公开(公告)号：US20070191419A1

公开(公告)日：2007-08-16

申请号：US10590585

申请日：2005-03-04

申请人： Hirobumi Takahashi ,  Yuichi Sugimoto ,  Takashi Yoshizumi ,  Tetsuya Kato ,  Masanori Asai ,  Hiroshi Miyazoe

发明人： Hirobumi Takahashi ,  Yuichi Sugimoto ,  Takashi Yoshizumi ,  Tetsuya Kato ,  Masanori Asai ,  Hiroshi Miyazoe

IPC分类号： A61K31/435 ,  C07D221/04

CPC分类号： C07D451/02 ,  C07D239/70 ,  C07D401/06 ,  C07D401/14 ,  C07D471/10 ,  C07D491/10

摘要： Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.

摘要翻译： 提供式[I]的环烷基吡啶衍生物：其中符号与说明书中所述的相同。 该化合物作为伤害感受肽受体拮抗剂起作用，并且可用作与伤害感受肽受体相关疾病的药物，例如作为抵抗麻醉止痛剂的缓解剂; 减轻对麻醉止痛药依赖或成瘾的缓解; 镇痛增强剂; 抗生素或食欲抑制剂; 用于认知障碍和痴呆/健忘症的治疗或预防剂; 治疗发育性认知异常的药剂; 精神分裂症补救办法 治疗神经变性疾病的药剂; 用于情感障碍的抗抑郁药或治疗剂; 尿崩症的治疗或预防剂; 多尿症的治疗或预防剂; 或补救低血压。

公开(公告)号：US07855294B2

公开(公告)日：2010-12-21

申请号：US10590585

申请日：2005-03-04

申请人： Hirobumi Takahashi ,  Yuichi Sugimoto ,  Takashi Yoshizumi ,  Tetsuya Kato ,  Masanori Asai ,  Hiroshi Miyazoe

发明人： Hirobumi Takahashi ,  Yuichi Sugimoto ,  Takashi Yoshizumi ,  Tetsuya Kato ,  Masanori Asai ,  Hiroshi Miyazoe

IPC分类号： C07D215/26 ,  C07D491/20 ,  C07D491/107 ,  C07D401/06 ,  A61K31/438 ,  A61K31/4709 ,  A61K31/46

CPC分类号： C07D451/02 ,  C07D239/70 ,  C07D401/06 ,  C07D401/14 ,  C07D471/10 ,  C07D491/10

摘要： Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.

摘要翻译： 提供式[I]的环烷基吡啶衍生物：其中符号与说明书中所述的相同。 该化合物作为伤害感受肽受体拮抗剂起作用，并且可用作与伤害感受肽受体相关疾病的药物，例如作为抵抗麻醉止痛剂的缓解剂; 减轻对麻醉止痛药依赖或成瘾的缓解; 镇痛增强剂; 抗生素或食欲抑制剂; 用于认知障碍和痴呆/健忘症的治疗或预防剂; 治疗发育性认知异常的药剂; 精神分裂症补救办法 治疗神经变性疾病的药剂; 用于情感障碍的抗抑郁药或治疗剂; 尿崩症的治疗或预防剂; 多尿症的治疗或预防剂; 或补救低血压。

公开(公告)号：US07125877B2

公开(公告)日：2006-10-24

申请号：US10437176

申请日：2003-05-14

申请人： Kensuke Kobayashi ,  Hirobumi Takahashi ,  Hiroshi Kawamoto ,  Tetsuya Kato ,  Satoru Itoh ,  Takashi Yoshizumi ,  Osamu Okamoto

发明人： Kensuke Kobayashi ,  Hirobumi Takahashi ,  Hiroshi Kawamoto ,  Tetsuya Kato ,  Satoru Itoh ,  Takashi Yoshizumi ,  Osamu Okamoto

IPC分类号： A61K31/496 ,  C07D403/04 ,  C07D405/14

CPC分类号： C07D235/24 ,  A61K31/496 ,  C07D235/12 ,  C07D235/14 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/08 ,  C07D405/06

摘要： This invention provides compounds which are represented by a general formula [I] [in which X stands for hydrogen or halogen; B stands for halogen, cyano or optionally fluorine-substituted lower alkyl; D stands for a 3–10 membered aliphatic nitrogen-containing heterocyclic group; R3, R4 and R5 may be same or different, and each stands for hydrogen, lower alkyl optionally having substituent group(s) and the like; and a is 0 or 1]. These compounds exhibit high affinity to nociceptin receptors and whereby inhibit actions of nociceptin, and are useful as an analgesic, antiobestic, agent for ameliorating brain function, treating agents for Alzheimer's disease and dementia, and therapeutic agents for schizophrenia, neurodegenerative diseases, depression, diabetes insipidus, polyuria, hypotension and the like.

摘要翻译： 本发明提供由通式[I]表示的化合物[其中X代表氢或卤素; B代表卤素，氰基或任选氟取代的低级烷基; D代表3-10元脂族含氮杂环基; R 3，R 4和R 5可以相同或不同，各自代表氢，任选具有取代基的低级烷基， 等等; a为0或1]。 这些化合物对伤害感受肽受体表现出高亲和力，并且由此抑制伤害感受肽的作用，并且可用作镇痛剂，抗胆碱药物，用于改善脑功能，治疗阿尔茨海默氏病和痴呆药物，以及用于精神分裂症，神经退行性疾病，抑郁症，糖尿病 尿崩症，多尿，低血压等。

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：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：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：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：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：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。