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公开(公告)号：US10100030B2
公开(公告)日：2018-10-16
申请号：US15034808
申请日：2014-11-06
发明人： Kazuo Shimizu , Takashi Miyagi , Kohsuke Ohno , Yasunori Ueno , Yusuke Onda , Hikaru Suzuki
IPC分类号： C07D401/04 , C07D413/14
摘要： The present invention provides a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to carboxymethyl piperidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Wherein, ring A is a benzene ring or the like; ring B is a pyridine ring or the like; R1 is C1-6 alkyl or C1-6 alkoxy; R2 and R3 are a hydrogen atom or methyl; and n is an integral number from 0 to 5.
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公开(公告)号：US09718771B2
公开(公告)日：2017-08-01
申请号：US15121522
申请日：2015-02-27
发明人： Hitoshi Inoue , Kohsuke Ohno , Tetsuya Nakamura , Yusuke Ohsawa
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： A compound having an S1P1 receptor antagonistic activity. A compound represented by general formula (I): (in the formula, R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group or the like, R4 is a C1-6 alkyl group or the like, R5 is a C1-6 alkyl group or the like, R6 is a C1-6 alkyl group or the like, R7 is a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like, R8 is a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group or the like, and R9 is a hydrogen atom or a C1-6 alkyl group.) or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same, and use thereof. The compounds have an excellent S1P1 receptor antagonistic activity and are useful for the treatment or prevention of autoimmune diseases.
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公开(公告)号：US20170320821A1
公开(公告)日：2017-11-09
申请号：US15659760
申请日：2017-07-26
发明人： Hitoshi Inoue , Kohsuke Ohno , Tetsuya Nakamura , Yusuke Ohsawa
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： [Problem] The present invention provides a novel compound having an S1P1 receptor antagonistic activity.[Solution] The present invention provides a compound represented by the general formula (I): (in the formula, Rl, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group or the like, R4 is a C1-6 alkyl group or the like, R5 is a C1-6 alkyl group or the like, R6 is a C1-6 alkyl group or the like, R7 is a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like, R8 is a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group or the like, and R9 is a hydrogen atom or a C1-6 alkyl group.) or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same, and use thereof. The compounds of the present invention have an excellent S1P1 receptor antagonistic activity and therefore are useful as an agent for the treatment or prevention of antoimmune diseases and the like.
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公开(公告)号：US10011568B2
公开(公告)日：2018-07-03
申请号：US15630238
申请日：2017-06-22
发明人： Kazuo Shimizu , Kohsuke Ohno , Takashi Miyagi , Yasunori Ueno , Hikaru Suzuki
IPC分类号： C07D213/75 , C07D213/84
摘要： A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof, wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; R1 is carboxymethyl or the like; R2 is alkyl or the like; Y is 0-2 or the like; U is —N(CH3)COC(CH3)2-3,5-bistrifluoromethylphenyl or the like.
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公开(公告)号：US09988350B2
公开(公告)日：2018-06-05
申请号：US15659760
申请日：2017-07-26
发明人： Hitoshi Inoue , Kohsuke Ohno , Tetsuya Nakamura , Yusuke Ohsawa
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： The present invention provides a compound represented by the general formula (I): in the formula, R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group or the like, R4 is a C1-6 alkyl group or the like, R5 is a C1-6 alkyl group or the like, R6 is a C1-6 alkyl group or the like, R7 is a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like, R8 is a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group or the like, and R9 is a hydrogen atom or a C1-6 alkyl group, or a pharmaceutically acceptable salt thereof. The compounds of the present invention have an excellent S1P1 receptor antagonistic activity and therefore are useful as an agent for the treatment or prevention of autoimmune diseases and the like.
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6.发明申请NOVEL ANILINE DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USE THEREOF 有权新型苯胺衍生物，含有它们的药物组合物及其用途公开(公告)号：US20160362368A1
公开(公告)日：2016-12-15
申请号：US15121522
申请日：2015-02-27
发明人： Hitoshi Inoue , Kohsuke Ohno , Tetsuya Nakamura , Yusuke Ohsawa
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： [Problem] The present invention provides a novel compound having an S1P1 receptor antagonistic activity.[Solution] The present invention provides a compound represented by the general formula (I): (in the formula, R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group or the like, R4 is a C1-6 alkyl group or the like, R5 is a C1-6 alkyl group or the like, R6 is a C1-6 alkyl group or the like, R7 is a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like, R8 is a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group or the like, and R9 is a hydrogen atom or a C1-6 alkyl group.) or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same, and use thereof. The compounds of the present invention have an excellent S1P1 receptor antagonistic activity and therefore are useful as an agent for the treatment or prevention of autoimmune diseases and the like.
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公开(公告)号：US20170298024A1
公开(公告)日：2017-10-19
申请号：US15630238
申请日：2017-06-22
发明人： Kazuo Shimizu , Kohsuke Ohno , Takashi Miyagi , Yasunori Ueno , Hikaru Suzuki
IPC分类号： C07D213/75 , C07D213/84
CPC分类号： C07D213/75 , A61K31/4418 , C07D213/76 , C07D213/84
摘要： A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof, wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; R1 is carboxymethyl or the like; R2 is alkyl or the like; Y is 0-2 or the like; U is —N(CH3)COC(CH3)2-3,5-bistrifluoromethylphenyl or the like.
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公开(公告)号：US09708266B2
公开(公告)日：2017-07-18
申请号：US15308996
申请日：2015-05-07
发明人： Kazuo Shimizu , Kohsuke Ohno , Takashi Miyagi , Yasunori Ueno , Hikaru Suzuki
IPC分类号： C07D213/75 , C07D213/84 , A61K31/4418 , C07D213/76
CPC分类号： C07D213/75 , A61K31/4418 , C07D213/76 , C07D213/84
摘要： A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; R1 is carboxymethyl or the like; R2 is alkyl or the like; Y is 0-2 or the like; U is —N(CH3)COC(CH3)2-3,5-bistrifluoromethylphenyl or the like.
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公开(公告)号：US20170057920A1
公开(公告)日：2017-03-02
申请号：US15308996
申请日：2015-05-07
发明人： Kazuo Shimizu , Kohsuke Ohno , Takashi Miyagi , Yasunori Ueno , Hikaru Suzuki
IPC分类号： C07D213/84 , C07D213/75
CPC分类号： C07D213/75 , A61K31/4418 , C07D213/76 , C07D213/84
摘要： A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; R1 is carboxymethyl or the like; R2 is alkyl or the like; Y is 0-2 or the like; U is —N(CH3)COC(CH3)2-3,5-bistrifluoromethylphenyl or the like.
摘要翻译： 提供了具有NK1受体拮抗作用的新型化合物，其可用于预防和治疗伴随施用抗肿瘤药物的恶心和呕吐，其与阿美瑞明相比具有减少的CYP3A4抑制作用。 也就是说，本发明涉及由式（I）表示的环己基 - 吡啶衍生物或其药理学上可接受的盐。 式中，环A为4-氟-2-甲基苯基等，X为氢原子等，R1为羧甲基等，R2为烷基等，Y为0-2 U是-N（CH 3）COC（CH 3）2-3,5-双（三氟甲基）苯基等。
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公开(公告)号：US20160289206A1
公开(公告)日：2016-10-06
申请号：US15034808
申请日：2014-11-06
发明人： Kazuo Shimizu , Takashi Miyagi , Kohsuke Ohno , Yasunori Ueno , Yusuke Onda , Hikaru Suzuki
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D413/14
摘要： The present invention provides a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to carboxymethyl piperidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Wherein, ring A is a benzene ring or the like; ring B is a pyridine ring or the like; R1 is C1-6 alkyl or C1-6 alkoxy; R2 and R3 are a hydrogen atom or methyl; and n is an integral number from 0 to 5.
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