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NOVEL PIPERIDINE COMPOUND OR SALT THEREOF
专利权人:
TAIHO PHARMACEUTICAL CO.; LTD.
发明人:
SUGIMOTO, TETSUYA,TAKAHASHI, HIDEKAZU,MITSUYA, MORIHIRO,MASUKO, NORIO,SOOTOME, HIROSHI
申请号:
SG11201405318P
公开号:
SG11201405318PA
申请日:
2013.02.27
申请国别(地区):
SG
年份:
2014
代理人:
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, R 1 represents a carboxyl group, -C(=O)NR 5 R 6 , or an oxadiazolyl group optionally having a C 1 -C 6 alkyl group or a trifluoromethyl group as a substituent R 2 represents a halogen atom or a C 1 -C 6 alkoxy group R 3 represents a phenyl group optionally having 1 to 3 same or different group(s) selected from a halogen atom, a C 1 -C 6 alkyl group, a C 1 -C 6 alkoxy group, and a trifluoromethyl group as a substituent R 4 represents a hydrogen atom or a C 1 -C 6 alkyl group and R 5 and R 6 are the same or different and each represent a hydrogen atom, a C 1 -C 6 alkyl group, or a C 3 -C 6 cycloalkyl group, or R 5 and R 6 optionally form a 3 to 6-membered nitrogen-containing saturated heterocyclic group together with a nitrogen atom to which R 5 and R 6 are bound, are provided.本發明提供一種具有優異之Aurora A選擇性抑制作用、用作可經口投予之抗癌劑的新穎化合物,進而提供一種含有紫杉烷系抗癌劑之微管促效劑的新穎抗腫瘤效果增強劑及併用療法。本發明係一種哌啶化合物或其鹽,該哌啶化合物係通式(I)所示者(式中,R1表示羧基、-C(=O)NR5R6、或可具有C1-C6烷基或三氟甲基作為取代基之二唑基;R2表示鹵素原子或C1-C6烷氧基;R3表示可具有1~3個相同或不同之選自鹵素原子、C1-C6烷基、C1-C6烷氧基及三氟甲基中之基作為取代基的苯基;R4表示氫原子或C1-C6烷基;R5及R6相同或不同,表示氫原子、C1-C6烷基或C3-C6環烷基,或者R5及R6亦可與所鍵結之氮原子一併形成3~6員之含氮飽和雜環基)。
来源网站:
中国工程科技知识中心
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