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公开(公告)号：US10759826B2
公开(公告)日：2020-09-01
申请号：US16305829
申请日：2017-06-07
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I. , USTAV MOLEKULARNI GENETIKY AKADEMIE VED CR, V.V.I. , UNIVERZITA PALACKEHO V OLOMOUCI , HELMHOLTZ ZENTRUM MUNCHEN
发明人： Martin Kotora , Eva Prchalova , Jerzy Adamski , Gabriele Moeller , Ondrej Stepanek , Petr Bartunek , David Sedlak , Marian Hajduch , Petr Dzubak
IPC分类号： A61K31/566 , C07J1/00
摘要： 15β-substituted derivatives of estrone of general formula I wherein R1, R2, R3, R4, R5 are independently selected from the group consisting of: C1-C4 alkyl, C1-C4 alkoxy, C1-C4 halogenalkyl, halogen, COOR6 wherein R6 is C1-C4 alkyl; H, OH; optionally, R3, R4 and R5 are each formed by a hydrogen atom, while R1 and R2 together form an aryl group, preferably naphthyl, in which the aromatic ring in position C-15 can be mono-, di-, tri-, tetra- and penta-substituted with substituents R1-R5. Compounds of the invention may be used for diagnosis and possibly also for the treatment of estrogen-dependent diseases.
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公开(公告)号：US11299510B2
公开(公告)日：2022-04-12
申请号：US16978093
申请日：2019-03-04
发明人： Lucia Veselovska , Michal Hocek , Marian Hajduch , Petr Dzubak
摘要： Substituted pyridopyrrolopyrimidine ribonucleosides of general formula I, wherein R is as described in the independent claim, preferably R is selected from the group comprising thiophen-3-yl, furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl; and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers. Compounds according to the invention show strong cytostatic and cytotoxic effects on cell lines of tumor origin in a wide variety of diseases including tumors of different histogenetic origin.
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公开(公告)号：US10730905B2
公开(公告)日：2020-08-04
申请号：US16308796
申请日：2017-07-31
发明人： Michal Hocek , Anna Tokarenko , Sabina Smolen , Marian Hajduch , Petr Dzubak
IPC分类号： A61K31/519 , A61K31/4985 , A61K31/407 , A61K31/341 , C07D487/16 , C07D487/14 , C07D491/14 , C07D491/16 , C07H19/23 , A61P35/02 , C07H19/24
摘要： Substituted heteropentadieno-pyrrolopyrimidine ribonucleosides of general formula I, where R is selected from the group comprising furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl or chloro, and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers.
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公开(公告)号：US10414788B2
公开(公告)日：2019-09-17
申请号：US16098068
申请日：2016-06-29
发明人： Michal Hocek , Michal Tichy , Marian Hajduch , Petr Dzubak
摘要： A group of substituted thienopyrrolopyrimidine ribonucleosides of general formula I, in which R shows strong cytostatic and cytotoxic activities preferably against cancer cell lines of broad spectrum of diseases including tumors of various histogenetic origin.
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公开(公告)号：US20140303390A1
公开(公告)日：2014-10-09
申请号：US14352210
申请日：2012-10-24
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CESKE REPUBLIKY, v.v.i. , USTAV MOLEKULARNI GENETIKY AKADEMIE VED CESKE REPUBLIKY v.v.i. , USTAV ANORGANICKE CHEME AKADEMIE VED CESKE REPUBLIKY, v.v.i. , UNIVERZITA PALACKEHO V OLOMOUCI
发明人： Jiri Brynda , Petr Cigler , Bohumir Gruner , Pavlina Maloy Rezacova , Pavel Mader , Vaclav Sicha , Mario Bakardjiev , Josef Holub , Petr Dzubak , Marian Hajduch
摘要： Derivatives of boron cluster compounds of general formula I and their pharmaceutically acceptable salts and solvates, and their specific inhibition effect on the enzyme carbonic anhydrase IX, a protein overexpressed in cancer tissues. Methods of synthesis and the use of the novel derivatives. These inhibitors of human carbonic anhydrase IX can be used as active compounds of pharmaceuticals for diagnostics and/or therapy of cancer diseases.
摘要翻译： 通式I的硼簇化合物的衍生物及其药学上可接受的盐和溶剂合物，以及它们对酶碳酸酐酶IX（一种在癌组织中过表达的蛋白质）的特异性抑制作用。 合成方法和新型衍生物的应用。 人类碳酸酐酶IX的这些抑制剂可以用作用于诊断和/或治疗癌症疾病的药物的活性化合物。
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公开(公告)号：US09290529B2
公开(公告)日：2016-03-22
申请号：US14352210
申请日：2012-10-24
申请人： USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CESKE REPUBLIKY, v.v.i. , USTAV MOLEKULARNI GENETIKY AKADEMIE VED CESKE REPUBLIKY, v.v.i. , USTAV ANORGANICKE CHEMIE AKADEMIE VED CESKE REPUBLIKY, v.v.i. , UNIVERZITA PALACKEHO V OLOMOUCI
发明人： Jiri Brynda , Petr Cigler , Bohumir Gruner , Pavlina Maloy Rezacova , Pavel Mader , Vaclav Sicha , Mario Bakardjiev , Josef Holub , Petr Dzubak , Marian Hajduch
摘要： Derivatives of boron cluster compounds of general formula I and their pharmaceutically acceptable salts and solvates, and their specific inhibition effect on the enzyme carbonic anhydrase IX, a protein overexpressed in cancer tissues. Methods of synthesis and the use of the novel derivatives. These inhibitors of human carbonic anhydrase IX can be used as active compounds of pharmaceuticals for diagnostics and/or therapy of cancer diseases.
摘要翻译： 通式I的硼簇化合物的衍生物及其药学上可接受的盐和溶剂合物，以及它们对酶碳酸酐酶IX（一种在癌组织中过表达的蛋白质）的特异性抑制作用。 合成方法和新型衍生物的应用。 人类碳酸酐酶IX的这些抑制剂可以用作用于诊断和/或治疗癌症疾病的药物的活性化合物。
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