专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2012034132A3 INHIBITORS OF HUMAN EZH2, AND METHODS OF USE THEREOF 审中-公开
标题翻译：人类EZH2的抑制剂及其使用方法
公开(公告)号：WO2012034132A3
公开(公告)日：2012-06-07
申请号：PCT/US2011051258
申请日：2011-09-12
申请人： EPIZYME INC , COPELAND ROBERT ALLEN , RICHON VICTORIA MARIE , SCOTT MARGARET DAVIS , SNEERINGER CHRISTOPHER JOHN , KUNTZ KEVIN WAYNE , KNUTSON SARAH KATHLEEN , POLLOCK ROY MACFARLANE
发明人： COPELAND ROBERT ALLEN , RICHON VICTORIA MARIE , SCOTT MARGARET DAVIS , SNEERINGER CHRISTOPHER JOHN , KUNTZ KEVIN WAYNE , KNUTSON SARAH KATHLEEN , POLLOCK ROY MACFARLANE
IPC分类号： G01N33/50 , A61K38/17 , A61P35/00 , C07D473/34 , G01N33/53 , G01N33/68
CPC分类号： A61K31/7076 , C07D473/34 , C07D493/04 , C12Q1/48 , C12Q1/6876 , G01N33/5011 , G01N33/57426 , G01N2333/91011
摘要： The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3- K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
摘要翻译：本发明涉及抑制人组蛋白甲基转移酶EZH2的野生型和某些突变形式，所述组蛋白甲基转移酶EZH2是催化组蛋白H3上赖氨酸27（H3-K27）的单 - 至三 - 甲基化的PRC2复合物的催化亚基。在一个实施方案中，抑制对EZH2的突变形式是选择性的，使得与某些癌症相关的H3-K27的三甲基化被抑制。该方法可用于治疗包括滤泡性淋巴瘤和弥漫性大B细胞淋巴瘤（DLBCL）的癌症。还提供了用于鉴定EZH2的突变形式的小分子选择性抑制剂的方法以及用于确定对象中对EZH2抑制剂的响应性的方法。

2. 发明专利

AU2022242157A1 INHIBITORS OF HUMAN EZH2, AND METHODS OF USE THEREOF 未知
公开(公告)号：AU2022242157A1
公开(公告)日：2022-10-27
申请号：AU2022242157
申请日：2022-10-04
申请人： EPIZYME INC
发明人： COPELAND ROBERT ALLEN , RICHON VICTORIA MARIE , SCOTT MARGARET DAVIS , SNEERINGER CHRISTOPHER JOHN , KUNTZ KEVIN WAYNE , KNUTSON SARAH KATHLEEN , POLLOCK ROY MACFARLANE
IPC分类号： C07D473/34 , A61K38/17 , A61P35/00 , G01N33/50 , G01N33/53 , G01N33/68
摘要： The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3- K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.

3. 发明专利

AU2020203245A1 INHIBITORS OF HUMAN EZH2, AND METHODS OF USE THEREOF 未知
公开(公告)号：AU2020203245A1
公开(公告)日：2020-06-04
申请号：AU2020203245
申请日：2020-05-19
申请人： EPIZYME INC
发明人： COPELAND ROBERT ALLEN , RICHON VICTORIA MARIE , SCOTT MARGARET DAVIS , SNEERINGER CHRISTOPHER JOHN , KUNTZ KEVIN WAYNE , KNUTSON SARAH KATHLEEN , POLLOCK ROY MACFARLANE
IPC分类号： C07D473/34 , A61K38/17 , A61P35/00 , G01N33/50 , G01N33/53 , G01N33/68
摘要： The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3- K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.

4. 发明专利

RU2765155C2 ИНГИБИТОРЫ EZH2 ЧЕЛОВЕКА И СПОСОБЫ ИХ ПРИМЕНЕНИЯ 未知
公开(公告)号：RU2765155C2
公开(公告)日：2022-01-26
申请号：RU2017113351
申请日：2011-09-12
申请人： EPIZYME INC
发明人： COPELAND ROBERT ALLEN , RICHON VICTORIA MARIE , SCOTT MARGARET DAVIS , SNEERINGER CHRISTOPHER JOHN , KUNTZ KEVIN WAYNE , KNUTSON SARAH KATHLEEN , POLLOCK ROY MACFARLANE
IPC分类号： A61P35/00 , G01N33/50 , C12Q1/48
摘要： Настоящееизобретениеотноситсяк ингибированиюформдикоготипаи определенныхмутантныхформметилтрансферазыгистонов EZH2 человека - каталитическойсубъединицыкомплекса PRC2, котораякатализируетотмоно- дотриметилированиялизина 27 нагистоне H3 (H3-K27), кспособамлеченияразличныхтиповрака, включающихфолликулярнуюлимфомуи диффузнуюкрупно-B-клеточнуюлимфому (DLBCL), ик способамопределенияспособностик ответунаингибитор EZH2 уиндивидуума. Способидентификациииндивидуумакакотвечающегонаселективныйингибитормутанта EZH2 по Y641 включает a) получениеобразцатканиотиндивидуума; b) выявлениеуровнядиметилирования (me2) H3-K27, еслионоприсутствуетв указанномобразцеткани, исравнениеуказанногоуровнядиметилирования (me2) сконтрольнымуровнемдиметилирования (me2); гдеуказанныйиндивидуумявляетсяотвечающимнаселективныйингибитормутанта EZH2 по Y641, когдауказанныйуровеньдиметилирования (me2) отсутствуетилинижеуказанногоконтрольногоуровнядиметилирования (me2), игдеконтрольныйуровеньпредставляетсобойуровеньдиметилирования (me2) H3-K27 вобразцетканиотиндивидуума, укоторогонеэкспрессируетсямутант EZH2 по Y641. 9 з.п. ф-лы, 4 табл., 14 ил., 11 пр.

5. 发明专利

PL2614369T3 SPOSÓB OKREŚLANIA PRZYDATNOŚCI INHIBITORÓW LUDZKIEGO EZH2 W LECZENIU 未知
公开(公告)号：PL2614369T3
公开(公告)日：2016-08-31
申请号：PL11824247
申请日：2011-09-12
申请人： EPIZYME INC
发明人： COPELAND ROBERT ALLEN , RICHON VICTORIA MARIE , SCOTT MARGARET DAVIS , SNEERINGER CHRISTOPHER JOHN , KUNTZ KEVIN WAYNE , KNUTSON SARAH KATHLEEN , POLLOCK ROY MACFARLANE
IPC分类号： G01N33/50 , A61K38/17 , A61P35/00 , C07D473/34 , G01N33/53 , G01N33/574 , G01N33/68

6. 发明专利

ES2570380T3 Método para determinar la aptitud de inhibidores de EZH2 humano en tratamiento 未知
公开(公告)号：ES2570380T3
公开(公告)日：2016-05-18
申请号：ES11824247
申请日：2011-09-12
申请人： EPIZYME INC
发明人： COPELAND ROBERT ALLEN , RICHON VICTORIA MARIE , SCOTT MARGARET DAVIS , SNEERINGER CHRISTOPHER JOHN , KUNTZ KEVIN WAYNE , KNUTSON SARAH KATHLEEN , POLLOCK ROY MACFARLANE
IPC分类号： G01N33/50 , A61K38/17 , A61P35/00 , C07D473/34 , G01N33/53 , G01N33/574 , G01N33/68
摘要： Un método para determinar si un sujeto que tiene o se sospecha que tiene cáncer seleccionado de linfoma y melanoma es un candidato para tratamiento con un inhibidor de EZH2, que comprende; detectar un mutante Y641 de un polipéptido EZH2, si está presente, en una muestra obtenida del sujeto; en donde la presencia del mutante Y641 indica que el sujeto es un candidato para tratamiento con un inhibidor de EZH2.

7. 发明专利

AU2017276284A1 INHIBITORS OF HUMAN EZH2, AND METHODS OF USE THEREOF 未知
公开(公告)号：AU2017276284A1
公开(公告)日：2018-01-18
申请号：AU2017276284
申请日：2017-12-14
申请人： EPIZYME INC
发明人： COPELAND ROBERT ALLEN , RICHON VICTORIA MARIE , SCOTT MARGARET DAVIS , SNEERINGER CHRISTOPHER JOHN , KUNTZ KEVIN WAYNE , KNUTSON SARAH KATHLEEN , POLLOCK ROY MACFARLANE
IPC分类号： C07D473/34 , A61K38/17 , A61P35/00 , G01N33/50 , G01N33/53 , G01N33/68
摘要： The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3- K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.

8. 发明专利

AU2011298987B2 Inhibitors of human EZH2, and methods of use thereof 未知
公开(公告)号：AU2011298987B2
公开(公告)日：2017-09-28
申请号：AU2011298987
申请日：2011-09-12
申请人： EPIZYME INC
发明人： COPELAND ROBERT ALLEN , RICHON VICTORIA MARIE , SCOTT MARGARET DAVIS , SNEERINGER CHRISTOPHER JOHN , KUNTZ KEVIN WAYNE , KNUTSON SARAH KATHLEEN , POLLOCK ROY MACFARLANE
IPC分类号： C07D473/34 , A61K38/17 , A61P35/00 , G01N33/50 , G01N33/53 , G01N33/68
摘要： The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3- K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式