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1.发明授权公开(公告)号：US09221872B2
公开(公告)日：2015-12-29
申请号：US14313264
申请日：2014-06-24
申请人： CanBas Co., Ltd.
发明人： Takumi Kawabe , Naoki Mine , Naoya Saito , Keiichi Sakakibara , Takuji Sato
摘要： This invention provides compounds including peptides and peptidomimetics that can be used to treat cell proliferative disorders, such as those associated with benign and malignant tumor cells. While the invention is not limited to any particular mechanism, the compounds of the invention appear to function at least in part by inhibiting G2 cell cycle checkpoint. Thus, invention compounds can be used to inhibit cell growth alone or be used in combination with a nucleic acid damaging treatment to inhibit cell growth.
摘要翻译： 本发明提供了可用于治疗细胞增殖性疾病（例如与良性和恶性肿瘤细胞相关的那些）的肽和肽模拟物的化合物。 虽然本发明不限于任何特定的机制，但是本发明的化合物至少部分通过抑制G2细胞周期检查点起作用。 因此，本发明化合物可用于单独抑制细胞生长或与核酸损伤处理组合使用以抑制细胞生长。
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2.发明授权Compounds that abrogate DNA-damage-induced cell cycle G2 checkpoint and/or augment the anti-cancer activity of DNA damaging treatments 失效消除DNA损伤诱导的细胞周期G2检查点和/或增加DNA损伤治疗的抗癌活性的化合物公开(公告)号：US07030111B2
公开(公告)日：2006-04-18
申请号：US10457029
申请日：2003-06-06
申请人： Takumi Kawabe , Hidetaka Kobayashi
发明人： Takumi Kawabe , Hidetaka Kobayashi
IPC分类号： A61K31/5375 , A61K31/495 , C07D265/30 , C07D241/04
CPC分类号： C07C327/26 , C07C69/76 , C07C327/36 , C07D213/65 , G01N33/5011
摘要： The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.
摘要翻译： 本发明提供抑制哺乳动物细胞（包括人细胞）中的细胞周期G2检查点，特别是DNA损伤诱导的G2检查点的组合物和方法。 具体地，本发明提供了通过废除细胞周期G2检查点来使细胞对DNA损伤剂敏感的组合物和方法。 本发明的化合物用于治疗增殖性疾病如癌症。 本发明提供了选择性地使G1检查点受损的癌细胞对DNA损伤剂和治疗敏感的组合物和方法。
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3.发明授权Compounds that abrogate DNA damage induced cell cycle G2 checkpoint and/or augment anti-cancer activity of DNA-damaging treatments 失效消除DNA损伤的化合物诱导细胞周期G2检查点和/或增加DNA损伤治疗的抗癌活性公开(公告)号：US07652042B2
公开(公告)日：2010-01-26
申请号：US12131564
申请日：2008-06-02
申请人： Takumi Kawabe , Hidetaka Kobayashi
发明人： Takumi Kawabe , Hidetaka Kobayashi
IPC分类号： A61K31/44 , A61K31/235 , A61K31/095
CPC分类号： C07C327/26 , C07C69/76 , C07C327/36 , C07D213/65 , G01N33/5011
摘要： The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.
摘要翻译： 本发明提供抑制哺乳动物细胞（包括人细胞）中的细胞周期G2检查点，特别是DNA损伤诱导的G2检查点的组合物和方法。 具体地，本发明提供了通过废除细胞周期G2检查点来使细胞对DNA损伤剂敏感的组合物和方法。 本发明的化合物用于治疗增殖性疾病如癌症。 本发明提供了选择性地使G1检查点受损的癌细胞对DNA损伤剂和治疗敏感的组合物和方法。
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4.发明申请COMPOUNDS THAT ABROGATE DNA DAMAGE INDUCED CELL CYCLE G2 CHECKPOINT AND/OR AUGMENT ANTI-CANCER ACTIVITY OF DNA-DAMAGING TREATMENTS 失效DNA损伤诱导的细胞周期G2检测点和/或损伤DNA损伤治疗的抗癌活性的化合物公开(公告)号：US20080293137A1
公开(公告)日：2008-11-27
申请号：US12131639
申请日：2008-06-02
申请人： TAKUMI KAWABE , Hidetaka Kobayashi
发明人： TAKUMI KAWABE , Hidetaka Kobayashi
CPC分类号： C07C327/26 , C07C69/76 , C07C327/36 , C07D213/65 , G01N33/5011
摘要： The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.
摘要翻译： 本发明提供抑制哺乳动物细胞（包括人细胞）中的细胞周期G2检查点，特别是DNA损伤诱导的G2检查点的组合物和方法。 具体地，本发明提供了通过废除细胞周期G2检查点来使细胞对DNA损伤剂敏感的组合物和方法。 本发明的化合物用于治疗增殖性疾病如癌症。 本发明提供了选择性地使G1检查点受损的癌细胞对DNA损伤剂和治疗敏感的组合物和方法。
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5.发明授权Compositions and methods for inhibiting G2 cell cycle arrest and sensitizing cells to DNA damaging agents 有权用于抑制G2细胞周期停滞和使细胞对DNA损伤剂敏感的组合物和方法公开(公告)号：US06881575B1
公开(公告)日：2005-04-19
申请号：US09667365
申请日：2000-09-21
申请人： Masashi Suganuma , Takumi Kawabe
发明人： Masashi Suganuma , Takumi Kawabe
IPC分类号： G01N33/50 , A61K31/506 , A61K31/704 , A61K33/24 , A61K35/76 , A61K38/00 , A61K38/04 , A61K45/00 , A61K48/00 , A61P35/00 , A61P43/00 , C07H15/252 , C07K14/16 , C07K14/47 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/12 , C12N9/16 , C12N9/99 , C12N15/09 , C12N15/11 , C12N15/62 , C12Q1/48 , G01N33/15 , G01N33/53 , G01N33/566 , G01N33/574 , G01N33/68 , C12N5/00
CPC分类号： C07K14/4738 , A61K38/00 , A61K48/00 , C07K2319/00
摘要： The invention provides compositions and methods for inhibiting Chk1 and/or Chk2 kinases. Also provided are compositions and methods for inhibiting G2 cell arrest checkpoint, particularly in mammalian, e.g. human cells. The compositions and methods of the invention are also used to treat disorders of cell growth, such as cancer. In particular, the invention provides methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA damaging agents and treatments. Also provided are methods for screening for compounds able to interact with, e.g., inhibit, enzymes involved in the G2 cell cycle arrest checkpoint, such as Chk1 and/or Chk2/Cds1 kinase.
摘要翻译： 本发明提供了用于抑制Chk1和/或Chk2激酶的组合物和方法。 还提供了用于抑制G2细胞停滞检查点的组合物和方法，特别是在哺乳动物中。 人类细胞。 本发明的组合物和方法也用于治疗诸如癌症的细胞生长障碍。 特别地，本发明提供了选择性地使G1检查点受损的癌细胞对DNA损伤剂和治疗敏感的方法。 还提供了筛选能够与例如Chk1和/或Chk2 / Cds1激酶参与的G2细胞周期停滞检查点相关的化合物例如抑制化合物的方法。
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公开(公告)号：US20220380305A1
公开(公告)日：2022-12-01
申请号：US17861673
申请日：2022-07-11
申请人： GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION , CanBas Co., Ltd.
发明人： Akira Asai , Naohisa Ogo , Daisuke Muraoka , Osamu Takikawa , Takumi Kawabe , Takuji Sato , Hisashi Murakami
IPC分类号： C07C335/32 , A61K31/155 , C07D251/08 , A61K31/53 , C07D333/24 , A61K31/381 , C07D239/38 , A61K31/505 , A61K31/513 , C07D239/545 , C07D209/42 , A61K31/4045 , C07D409/14 , C07D213/32 , A61K31/44 , A61K31/165 , A61K31/277 , C07D213/81 , C07C391/00 , C07D241/42 , C07D333/72 , A61P35/00 , A61P1/00
摘要： A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, and a heterocyclic ring, wherein ring A is selected from the group consisting of a benzene ring, a naphthalene ring, a quinoxaline ring, a thiophene ring, an indole ring, a benzothiophene ring, an imidazole ring, a quinoline ring, a quinazoline ring, and a pyridine ring; X, R1 and R2 represent a substituent on a ring atom constituting ring A, wherein R1 and R2 are bonded to adjacent ring atoms of ring A; m represents an integer of 1 or 2; X is a halogen atom, and when m is 2, each X is the same or different; R1 and R2 are the same or different; R1 and R2 independently represent a group represented from the following groups: —(CH2)n—Y—R4 wherein Y is selected from the group consisting of O, S, SO, SO2, and Se, n represents an integer of 1 to 8, R4 represents wherein R41, R42 and R47 are the same and are a hydrogen atom
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公开(公告)号：US08084454B2
公开(公告)日：2011-12-27
申请号：US12082643
申请日：2008-04-11
申请人： Takumi Kawabe , Machiyo Ishigaki , Takuji Sato , Sayaka Yamamoto , Yoko Hasegawa
发明人： Takumi Kawabe , Machiyo Ishigaki , Takuji Sato , Sayaka Yamamoto , Yoko Hasegawa
IPC分类号： A61K31/497 , A61K31/505 , A61K31/47 , A61K31/44 , C07D401/12 , C07D239/02 , C07D215/46
CPC分类号： A61K31/4439 , A61K31/4725 , A61K31/496 , C07D207/452 , C07D207/50 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/12
摘要： Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.
摘要翻译： 提供了新型取代的唑类二恶英，其杀死细胞，抑制细胞增殖，抑制细胞生长，消除细胞周期G2检查点和/或引起适应G2细胞周期停滞。 提供了制备和使用本发明化合物的方法。 本发明提供取代的唑类二恶英以治疗细胞增殖障碍。 本发明包括使用取代的唑类二聚体来选择性地杀死或抑制癌细胞而无需额外的抗癌治疗。 本发明包括使用细胞周期G2-检查点 - 取代的取代唑类二恶英来选择性地使癌细胞对DNA损伤试剂，治疗和/或其它类型的抗癌试剂敏感。
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公开(公告)号：US20110092514A1
公开(公告)日：2011-04-21
申请号：US12950297
申请日：2010-11-19
申请人： TAKUMI KAWABE , Machiyo Ishigaki , Takuji Sato , Sayaka Yamamoto , Yoko Hasegawa
发明人： TAKUMI KAWABE , Machiyo Ishigaki , Takuji Sato , Sayaka Yamamoto , Yoko Hasegawa
IPC分类号： A61K31/496 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/473 , A61P35/00
CPC分类号： A61K31/4439 , A61K31/4725 , A61K31/496 , C07D207/452 , C07D207/50 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/12
摘要： Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.
摘要翻译： 提供了新型取代的唑类二恶英，其杀死细胞，抑制细胞增殖，抑制细胞生长，消除细胞周期G2检查点和/或引起适应G2细胞周期停滞。 提供了制备和使用本发明化合物的方法。 本发明提供取代的唑类二恶英以治疗细胞增殖障碍。 本发明包括使用取代的唑类二聚体来选择性地杀死或抑制癌细胞而无需额外的抗癌治疗。 本发明包括使用细胞周期G2-检查点 - 取代的取代唑类二恶英来选择性地使癌细胞对DNA损伤试剂，治疗和/或其它类型的抗癌试剂敏感。
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9.发明授权Compositions and methods for inhibiting G2 cell cycle arrest and sensitizing cells to DNA damaging agents 有权用于抑制G2细胞周期停滞和使细胞对DNA损伤剂敏感的组合物和方法公开(公告)号：US07851592B2
公开(公告)日：2010-12-14
申请号：US10967008
申请日：2004-10-15
申请人： Masashi Suganuma , Takumi Kawabe
发明人： Masashi Suganuma , Takumi Kawabe
IPC分类号： C07K14/435 , C07K14/47 , A61K38/00 , A61K48/00
CPC分类号： C07K14/4738 , A61K38/00 , A61K48/00 , C07K2319/00
摘要： The invention provides compositions and methods for inhibiting Chk1 and/or Chk2 kinases. Also provided are compositions and methods for inhibiting G2 cell arrest checkpoint, particularly in mammalian, e.g., human, cells. The compositions and methods of the invention are also used to treat disorders of cell growth, such as cancer. In particular, the invention provides methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA damaging agents and treatments. Also provided are methods for screening for compounds able to interact with, e.g., inhibit, enzymes involved in the G2 cell cycle arrest checkpoint, such as Chk1 and/or Chk2/Cds1 kinase.
摘要翻译： 本发明提供了用于抑制Chk1和/或Chk2激酶的组合物和方法。 还提供了用于抑制G2细胞停滞检查点的组合物和方法，特别是在哺乳动物例如人的细胞中。 本发明的组合物和方法也用于治疗诸如癌症的细胞生长障碍。 特别地，本发明提供了选择性地使G1检查点受损的癌细胞对DNA损伤剂和治疗敏感的方法。 还提供了筛选能够与例如Chk1和/或Chk2 / Cds1激酶参与的G2细胞周期停滞检查点相关的化合物例如抑制化合物的方法。
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公开(公告)号：US08415357B2
公开(公告)日：2013-04-09
申请号：US12950297
申请日：2010-11-19
申请人： Takumi Kawabe , Machiyo Ishigaki , Takuji Sato , Sayaka Yamamoto , Yoko Hasegawa
发明人： Takumi Kawabe , Machiyo Ishigaki , Takuji Sato , Sayaka Yamamoto , Yoko Hasegawa
IPC分类号： A61K31/497 , A61K31/44 , A61K31/47
CPC分类号： A61K31/4439 , A61K31/4725 , A61K31/496 , C07D207/452 , C07D207/50 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/12
摘要： Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.
摘要翻译： 提供了新型取代的唑类二恶英，其杀死细胞，抑制细胞增殖，抑制细胞生长，消除细胞周期G2检查点和/或引起适应G2细胞周期停滞。 提供了制备和使用本发明化合物的方法。 本发明提供取代的唑类二恶英以治疗细胞增殖障碍。 本发明包括使用取代的唑类二聚体来选择性地杀死或抑制癌细胞而无需额外的抗癌治疗。 本发明包括使用细胞周期G2-检查点 - 取代的取代唑类二恶英来选择性地使癌细胞对DNA损伤试剂，治疗和/或其它类型的抗癌试剂敏感。
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