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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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