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    CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND IMMUNE CHECKPOINT INHIBITOR
    1.
    发明申请
    CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND IMMUNE CHECKPOINT INHIBITOR 有权

    公开(公告)号：US20220125793A1

    公开(公告)日：2022-04-28

    申请号：US17434573

    申请日：2020-02-28

    申请人： TAIHO PHARMACEUTICAL CO., LTD.

    发明人： Kazuhiko YONEKURA ,  Hiroshi HIRAI ,  Kazuaki MATSUOKA

    IPC分类号： A61K31/519 ,  A61K39/395 ,  A61P35/00

    摘要： The problem to be solved by the present disclosure is to provide a novel combination therapy using (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof, the combination therapy exhibiting an excellent antitumor effect on cancer patients with resistance to immune checkpoint inhibitors. The present disclosure provides an antitumor agent comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient, the antitumor agent being administered in combination with an immune checkpoint inhibitor, except for pembrolizumab, to a cancer patient with resistance to immune checkpoint inhibitors.

    METHOD FOR ENHANCING ANTI-TUMOR EFFECT OF A MICROTUBULE-TARGETING DRUG, AND A METHOD FOR TREATMENT OF TUMOR
    2.
    发明申请
    METHOD FOR ENHANCING ANTI-TUMOR EFFECT OF A MICROTUBULE-TARGETING DRUG, AND A METHOD FOR TREATMENT OF TUMOR 有权
    用于增强微血管收缩药物的抗肿瘤效果的方法和用于治疗肿瘤的方法

    公开(公告)号：US20150065479A1

    公开(公告)日：2015-03-05

    申请号：US14010684

    申请日：2013-08-27

    申请人： TAIHO PHARMACEUTICAL CO., LTD.

    发明人： Hiroshi HIRAI ,  Hiroshi SOOTOME

    IPC分类号： A61K47/22 ,  A61K31/337

    CPC分类号： A61K47/22 ,  A61K31/337 ,  A61K31/415 ,  A61K31/4545 ,  A61K2300/00

    摘要： A method for treating a tumor by combining a piperidine compound of formula (I) or salt thereof and a microtubule-targeting drug, in which the microtubule-targeting drug is administered once per 7 days or more one cycle, and the piperidine compound is administered once or more per day for 4 days or more: R1 represents a carboxyl group, —C(═O)NR5R6, or an oxadiazolyl group optionally substituted with a C1-C6 alkyl group or trifluoromethyl group; R2 represents a halogen atom or C1-C6 alkoxy group; R3 represents a phenyl group optionally having 1 to 3 groups, selected from a halogen atom, and a C1-C6 alkyl, C1-C6 alkoxy, or trifluoromethyl group; R4 represents a hydrogen atom or C1-C6 alkyl group; and R5 and R6, each represent a hydrogen atom, a C1-C6 alkyl or C3-C6 cycloalkyl group; or R5 and R6, together with a nitrogen atom, optionally form a 3 to 6-membered nitrogen-containing saturated heterocyclic group.

    摘要翻译： 通过将式（I）的哌啶化合物或其盐与微管靶向药物组合来治疗肿瘤的方法，其中微管靶向药物每7天或更多个循环施用一次，给予哌啶化合物 每天一次或多次4天以上：R1表示羧基，-C（= O）NR5R6或任选被C1-C6烷基或三氟甲基取代的恶二唑基; R2表示卤素原子或C1-C6烷氧基; R3表示任选具有1至3个选自卤素原子和C 1 -C 6烷基，C 1 -C 6烷氧基或三氟甲基的苯基; R4表示氢原子或C1-C6烷基; 和R 5和R 6各自表示氢原子，C 1 -C 6烷基或C 3 -C 6环烷基; 或R 5和R 6与氮原子一起任选形成3至6元含氮饱和杂环基。

    CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND PEMBROLIZUMAB
    3.
    发明申请
    CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND PEMBROLIZUMAB 有权

    公开(公告)号：US20220184082A1

    公开(公告)日：2022-06-16

    申请号：US17434655

    申请日：2020-02-28

    申请人： TAIHO PHARMACEUTICAL CO., LTD.

    发明人： Kazuhiko YONEKURA ,  Hiroshi HIRAI ,  Kazuaki MATSUOKA

    IPC分类号： A61K31/519 ,  A61K39/395 ,  A61P35/00

    摘要： The problem to be solved by the present disclosure is to provide a novel combination therapy using (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof, the combination therapy exhibiting an excellent antitumor effect on cancer patients with resistance to immune checkpoint inhibitors. The present disclosure provides an antitumor agent comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient, the antitumor agent being administered in combination with pembrolizumab to a cancer patient with resistance to immune checkpoint inhibitors.

    ANTITUMOR DRUG FOR INTERMITTENT ADMINISTRATION OF FGFR INHIBITOR
    4.
    发明申请
    ANTITUMOR DRUG FOR INTERMITTENT ADMINISTRATION OF FGFR INHIBITOR 审中-公开

    公开(公告)号：US20190183897A1

    公开(公告)日：2019-06-20

    申请号：US16274573

    申请日：2019-02-13

    申请人： Taiho Pharmaceutical Co., Ltd.

    发明人： Hiroaki OCHIIWA ,  Hiroshi HIRAI

    IPC分类号： A61K31/519 ,  A61K31/5377 ,  C07D487/04 ,  A61K31/437

    CPC分类号： A61K31/519 ,  A61K31/437 ,  A61K31/5377 ,  C07D487/04

    摘要： The problems to be solved by the present invention are to provide a novel FGFR inhibitor that is potent and highly selective, and to provide an antitumor agent with which side effects such as an elevated blood phosphorus concentration are alleviated while maintaining the antitumor effect of the FGFR inhibitor. The present invention provides an antitumor agent comprising a 3,5-di-substituted benzene alkynyl compound represented by general formula (I) or salt thereof, which is used by administering the 3,5-di-substituted benzene alkynyl compound or salt thereof according to an administration schedule of two or more times/week at an administration interval of at least one day between doses.

    ANTITUMOR AGENT AND METHOD FOR TUMOR THERAPY
    6.
    发明申请
    ANTITUMOR AGENT AND METHOD FOR TUMOR THERAPY 有权

    公开(公告)号：US20210236475A1

    公开(公告)日：2021-08-05

    申请号：US17059376

    申请日：2019-05-28

    申请人： TAIHO PHARMACEUTICAL CO., LTD.

    发明人： Hiroshi HIRAI

    IPC分类号： A61K31/4545 ,  A61K31/337 ,  A61P35/00

    摘要： Provided is an effective method for using an orally administrable compound having an excellent Aurora A selective inhibitory effect, and a microtubule-targeting drug in combination. The present invention provides a method for treatment of malignant tumor by a combination of 1-(2,3-dichlorobenzoyl)-4-[5-fluoro-6-(5-methyl-1H-pyrazol-3-ylamino)pyridin-2-yl]methyl-4-piperidinecarboxylic acid (compound I) or a salt thereof and a microtubule-targeting drug, wherein the following administration schedule thereof is performed: one cycle involves 7 days; the microtubule-targeting drug is administered once; and the compound I or the salt thereof is administered for 3 consecutive days with cessation of the drug for remaining 4 days.

    ANTITUMOR DRUG FOR INTERMITTENT ADMINISTRATION OF FGFR INHIBITOR
    7.
    发明申请
    ANTITUMOR DRUG FOR INTERMITTENT ADMINISTRATION OF FGFR INHIBITOR 审中-公开
    抗生素药物用于FGFR抑制剂的间歇性给药

    公开(公告)号：US20160193210A1

    公开(公告)日：2016-07-07

    申请号：US14905420

    申请日：2014-07-17

    申请人： TAIHO PHARMACEUTICAL CO., LTD.

    发明人： Hiroaki OCHIIWA ,  Hiroshi HIRAI

    IPC分类号： A61K31/519

    摘要： The problem to be solved by the present invention is to provide a potent and highly selective novel FGFR inhibitor, and an antitumor agent having reduced side effects, such as increased blood phosphorus levels, while maintaining the antitumor effect of the FGFR inhibitor. The present invention provides an antitumor agent comprising a 3,5-disubstituted benzene alkynyl compound represented by Formula (I) or a salt thereof that is used so that the 3,5-disubstituted benzene alkynyl compound or a salt thereof is administered on an administration schedule of at least twice a week and a dosing interval of at least one day.

    摘要翻译： 本发明要解决的问题是提供一种有效和高度选择性的新型FGFR抑制剂和具有降低的副作用的抗肿瘤剂，例如增加血磷水平，同时保持FGFR抑制剂的抗肿瘤作用。 本发明提供一种抗肿瘤剂，其包含由式（I）表示的3,5-二取代苯炔基化合物或其盐，其用于使得3,5-二取代的苯炔基化合物或其盐在给药 每周至少两次的时间表和至少一天的给药间隔。