公开(公告)号：US08552018B2

公开(公告)日：2013-10-08

申请号：US13051790

申请日：2011-03-18

申请人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Steven L. Warner ,  James Welsh

发明人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Steven L. Warner ,  James Welsh

IPC分类号： A61K31/519 ,  A61K31/496 ,  A61P35/04 ,  C07D491/14 ,  C07D471/14 ,  C07D239/70 ,  A61K31/517

CPC分类号： A61K31/519 ,  A61K45/06 ,  A61N5/00 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D495/14

摘要： Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

摘要翻译： 公开了可用于治疗蛋白激酶介导的疾病和病症（例如癌症）的蛋白激酶抑制剂。 本发明化合物具有以下结构：包括立体异构体，前体药物和药学上可接受的盐，其中A是选自以下的环部分：其中R1，R2，R3，X，Z，L1，Cyc11，L2和Cyc22为 本文定义。 还公开了含有本发明化合物的组合物以及与其用途有关的方法。

公开(公告)号：US20090099165A1

公开(公告)日：2009-04-16

申请号：US11735344

申请日：2007-04-13

申请人： Laurence H. Hurley ,  Daruka Mahadevan ,  Haiyong Han ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Ruben M. Munoz ,  Steven L. Warner ,  Kimiko Della Croce ,  Daniel D. Von Hoff ,  Cory L. Grand ,  James Welsh

发明人： Laurence H. Hurley ,  Daruka Mahadevan ,  Haiyong Han ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Ruben M. Munoz ,  Steven L. Warner ,  Kimiko Della Croce ,  Daniel D. Von Hoff ,  Cory L. Grand ,  James Welsh

IPC分类号： A61K31/5377 ,  C07D487/04 ,  A61K31/519

CPC分类号： A61K31/519 ,  A61K45/06 ,  A61N5/00 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D495/14

摘要： Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

公开(公告)号：US07312226B2

公开(公告)日：2007-12-25

申请号：US11092168

申请日：2005-03-29

申请人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Steven L. Warner

发明人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Steven L. Warner

IPC分类号： A61K31/519 ,  C07D487/14 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D239/94 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D495/14

摘要： Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

摘要翻译： 公开了可用于治疗蛋白激酶介导的疾病和病症（例如癌症）的蛋白激酶抑制剂。 本发明的化合物具有以下结构：包括立体异构体，其前药和药学上可接受的盐，其中A是选自以下的环部分：其中R 1，R 2，R 3，X，Z，L 1，Cyc 11， L 2和Cyc 2如本文所定义。 还公开了含有本发明化合物的组合物以及与其用途有关的方法。

公开(公告)号：US20110212929A1

公开(公告)日：2011-09-01

申请号：US13051790

申请日：2011-03-18

申请人： Laurence H. Hurley ,  Daruka Mahadevan ,  Haiyong Han ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Ruben M. Munoz ,  Steven L. Warner ,  Kimiko Della Croce ,  Daniel D. Von Hoff ,  Cory L. Grand ,  James Welsh

发明人： Laurence H. Hurley ,  Daruka Mahadevan ,  Haiyong Han ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Ruben M. Munoz ,  Steven L. Warner ,  Kimiko Della Croce ,  Daniel D. Von Hoff ,  Cory L. Grand ,  James Welsh

IPC分类号： A61K31/635 ,  C07D487/04 ,  A61K31/496 ,  C07D471/14 ,  A61K31/519 ,  C07D413/14 ,  A61K31/5377 ,  A61P35/00

CPC分类号： A61K31/519 ,  A61K45/06 ,  A61N5/00 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D495/14

摘要： Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

摘要翻译： 公开了可用于治疗蛋白激酶介导的疾病和病症（例如癌症）的蛋白激酶抑制剂。 本发明化合物具有以下结构：包括立体异构体，前体药物和药学上可接受的盐，其中A是选自以下的环部分：其中R1，R2，R3，X，Z，L1，Cyc11，L2和Cyc22为 本文定义。 还公开了含有本发明化合物的组合物以及与其用途有关的方法。

公开(公告)号：US07326713B2

公开(公告)日：2008-02-05

申请号：US11092809

申请日：2005-03-29

申请人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Steven L. Warner

发明人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Steven L. Warner

IPC分类号： A61K31/519 ,  C07D487/14 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D239/94 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D495/14

摘要： Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

摘要翻译： 公开了可用于治疗蛋白激酶介导的疾病和病症（例如癌症）的蛋白激酶抑制剂。 本发明化合物具有以下结构：包括立体异构体，前体药物和药学上可接受的盐，其中A是选自以下的环部分：其中R1，R2，R3，X，Z，L1，Cyc11，L2和Cyc22为 本文定义。 还公开了含有本发明化合物的组合物以及与其用途有关的方法。

公开(公告)号：US20090143399A1

公开(公告)日：2009-06-04

申请号：US11841574

申请日：2007-08-20

申请人： Laurence H. Hurley ,  Daruka Mahadevan ,  Haiyong Han ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Ruben M. Munoz ,  Steven L. Warner ,  Kimiko Della Croce ,  Daniel D. Von Hoff ,  Cory L. Grand ,  James Welsh

发明人： Laurence H. Hurley ,  Daruka Mahadevan ,  Haiyong Han ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Ruben M. Munoz ,  Steven L. Warner ,  Kimiko Della Croce ,  Daniel D. Von Hoff ,  Cory L. Grand ,  James Welsh

IPC分类号： A61K31/496 ,  C07D487/04 ,  C07D495/14 ,  C07D491/048 ,  A61P35/04

CPC分类号： C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D495/14

摘要： Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

摘要翻译： 公开了可用于治疗蛋白激酶介导的疾病和病症（例如癌症）的蛋白激酶抑制剂。 本发明化合物具有以下结构：包括立体异构体，前体药物和药学上可接受的盐，其中A是选自以下的环部分：其中R1，R2，R3，X，Z，L1，Cyc11，L2和Cyc22为 本文定义。 还公开了含有本发明化合物的组合物以及与其用途有关的方法。

公开(公告)号：US07335662B2

公开(公告)日：2008-02-26

申请号：US11092863

申请日：2005-03-29

申请人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Steven L. Warner

发明人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Steven L. Warner

IPC分类号： A61K31/519 ,  C07D487/14 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D239/94 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D495/14

摘要： Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

公开(公告)号：US07326712B2

公开(公告)日：2008-02-05

申请号：US10965313

申请日：2004-10-14

申请人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Steven L. Warner

发明人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Sridevi Bashyam ,  Steven L. Warner

IPC分类号： C07D471/14 ,  A61K31/519 ,  A61P35/04 ,  C07D239/70 ,  A61K31/517

CPC分类号： C07D487/04 ,  C07D239/94 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D495/14

摘要： Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

摘要翻译： 公开了可用于治疗蛋白激酶介导的疾病和病症（例如癌症）的蛋白激酶抑制剂。 本发明化合物具有以下结构：包括立体异构体，前体药物和药学上可接受的盐，其中A是选自以下的环部分：其中R1，R2，R3，X，Z，L1，Cyc11，L2和Cyc22为 本文定义。 还公开了含有本发明化合物的组合物以及与其用途有关的方法。

公开(公告)号：US20130302303A1

公开(公告)日：2013-11-14

申请号：US13947691

申请日：2013-07-22

申请人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Steven L. Warner ,  James Welsh

发明人： Laurence H. Hurley ,  Daruka Mahadevan ,  David J. Bearss ,  Hariprasad Vankayalapati ,  Steven L. Warner ,  James Welsh

IPC分类号： A61K31/519 ,  A61K45/06 ,  A61N5/00 ,  C07D491/048

CPC分类号： A61K31/519 ,  A61K45/06 ,  A61N5/00 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D495/14

摘要： Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

摘要翻译： 公开了可用于治疗蛋白激酶介导的疾病和病症（例如癌症）的蛋白激酶抑制剂。 本发明化合物具有以下结构：包括立体异构体，前体药物和药学上可接受的盐，其中A是选自以下的环部分：其中R1，R2，R3，X，Z，L1，Cyc11，L2和Cyc22为 本文定义。 还公开了含有本发明化合物的组合物以及与其用途有关的方法。

公开(公告)号：US20140163017A1

公开(公告)日：2014-06-12

申请号：US13921895

申请日：2013-06-19

申请人： Hariprasad Vankayalapati ,  Venkataswamy Sorna ,  Steven L. Warner ,  Bret Stephens ,  David J. Bearss ,  Sunil Sharma

发明人： Hariprasad Vankayalapati ,  Venkataswamy Sorna ,  Steven L. Warner ,  Bret Stephens ,  David J. Bearss ,  Sunil Sharma

IPC分类号： C07D231/12 ,  C07D213/71 ,  C07D213/61 ,  C07D207/48 ,  C07C251/86 ,  C07C311/37

CPC分类号： A61K31/54 ,  A61K31/18 ,  A61K31/40 ,  A61K31/4453 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/5377 ,  C07C251/86 ,  C07C311/16 ,  C07C311/37 ,  C07D207/48 ,  C07D213/53 ,  C07D213/61 ,  C07D213/71 ,  C07D213/81 ,  C07D231/12 ,  C07D295/26

摘要： In one aspect, the invention relates to substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.