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公开(公告)号：US10124003B2
公开(公告)日：2018-11-13
申请号：US14905047
申请日：2014-07-17
发明人： Hiroshi Sootome
IPC分类号： A61K31/519 , A61K31/437 , A61K31/404 , A61K31/44 , A61K31/47 , A61K31/496 , A61K31/5025 , A61K31/506 , A61K31/53 , A61K31/5377
摘要： The problem to be solved by the present invention is to provide an anticancer agent for treating tumors resistant to other antitumor agents that inhibit FGFR, and a method for treating such tumors. The present invention provides an antitumor agent for administration to a tumor patient resistant to an FGFR inhibitor, the antitumor agent comprising a 3,5-disubstituted benzene alkynyl compound represented by Formula (I) below or a salt thereof. The present invention also provides a therapeutic method using the anticancer agent.
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2.发明授权公开(公告)号：US09012475B2
公开(公告)日：2015-04-21
申请号：US14010684
申请日：2013-08-27
发明人： Hiroshi Hirai , Hiroshi Sootome
IPC分类号： A61K31/445 , A61K31/335 , A61K47/22 , A61K31/337 , A61K31/415
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，并给予哌啶化合物 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。
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公开(公告)号：US11883404B2
公开(公告)日：2024-01-30
申请号：US16448648
申请日：2019-06-21
发明人： Akihiro Miura , Hiroshi Sootome , Junya Iwasaki
IPC分类号： A61K31/519 , A61K31/5383 , A61P35/00
CPC分类号： A61K31/519 , A61K31/5383 , A61P35/00
摘要： It is intended to provide a novel method for treating a cancer using an FGFR inhibitor that exhibits a remarkably excellent antitumor effect and has fewer side effects. The present invention provides a combination preparation for the treatment of a malignant tumor comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof, and one or more additional compound(s) having an antitumor effect or pharmaceutically acceptable salt(s) thereof, and a pharmaceutical composition comprising both the active ingredients. The present invention also provides an antitumor effect enhancer, an antitumor agent, a kit for malignant tumor treatment, etc. comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US11975002B2
公开(公告)日：2024-05-07
申请号：US16082117
申请日：2017-03-03
发明人： Akihiro Miura , Hiroshi Sootome
IPC分类号： A61K31/5025 , A61K33/243 , A61K45/06
CPC分类号： A61K31/5025 , A61K33/243 , A61K45/06
摘要： It is intended to provide a novel method for treating a cancer using an FGFR inhibitor that exhibits a remarkably excellent antitumor effect and has fewer side effects. The present invention provides a combination preparation for the treatment of a malignant tumor comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof, and one or more additional compound(s) having an antitumor effect or pharmaceutically acceptable salt(s) thereof, and a pharmaceutical composition comprising both the active ingredients. The present invention also provides an antitumor effect enhancer, an antitumor agent, a kit for malignant tumor treatment, etc. comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US11690843B2
公开(公告)日：2023-07-04
申请号：US16082117
申请日：2017-03-03
发明人： Akihiro Miura , Hiroshi Sootome
IPC分类号： A61K31/5025 , A61K33/243 , A61K45/06
CPC分类号： A61K31/5025 , A61K33/243 , A61K45/06
摘要： It is intended to provide a novel method for treating a cancer using an FGFR inhibitor that exhibits a remarkably excellent antitumor effect and has fewer side effects. The present invention provides a combination preparation for the treatment of a malignant tumor comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof, and one or more additional compound(s) having an antitumor effect or pharmaceutically acceptable salt(s) thereof, and a pharmaceutical composition comprising both the active ingredients. The present invention also provides an antitumor effect enhancer, an antitumor agent, a kit for malignant tumor treatment, etc. comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US09108973B2
公开(公告)日：2015-08-18
申请号：US14344935
申请日：2013-01-17
发明人： Takeshi Sagara , Satoru Ito , Sachie Otsuki , Hiroshi Sootome
IPC分类号： C07D487/04 , C07D471/04 , A61K31/519 , A61K31/437
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention provides a compound represented by Formula (I) (wherein R1, X1, X2, Y, and Z are as defined in the specification), or a salt thereof.
摘要翻译： 本发明提供由式（I）表示的化合物或其盐，其中R1，X1，X2，Y和Z如说明书中所定义。
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公开(公告)号：US10092556B2
公开(公告)日：2018-10-09
申请号：US15131372
申请日：2016-04-18
IPC分类号： A61K31/4545 , C07D401/14 , C07D413/14 , A61K31/337 , C07D417/14 , A61K45/06
摘要： A novel compound which has an excellent aurora A-selective inhibitory action and is useful as an orally administrable anticancer agent is provided. Also, a novel agent for potentiation of anti-tumor effect of microtubule agonists, which include a taxane anticancer agent, and a combination therapy are provided. A piperidine compound represented by a general formula (I) or a salt thereof: wherein, R1 represents a carboxyl group, —C(═O)NR5R6, or an oxadiazolyl group optionally having a C1-C6 alkyl group or a trifluoromethyl group as a substituent; R2 represents a halogen atom or a C1-C6 alkoxy group; R3 represents a phenyl group optionally having 1 to 3 same or different group(s) selected from a halogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group, and a trifluoromethyl group as a substituent; R4 represents a hydrogen atom or a C1-C6 alkyl group; and R5 and R6 are the same or different and each represent a hydrogen atom, a C1-C6 alkyl group, or a C3-C6 cycloalkyl group, or R5 and R6 optionally form a 3 to 6-membered nitrogen-containing saturated heterocyclic group together with a nitrogen atom to which R5 and R6 are bound, are provided.
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公开(公告)号：US09346787B2
公开(公告)日：2016-05-24
申请号：US14381814
申请日：2013-02-27
IPC分类号： C07D417/14 , A61K31/4545 , A61K45/06 , C07D401/14 , C07D413/14 , A61K31/337
CPC分类号： A61K31/4545 , A61K31/337 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： A novel compound which has an excellent aurora A-selective inhibitory action and is useful as an orally administrable anticancer agent is provided. Also, a novel agent for potentiation of anti-tumor effect of microtubule agonists, which include a taxane anticancer agent, and a combination therapy are provided. A piperidine compound represented by a general formula (I) or a salt thereof: wherein, R1 represents a carboxyl group, —C(═O)NR5R6, or an oxadiazolyl group optionally having a C1-C6 alkyl group or a trifluoromethyl group as a substituent; R2 represents a halogen atom or a C1-C6 alkoxy group; R3 represents a phenyl group optionally having 1 to 3 same or different group(s) selected from a halogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group, and a trifluoromethyl group as a substituent; R4 represents a hydrogen atom or a C1-C6 alkyl group; and R5 and R6 are the same or different and each represent a hydrogen atom, a C1-C6 alkyl group, or a C3-C6 cycloalkyl group, or R5 and R6 optionally form a 3 to 6-membered nitrogen-containing saturated heterocyclic group together with a nitrogen atom to which R5 and R6 are bound, are provided.
摘要翻译： 提供了具有优异的极光A选择性抑制作用并可用作口服给药的抗癌剂的新型化合物。 另外，提供了增强微管激动剂的抗肿瘤作用的新型药剂，其包括紫杉烷抗癌剂和联合疗法。 由通式（I）表示的哌啶化合物或其盐：其中，R 1表示羧基，-C（= O）NR 5 R 6或任选具有C 1 -C 6烷基或三氟甲基的恶二唑基作为 取代基; R2表示卤素原子或C1-C6烷氧基; R3表示任选具有1〜3个相同或不同的选自卤素原子，C1-C6烷基，C1-C6烷氧基和三氟甲基作为取代基的苯基; R4表示氢原子或C1-C6烷基; 并且R 5和R 6相同或不同，各自表示氢原子，C 1 -C 6烷基或C 3 -C 6环烷基，或者R 5和R 6可以一起形成3至6元含氮饱和杂环基 与其中R 5和R 6结合的氮原子。
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公开(公告)号：US20150045342A1
公开(公告)日：2015-02-12
申请号：US14381814
申请日：2013-02-27
IPC分类号： C07D401/14 , A61K45/06 , A61K31/4545
CPC分类号： A61K31/4545 , A61K31/337 , A61K45/06 , C07D401/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： A novel compound which has an excellent aurora A-selective inhibitory action and is useful as an orally administrable anticancer agent is provided. Also, a novel agent for potentiation of anti-tumor effect of microtubule agonists, which include a taxane anticancer agent, and a combination therapy are provided. A piperidine compound represented by a general formula (I) or a salt thereof: wherein, R1 represents a carboxyl group, —C(═O)NR5R6, or an oxadiazolyl group optionally having a C1-C6 alkyl group or a trifluoromethyl group as a substituent; R2 represents a halogen atom or a C1-C6 alkoxy group; R3 represents a phenyl group optionally having 1 to 3 same or different group(s) selected from a halogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group, and a trifluoromethyl group as a substituent; R4 represents a hydrogen atom or a C1-C6 alkyl group; and R5 and R6 are the same or different and each represent a hydrogen atom, a C1-C6 alkyl group, or a C3-C6 cycloalkyl group, or R5 and R6 optionally form a 3 to 6-membered nitrogen-containing saturated heterocyclic group together with a nitrogen atom to which R5 and R6 are bound, are provided.
摘要翻译： 提供了具有优异的极光A选择性抑制作用并可用作口服给药的抗癌剂的新型化合物。 另外，提供了增强微管激动剂的抗肿瘤作用的新型药剂，其包括紫杉烷抗癌剂和联合疗法。 由通式（I）表示的哌啶化合物或其盐：其中，R 1表示羧基，-C（= O）NR 5 R 6或任选具有C 1 -C 6烷基或三氟甲基的恶二唑基作为 取代基; R2表示卤素原子或C1-C6烷氧基; R3表示任选具有1〜3个相同或不同的选自卤素原子，C1-C6烷基，C1-C6烷氧基和三氟甲基作为取代基的苯基; R4表示氢原子或C1-C6烷基; 并且R 5和R 6相同或不同，各自表示氢原子，C 1 -C 6烷基或C 3 -C 6环烷基，或者R 5和R 6可以一起形成3至6元含氮饱和杂环基 与其中R 5和R 6结合的氮原子。
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公开(公告)号：US20140343035A1
公开(公告)日：2014-11-20
申请号：US14344935
申请日：2013-01-17
发明人： Takeshi Sagara , Satoru Ito , Sachie Otsuki , Hiroshi Sootome
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention provides a compound represented by Formula (I) (wherein R1, X1, X2, Y, and Z are as defined in the specification), or a salt thereof.
摘要翻译： 本发明提供由式（I）表示的化合物或其盐，其中R1，X1，X2，Y和Z如说明书中所定义。
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