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公开(公告)号:US08288396B2
公开(公告)日:2012-10-16
申请号:US13202773
申请日:2010-02-18
申请人: Yasuhiro Goto , Kenji Niiyama , Satoshi Sunami , Keiji Takahashi
发明人: Yasuhiro Goto , Kenji Niiyama , Satoshi Sunami , Keiji Takahashi
IPC分类号: A61K31/519 , C07D487/14
CPC分类号: C07D487/14 , C07D519/00
摘要: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a): R1 means a —(C═O)aOb(C1-C6)alkyl group, a —(C═O)aOb(C2-C6)alkenyl group, a —(C═O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C═O)aOb(C1-C6)alkyl group or a group of —(C═O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.
摘要翻译: 本发明提供一种用于癌症化疗或放射治疗的新型抗癌剂或敏化剂。 通式(I)的化合物:其中A表示芳基或杂芳基,或式(a)的基团:R 1表示 - (C = O)a O b(C 1 -C 6)烷基, - (C = O)a O b(C 2 -C 6)烯基, - (C = O)a O b(C 3 -C 6)环烷基,芳基或杂芳基; R2和R3各自表示氢原子,卤素原子,羟基,羧基, - (C = O)aOb(C1-C6)烷基或 - (C = O)aN(R1e) R2e; R4表示氢原子或(C1-C6)烷基等具有优异的Wee1激酶抑制作用,因此可用于医学领域,特别是在各种癌症治疗领域。
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公开(公告)号:US20110189130A1
公开(公告)日:2011-08-04
申请号:US13053798
申请日:2011-03-22
申请人: Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人: Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号: A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/664 , A61K31/675 , A61K31/7008 , A61K31/7076 , A61K31/52 , A61K31/708 , A61K31/704 , A61K33/24 , A61K39/395 , A61K38/21 , A61P35/00 , A61P35/02
CPC分类号: C07D487/04 , A61K31/4162 , A61K31/519
摘要: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc.The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译: 本发明涉及通式(I)的化合物:其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子,卤素原子,羟基,低级烷基或-N(R1k)R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。
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公开(公告)号:US07935708B2
公开(公告)日:2011-05-03
申请号:US12226707
申请日:2007-04-25
申请人: Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人: Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号: A01N43/90 , A01N43/56 , A61K31/519 , A61K31/415 , C07D487/00 , C07D403/02
CPC分类号: C07D487/04 , A61K31/4162 , A61K31/519
摘要: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译: 本发明涉及通式(I)的化合物:其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子,卤素原子,羟基,低级烷基或-N(R1k)R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。
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公开(公告)号:US07834019B2
公开(公告)日:2010-11-16
申请号:US11789548
申请日:2007-04-25
申请人: Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人: Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号: A61K31/519 , A61K31/497 , C07D487/04 , A61P35/00
CPC分类号: C07D487/04 , A61K31/4162 , A61K31/519
摘要: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译: 本发明涉及通式(I)的化合物:其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子,卤素原子,羟基,低级烷基或-N(R1k)R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。
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公开(公告)号:US08791125B2
公开(公告)日:2014-07-29
申请号:US13053798
申请日:2011-03-22
申请人: Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人: Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号: A01N43/90 , A61K31/519 , C07D487/00
CPC分类号: C07D487/04 , A61K31/4162 , A61K31/519
摘要: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译: 本发明涉及通式(I)的化合物:其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子,卤素原子,羟基,低级烷基或-N(R1k)R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。
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公开(公告)号:US20070254892A1
公开(公告)日:2007-11-01
申请号:US11789548
申请日:2007-04-25
申请人: Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人: Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Toshihiro Sakamoto , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号: A61K31/519 , C07D487/02
CPC分类号: C07D487/04 , A61K31/4162 , A61K31/519
摘要: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc.The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译: 本发明涉及通式(I)的化合物:其中Ar 1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环 - 低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳族基团; R 2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R 3是氢原子或低级烷基; R 4是氢原子,卤素原子,羟基,低级烷基或-N(R 1)1个基团)的基团, SUP>; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。
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公开(公告)号:US20100063024A1
公开(公告)日:2010-03-11
申请号:US12226707
申请日:2007-04-25
申请人: Toshihiro Sakamoto , Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
发明人: Toshihiro Sakamoto , Takeshi Sagara , Sachie Otsuki , Satoshi Sunami , Kenji Niiyama , Fuyuki Yamamoto , Takashi Yoshizumi , Hidetomo Furuyama , Yasuhiro Goto , Makoto Bamba , Keiji Takahashi , Hiroshi Hirai , Toshihide Nishibata
IPC分类号: A61K31/397 , C07D487/04 , C07D413/14 , C07D417/14 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P35/00
CPC分类号: C07D487/04 , A61K31/4162 , A61K31/519
摘要: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc.The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
摘要翻译: 本发明涉及通式(I)的化合物:其中Ar1是任选取代的芳基或杂芳基; R 1是任选取代的低级烷基,低级烯基,低级炔基或环低级烷基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R2是氢原子,低级烷基,低级烯基或低级炔基,或者是任选具有取代基的芳基,芳烷基或杂芳基; R3是氢原子或低级烷基; R4是氢原子,卤素原子,羟基,低级烷基或-N(R1k)R1m基团; T和U是氮原子或次甲基等。本发明的化合物具有优异的韦尔激酶抑制作用,因此可用于药物领域,特别是治疗各种癌症。
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公开(公告)号:US08436004B2
公开(公告)日:2013-05-07
申请号:US12663729
申请日:2008-06-12
申请人: Makoto Bamba , Hidetomo Furuyama , Kenji Niiyama , Toshihiro Sakamoto , Satoshi Sunami , Keiji Takahashi , Fuyuki Yamamoto , Takashi Yoshizumi
发明人: Makoto Bamba , Hidetomo Furuyama , Kenji Niiyama , Toshihiro Sakamoto , Satoshi Sunami , Keiji Takahashi , Fuyuki Yamamoto , Takashi Yoshizumi
IPC分类号: A01N43/90 , A61K31/519 , C07D487/00
CPC分类号: C07D487/04 , A61K31/522 , A61K31/5415 , A61K31/55 , A61K45/06 , C07D519/00
摘要: The invention relates to a compound of a general formula (I): wherein A1 and A2 each mean a nitrogen atom or an optionally-substituted methine group; Ring B means a 5-membered to 7-membered aliphatic ring, or a spiro or bicyclo ring formed from the aliphatic ring and any other 3-membered to 7-membered aliphatic ring; R1 means a hydrogen atom, or an optionally-substituted C1-C6 alkyl group, or an optionally-substituted aryl, aralkyl or heteroaryl group; R2 means an optionally-substituted aryl, aralkyl or heteroaryl group; and X means a group of ═NH or ═O, etc. Based on its excellent Wee1 kinase-inhibitory effect, the compound of the invention has cell growth-inhibitory effect and has an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.
摘要翻译: 本发明涉及通式(I)的化合物:其中A1和A2各自表示氮原子或任选取代的次甲基; 环B表示由脂族环和任何其它3元至7元脂肪环形成的5元至7元脂族环或螺环或双环; R 1表示氢原子或任选取代的C 1 -C 6烷基,或任选取代的芳基,芳烷基或杂芳基; R 2表示任选取代的芳基,芳烷基或杂芳基; X表示一组= NH或= O等。基于其优异的Wee1激酶抑制作用,本发明化合物具有细胞生长抑制作用,与任何其他抗癌剂具有添加/协同作用,并且 因此在医学领域是有用的。
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公开(公告)号:US20120134955A1
公开(公告)日:2012-05-31
申请号:US13202773
申请日:2010-02-18
申请人: Yasuhiro Goto , Kenji Niyama , Satoshi Sunami , Keiji Takahashi
发明人: Yasuhiro Goto , Kenji Niyama , Satoshi Sunami , Keiji Takahashi
IPC分类号: A61K31/519 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/538 , A61K31/664 , A61K31/675 , A61K31/7068 , A61K31/7076 , A61K38/12 , A61K31/7048 , A61K33/24 , A61K38/21 , A61K31/716 , A61K38/50 , A61K31/566 , A61K31/567 , A61K38/20 , A61K33/36 , A61K39/395 , A61K31/43 , A61P35/00 , C07D487/14
CPC分类号: C07D487/14 , C07D519/00
摘要: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a):; R1 means a —(C═O)aOb(C1-C6)alkyl group, a —(C═O)aOb(C2-C6)alkenyl group, a —(C═O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C═O)aOb(C1-C6)alkyl group or a group of —(C═O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee 1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.
摘要翻译: 本发明提供一种用于癌症化疗或放射治疗的新型抗癌剂或敏化剂。 通式(I)的化合物:其中A表示芳基或杂芳基,或式(a)的基团:。 R1表示 - (C = O)aOb(C1-C6)烷基, - (C = O)aOb(C2-C6)烯基, - (C = O)aOb(C3-C6) 芳基或杂芳基; R2和R3各自表示氢原子,卤素原子,羟基,羧基, - (C = O)aOb(C1-C6)烷基或 - (C = O)aN(R1e) R2e; R4表示氢原子或(C1-C6)烷基等具有优异的Wee 1-激酶抑制作用,因此可用于医学领域,特别是在各种癌症治疗领域。
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公开(公告)号:US08507505B2
公开(公告)日:2013-08-13
申请号:US13133673
申请日:2009-12-09
申请人: Makoto Bamba , Hidetomo Furuyama , Toshihiro Sakamoto , Satoshi Sunami , Keiji Takahashi , Fuyuki Yamamoto , Takashi Yoshizumi
发明人: Makoto Bamba , Hidetomo Furuyama , Toshihiro Sakamoto , Satoshi Sunami , Keiji Takahashi , Fuyuki Yamamoto , Takashi Yoshizumi
IPC分类号: C07D487/04 , C07D519/00 , A61K31/519 , A61K31/5377 , A61P35/00 , A61P35/02
CPC分类号: A61K31/519 , A61K31/5377 , C07D487/04 , C07D519/00
摘要: The present invention relates to a compound of General Formula (I) below, among others. In the Formula, Ar1 is an optionally substituted aryl or heteroaryl group; R1 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, or an optionally substituted aryl, aralkyl, or heteroaryl group; R2 is an optionally substituted aryl, aralkyl, or heteroaryl group; and R3 is a hydrogen atom or a C1-C6 alkyl group. A compound of the present invention has an excellent Wee1 kinase inhibiting effect, and is therefore useful in the filed of medicine, particularly in various types of cancer therapy.
摘要翻译: 本发明涉及以下通式(I)的化合物等。 在式中,Ar 1是任选取代的芳基或杂芳基; R 1是氢原子,任选取代的C 1 -C 6烷基,或任选取代的芳基,芳烷基或杂芳基; R2是任选取代的芳基,芳烷基或杂芳基; 并且R 3是氢原子或C 1 -C 6烷基。 本发明的化合物具有优异的Wee1激酶抑制作用,因此可用于医药领域,特别是在各种类型的癌症治疗中。
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