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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: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。
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公开(公告)号:US20060229264A1
公开(公告)日:2006-10-12
申请号:US10565327
申请日:2004-07-21
IPC分类号: A61K31/7056 , C07H19/22
CPC分类号: C07H17/02
摘要: The present invention relates to crystalline free base compound having the following formula: wherein R is an unsubstituted pyridyl methyl group or a pyridyl methyl group substituted by a hydroxy methyl group; or a pharmaceutically acceptable salt or a solvate thereof.
摘要翻译: 本发明涉及具有下式的结晶游离碱化合物:其中R是未取代的吡啶基甲基或被羟基甲基取代的吡啶基甲基; 或其药学上可接受的盐或溶剂合物。
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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: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: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。
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17.
公开(公告)号:US20070042975A1
公开(公告)日:2007-02-22
申请号:US10571861
申请日:2004-09-14
IPC分类号: A61K31/7056 , C07H19/22
CPC分类号: A61K31/7056
摘要: The present invention relates to a novel indolopyrrolocarbazole derivative which is represented by the formula [I]: wherein: A represents O, NH, or CH2; R1 represents a single bond, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, etc.; R2 represents a phenyl group, a naphthyl group, or a five- or six-membered aromatic or aliphatic heterocyclic ring having at least one atom selected from N, S, or O, wherein the phenyl group, naphthyl group, aromatic or aliphatic heterocyclic ring may be substituted; and G represents a hexose group or a pentose group, or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明涉及由式[I]表示的新型吲哚并吡咯并唑衍生物:其中:A表示O,NH或CH 2。 R 1表示单键,低级烷基,低级烯基,低级炔基等; R 2表示具有至少一个选自N,S或O的原子的苯基,萘基或五元或六元芳族或脂族杂环,其中苯基, 萘基,芳族或脂肪族杂环可以被取代; G表示己糖基或戊糖基,或其药学上可接受的盐。
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