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公开(公告)号：US08420630B2
公开(公告)日：2013-04-16
申请号：US12711364
申请日：2010-02-24
申请人： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schnapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
发明人： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schnapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
IPC分类号： C07D239/48 , C07D403/12 , C07D401/12 , A61K31/506
CPC分类号： C07D239/48 , C07D231/12 , C07D233/56 , C07D239/50 , C07D239/80 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D451/04 , C07D451/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
摘要： The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterized by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
摘要翻译： 本发明涉及式（I）的三取代嘧啶，其中0Ra至Re如权利要求1所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，其用于制备具有上述药物组合物的用途 性质及其制备方法。
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2.发明授权公开(公告)号：US07166615B2
公开(公告)日：2007-01-23
申请号：US10646495
申请日：2003-08-22
申请人： Rainer Walter , Armin Heckel , Gerald Roth , Joerg Kley , Gisela Schnapp , Martin Lenter , Jacobus Van Meel , Walter Spevak , Ulrike Weyer-Czernilofsky
发明人： Rainer Walter , Armin Heckel , Gerald Roth , Joerg Kley , Gisela Schnapp , Martin Lenter , Jacobus Van Meel , Walter Spevak , Ulrike Weyer-Czernilofsky
IPC分类号： A61K31/4545 , C07D401/14
CPC分类号： C07D401/12 , C07D209/34 , C07D401/14 , C07D403/12 , C07D413/12
摘要： Indolinones of general formula I which are inhibitors of cell proliferation, particularly of tumor cells, and inhibitors of protein kinases.
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公开(公告)号：US06762180B1
公开(公告)日：2004-07-13
申请号：US09678682
申请日：2000-10-03
申请人： Gerald Juergen Roth , Armin Heckel , Rainer Walter , Jacobus Van Meel , Norbert Redemann , Ulrike Tontsch-Grunt , Walter Spevak , Frank Hilberg
发明人： Gerald Juergen Roth , Armin Heckel , Rainer Walter , Jacobus Van Meel , Norbert Redemann , Ulrike Tontsch-Grunt , Walter Spevak , Frank Hilberg
IPC分类号： C07D20934
CPC分类号： C07D231/12 , C07D209/30 , C07D209/34 , C07D233/56 , C07D249/08 , C07D403/12 , C07D405/12
摘要： Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
摘要翻译： 该公式的吲哚酮对受体酪氨酸激酶和细胞周期蛋白/ CDK复合物具有抑制作用，以及内皮细胞和各种肿瘤细胞的增殖。 示例是：（a）3-Z- [1-（4-（哌啶-1-基 - 甲基） - 苯胺基）-1-苯基 - 亚甲基] -6-乙氧基羰基-2-二氢吲哚酮，（b）3-Z - [（1-（4-（哌啶-1-基 - 甲基） - 苯胺基）-1-苯基 - 亚甲基] -6-氨甲酰基-2-二氢吲哚酮，和（c）3-Z- [1- （哌啶-1-基 - 甲基） - 苯胺基）-1-苯基 - 亚甲基] -6-甲基羰基-2-二氢吲哚酮。
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4.发明授权Substituted indolinones, preparation thereof and their use as pharmaceutical compositions 有权取代的吲哚啉酮，其制备及其作为药物组合物的用途公开(公告)号：US06638965B2
公开(公告)日：2003-10-28
申请号：US10002939
申请日：2001-11-01
申请人： Rainer Walter , Armin Heckel , Gerald Roth , Joerg Kley , Gisela Schnapp , Martin Lenter , Jacobus Van Meel , Walter Spevak , Ulrike Weyer-Czernilofsky
发明人： Rainer Walter , Armin Heckel , Gerald Roth , Joerg Kley , Gisela Schnapp , Martin Lenter , Jacobus Van Meel , Walter Spevak , Ulrike Weyer-Czernilofsky
IPC分类号： A61K31404
CPC分类号： C07D401/12 , C07D209/34 , C07D401/14 , C07D403/12 , C07D413/12
摘要： Indolinones of general formula I which are inhibitors of cell proliferation, particularly of tumour cells, and inhibitors of protein kinases. The following compounds are exemplary: (Z)-3-{1-[4-(N-(2-aminoethyl)-N-methylsulphonyl-amino)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone, (Z)-3-{1-[4-(N-(2-dimethylaminoethyl)-N-phenylsulphonyl-amino)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone, and (Z)-3-{1-[4-(4-methylpiperazinomethyl)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone.
摘要翻译： 通式I的吲哚酮，其是细胞增殖抑制剂，特别是肿瘤细胞的抑制剂，以及蛋白激酶抑制剂。 以下化合物为：（Z）-3- {1- [4-（N-（2-氨基乙基）-N-甲基磺酰基 - 氨基） - 苯基氨基] -1-苯基 - 亚甲基} -5-苯基磺酰基氨基-2- 吲哚酮，（Z）-3- {1- [4-（N-（2-二甲基氨基乙基）-N-苯基磺酰基 - 氨基） - 苯基氨基] -1-苯基 - 亚甲基} -5-苯基磺酰基氨基-2-二氢吲哚酮和（ Z）-3- {1- [4-（4-甲基哌嗪基甲基） - 苯基氨基] -1-苯基 - 亚甲基} -5-苯基磺酰基氨基-2-二氢吲哚酮。
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公开(公告)号：US08859541B2
公开(公告)日：2014-10-14
申请号：US13769934
申请日：2013-02-19
IPC分类号： C07D413/00 , C07D495/04 , C07D213/80 , C07D401/14 , C07D405/14 , C07D401/04 , C07D413/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D213/75 , C07D217/22 , C07D401/06 , C07D407/06 , C07D407/12 , C07D409/04 , C07D409/06 , C07D413/04 , C07D417/04 , C07D417/06 , C07D519/00
CPC分类号： C07D495/04 , C07D213/75 , C07D213/80 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/14 , C07D407/06 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D519/00
摘要： 6-Alkynylpyridines which are SMAC mimetics and are useful as medicaments for the treatment of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The following compounds are exemplary: methyl 5-[6-[[2-(methylamino)propanoyl]amino]-2-[2-(3-methylphenyl)ethynyl]pyridin-3-yl]-pyridine-3-carboxylate and 2-(methylamino)-N-[5-(2-methylimidazo[1,2-a]pyridin-3-yl)-6-[2-(1-methyl-2-oxoquinolin-6-yl)-ethynyl]pyridin-2-yl]propanamid.
摘要翻译： 作为SMAC模拟物的6-炔基吡啶并且可用作用于治疗特征在于过度或异常细胞增殖和相关病症如癌症的疾病的药物。 以下化合物是示例性的：5- [6 - [[2-（甲基氨基）丙酰基]氨基] -2- [2-（3-甲基苯基）乙炔基]吡啶-3-基] - 吡啶-3-甲酸甲酯和2 - （甲基氨基）-N- [5-（2-甲基咪唑并[1,2-a]吡啶-3-基）-6- [2-（1-甲基-2-氧代喹啉-6-基） - 乙炔基]吡啶 -2-基]丙酰胺。
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公开(公告)号：US07173028B2
公开(公告)日：2007-02-06
申请号：US10271763
申请日：2002-10-16
申请人： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schnapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
发明人： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schnapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
IPC分类号： C07D417/10 , C07D239/48 , A61K31/506
CPC分类号： C07D239/48 , C07D231/12 , C07D233/56 , C07D239/50 , C07D239/80 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D451/04 , C07D451/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
摘要： The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterised by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
摘要翻译： 本发明涉及如权利要求1所定义的式（I）的三取代嘧啶，其中R 1和R 2定义如权利要求1所述，其适用于治疗以过量为特征的疾病 或异常细胞增殖，其用于制备具有上述性质的药物组合物的用途及其制备方法。
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公开(公告)号：US06794395B1
公开(公告)日：2004-09-21
申请号：US10069557
申请日：2002-07-22
申请人： Gerald Juergen Roth , Armin Heckel , Rainer Walter , Ulrike Tontsch-Grunt , Walter Spevak , Jacobus C. A. Van Meel
发明人： Gerald Juergen Roth , Armin Heckel , Rainer Walter , Ulrike Tontsch-Grunt , Walter Spevak , Jacobus C. A. Van Meel
IPC分类号： A61K31404
CPC分类号： C07D401/04 , C04B35/632 , C07D209/34 , C07D401/12 , C07D401/14 , C07D403/12 , C07D491/04
摘要： The present invention relates to substituted indolinones of general formula wherein R1 to R6 and X are defined as in claim 1, the isomers and the salts thereof, in particular the physiologically acceptable salts thereof which have valuable pharmacological properties, especially an inhibitory effect on various receptor-tyrosine kinases, and cycline/CDK complexes as well as on the proliferation of endothelial cells and various tumor cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
摘要翻译： 本发明涉及通式为R 1至R 6的取代的二氢吲哚酮和X如权利要求1所定义，其异构体及其盐，特别是其生理上可接受的盐具有有价值的药理学性质，特别是对各种受体酪氨酸的抑制作用 激酶和循环/ CDK复合物以及内皮细胞和各种肿瘤细胞的增殖，含有这些化合物的药物组合物，其用途和制备方法。
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公开(公告)号：US5436162A
公开(公告)日：1995-07-25
申请号：US945240
申请日：1992-09-15
申请人： Konrad Heckl , Walter Spevak , Elinborg Ostermann , Andreas Zophel , Edeltraud Krystek , Ingrid Maurer-Fogy , Maria J. Wiche-Castanon , Christian Stratowa , Rudolf Hauptmann
发明人： Konrad Heckl , Walter Spevak , Elinborg Ostermann , Andreas Zophel , Edeltraud Krystek , Ingrid Maurer-Fogy , Maria J. Wiche-Castanon , Christian Stratowa , Rudolf Hauptmann
IPC分类号： C12N1/20 , A61K38/44 , A61K38/45 , A61P29/00 , A61P37/08 , C07H21/04 , C07K14/00 , C12N1/16 , C12N1/19 , C12N1/21 , C12N9/02 , C12N15/09 , C12N15/53 , C12N15/62 , C12P21/00 , C12R1/19 , C12R1/865 , C12R1/91 , C12N15/63 , C12N15/81
CPC分类号： C12N9/0089 , C12N15/625 , C07K2319/02 , C07K2319/07
摘要： The present invention relates to a method of preparing human Mn-superoxide dismutase (hMn-SOD) by genetic engineering, the DNA sequences which code for this enzyme, suitable vectors which contain these DNA sequences and host cells which can express these DNA sequences, and the enzyme hMn-SOD itself. Suggestions as to the use of this enzyme are also described.
摘要翻译： 本发明涉及通过遗传工程制备人类Mn超氧化物歧化酶（hMn-SOD）的方法，编码该酶的DNA序列，含有这些DNA序列的合适载体和可表达这些DNA序列的宿主细胞，以及 酶hMn-SOD本身。 还描述了关于使用该酶的建议。
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公开(公告)号：US5260204A
公开(公告)日：1993-11-09
申请号：US944939
申请日：1992-09-15
申请人： Konrad Heckl , Walter Spevak , Elinborg Ostermann , Andreas Zophel , Edeltraud Krystek , Ingrid Maurer-Fogy , Maria J. Wiche-Castanon , Christian Stratowa , Rudolf Hauptmann
发明人： Konrad Heckl , Walter Spevak , Elinborg Ostermann , Andreas Zophel , Edeltraud Krystek , Ingrid Maurer-Fogy , Maria J. Wiche-Castanon , Christian Stratowa , Rudolf Hauptmann
CPC分类号： C12N9/0089 , C12N15/625 , C07K2319/02 , C07K2319/07
摘要： The present invention relates to a method of preparing human Mn-superoxide dismutase (hMn-SOD) by genetic engineering, the DNA sequences which code for this enzyme, suitable vectors which contain these DNA sequences and host cells which can express these DNA sequences, and the enzyme hMn-SOD itself. Suggestions as to the use of this enzyme are also described.
摘要翻译： 本发明涉及通过遗传工程制备人类Mn超氧化物歧化酶（hMn-SOD）的方法，编码该酶的DNA序列，含有这些DNA序列的合适载体和可表达这些DNA序列的宿主细胞，以及 酶hMn-SOD本身。 还描述了关于使用该酶的建议。
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公开(公告)号：US07709480B2
公开(公告)日：2010-05-04
申请号：US11313380
申请日：2005-12-21
申请人： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
发明人： Georg Dahmann , Frank Himmelsbach , Bernd Krist , Martin Lenter , Alexander Pautsch , Gisela Schapp , Martin Steegmaier , Helmut Wittneben , Anthony S. Prokopowicz , Walter Spevak , Andreas Schoop , Steffen Steurer
IPC分类号： C07D417/00 , C07D239/48 , A61K31/506
CPC分类号： C07D239/48 , C07D231/12 , C07D233/56 , C07D239/50 , C07D239/80 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D451/04 , C07D451/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
摘要： The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterized by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
摘要翻译： 本发明涉及式（I）的三取代嘧啶，其中0Ra至Re如权利要求1所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，其用于制备具有上述药物组合物的用途 性质及其制备方法。
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