公开(公告)号：US07718801B2

公开(公告)日：2010-05-18

申请号：US11661486

申请日：2005-08-30

申请人： Mikako Kawamura ,  Takashi Hashihayata ,  Satoshi Sunami ,  Tetsuya Sugimoto ,  Fuyuki Yamamoto ,  Yoshiyuki Sato ,  Kaori Kamijo ,  Morihiro Mitsuya ,  Yoshikazu Iwasawa ,  Hideya Komatani

发明人： Mikako Kawamura ,  Takashi Hashihayata ,  Satoshi Sunami ,  Tetsuya Sugimoto ,  Fuyuki Yamamoto ,  Yoshiyuki Sato ,  Kaori Kamijo ,  Morihiro Mitsuya ,  Yoshikazu Iwasawa ,  Hideya Komatani

IPC分类号： C07D239/00 ,  C07D239/02

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1′, R2, R2′, R3, R3′, R4, and R4′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.

摘要翻译： 本发明涉及由式[I]表示的化合物或其药学上可接受的盐或酯：其中：X 1，X 2，X 3和X 4可以相同或不同，各自为C或N，条件是 X1，X2，X3和X4中的两个为N; Y是CH或N; R1，R1'，R2，R2'，R3，R3'，R4和R4'可以相同或不同，分别为氢原子，低级烷基等; R5是氢原子或甲基; R 6和R 7可以相同或不同，分别为氢原子，低级烷基等; R 8和R 8'可以相同或不同，分别为氢原子，低级烷基等; R9是可以被取代的芳基或杂芳基; n为1〜3的整数，PLK1抑制剂或含有该PLK1抑制剂的抗癌剂。

公开(公告)号：US20080070894A1

公开(公告)日：2008-03-20

申请号：US11661486

申请日：2005-08-30

申请人： Mikako Kawamura ,  Takashi Hashihayata ,  Satoshi Sunami ,  Tetsuya Sugimoto ,  Fuyuki Yamamoto ,  Yoshiyuki Sato ,  Kaori Kamijo ,  Morihiro Mitsuya ,  Yoshikazu Iwasawa ,  Hideya Komatani

发明人： Mikako Kawamura ,  Takashi Hashihayata ,  Satoshi Sunami ,  Tetsuya Sugimoto ,  Fuyuki Yamamoto ,  Yoshiyuki Sato ,  Kaori Kamijo ,  Morihiro Mitsuya ,  Yoshikazu Iwasawa ,  Hideya Komatani

IPC分类号： A61K31/397 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/5513 ,  A61P35/00 ,  C07D237/06 ,  C07D239/24 ,  C07D243/14 ,  C07D295/00 ,  C07D473/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1′, R2, R2′, R3, R3′, R4, and R4′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.

摘要翻译： 本发明涉及由式[I]表示的化合物或其药学上可接受的盐或酯：其中：X 1，X 2，X 3， / SUB>和X 4可以相同或不同，各自为C或N，条件是X 1，X 2， / SUB>，X 3和X 4是N; Y是CH或N; R 1，R 1，R 2，R 2，R 3，N 3， R 3，R 4，R 4，R 4和R 4可以相同或不同，分别为氢原子，低级 烷基等; R 5是氢原子或甲基; R 6和R 7可以相同或不同，分别为氢原子，低级烷基等; R 8和R 8可以相同或不同，分别为氢原子，低级烷基等; R 9是可以被取代的芳基或杂芳基; n为1〜3的整数，PLK1抑制剂或含有该PLK1抑制剂的抗癌剂。

公开(公告)号：US20100221211A1

公开(公告)日：2010-09-02

申请号：US12738885

申请日：2008-10-20

申请人： Hidetomo Furuyama ,  Mikako Kawamura ,  Toshihiro Sakamoto ,  Fuyuki Yamamoto ,  Takashi Yoshizumi

发明人： Hidetomo Furuyama ,  Mikako Kawamura ,  Toshihiro Sakamoto ,  Fuyuki Yamamoto ,  Takashi Yoshizumi

IPC分类号： A61K38/20 ,  C07D487/04 ,  A61K31/519 ,  A61K31/397 ,  A61K39/395 ,  A61K38/21 ,  A61K31/675 ,  A61K31/7028 ,  A61K31/52 ,  A61K31/7068 ,  A61K31/7076 ,  A61K38/12 ,  A61K31/704 ,  A61K31/7048 ,  A61K38/14 ,  A61K33/24 ,  A61K31/555 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/715 ,  A61K38/46 ,  A61K31/7056 ,  A61K31/5685 ,  A61K33/36 ,  A61K38/08 ,  A61P35/00

CPC分类号： A61K31/519 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00 ,  A61K2300/00

摘要： The invention relates to a compound of general formula (I-0): wherein R1 means a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, or a C3-C6 cycloalkyl group; R2, R3, R4 and R5 mean a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo-C1-C6 alkoxy group; R6 means a hydrogen atom, or a C1-C6 alkyl group; R7a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxy-C1-C6 alkyl group, -Q2-N(R1c)R1d or a nitrogen-containing heterocyclic group; R8a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group or a hydroxy-C1-C6 alkyl group; or R7a and R8a form, as taken together, a C2-C6 alkylene group, or R7a and R8a and the ring atoms to which they bond may form a spiro ring or a bicyclo ring; and X and Y mean a methine group or a nitrogen atom.The compound of the invention has, based on its excellent Wee1 kinase-inhibitory effect, a cell growth-inhibitory effect and 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-0）的化合物：其中R1表示C1-C6烷基，C2-C6烯基，C2-C6炔基或C3-C6环烷基; R2，R3，R4和R5表示氢原子，卤素原子，C1-C6烷基，卤代-C1-C6烷基，C1-C6烷氧基或卤代-C1-C6烷氧基; R6表示氢原子或C1-C6烷基; R7a表示氢原子，卤素原子，C1-C6烷基，卤代-C1-C6烷基，C1-C6烷氧基，羟基-C1-C6烷基，-Q2-N（R1c）R1d 或含氮杂环基; R8a表示氢原子，卤素原子，C1-C6烷基，卤代-C1-C6烷基，C1-C6烷氧基或羟基-C1-C6烷基; 或R 7a和R 8a一起形成C 2 -C 6亚烷基或R 7a和R 8a，并且它们键合的环原子可以形成螺环或双环; X和Y表示次甲基或氮原子。 本发明的化合物基于其优异的Wee1激酶抑制作用，具有细胞生长抑制作用和与任何其它抗癌剂的添加/协同效应，因此在医学领域是有用的。

公开(公告)号：US08329711B2

公开(公告)日：2012-12-11

申请号：US12738885

申请日：2008-10-20

申请人： Hidetomo Furuyama ,  Mikako Kawamura ,  Toshihiro Sakamoto ,  Fuyuki Yamamoto ,  Takashi Yoshizumi

发明人： Hidetomo Furuyama ,  Mikako Kawamura ,  Toshihiro Sakamoto ,  Fuyuki Yamamoto ,  Takashi Yoshizumi

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC分类号： A61K31/519 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00 ,  A61K2300/00

摘要： The invention relates to compounds of general formula (I-0): wherein R1, R2, R3, R4, R5, R6, R7a, R8a, X, and Y are as defined herein. Compounds of the invention have, based on excellent Wee1 kinase-inhibitory effect, a cell growth-inhibitory effect and an additive/synergistic effect with any other anticancer agent, and are therefore useful in the field of medicine.

摘要翻译： 本发明涉及通式（I-0）的化合物：其中R1，R2，R3，R4，R5，R6，R7a，R8a，X和Y如本文所定义。 本发明的化合物基于优异的Wee1激酶抑制作用，具有细胞生长抑制作用和与任何其它抗癌剂的添加/协同作用，因此可用于医学领域。

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：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：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：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。