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公开(公告)号：US10774087B2
公开(公告)日：2020-09-15
申请号：US16463792
申请日：2017-11-22
发明人： Masahiro Ota , Hidekazu Inoue , Junya Kawai , Hitoshi Ohki , Tadashi Toki
IPC分类号： C07D491/052 , A61K31/496 , A61P35/00 , A61P43/00
摘要： Provided is a novel compound or a salt thereof inhibiting MTHFD2 and useful for treating a disease caused by overexpression of MTHFD2, a disease involved in overexpression of MTHFD2 and/or a disease associated with overexpression of MTHFD2.SolutionProvided is a sulfonamide derivative having a coumarin skeleton represented by the following formula (I) and having various substituents: wherein R1, R2, R3, R4, R5, R6 and R7 are the same as defined in the specification, and a salt thereof.
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公开(公告)号：US20190284198A1
公开(公告)日：2019-09-19
申请号：US16463792
申请日：2017-11-22
发明人： Masahiro Ota , Hidekazu Inoue , Junya Kawai , Hitoshi Ohki , Tadashi Toki
IPC分类号： C07D491/052 , A61P35/00
摘要： Provided is a novel compound or a salt thereof inhibiting MTHFD2 and useful for treating a disease caused by overexpression of MTHFD2, a disease involved in overexpression of MTHFD2 and/or a disease associated with overexpression of MTHFD2.SolutionProvided is a sulfonamide derivative having a coumarin skeleton represented by the following formula (I) and having various substituents: wherein R1, R2, R3, R4, R5, R6 and R7 are the same as defined in the specification, and a salt thereof.
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公开(公告)号：US20140371249A1
公开(公告)日：2014-12-18
申请号：US14473733
申请日：2014-08-29
发明人： Yasusi Ueda , Nobuyuki Suzuki , Hitoshi Ohki
IPC分类号： C07D495/16
CPC分类号： C07D495/16 , A61K31/55 , C07D417/06
摘要： To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like.
摘要翻译： 提供抑制HSP90作用的三环吡唑并嘧啶化合物的晶体。 本发明提供2- {4-氨基-2 - [（3-氯-4-甲氧基-5-甲基吡啶-2-基）甲基] -2,7-二氢-6-硫杂-1,2 ，抑制HSP90的ATP酶活性，具有抗肿瘤活性的3,5-四氮杂苯并[cd]薁-8-基} -N-甲基乙酰胺，含有它们的药物，含有该抗体的抗癌剂等。
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公开(公告)号：US08846703B2
公开(公告)日：2014-09-30
申请号：US13773419
申请日：2013-02-21
发明人： Yasusi Ueda , Nobuyuki Suzuki , Hitoshi Ohki
IPC分类号： A61K31/55 , C07D417/06 , C07D495/16
CPC分类号： C07D495/16 , A61K31/55 , C07D417/06
摘要： To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like.
摘要翻译： 提供抑制HSP90作用的三环吡唑并嘧啶化合物的晶体。 本发明提供2- {4-氨基-2 - [（3-氯-4-甲氧基-5-甲基吡啶-2-基）甲基] -2,7-二氢-6-硫杂-1,2 ，抑制HSP90的ATP酶活性，具有抗肿瘤活性的3,5-四氮杂苯并[cd]薁-8-基} -N-甲基乙酰胺，含有它们的药物，含有该抗体的抗癌剂等。
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公开(公告)号：US20130211084A1
公开(公告)日：2013-08-15
申请号：US13773419
申请日：2013-02-21
发明人： Yasusi Ueda , Nobuyuki Suzuki , Hitoshi Ohki
IPC分类号： C07D495/16
CPC分类号： C07D495/16 , A61K31/55 , C07D417/06
摘要： To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like.
摘要翻译： 提供抑制HSP90作用的三环吡唑并嘧啶化合物的晶体。 本发明提供2- {4-氨基-2 - [（3-氯-4-甲氧基-5-甲基吡啶-2-基）甲基] -2,7-二氢-6-硫杂-1,2 ，抑制HSP90的ATP酶活性，具有抗肿瘤活性的3,5-四氮杂苯并[cd]薁-8-基} -N-甲基乙酰胺，含有它们的药物，含有该抗体的抗癌剂等。
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公开(公告)号：US08933103B2
公开(公告)日：2015-01-13
申请号：US13753926
申请日：2013-01-30
发明人： Hitoshi Ohki , Masahiro Ota , Kosuke Takeuchi , Hideaki Watanabe , Akitake Yamaguchi , Yoshihiro Shibata , Yuichi Tominaga , Takeshi Jimbo , Keijiro Kobayashi , Katsuhiro Kobayashi , Daisuke Fukatsu
IPC分类号： C07D401/12 , C07D413/14 , A61K31/44 , A61P35/00 , C07D213/82 , C07D401/14 , C07D405/14 , C07D451/02
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D451/02
摘要： Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.
摘要翻译： 提供了抑制Ax1并可用于治疗由Axl功能障碍引起的疾病，与Axl功能异常和/或伴有Axl功能障碍的疾病有关的疾病的新型化合物或其盐或其结晶。 具有各种取代基或其盐的式（1）表示的吡啶酮衍生物或其结晶（式（1）中的R 1，R 2，R 3，R 5，R 6，A，W，X和n如本说明书中所定义） ，分别）。
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公开(公告)号：US20130281428A1
公开(公告)日：2013-10-24
申请号：US13753926
申请日：2013-01-30
发明人： Hitoshi Ohki , Masahiro Ota , Kosuke Takeuchi , Hideaki Watanabe , Akitake Yamaguchi , Yoshihiro Shibata , Yuichi Tominaga , Takeshi Jimbo , Keijiro Kobayashi , Katsuhiro Kobayashi , Daisuke Fukatsu
IPC分类号： C07D213/82 , C07D401/12 , C07D413/14 , C07D451/02 , C07D405/14 , C07D401/14
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D451/02
摘要： Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.
摘要翻译： 提供了抑制Ax1并可用于治疗由Axl功能障碍引起的疾病，与Axl功能异常和/或伴有Axl功能障碍的疾病有关的疾病的新型化合物或其盐或其结晶。 具有各种取代基或其盐的式（1）表示的吡啶酮衍生物或其结晶（式（1）中的R 1，R 2，R 3，R 5，R 6，A，W，X和n如本说明书中所定义） ，分别）。
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