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公开(公告)号：US20130273063A1
公开(公告)日：2013-10-17
申请号：US13642430
申请日：2011-04-19
Applicant: Haiyong Han , Daniel Von Hoff , Caroline Huynh Diep , Hongwei Yin
Inventor： Haiyong Han , Daniel Von Hoff , Caroline Huynh Diep , Hongwei Yin
IPC: C12Q1/68
CPC classification number: A61K31/519 , A61K9/0019 , A61K9/0053 , C12Q1/6886 , C12Q2600/106 , C12Q2600/136 , C12Q2600/156 , C12Q2600/158
Abstract: Methods of tests that assess the expression of DPC4 (SMAD4) to identify subjects with pancreatic cancer that are likely or unlikely to respond to treatment with BTK inhibitors; methods of treating subjects based on identification of said subjects as likely to respond to treatment with BTK inhibitors; therapeutic targets for cancers, particularly cancers with inactivated DPC4 gene or protein; methods of screening of new therapeutic agents using the target; pharmaceutical composition comprising BTK inhibitors, such as PCI-32765 or derivatives thereof, for cancer treatment; and kits that facilitate the performance of the methods are disclosed.
Abstract translation: 评估DPC4（SMAD4）表达以鉴别可能或不可能对用BTK抑制剂治疗反应的胰腺癌患者的测试方法; 基于鉴定所述受试者可能对BTK抑制剂治疗作出反应的治疗受试者的方法; 癌症特别是具有灭活DPC4基因或蛋白质的癌症的治疗靶点; 使用靶标筛选新治疗剂的方法; 包含用于癌症治疗的BTK抑制剂（例如PCI-32765或其衍生物）的药物组合物; 并且公开了促进方法的性能的试剂盒。
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公开(公告)号：US20090143399A1
公开(公告)日：2009-06-04
申请号：US11841574
申请日：2007-08-20
Applicant: 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
Inventor： 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: A61K31/496 , C07D487/04 , C07D495/14 , C07D491/048 , A61P35/04
CPC classification number: C07D403/14 , C07D405/14 , C07D487/04 , C07D491/048 , C07D495/04 , C07D495/14
Abstract: 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.
Abstract translation: 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。
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3.发明申请COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF 2-ARYL PYRIDYLAZOLES 有权化合物，药物组合物和2-亚苄基吡唑啉的使用方法公开(公告)号：US20120136029A1
公开(公告)日：2012-05-31
申请号：US13264967
申请日：2010-04-19
Applicant: Robert Dorr , Gary Flynn , Haiyong Han , Laurence Hurley
Inventor： Robert Dorr , Gary Flynn , Haiyong Han , Laurence Hurley
IPC: A61K31/4439 , C07D263/32 , C12N5/02 , A61P35/04 , A61K31/4409 , C07D413/04 , A61P35/00
CPC classification number: C07D213/81 , A61K31/42 , A61K45/06 , C07D263/32 , C07D413/04 , C07D413/10 , C07D413/14 , A61K2300/00
Abstract: A 2-aryl-pyridylazole compound and derivatives useful in slowing the growth of cancer cells are disclosed. Also disclosed are methods of synthesizing the compound, methods of using pharmaceutical compositions containing the compound as an ingredient to slow the growth of cancer cells, and methods of treating cancer patients with pharmaceutical compositions containing the compound as an ingredient.
Abstract translation: 公开了2-芳基 - 吡啶基唑化合物和用于减缓癌细胞生长的衍生物。 还公开了合成化合物的方法，使用含有该化合物作为成分以减缓癌细胞生长的药物组合物的方法，以及使用含有该化合物作为成分的药物组合物治疗癌症患者的方法。
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公开(公告)号：US20050277658A1
公开(公告)日：2005-12-15
申请号：US11092168
申请日：2005-03-29
Applicant: Laurence Hurley , Daruka Mahadevan , Haiyong Han , David Bearss , Hariprasad Vankayalapati , Sridevi Bashyam , Ruben Munoz , Steven Warner , Kimiko Della Croce , Daniel Von Hoff , Cory Grand
Inventor： Laurence Hurley , Daruka Mahadevan , Haiyong Han , David Bearss , Hariprasad Vankayalapati , Sridevi Bashyam , Ruben Munoz , Steven Warner , Kimiko Della Croce , Daniel Von Hoff , Cory Grand
IPC: A61K31/517 , A61K31/519 , C07D239/94 , C07D405/12 , C07D405/14 , C07D487/02 , C07D487/04 , C07D487/14 , C07D491/04 , C07D495/04
CPC classification number: C07D487/04 , C07D239/94 , C07D403/14 , C07D405/12 , C07D405/14 , C07D491/04 , C07D491/048 , C07D495/04 , C07D495/14
Abstract: 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.
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5.发明授权Methods, compounds and compositions with genotype selective anticancer activity 有权具有基因型选择性抗癌活性的方法，化合物和组合物公开(公告)号：US08394742B2
公开(公告)日：2013-03-12
申请号：US11910591
申请日：2006-04-14
Applicant: Daniel D. Von Hoff , Haiyong Han , Hong Wang , Gary A. Flynn
Inventor： Daniel D. Von Hoff , Haiyong Han , Hong Wang , Gary A. Flynn
CPC classification number: C07C235/84 , C07D231/54 , C07D233/64 , C07D263/32 , C07D277/48 , C07D413/04 , C07D413/12 , C07D417/04 , C12Q1/6886 , C12Q2600/136 , C12Q2600/158 , G01N33/5011
Abstract: This invention is directed to methods for screening and identification of compounds capable of selectively eliminating cancer cells with specific loss-of-function alterations, including but not limited to mutations, deletions, hypermethylations, and other types of gene silencing. This invention is also directed to novel compounds that selectively eliminate cancer cells with specific loss-of-function alterations. Furthermore, this invention is directed to methods for production and therapeutic use of compounds that selectively eliminate cancer cells with specific loss-of-function alterations.
Abstract translation: 本发明涉及用于筛选和鉴定能够以特定功能丧失功能改变选择性地除去癌细胞的化合物的方法，包括但不限于突变，缺失，高甲基化和其他类型的基因沉默。 本发明还涉及以特定的功能丧失改变选择性地消除癌细胞的新型化合物。 此外，本发明涉及用于特异性功能丧失改变选择性地消除癌细胞的化合物的生产和治疗用途的方法。
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Patent Agency Ranking
公开(公告)号：US20110212929A1
公开(公告)日：2011-09-01
申请号：US13051790
申请日：2011-03-18
Applicant: 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
Inventor： 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: A61K31/635 , C07D487/04 , A61K31/496 , C07D471/14 , A61K31/519 , C07D413/14 , A61K31/5377 , A61P35/00
CPC classification number: A61K31/519 , A61K45/06 , A61N5/00 , C07D403/14 , C07D405/14 , C07D487/04 , C07D491/048 , C07D495/04 , C07D495/14
Abstract: 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.
Abstract translation: 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。
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7.发明申请METHODS, COMPOUNDS AND COMPOSITIONS WITH GENOTYPE SELECTIVE ANTICANCER ACTIVITY 有权方法，化合物和组合物与基因选择性反应活性公开(公告)号：US20090137420A1
公开(公告)日：2009-05-28
申请号：US11910591
申请日：2006-04-14
Applicant: Daniel D. Von Hoff , Haiyong Han , Hong Wang , Gary A. Flynn
Inventor： Daniel D. Von Hoff , Haiyong Han , Hong Wang , Gary A. Flynn
IPC: C40B30/06 , C07C233/77 , C07D263/32 , C07D231/54 , C07D277/46
CPC classification number: C07C235/84 , C07D231/54 , C07D233/64 , C07D263/32 , C07D277/48 , C07D413/04 , C07D413/12 , C07D417/04 , C12Q1/6886 , C12Q2600/136 , C12Q2600/158 , G01N33/5011
Abstract: This invention is directed to methods for screening and identification of compounds capable of selectively eliminating cancer cells with specific loss-of-function alterations, including but not limited to mutations, deletions, hypermethylations, and other types of gene silencing. This invention is also directed to novel compounds that selectively eliminate cancer cells with specific loss-of-function alterations. Furthermore, this invention is directed to methods for production and therapeutic use of compounds that selectively eliminate cancer cells with specific loss-of-function alterations.
Abstract translation: 本发明涉及用于筛选和鉴定能够以特定功能丧失功能改变选择性地除去癌细胞的化合物的方法，包括但不限于突变，缺失，高甲基化和其他类型的基因沉默。 本发明还涉及以特定的功能丧失改变选择性地消除癌细胞的新型化合物。 此外，本发明涉及用于特异性功能丧失改变选择性地消除癌细胞的化合物的生产和治疗用途的方法。
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公开(公告)号：US20080261818A1
公开(公告)日：2008-10-23
申请号：US12041350
申请日：2008-03-03
Applicant: Haiyong Han , Robert J. Gillies , Victor J. Hruby , David L. Morse
Inventor： Haiyong Han , Robert J. Gillies , Victor J. Hruby , David L. Morse
CPC classification number: G01N33/57438 , C12Q1/6886 , C12Q2600/158
Abstract: Methods that identify cells as pancreatic cancer cells based on assessing the expression of combinations of target molecules expressed preferentially on pancreatic cancer cells are disclosed. Combinations were initially discovered by microarray analysis and selected based upon tumor specificity, relative lack of cross-reactivity with normal tissues, and applicability as targets of multispecific ligands. The claimed methods encompass measuring the expression of three or more specific target molecules in combination and correlating positive expression of the combination with an identification of the cell as a pancreatic cancer cell.
Abstract translation: 公开了基于评估胰腺癌细胞优先表达的靶分子的组合的表达来鉴定细胞作为胰腺癌细胞的方法。 组合最初通过微阵列分析发现，并且基于肿瘤特异性，与正常组织的相对缺乏交叉反应性和作为多特异性配体的靶标的适用性来选择。 要求保护的方法包括组合测量三种或更多种特异性靶分子的表达，并将组合的阳性表达与作为胰腺癌细胞的细胞鉴定相关联。
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公开(公告)号：US20050239793A1
公开(公告)日：2005-10-27
申请号：US11092809
申请日：2005-03-29
Applicant: Laurence Hurley , Daruka Mahadevan , Haiyong Han , David Bearss , Hariprasad Vankayalapati , Sridevi Bashyam , Ruben Munoz , Steven Warner , Kimiko Della Croce , Daniel Von Hoff , Cory Grand
Inventor： Laurence Hurley , Daruka Mahadevan , Haiyong Han , David Bearss , Hariprasad Vankayalapati , Sridevi Bashyam , Ruben Munoz , Steven Warner , Kimiko Della Croce , Daniel Von Hoff , Cory Grand
IPC: A61K31/517 , A61K31/519 , C07D239/94 , C07D405/12 , C07D405/14 , C07D487/02 , C07D487/04 , C07D487/14 , C07D491/04 , C07D495/04
CPC classification number: C07D487/04 , C07D239/94 , C07D403/14 , C07D405/12 , C07D405/14 , C07D491/04 , C07D491/048 , C07D495/04 , C07D495/14
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US20050227992A1
公开(公告)日：2005-10-13
申请号：US10965313
申请日：2004-10-14
Applicant: Laurence Hurley , Daruka Mahadevan , Haiyong Han , David Bearss , Hariprasad Vankayalapati , Sridevi Bashyam , Ruben Munoz , Steven Warner , Kimiko Della Croce , Daniel Von Hoff , Cory Grand
Inventor： Laurence Hurley , Daruka Mahadevan , Haiyong Han , David Bearss , Hariprasad Vankayalapati , Sridevi Bashyam , Ruben Munoz , Steven Warner , Kimiko Della Croce , Daniel Von Hoff , Cory Grand
IPC: A61K31/517 , A61K31/519 , C07D239/94 , C07D405/12 , C07D405/14 , C07D487/02 , C07D487/04 , C07D487/14 , C07D491/04 , C07D495/04
CPC classification number: C07D487/04 , C07D239/94 , C07D403/14 , C07D405/12 , C07D405/14 , C07D491/04 , C07D491/048 , C07D495/04 , C07D495/14
Abstract: 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.
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