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1.发明授权Indolinone derivatives substituted in the 6 position, the preparation thereof and their use as pharmaceutical compositions 有权6位取代的吲哚啉酮衍生物及其制备及其作为药物组合物的用途公开(公告)号：US07514468B2
公开(公告)日：2009-04-07
申请号：US10624983
申请日：2003-07-22
申请人： Armin Heckel , Frank Hilberg , Thorsten Lehmann-Lintz , Guenter Linz , Joerg Kley , Jacobus C. A. Van Meel , Werner Rall , Gerald Juergen Roth , Peter Sieger , Ulrike Tontsch-Grunt
发明人： Armin Heckel , Frank Hilberg , Thorsten Lehmann-Lintz , Guenter Linz , Joerg Kley , Jacobus C. A. Van Meel , Werner Rall , Gerald Juergen Roth , Peter Sieger , Ulrike Tontsch-Grunt
IPC分类号： A61K31/404 , C07D209/34
CPC分类号： C07D209/48 , C07D209/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to indolinone derivatives substituted in the 6 position of general formula wherein R1 to R6 and X are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
摘要翻译： 本发明涉及在通式6的取代基中取代的二氢吲哚衍生物，其中R 1至R 6和X如权利要求1所定义，互变异构体，对映体，非对映体，其混合物及其盐，特别是其生理上可接受的盐，其中 具有有价值的药理学特性，特别是对各种受体酪氨酸激酶的抑制作用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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2.发明授权Indolinone derivatives substituted in the 6 position, their preparation and their use as medicaments 有权6位置取代的吲哚啉酮衍生物及其作为药物的用途公开(公告)号：US07858616B2
公开(公告)日：2010-12-28
申请号：US12421820
申请日：2009-04-10
申请人： Gerald Juergen Roth , Armin Heckel , Thorsten Lehmann-Lintz , Joerg Kley , Frank Hilberg , Jacobus C. A. Van Meel , Ulrike Tontsch-Grunt
发明人： Gerald Juergen Roth , Armin Heckel , Thorsten Lehmann-Lintz , Joerg Kley , Frank Hilberg , Jacobus C. A. Van Meel , Ulrike Tontsch-Grunt
IPC分类号： A61K31/541 , A61K31/404 , A61K31/496 , A61P35/00
CPC分类号： C07D209/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in Claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.
摘要翻译： 本发明涉及其中R 1至R 6和X如权利要求1中所定义的式6取代的二氢吲哚衍生物与其互变异构体，对映异构体，非对映体，其混合物及其盐，特别是 其生理上可接受的盐，其具有有用的药理学性质，特别是抑制对各种受体酪氨酸激酶的作用，以及对内皮细胞和各种肿瘤细胞的增殖，对包含这些化合物的药物的用途及其制备方法。
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3.发明授权Indoline derivatives substituted in the 6-position, their preparation and their use as medicaments 失效6-位取代的二氢吲哚衍生物，其制备方法及其作为药物的用途公开(公告)号：US07547703B2
公开(公告)日：2009-06-16
申请号：US11470716
申请日：2006-09-07
申请人： Gerald Juergen Roth , Armin Heckel , Thorsten Lehmann-Lintz , Joerg Kley , Frank Hilberg , Jacobus C. A. Van Meel , Ulrike Tontsch-Grunt
发明人： Gerald Juergen Roth , Armin Heckel , Thorsten Lehmann-Lintz , Joerg Kley , Frank Hilberg , Jacobus C. A. Van Meel , Ulrike Tontsch-Grunt
IPC分类号： A61K31/496 , A61K31/4178
CPC分类号： C07D209/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.
摘要翻译： 本发明涉及其中R 1至R 6和X如权利要求1中所定义的式6-取代的吲哚啉酮衍生物与其互变异构体，对映异构体，非对映异构体及其盐，特别是其盐 其生理上可接受的盐，其具有有用的药理学性质，特别是抑制对各种受体酪氨酸激酶的作用，以及对内皮细胞和各种肿瘤细胞的增殖，对包含这些化合物的药物的用途及其制备方法。
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4.发明授权Indolinone derivatives substituted in the 6-position, their preparation and their use as medicaments 有权6位置取代的吲哚啉酮衍生物，其制备及其用作药物公开(公告)号：US07169936B2
公开(公告)日：2007-01-30
申请号：US10625101
申请日：2003-07-22
申请人： Gerald Juergen Roth , Armin Heckel , Thorsten Lehmann-Lintz , Joerg Kley , Frank Hilberg , Jacobus C. A. Van Meel , Ulrike Tontsch-Grunt
发明人： Gerald Juergen Roth , Armin Heckel , Thorsten Lehmann-Lintz , Joerg Kley , Frank Hilberg , Jacobus C. A. Van Meel , Ulrike Tontsch-Grunt
IPC分类号： C07D209/04
CPC分类号： C07D209/34 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.
摘要翻译： 本发明涉及其中R 1至R 6和X如权利要求1中定义的下式所示的6-位取代的吲哚啉酮衍生物与它们的 互变异构体，对映异构体，非对映异构体，它们的混合物及其盐，特别是其生理上可接受的盐，其具有有用的药理学性质，特别是抑制对各种受体酪氨酸激酶的作用以及内皮细胞和各种肿瘤细胞的增殖， 包含这些化合物的药物，其用途及其制备方法。
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5.发明授权Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments 有权被杂环取代的吲哚啉酮，其制备方法及其作为药物的用途公开(公告)号：US07148249B2
公开(公告)日：2006-12-12
申请号：US10656863
申请日：2003-09-05
申请人： Joerg Kley , Frank Hilberg , Armin Heckel , Gerald Juergen Roth , Thorsten Lehmann-Lintz , Ralf R. H. Lotz , Ulrike Tontsch-Grunt , Jacobus C. A. Van Meel
发明人： Joerg Kley , Frank Hilberg , Armin Heckel , Gerald Juergen Roth , Thorsten Lehmann-Lintz , Ralf R. H. Lotz , Ulrike Tontsch-Grunt , Jacobus C. A. Van Meel
IPC分类号： A61K31/403 , C07D209/34
CPC分类号： C07D413/06 , C07D209/34 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D413/14
摘要： The present invention relates to heterocyclically substituted indolinones of general formula wherein R1 to R5 and X are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and cyclin/CDK complexes and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
摘要翻译： 本发明涉及通式其中R 1至R 5和X如权利要求1中定义的杂环取代的二氢吲哚酮，互变异构体，非对映异构体，对映异构体， 其前体药物及其盐，特别是其具有有价值的药理学特性的生理上可接受的盐，特别是对各种受体酪氨酸激酶和细胞周期蛋白/ CDK复合物的抑制作用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：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：US06545035B1
公开(公告)日：2003-04-08
申请号：US09969912
申请日：2001-10-03
IPC分类号： A61K314035
CPC分类号： C07D209/30 , C07D209/34
摘要： Substituted indolinones of general formula having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone and 3-Z-[1-(4-(2,3,4,5-Tetrahydro-benzo(d)azepin-3-yl-methyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone.
摘要翻译： 通用结构式取代的吲哚酮对各种激酶和cyclin / CDK复合物的影响以及各种肿瘤细胞的增殖。 示例性化合物是：3-Z- [1-（4-（N-苄基-N-甲基 - 氨基甲基） - 苯基氨基）-1-甲基 - 亚甲基] -5-酰氨基-2-二氢吲哚酮和3-Z- [1- （4-（2,3,4,5-四氢 - 苯并（d）氮杂-3-基 - 甲基） - 苯基氨基）-1-甲基 - 亚甲基] -5-酰氨基-2-二氢吲哚酮。
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公开(公告)号：US4656171A
公开(公告)日：1987-04-07
申请号：US675299
申请日：1984-11-27
申请人： Volkhard Austel , Norbert Hauel , Joachim Heider , Manfred Reiffen , Jacobus C. A. Van Meel , Willi Diederen
发明人： Volkhard Austel , Norbert Hauel , Joachim Heider , Manfred Reiffen , Jacobus C. A. Van Meel , Willi Diederen
IPC分类号： A61K31/50 , A61K31/53 , A61P9/02 , A61P9/04 , C07D487/04 , A61K31/495 , C07D471/02
CPC分类号： C07D487/04
摘要： Compounds of the formula ##STR1## wherein A, B, C and D are each independently --N.dbd. or --CH.dbd., provided, however, that at least two of them must be --N.dbd., and when A and C are both --N.dbd., at least one or both of B and D must be --N.dbd.; andR.sub.1, R.sub.2 and R.sub.3 are substituents of diverse types;tautomers thereof; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as cardiotonics.
摘要翻译： 其中A，B，C和D各自独立地为-N =或-CH =，但条件是其中至少两个必须为-N =，并且当A和C均为 - N =，B和D中的至少一个或两个必须为-N =; 并且R1，R2和R3是不同类型的取代基; 互变异构体 和无毒的，药学上可接受的酸加成盐。 这些化合物可用作强心剂。
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公开(公告)号：US08404697B2
公开(公告)日：2013-03-26
申请号：US12093321
申请日：2006-11-09
IPC分类号： A61K31/517
CPC分类号： A61K31/517 , A61K31/553 , A61K33/24
摘要： The present invention relates to the use of quinazolines of formula (I), wherein the groups Ra to Rd have the meanings given in the claims and specification, in cancer therapy.
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公开(公告)号：US4746658A
公开(公告)日：1988-05-24
申请号：US71329
申请日：1987-07-09
申请人： Volkhard Austel , Norbert Hauel , Joachim Heider , Manfred Reiffen , Jacobus C. A. Van Meel , Willi Diederen
发明人： Volkhard Austel , Norbert Hauel , Joachim Heider , Manfred Reiffen , Jacobus C. A. Van Meel , Willi Diederen
IPC分类号： A61K31/50 , A61K31/53 , A61P9/02 , A61P9/04 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of the formula ##STR1## wherein A, B, C and D are each independently --N.dbd. or --CH.dbd., provided, however, that at least two of them must be --N.dbd., and when A and C are both --N.dbd., at least one or both of B and D must be --N.dbd.; andR.sub.1, R.sub.2 and R.sub.3 are substituents of diverse types;tautomers thereof; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as cardiotonics.
摘要翻译： 其中A，B，C和D各自独立地为-N =或-CH =，但条件是其中至少两个必须为-N =，并且当A和C均为 - N =，B和D中的至少一个或两个必须为-N =; 并且R1，R2和R3是不同类型的取代基; 互变异构体 和无毒的，药学上可接受的酸加成盐。 这些化合物可用作强心剂。
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