公开(公告)号：US11826399B2

公开(公告)日：2023-11-28

申请号：US16646998

申请日：2018-09-14

申请人： Eisai Inc.

发明人： Sharon McGonigle ,  Utpal Majumder ,  Maarten H. D. Postema

IPC分类号： A61K38/17 ,  A61K47/68 ,  A61P35/00 ,  A61K31/337 ,  A61K45/06 ,  A61K49/00

CPC分类号： A61K38/1767 ,  A61K31/337 ,  A61K45/06 ,  A61K47/6817 ,  A61K49/0019 ,  A61K49/0026 ,  A61K49/0065 ,  A61P35/00

摘要： The present invention provides, among other things, compositions and methods relating to detection and/or treatment cancer (e.g., one or more tumors) that expresses Neuropilin 1 (NRP1). The present invention provides methods of treating cancer that include administering a chlorotoxin agent to a subject (e.g., to a subject suffering from or susceptible to the cancer which may, in some embodiments, be a cancer that expresses NRP1). In some embodiments, a chlorotoxin agent for use in accordance with the present invention can be or comprise a chlorotoxin polypeptide and a payload moiety (e.g., as a covalent conjugate).

公开(公告)号：US20190202930A1

公开(公告)日：2019-07-04

申请号：US16357577

申请日：2019-03-19

申请人： Eisai Inc.

发明人： Charles SCHWEIZER ,  Daniel John O'SHANNESSY

IPC分类号： C07K16/30 ,  C07K16/28 ,  A61K39/395 ,  G01N33/574 ,  A61K9/00 ,  A61K45/06 ,  A61K49/00

CPC分类号： C07K16/3092 ,  A61K9/0019 ,  A61K39/39558 ,  A61K45/06 ,  A61K49/00 ,  A61K2039/505 ,  A61K2039/545 ,  C07K16/28 ,  G01N33/57449 ,  G01N2333/4725 ,  G01N2800/52 ,  A61K2300/00

摘要： Provided herein are methods of identifying a subpopulation of ovarian cancer patients who would be responsive to treatment regimens that target folate receptor alpha (FRA)-expressing ovarian tumors and methods of treatment of such patients using an anti-FRA therapeutic agent, such as an antigen-binding protein (e.g., antibody or antigen-binding fragment thereof) that specifically binds to FRA. Also provided are related kits for identification and treatment of the subpopulation of ovarian cancer patients.

公开(公告)号：US20190064172A1

公开(公告)日：2019-02-28

申请号：US16093180

申请日：2017-04-20

申请人： EISAI INC.

发明人： Daniel John O'SHANNESSY

IPC分类号： G01N33/574 ,  G06F19/12

摘要： Described herein are methods of using biomarker levels to detect proteins in a biological sample obtained from a patient with ovarian cancer, calculate a quantitative score for a patient with ovarian cancer, and predict a likelihood of a clinical outcome in a patient with ovarian cancer. The methods involve determining a level of at least three proteins in the biological sample obtained from the patient wherein the at least three proteins are selected from ANG-2, HE4, PROSTASIN, EGFR and IL-8, calculating a quantitative score for the patient by weighting the level of the at least three proteins by their contribution to a clinical outcome, and/or predicting a likelihood of a clinical outcome for the patient based on the quantitative score. Also provided are sets of reagents and test kits to the levels of the biomarkers described herein.

公开(公告)号：US08883787B2

公开(公告)日：2014-11-11

申请号：US13914067

申请日：2013-06-10

申请人： Eisai Inc.

发明人： Weizheng Xu ,  Greg Delahanty ,  Jie Zhang

IPC分类号： A61K31/5025

CPC分类号： C07D491/06 ,  A61K31/495 ,  A61K31/5025

摘要： The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.

摘要翻译： 本发明涉及抑制聚（ADP-核糖）聚合酶（“PARP”）的二氮杂苯并[de]蒽-3-酮化合物，含有这些化合物的组合物和使用这些PARP抑制剂治疗，预防和/或改善 本文所述条件的效果。

公开(公告)号：US20150141429A1

公开(公告)日：2015-05-21

申请号：US14538447

申请日：2014-11-11

申请人： EISAI INC.

发明人： Weizheng XU ,  Greg Delahanty ,  Ling Wei ,  Jie Zhang

IPC分类号： A61K31/519 ,  A61K31/53

CPC分类号： A61K31/519 ,  A61K31/53 ,  C07D487/06 ,  C07D519/00

摘要： The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.

公开(公告)号：US20140186335A1

公开(公告)日：2014-07-03

申请号：US14088465

申请日：2013-11-25

申请人： Eisai Inc.

发明人： Gregory S. Hamilton ,  Takashi Tsukamoto ,  Dana V. Ferraris ,  Bridget Duvall ,  Rena Lapidus

IPC分类号： A61K31/7068 ,  A61K45/06 ,  C07H19/06

CPC分类号： C07H19/06 ,  A61K31/7068 ,  A61K45/06 ,  C07B2200/13 ,  C07H1/00 ,  C07H19/04 ,  C07H19/073

摘要： The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.

摘要翻译： 本发明提供某些四氢尿苷衍生物化合物，包含这些化合物的药物组合物和试剂盒，以及制备和使用这些化合物的方法。

公开(公告)号：US10509037B2

公开(公告)日：2019-12-17

申请号：US15454412

申请日：2017-03-09

申请人： Eisai, Inc.

发明人： Luigi Grasso ,  Nicholas C. Nicolaides ,  Philip M. Sass

IPC分类号： G01N33/574 ,  C07K16/28 ,  C07K16/30 ,  A61K49/00 ,  A61K39/00

摘要： This invention relates to novel monoclonal antibodies that specifically bind to the alpha-folate receptor. In some embodiments, the antibodies inhibit a biological activity of folate receptor-α (FR-α). The antibodies are useful in the treatment of certain cancers, particularly cancers that have increased cell surface expression of the alpha-folate receptor (“FR-α”), such as ovarian, breast, renal, colorectal, lung, endometrial, or brain cancer. The invention also relates to cells expressing the monoclonal antibodies, antibody derivatives, such as chimeric and humanized monoclonal antibodies, antibody fragments, and methods of detecting and treating cancer using the antibodies, derivatives, and fragments.

公开(公告)号：US09040501B2

公开(公告)日：2015-05-26

申请号：US14079944

申请日：2013-11-14

申请人： Eisai Inc.

发明人： Sergel Belyakov ,  Bridget Duvall ,  Dana Ferraris ,  Gregory Hamilton ,  Mark Vaal

IPC分类号： A61K31/7052 ,  A61K31/7068 ,  C07H19/04 ,  A61K45/06 ,  A61K31/7064

CPC分类号： A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K45/06 ,  C07H19/04 ,  A61K2300/00

摘要： Provided herein are compounds used to inhibit the deamination enzyme responsible for the inactivation of therapeutic compounds, and methods of using them.

摘要翻译： 本文提供了用于抑制负责灭活治疗化合物的脱氨酶的化合物及其使用方法。

公开(公告)号：US08951987B2

公开(公告)日：2015-02-10

申请号：US14088465

申请日：2013-11-25

申请人： Eisai Inc.

发明人： Gregory S. Hamilton ,  Takashi Tsukamoto ,  Dana V. Ferraris ,  Bridget Duvall ,  Rena Lapidus

IPC分类号： A61K31/70 ,  A61K31/7068 ,  C07H19/04 ,  A61K45/06 ,  C07H19/06

CPC分类号： C07H19/06 ,  A61K31/7068 ,  A61K45/06 ,  C07B2200/13 ,  C07H1/00 ,  C07H19/04 ,  C07H19/073

摘要： The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.

摘要翻译： 本发明提供某些四氢尿苷衍生物化合物，包含这些化合物的药物组合物和试剂盒，以及制备和使用这些化合物的方法。

公开(公告)号：US08609631B2

公开(公告)日：2013-12-17

申请号：US13665184

申请日：2012-10-31

申请人： Eisai Inc.

发明人： Sergei Belyakov ,  Bridget Duvall ,  Dana Ferraris ,  Gregory Hamilton ,  Mark Vaal

IPC分类号： A61K31/7052 ,  C07H19/04

CPC分类号： A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K45/06 ,  C07H19/04 ,  A61K2300/00

摘要： Provided herein are compounds used to inhibit the deamination enzyme responsible for the inactivation of therapeutic compounds, and methods of using them.