发明人： Steffen Breitfelder , Udo Maier , Christoph Hoenke , Anne Joergensen , Alexander Pautsch , Trixi Brandl , Matthias Grauert , Matthias Hoffmann , Stefan Scheuerer , Klaus Erb , Michael Pieper , Ingo Pragst
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/43 , C07D498/02
CPC分类号： C07D513/04
摘要： Disclosed are compounds of general formula (I), wherein the groups R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-cyclopentapyrazoles and the use thereof as pharmaceutical compositions.
摘要翻译： 公开了通式（I）的化合物，其中基团R 1，R 2，R a和R b， SUP>具有权利要求书和说明书中给出的含义，互变异构体，外消旋物，对映异构体，非对映异构体及其混合物，以及任选的药理学上可接受的酸加成盐，溶剂合物和水合物，以及制备这些噻唑基 - 二氢环戊吡唑和 其作为药物组合物的用途。
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73.发明申请SPECIFIC SALT, ANHYDROUS AND CRYSTALLINE FORM OF A DIHYDROPTERIDIONE DERIVATIVE 有权二盐酸盐衍生物的特殊盐，无机和结晶形式公开(公告)号：US20070203146A1
公开(公告)日：2007-08-30
申请号：US11668681
申请日：2007-01-30
申请人： Guenter Linz , Peter Sieger , Matthias Grauert , Rolf Schmid
发明人： Guenter Linz , Peter Sieger , Matthias Grauert , Rolf Schmid
IPC分类号： A61K31/525 , C07D475/08
CPC分类号： C07D475/00
摘要： The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallisation in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.
摘要翻译： 本发明涉及二氢二萜二酮衍生物的具体盐，即化合物N- [反式-4- [4-（环丙基甲基）-1-哌嗪基]环己基] -4 - [[（7R）-7 - 乙基-5,6,7,8-四氢-5-甲基-8-（1-甲基乙基）-6-氧代-2-吖啶基]氨基] -3-甲氧基 - 苯甲酰胺，其结晶形式为 水合物，其制备方法及其在药物组合物中的用途。
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公开(公告)号：US07241769B2
公开(公告)日：2007-07-10
申请号：US11132091
申请日：2005-05-18
申请人： Heinz Stadtmueller , Harald Engelhardt , Ulrich Reiser , Stephan Karl Zahn , Rudolf Hauptmann , Martin Steegmaier , Ulrich Guertler , Matthias Hoffmann , Matthias Grauert
发明人： Heinz Stadtmueller , Harald Engelhardt , Ulrich Reiser , Stephan Karl Zahn , Rudolf Hauptmann , Martin Steegmaier , Ulrich Guertler , Matthias Hoffmann , Matthias Grauert
IPC分类号： C07D239/42 , C07D239/46 , A61K31/505 , A61P35/00
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12
摘要： The present invention comprises compounds of general formula (1) wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.
摘要翻译： 本发明包括通式（1）的化合物，其中A，X，Y，Z，R a，O，R b，R c， R 1，R 2和R 3定义如权利要求1所述，其适用于治疗以过度或异常细胞为特征的疾病 增殖及其用于制备具有上述性质的药物组合物的用途。
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75.发明授权公开(公告)号：US07094788B2
公开(公告)日：2006-08-22
申请号：US10396147
申请日：2003-03-25
IPC分类号： C07D31/403 , C07D221/22 , C07D471/08 , C07D471/10 , C07D409/10
CPC分类号： C07D451/02 , A61K31/46 , A61K45/06
摘要： The present invention relates to new compounds of general formula 1 wherein X− and the groups A, B, R, R1, R2, R3, R3′, R4, R4′, Rx and Rx′ may have the meanings given in the claims and in the specification, processes for preparing them and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及通式1的新化合物，其中X，O和A，B，R，R 1，R 2， R 3，R 3，R 4，R 4，R 4，R 12， >和R“X”可以具有权利要求书和说明书中给出的含义，其制备方法及其作为药物组合物的用途。
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76.发明申请公开(公告)号：US20060058344A1
公开(公告)日：2006-03-16
申请号：US11270303
申请日：2005-11-09
IPC分类号： A61K31/46
CPC分类号： C07D451/02 , A61K31/46 , A61K45/06
摘要： The present invention relates to new compounds of general formula 1 wherein X− and the groups A, B, R, R1, R2, R3, R3′, R4, R4′, Rx and Rx′ may have the meanings given in the claims and in the specification, processes for preparing them and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及通式1的新化合物
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77.发明申请New dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions 有权新的二氢蝶啶酮，其制备方法及其作为药物组合物的用途公开(公告)号：US20060046990A1
公开(公告)日：2006-03-02
申请号：US11211783
申请日：2005-08-25
申请人： Heinz Stadtmueller , Harald Engelhardt , Andreas Schoop , Martin Steegmaier , Matthias Hoffmann , Matthias Grauert
发明人： Heinz Stadtmueller , Harald Engelhardt , Andreas Schoop , Martin Steegmaier , Matthias Hoffmann , Matthias Grauert
IPC分类号： A61K31/525 , C07D475/04
CPC分类号： C07D475/04
摘要： Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.
摘要翻译： 公开了通式（I）的新的二氢蝶啶酮，其中基团R 1至R 5，R a至R c， SUP，W，Q 1和Q 2具有权利要求书和说明书中给出的含义，其异构体及其用于制备治疗药物组合物的用途 以细胞增殖过度或异常为特征的疾病。
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78.发明申请New pyridodihydropyrazinones, process for their manufacture and use thereof as medicaments 有权新的吡啶二氢吡嗪酮，其制备方法和用途作为药物公开(公告)号：US20060009457A1
公开(公告)日：2006-01-12
申请号：US11176737
申请日：2005-07-07
IPC分类号： A61K31/498 , C07D487/02
CPC分类号： C07D471/04
摘要： Disclosed are pyridodihydropyrazinone compounds, processes for preparing them and their use as pharmaceutical compositions. The compounds according to the invention correspond to general formula (I), while the groups L, R1, R2, R3, R4 and R5 may have the meanings given in the claims and specification.
摘要翻译： 公开了吡啶二氢吡嗪酮化合物，其制备方法及其作为药物组合物的用途。 根据本发明的化合物对应于通式（I），而基团L，R 1，R 2，R 3，R “4”和“5”可以具有权利要求书和说明书中给出的含义。
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79.发明申请Intermediate compounds for making dihydropteridinones useful as pharmaceutical compositions 审中-公开用作制备二氢蝶啶酮的中间体化合物，可用作药物组合物公开(公告)号：US20050014761A1
公开(公告)日：2005-01-20
申请号：US10909008
申请日：2004-07-30
申请人： Matthias Hoffmann , Matthias Grauert , Trixi Brandl , Steffen Breitfelder , Christian Eickmeier , Martin Steegmaier , Gisela Schnapp , Anke Baum , Jens Quant , Flavio Solca , Florian Colbatzky
发明人： Matthias Hoffmann , Matthias Grauert , Trixi Brandl , Steffen Breitfelder , Christian Eickmeier , Martin Steegmaier , Gisela Schnapp , Anke Baum , Jens Quant , Flavio Solca , Florian Colbatzky
IPC分类号： A61P35/00 , C07D475/00 , C07D519/00 , A61K31/525 , C07D475/02
CPC分类号： C07D295/073 , C07D475/00
摘要： Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.
摘要翻译： 公开了通式（I）的新的二氢蝶啶酮，其中基团L和R 1 -R 5具有权利要求书和说明书中给出的含义，其异构体，制备这些二氢蝶呤的中间体和方法及其用途 药物组合物。
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80.发明授权2,3,3a,4,9,9a-hexahydro-8-hydroxy-1H-benz[f]indoles, processes for preparing them and their use as pharmaceutical compositions 有权2,3,3a，4,9,9a-六氢-8-羟基-1H-苯并[f]吲哚，其制备方法及其作为药物组合物的用途
公开(公告)号：US06051583A
公开(公告)日：2000-04-18
申请号：US365064
申请日：1999-07-30
申请人： Matthias Grauert , Christoph Hoenke , Adrian Carter , Wolf-Dietrich Bechtel , Thomas Weiser , Rainer Palluk , Uwe Pschorn
发明人： Matthias Grauert , Christoph Hoenke , Adrian Carter , Wolf-Dietrich Bechtel , Thomas Weiser , Rainer Palluk , Uwe Pschorn
IPC分类号： A61K31/403 , A61P3/08 , A61P9/00 , A61P9/06 , A61P9/10 , A61P11/00 , A61P23/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P43/00 , C07D209/60 , A61K31/40 , C07D209/56 , C07D215/00 , C07D215/16 , C07D401/00
CPC分类号： C07D209/60
摘要： The present invention relates to new substituted 2,3,3a,4,9,9a-hexahydro-8-hydroxy-1H-benz[f]indole derivatives, processes for preparing them and their use as pharmaceutical compositions. The indole derivatives according to the invention correspond to general formula 1:
摘要翻译： 本发明涉及新的取代的2,3,3a，4,9,9a-六氢-8-羟基-1H-苯并[f]吲哚衍生物，其制备方法及其作为药物组合物的用途。 根据本发明的吲哚衍生物对应于通式1：
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