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公开(公告)号:US20070276017A1
公开(公告)日:2007-11-29
申请号:US10560230
申请日:2004-06-09
申请人: Chikara Murakata , Yoji Ino , Kazuhiko Kato , Junichiro Yamamoto , Yushi Kitamura , Ryuichiro Nakai , Tomohisa Nakano , Tetsuya Tsujita
发明人: Chikara Murakata , Yoji Ino , Kazuhiko Kato , Junichiro Yamamoto , Yushi Kitamura , Ryuichiro Nakai , Tomohisa Nakano , Tetsuya Tsujita
IPC分类号: A61K31/454 , C07D285/12 , A61K31/433 , C07D417/02
CPC分类号: C07D285/135
摘要: A thiadiazoline derivative represented by the general formula (I), or a pharmacologically acceptable salt thereof: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —COR5 (wherein R5 represents lower alkyl and the like) and the like, R3 represents lower alkyl and the like, R4 represents aryl and the like, A represents —(CH2)n— (wherein n represents an integer of 1 to 6) and the like, and B represents —NR6R7 (wherein R6 and R7 are the same or different and represent a hydrogen atom, lower alkyl and the like) and the like] is provided.
摘要翻译: 由通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐:[其中R 1表示氢原子等,R 2表示氢 原子,-COR 5(其中R 5表示低级烷基等)等,R 3表示低级烷基等, R 4表示芳基等,A表示 - (CH 2 CH 2)n - (其中n表示1至6的整数)和 和B代表-NR 6 R 7(其中R 6和R 7和R 7相同或不同) 不同,表示氢原子,低级烷基等)等。
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公开(公告)号:US20080194653A1
公开(公告)日:2008-08-14
申请号:US11909289
申请日:2006-03-22
申请人: Chikara Murakata , Kazuhiko Kato , Junichiro Yamamoto , Ryuichiro Nakai , Seiho Okamoto , Yoji Ino , Yushi Kitamura , Toshikazu Saitoh , Takeshi Katsuhira
发明人: Chikara Murakata , Kazuhiko Kato , Junichiro Yamamoto , Ryuichiro Nakai , Seiho Okamoto , Yoji Ino , Yushi Kitamura , Toshikazu Saitoh , Takeshi Katsuhira
IPC分类号: A61K31/433 , C07D285/08 , A61P35/00
CPC分类号: A61K31/433 , A61K31/454 , C07D285/135 , C07D417/04
摘要: A therapeutic and/or prophylactic agent for a solid tumor, which comprises a thiadiazoline derivative represented by the general formula (I), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, R1 represents a hydrogen atom, R2 represents lower alkyl, or R1 and R2 are combined together to represent alkylene, R3 represents lower alkyl, R4 represents NHSO2R6 (wherein R6 represents hydroxy or the like) or the like, and R5 represents aryl or the like] and the like are provided.
摘要翻译: 含有通式(I)表示的噻二唑啉衍生物或其药学上可接受的盐的固体肿瘤治疗剂和/或预防剂,其中n表示1〜3的整数,R 1 R 2表示氢原子,R 2表示低级烷基,或R 1和R 2结合在一起代表亚烷基,R 低级烷基表示低级烷基,R 4表示NHSO 2 R 6(其中R 6或以上) >表示羟基等)等,R 5表示芳基等]等。
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公开(公告)号:US20070155804A1
公开(公告)日:2007-07-05
申请号:US10553222
申请日:2004-04-16
申请人: Chikara Murakata , Yoshinori Yamashita , Ryuichiro Nakai , Kazuhito Akasaka , Yoji Ino , Kazuhiko Kato , Yushi Kitamura
发明人: Chikara Murakata , Yoshinori Yamashita , Ryuichiro Nakai , Kazuhito Akasaka , Yoji Ino , Kazuhiko Kato , Yushi Kitamura
IPC分类号: A61K31/433 , C07D285/12 , C07D417/02
CPC分类号: C07D285/13 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/5377 , C07D285/135
摘要: A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —C(═W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents —C(═Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.
摘要翻译: 一种有丝分裂驱动蛋白Eg5抑制剂,其包含由通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐作为有效成分:[其中R 1表示氢原子等, O 2表示氢原子,-C(-W)R 6(其中W表示氧原子或硫原子,R 6表示 取代或未取代的低级烷基等)等,R 3表示-C(-Z)R 19(其中Z表示氧原子或硫原子, 和R 19表示取代或未取代的低级烷基等)等,R 4表示取代或未取代的低级烷基等,R 5, / SUP>表示取代或未取代的芳基等〕等。
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公开(公告)号:US20080207706A1
公开(公告)日:2008-08-28
申请号:US12098736
申请日:2008-04-07
申请人: Chikara MURAKATA , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi , Tomohisa Nakano , Yoji Ino
发明人: Chikara MURAKATA , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi , Tomohisa Nakano , Yoji Ino
IPC分类号: A61K31/433 , A61P35/00
CPC分类号: C07D285/135 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/5377
摘要: (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(═W)R6 or the like; R3 represents a hydrogen atom, —C(═WA)R6A, or the like)Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
摘要翻译: (其中R 1和R 4相同或不同,各自表示氢原子,取代或未取代的低级烷基,取代或未取代的低级炔基,取代或未取代的低级链烯基 等等; R 5表示取代或未取代的杂环基,取代或未取代的芳基等; R 2表示-C(-W)R SUP > 6个等等; R 3表示氢原子,-C(-W A)SO 6,或者 提供包含由上述通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐作为有效成分的抗肿瘤剂。
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公开(公告)号:US20070213380A1
公开(公告)日:2007-09-13
申请号:US11798214
申请日:2007-05-11
申请人: Chikara Murakata , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi , Tomohisa Nakano , Yoji Ino
发明人: Chikara Murakata , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi , Tomohisa Nakano , Yoji Ino
IPC分类号: A61K31/433 , C07D285/135
CPC分类号: C07D285/135 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/5377
摘要: (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(═W)R6 or the like; R3 represents a hydrogen atom, —C(═WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
摘要翻译: (其中R 1和R 4相同或不同,各自表示氢原子,取代或未取代的低级烷基,取代或未取代的低级炔基,取代或未取代的低级链烯基 等等; R 5表示取代或未取代的杂环基,取代或未取代的芳基等; R 2表示-C(-W)R SUP > 6个等等; R 3表示氢原子,-C(-W A)SO 6,或者 提供包含由上述通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐作为有效成分的抗肿瘤剂。
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公开(公告)号:US20060074113A1
公开(公告)日:2006-04-06
申请号:US10497531
申请日:2002-12-11
申请人: Chikara Murakata , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi , Tomohisa Nakano , Yoji Ino
发明人: Chikara Murakata , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi , Tomohisa Nakano , Yoji Ino
IPC分类号: A61K31/433 , C07D285/12
CPC分类号: C07D285/135 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/5377
摘要: (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(═W)R6 or the like; R3 represents a hydrogen atom, —C(═WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
摘要翻译: (其中R 1和R 4相同或不同,各自表示氢原子,取代或未取代的低级烷基,取代或未取代的低级炔基,取代或未取代的低级链烯基 等等; R 5表示取代或未取代的杂环基,取代或未取代的芳基等; R 2表示-C(-W)R SUP > 6个等等; R 3表示氢原子,-C(-W A)SO 6,或者 提供包含由上述通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐作为有效成分的抗肿瘤剂。
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公开(公告)号:US07902234B2
公开(公告)日:2011-03-08
申请号:US12792448
申请日:2010-06-02
申请人: Chikara Murakata , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi
发明人: Chikara Murakata , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi
IPC分类号: A61K31/433 , C07D285/125
CPC分类号: C07D285/135 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/5377
摘要: (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R6 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(═W)R6 or the like; R3 represents a hydrogen atom, —C(═WA)R6A, or the like)Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
摘要翻译: (其中R 1和R 4相同或不同,各自表示氢原子,取代或未取代的低级烷基,取代或未取代的低级炔基,取代或未取代的低级烯基等; R 6表示取代或未取代的杂环基,取代或未取代的 未取代的芳基等; R 2表示-C(= W)R 6等; R 3表示氢原子,-C(= W)R 6 A等)。 提供包含由上述通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐作为活性成分的抗肿瘤剂。
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公开(公告)号:US07759371B2
公开(公告)日:2010-07-20
申请号:US12098736
申请日:2008-04-07
申请人: Chikara Murakata , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi
发明人: Chikara Murakata , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi
IPC分类号: A61K31/433
CPC分类号: C07D285/135 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/5377
摘要: (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(═W)R6 or the like; R3 represents a hydrogen atom, —C(═WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
摘要翻译: (其中R 1和R 4相同或不同,各自表示氢原子,取代或未取代的低级烷基,取代或未取代的低级炔基,取代或未取代的低级烯基等; R 5表示取代或未取代的杂环基,取代或未取代的 未取代的芳基等; R 2表示-C(= W)R 6等; R 3表示氢原子,-C(= W)R 6 A等)。抗肿瘤剂包含上述一般所述的噻二唑啉衍生物 提供式(I)或其药理学上可接受的盐作为活性成分。
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公开(公告)号:US07425636B2
公开(公告)日:2008-09-16
申请号:US10497531
申请日:2002-12-11
申请人: Chikara Murakata , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi
发明人: Chikara Murakata , Kazuhiko Kato , Yoshihisa Ohta , Ryuichiro Nakai , Yoshinori Yamashita , Takeshi Takahashi
IPC分类号: C07D285/135 , A61K31/433
CPC分类号: C07D285/135 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/5377
摘要: (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(═W)R6 or the like; R3 represents a hydrogen atom, —C(═WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
摘要翻译: (其中R 1和R 4相同或不同,各自表示氢原子,取代或未取代的低级烷基,取代或未取代的低级炔基,取代或未取代的低级链烯基 等等; R 5表示取代或未取代的杂环基,取代或未取代的芳基等; R 2表示-C(-W)R SUP > 6个等等; R 3表示氢原子,-C(-W A)SO 6,或者 提供包含由上述通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐作为有效成分的抗肿瘤剂。
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公开(公告)号:US08318782B2
公开(公告)日:2012-11-27
申请号:US13188819
申请日:2011-07-22
申请人: Kazuhiko Kato , Yushi Kitamura
发明人: Kazuhiko Kato , Yushi Kitamura
IPC分类号: A61K31/433 , C07D285/125
CPC分类号: C07D285/13 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/5377 , C07D285/135
摘要: A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —C(═W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents —C(═Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.
摘要翻译: 一种有丝分裂驱动蛋白Eg5抑制剂,其包含由通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐作为活性成分:[其中R 1表示氢原子等,R 2表示氢原子,-C(= W)R6(其中W表示氧原子或硫原子,R6表示取代或未取代的低级烷基等)等,R3表示-C(= Z)R19(其中Z表示氧原子或硫原子 原子,R 19表示取代或未取代的低级烷基等)等,R 4表示取代或未取代的低级烷基等,R 5表示取代或未取代的芳基等〕等。
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