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。

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。

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。

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。

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。

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。

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。

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。

公开(公告)号：US20110243891A1

公开(公告)日：2011-10-06

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： A61K31/519 ,  C07D487/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/664 ,  A61K31/675 ,  A61K31/7028 ,  A61K31/7076 ,  A61K31/52 ,  A61K31/7068 ,  A61K38/12 ,  A61K33/24 ,  A61K39/395 ,  A61K38/21 ,  A61K31/716 ,  A61K38/50 ,  A61K33/36 ,  A61P35/00

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 Weel 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韦尔激酶抑制作用，因此可用于医药领域，特别是在各种类型的癌症治疗中。

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。