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1.发明申请Cycloalkyl - containing 5-acylindolinones, the preparation thereof and their use as medicaments 有权含环烷基的5-丙烯基吲哚酮，其制备及其作为药物的用途公开(公告)号：US20050203104A1
公开(公告)日：2005-09-15
申请号：US11077355
申请日：2005-03-10
申请人： Armin Heckel , Gerald Roth , Joerg Kley , Stefan Hoerer , Ingo Uphues
发明人： Armin Heckel , Gerald Roth , Joerg Kley , Stefan Hoerer , Ingo Uphues
IPC分类号： A61K31/404 , A61K31/454 , A61K31/496 , C07D209/34 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/14 , C07D409/14 , C07D451/14
CPC分类号： C07D209/34 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/14 , C07D409/14 , C07D451/14
摘要： The present invention relates to cycloalkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).
摘要翻译： 本发明涉及通式如下的环烷基5-丙烯基吲哚酮：其中R 1至R 3定义如权利要求1至6中所述，互变异构体，对映异构体， 具有有价值的药理学特性，特别是对蛋白激酶的抑制作用，特别是对糖原合酶激酶（GSK-3）的活性的抑制作用的非对映异构体，其混合物及其盐。
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2.发明申请Alkyl-containing 5-acylindolinones, the preparation thereof and their use as medicaments 有权含烷基的5-丙烯基吲哚酮，其制备及其作为药物的用途公开(公告)号：US20050209302A1
公开(公告)日：2005-09-22
申请号：US11077399
申请日：2005-03-10
申请人： Armin Heckel , Gerald Roth , Joerg Kley , Stefan Hoerer , Ingo Uphues
发明人： Armin Heckel , Gerald Roth , Joerg Kley , Stefan Hoerer , Ingo Uphues
IPC分类号： A61K31/404 , A61K31/4045 , A61K31/501 , A61P3/10 , A61P25/28 , C07D209/34 , C07D209/36 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/14 , C07D407/06 , C07D407/14 , C07D45/02
CPC分类号： C07D401/06 , C07D209/34 , C07D401/12 , C07D403/06 , C07D405/06 , C07D405/14
摘要： The present invention relates to alkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).
摘要翻译： 本发明涉及通式为其中R 1至R 3的烷基的5-丙烯基吲哚酮，其互变异构体，对映异构体，非对映异构体，其混合物 其具有有价值的药理学特性，特别是对蛋白激酶的抑制作用，特别是对糖原合酶激酶（GSK-3）的活性的抑制作用。
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3.发明申请Aryl-containing 5-acylindolinones, the preparation thereof and their use as medicaments 有权含芳基的5-丙烯基吲哚酮，其制备及其作为药物的用途公开(公告)号：US20050234120A1
公开(公告)日：2005-10-20
申请号：US11077259
申请日：2005-03-10
申请人： Armin Heckel , Gerald Roth , Joerg Kley , Stefan Hoerer , Ingo Uphues
发明人： Armin Heckel , Gerald Roth , Joerg Kley , Stefan Hoerer , Ingo Uphues
IPC分类号： A61K31/404 , C07D209/34 , C07D403/12 , C07D405/06 , C07D47/02
CPC分类号： C07D209/34 , C07D403/12 , C07D405/06
摘要： The present invention relates to aryl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).
摘要翻译： 本发明涉及通式为其中R 1至R 3的芳基的5-丙烯基吲哚酮，其互变异构体，对映异构体，非对映异构体，其混合物 其具有有价值的药理学特性，特别是对蛋白激酶的抑制作用，特别是对糖原合酶激酶（GSK-3）的活性的抑制作用。
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4.发明授权Aryl-containing 5-acylindolinones, the preparation thereof and their use as medicaments 有权含芳基的5-丙烯基吲哚酮，其制备及其作为药物的用途公开(公告)号：US07176231B2
公开(公告)日：2007-02-13
申请号：US11077259
申请日：2005-03-10
申请人： Armin Heckel , Gerald Juergen Roth , Joerg Kley , Stefan Hoerer , Ingo Uphues
发明人： Armin Heckel , Gerald Juergen Roth , Joerg Kley , Stefan Hoerer , Ingo Uphues
IPC分类号： A61K31/40 , C07D209/34
CPC分类号： C07D209/34 , C07D403/12 , C07D405/06
摘要： The present invention relates to aryl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).
摘要翻译： 本发明涉及通式为其中R 1至R 3的芳基的含5-羟基吲哚酮，其互变异构体，对映异构体，非对映异构体，其混合物 其具有有价值的药理学特性，特别是对蛋白激酶的抑制作用，特别是对糖原合酶激酶（GSK-3）的活性的抑制作用。
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5.发明授权Alkyl-containing 5-acylindolinones, the preparation thereof and their use as medicaments 有权含烷基的5-丙烯基吲哚酮，其制备及其作为药物的用途公开(公告)号：US07560480B2
公开(公告)日：2009-07-14
申请号：US11077399
申请日：2005-03-10
申请人： Armin Heckel , Gerald Juergen Roth , Joerg Kley , Stefan Hoerer , Ingo Uphues
发明人： Armin Heckel , Gerald Juergen Roth , Joerg Kley , Stefan Hoerer , Ingo Uphues
IPC分类号： A61K31/404 , A61K31/4045 , A61K31/4439 , C07D401/12 , C07D209/34
CPC分类号： C07D401/06 , C07D209/34 , C07D401/12 , C07D403/06 , C07D405/06 , C07D405/14
摘要： The present invention relates to alkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).
摘要翻译： 本发明涉及通式为其中R 1至R 3在本文中定义的含烷基的5-丙烯基吲哚酮，其互变异构体，对映异构体，非对映体，其混合物及其盐，其具有有价值的药理学性质，特别是对 蛋白激酶，特别是对糖原合酶激酶（GSK-3）的活性的抑制作用。
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6.发明申请New (hetero)aryl compounds with MCH antagonistic activity and medicaments comprising these compounds 审中-公开具有MCH拮抗活性的新（杂）芳基化合物和包含这些化合物的药物公开(公告)号：US20070111981A1
公开(公告)日：2007-05-17
申请号：US11552836
申请日：2006-10-25
申请人： Gerald Roth , Stephan Mueller , Thorsten Lehmann-Lintz , Dirk Stenkamp , Philipp Lustenberger , Joerg Kley , Klaus Rudolf , Armin Heckel , Marcus Schindler , Leo Thomas , Ralf Lotz
发明人： Gerald Roth , Stephan Mueller , Thorsten Lehmann-Lintz , Dirk Stenkamp , Philipp Lustenberger , Joerg Kley , Klaus Rudolf , Armin Heckel , Marcus Schindler , Leo Thomas , Ralf Lotz
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454
CPC分类号： C07D237/08
摘要： The present invention relates to (hetero)aryl compounds of general formula I wherein the groups and radicals A, B, Q, W, X, Y, Z, R1, R2, R4a, R4b, R5a, R5b, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
摘要翻译： 本发明涉及通式I的（杂）芳基化合物，其中基团A，B，Q，W，X，Y，Z，R 1，R 2， R 4，R 4a，R 4b，R 5a，R 5b，R 5b具有权利要求1中给出的含义 。 此外，本发明涉及含有至少一种本发明化合物的药物组合物。 由于它们的MCH受体拮抗活性，本发明的药物组合物适用于治疗代谢紊乱和/或进食障碍，特别是肥胖症，食欲过剩，厌食症，食欲过盛和糖尿病。
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7.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：US07160901B2
公开(公告)日：2007-01-09
申请号：US10646423
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： A61K31/454 , C07D401/10
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.
摘要翻译： 作为细胞增殖抑制剂，特别是肿瘤细胞抑制剂的通式I的吲哚酮和蛋白激酶抑制剂。
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8.发明申请INDOLINE DERIVATIVES SUBSTITUTED IN THE 6 POSITION, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS 失效在6个位置取代的吲哚衍生物，其制备及其作为药物使用公开(公告)号：US20070004757A1
公开(公告)日：2007-01-04
申请号：US11470716
申请日：2006-09-07
申请人： Gerald Roth , Armin Heckel , Thorsten Lehmann-Lintz , Joerg Kley , Frank Hilberg , Jacobus Van Meel , Ulrik Tontsch-Grunt
发明人： Gerald Roth , Armin Heckel , Thorsten Lehmann-Lintz , Joerg Kley , Frank Hilberg , Jacobus Van Meel , Ulrik Tontsch-Grunt
IPC分类号： A61K31/496 , A61K31/4178 , A61K31/405 , C07D403/02
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所定义的下式的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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公开(公告)号：US20060154939A1
公开(公告)日：2006-07-13
申请号：US11275225
申请日：2005-12-20
申请人： John Park , Nveed Chaudhary , Thorsten Lehmann-Lintz , Armin Heckel , Gerald Roth , Joerg Kley , Trixi Brandl , Georg Dahmann , Matthias Grauert
发明人： John Park , Nveed Chaudhary , Thorsten Lehmann-Lintz , Armin Heckel , Gerald Roth , Joerg Kley , Trixi Brandl , Georg Dahmann , Matthias Grauert
IPC分类号： A61K31/496 , A61K31/454 , A61K31/404
CPC分类号： A61K31/404
摘要： The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
摘要翻译： 本发明涉及在6位上被取代的通式的二氢吲哚酮的用途，其中R 1至R 5和X如权利要求1所定义，异构体和 其盐，特别是其生理上可接受的盐作为预防或治疗特定纤维化疾病的药物。
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公开(公告)号：US20060148883A1
公开(公告)日：2006-07-06
申请号：US11275226
申请日：2005-12-20
申请人： John Park , Nveed Chaudhary , Gerald Roth , Armin Heckel , Thorsten Lehmann-Lintz , Joerg Kley
发明人： John Park , Nveed Chaudhary , Gerald Roth , Armin Heckel , Thorsten Lehmann-Lintz , Joerg Kley
IPC分类号： A61K31/404
CPC分类号： A61K31/496 , A61K31/404 , A61K31/4178 , C07D209/34 , C07D403/06
摘要： The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R6 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
摘要翻译： 本发明涉及在6位上被取代的通式的二氢吲哚酮的用途，其中R 1至R 6和X如权利要求1所定义，异构体和 其盐，特别是其生理上可接受的盐作为预防或治疗特定纤维化疾病的药物。
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