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公开(公告)号:US08603975B2
公开(公告)日:2013-12-10
申请号:US12598404
申请日:2008-04-25
申请人: Toshio Yamanaka , Hidenori Ohki , Junya Ishida , Ayako Toda , Yu Harayama , Takuya Makino , Shigeki Kunikawa , Hiroaki Mizuno , Hiroaki Ohtake
发明人: Toshio Yamanaka , Hidenori Ohki , Junya Ishida , Ayako Toda , Yu Harayama , Takuya Makino , Shigeki Kunikawa , Hiroaki Mizuno , Hiroaki Ohtake
摘要: The present invention relates to a new cyclic peptide compound or a salt thereof, which has anti-hepatitis C virus activities based on inhibitory activity against the RNA replication of hepatitis C virus replicon, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for prophylactic and/or therapeutic treatment of hepatitis C in a human being or an animal.
摘要翻译: 本发明涉及一种基于对丙型肝炎病毒复制子的RNA复制的抑制活性的抗丙型肝炎病毒活性的新的环肽化合物或其盐,其制备方法,包含其的药物组合物, 以及在人或动物中预防和/或治疗丙型肝炎的方法。
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公开(公告)号:US20100120672A1
公开(公告)日:2010-05-13
申请号:US12598404
申请日:2008-04-25
申请人: Toshio Yamanaka , Hidenori Ohki , Junya Ishida , Ayako Toda , Yu Harayama , Takuya Makino , Shigeki Kunikawa , Hiroaki Mizuno , Hiroaki Ohtake
发明人: Toshio Yamanaka , Hidenori Ohki , Junya Ishida , Ayako Toda , Yu Harayama , Takuya Makino , Shigeki Kunikawa , Hiroaki Mizuno , Hiroaki Ohtake
摘要: The present invention relates to a new cyclic peptide compound or a salt thereof, which has anti-hepatitis C virus activities based on inhibitory activity against the RNA replication of hepatitis C virus replicon, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for prophylactic and/or therapeutic treatment of hepatitis C in a human being or an animal.
摘要翻译: 本发明涉及一种基于对丙型肝炎病毒复制子的RNA复制的抑制活性的抗丙型肝炎病毒活性的新的环肽化合物或其盐,其制备方法,包含其的药物组合物, 以及在人或动物中预防和/或治疗丙型肝炎的方法。
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公开(公告)号:US07129232B2
公开(公告)日:2006-10-31
申请号:US10695895
申请日:2003-10-30
申请人: Hidenori Ohki , Shinya Okuda , Toshio Yamanaka , Masaru Ohgaki , Ayako Toda , Kohji Kawabata , Satoshi Inoue , Keiji Misumi , Kenji Itoh , Kenji Satoh
发明人: Hidenori Ohki , Shinya Okuda , Toshio Yamanaka , Masaru Ohgaki , Ayako Toda , Kohji Kawabata , Satoshi Inoue , Keiji Misumi , Kenji Itoh , Kenji Satoh
IPC分类号: C07D501/46 , C07D501/38 , A61K31/546 , A61P31/04
CPC分类号: C07D501/00 , Y02P20/55
摘要: The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl, hydroxy(lower)alkyl or halo(lower)alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower alkylene or lower alkenylene; R3 is hydrogen or lower alkyl; R4 is R5 is carboxy or protected carboxy; and R6 is amino or protected amino, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.
摘要翻译: 本发明涉及式[I]化合物:其中R 1是低级烷基,羟基(低级)烷基或卤代(低级)烷基,R 2是 是氢或氨基保护基,或R 1和R 2结合在一起形成低级亚烷基或低级亚烯基; R 3是氢或低级烷基; R 4是R 5是羧基或被保护的羧基; 和R 6是氨基或被保护的氨基或其药学上可接受的盐,制备式[I]化合物的方法,以及药物组合物,其包含式[I]化合物 与药学上可接受的载体混合。
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公开(公告)号:US20090012054A1
公开(公告)日:2009-01-08
申请号:US12280419
申请日:2007-03-16
申请人: Toshio Yamanaka , Ayako Toda , Hidenori Ohki , Shinya Okuda , Kohji Kawabata , Kenji Murano , Kazuo Hatano , Shinobu Takeda , Toru Nakai , Masaru Oogaki , Satoshi Inoue , Keiji Misumi , Kenji Itoh
发明人: Toshio Yamanaka , Ayako Toda , Hidenori Ohki , Shinya Okuda , Kohji Kawabata , Kenji Murano , Kazuo Hatano , Shinobu Takeda , Toru Nakai , Masaru Oogaki , Satoshi Inoue , Keiji Misumi , Kenji Itoh
IPC分类号: A61K31/546 , C07D501/16 , A61P31/00
CPC分类号: C07D501/46
摘要: The present invention provides a compound of the formula [I]: wherein R1 is lower alkyl, etc. and R2 is hydrogen, etc., or R1 and R2 are bonded together to form lower alkylene; R3 is a group represented by wherein R6 and R7 are independently optionally protected amino, etc.; m and n are independently an integer of 0 to 6; R8 and R9 are independently optionally protected amino, etc., and q and r are independently an integer of 0 to 6, or R8 and R9, together with the adjacent alkylene(s) and the nitrogen atom, form saturated nitrogen-containing heterocycle optionally having substituent(s); R4 is lower alkyl, etc.; and R5 is amino, etc., or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供式[I]化合物:其中R1是低级烷基等,R2是氢等,或者R1和R2键合在一起形成低级亚烷基; R3是由R6和R7独立地是任意保护的氨基等表示的基团。 m和n分别为0〜6的整数。 R8和R9独立地是任选被保护的氨基等,q和r独立地是0-6的整数,或者R8和R9与相邻的亚烷基和氮原子一起形成饱和的含氮杂环, 具有取代基; R4是低级烷基等; R5为氨基等,或其药学上可接受的盐。
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公开(公告)号:US20050004094A1
公开(公告)日:2005-01-06
申请号:US10833088
申请日:2004-04-28
申请人: Toshio Yamanaka , Hidenori Ohki , Masaru Ohgaki , Shinya Okuda , Ayako Toda , Kohji Kawabata , Satoshi Inoue , Keiji Misumi , Kenji Itoh , Kenji Satoh
发明人: Toshio Yamanaka , Hidenori Ohki , Masaru Ohgaki , Shinya Okuda , Ayako Toda , Kohji Kawabata , Satoshi Inoue , Keiji Misumi , Kenji Itoh , Kenji Satoh
IPC分类号: A61P31/04 , C07D501/00 , C07D501/14 , C07D501/46 , A61K31/545
CPC分类号: C07D501/00
摘要: The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl which may have suitable substituent(s), R2 is amino, protected amino or guanidino, R3 is carboxy or protected carboxy, R4 is amino or protected amino, and A is lower alkylene, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.
摘要翻译: 本发明涉及式[I]化合物:其中R 1为可具有合适取代基的低级烷基,R 2为氨基,保护的氨基或胍基,R 3为羧基或 保护的羧基,R 4是氨基或被保护的氨基,A是低级亚烷基或其药学上可接受的盐,制备式[I]化合物的方法,以及药物组合物,其包含式[ I]与药学上可接受的载体混合。
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公开(公告)号:US07192943B2
公开(公告)日:2007-03-20
申请号:US10942916
申请日:2004-09-17
申请人: Toshio Yamanaka , Kenji Murano , Ayako Toda , Hidenori Ohki , Masaru Oogaki , Shinya Okuda , Kohji Kawabata , Satoshi Inoue , Keiji Misumi , Kenji Itoh , Kenji Sato
发明人: Toshio Yamanaka , Kenji Murano , Ayako Toda , Hidenori Ohki , Masaru Oogaki , Shinya Okuda , Kohji Kawabata , Satoshi Inoue , Keiji Misumi , Kenji Itoh , Kenji Sato
IPC分类号: C07D501/46 , A61K31/546 , A61P31/04
CPC分类号: C07D501/00 , Y02P20/55
摘要: The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl or hydroxy(lower)alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower alkylene; R is -A-R6 wherein A is bond, —NHCO—(CH2CO)n—, lower alkylene, —NH—CO—CO— or the like, and R6 is wherein R7, R8, R9 and R10 are independently amino, guanidino, amidino or the like; R4 is carboxy or protected carboxy; and R5 is amino or protected amino, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.
摘要翻译: 本发明涉及式[I]化合物:其中R 1是低级烷基或羟基(低级)烷基,R 2是氢或氨基保护基 或R 1和R 2结合在一起形成低级亚烷基; R为-AR 6,其中A为键,-NHCO-(CH 2 CO 2)n - ,低级亚烷基,-NH-CO- CO-等,并且R 6是其中R 7,R 8,R 9和R 9, 胍基10是独立的氨基,胍基,脒基等; R 4是羧基或被保护的羧基; 和R 5是氨基或被保护的氨基或其药学上可接受的盐,制备式[I]化合物的方法,以及药物组合物,其包含式[I]化合物 与药学上可接受的载体混合。
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公开(公告)号:US20070037786A1
公开(公告)日:2007-02-15
申请号:US11585262
申请日:2006-10-24
申请人: Hidenori Ohki , Shinya Okuda , Toshio Yamanaka , Masaru Ohgaki , Ayako Toda , Kohji Kawabata , Satoshi Inoue , Keiji Misumi , Kenji Itoh , Kenji Satoh
发明人: Hidenori Ohki , Shinya Okuda , Toshio Yamanaka , Masaru Ohgaki , Ayako Toda , Kohji Kawabata , Satoshi Inoue , Keiji Misumi , Kenji Itoh , Kenji Satoh
IPC分类号: A61K31/545 , C07D501/14
CPC分类号: C07D501/00 , Y02P20/55
摘要: The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl, hydroxy(lower)alkyl or halo(lower)alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower alkylene or lower alkenylene; R3 is hydrogen or lower alkyl; R4 is R5 is carboxy or protected carboxy; and R6 is amino or protected amino, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.
摘要翻译: 本发明涉及式[I]化合物:其中R 1是低级烷基,羟基(低级)烷基或卤代(低级)烷基,R 2是 是氢或氨基保护基,或R 1和R 2结合在一起形成低级亚烷基或低级亚烯基; R 3是氢或低级烷基; R 4是R 5是羧基或被保护的羧基; 和R 6是氨基或保护的氨基或其药学上可接受的盐,制备式[I]化合物的方法,以及药物组合物,其包含式[I]化合物 与药学上可接受的载体混合。
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公开(公告)号:US20050096306A1
公开(公告)日:2005-05-05
申请号:US10942916
申请日:2004-09-17
申请人: Toshio Yamanaka , Kenji Murano , Ayako Toda , Hidenori Ohki , Masaru Oogaki , Shinya Okuda , Kohji Kawabata , Satoshi Inoue , Keiji Misumi , Kenji Itoh , Kenji Sato
发明人: Toshio Yamanaka , Kenji Murano , Ayako Toda , Hidenori Ohki , Masaru Oogaki , Shinya Okuda , Kohji Kawabata , Satoshi Inoue , Keiji Misumi , Kenji Itoh , Kenji Sato
IPC分类号: A61K31/546 , C07D501/00 , A61K31/545 , C07D501/14
CPC分类号: C07D501/00 , Y02P20/55
摘要: The present invention relates to a compound of the formula [I]: wherein R1 is lower alkyl or hydroxy(lower)alkyl, and R2 is hydrogen or amino protecting group, or R1 and R2 are bonded together and form lower alkylene; R is -A-R6 wherein A is bond, —NHCO—(CH2CO)n—, lower alkylene, —NH—CO—CO— or the like, and R6 is wherein R7, R8, R9 and R10 are independently amino, guanidino, amidino or the like; R4 is carboxy or protected carboxy; and R5 is amino or protected amino, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.
摘要翻译: 本发明涉及式[I]化合物:其中R 1是低级烷基或羟基(低级)烷基,R 2是氢或氨基保护基 或R 1和R 2结合在一起形成低级亚烷基; R为-AR 6,其中A为键,-NHCO-(CH 2 CO 2)n - ,低级亚烷基,-NH-CO- CO-等,并且R 6是其中R 7,R 8,R 9和R 9, 胍基10是独立的氨基,胍基,脒基等; R 4是羧基或被保护的羧基; 和R 5是氨基或被保护的氨基或其药学上可接受的盐,制备式[I]化合物的方法,以及药物组合物,其包含式[I]化合物 与药学上可接受的载体混合。
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公开(公告)号:US06232290B1
公开(公告)日:2001-05-15
申请号:US09446101
申请日:1999-12-22
申请人: Hidenori Ohki , Kenji Murano , Takashi Tojo , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Hiroaki Mizuno , David Barrett , Keiji Matsuda , Kohji Kawabata
发明人: Hidenori Ohki , Kenji Murano , Takashi Tojo , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Hiroaki Mizuno , David Barrett , Keiji Matsuda , Kohji Kawabata
IPC分类号: A61K3812
摘要: This invention relates to new polypeptide compounds represented by general formula (I), wherein R1, R2, R3 and R4 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on &bgr;-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译: 本发明涉及由通式(I)表示的新的多肽化合物,其中R1,R2,R3和R4如说明书中所定义或其具有抗微生物活性(特别是抗真菌活性)的盐,对β-1的抑制活性 3-葡聚糖合酶,其制备方法,涉及含有该组合物的药物组合物,以及用于预防和/或治疗感染性疾病的方法,包括卡介菌肺炎卡介菌感染(例如肺孢子虫卡氏肺炎)在人或 动物。
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公开(公告)号:US06743776B2
公开(公告)日:2004-06-01
申请号:US09308237
申请日:1999-05-21
IPC分类号: A61K3812
摘要: This invention relates to new polypeptide compounds represented by general formula [I]: wherein R1 and R2 are as defined in the description and pharmaceutically acceptable salt thereof which have antimicrobial activities (especially, antifungal activities), inhibitory activity on &bgr;-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for the prophylactic and/or therapeutic treatment of infectious disease including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译: 本发明涉及由通式[I]表示的新的多肽化合物:其中R 1和R 2如说明书及其药学上可接受的盐中所定义,其具有抗微生物活性(特别是抗真菌活性),对β -1,3-葡聚糖合酶,其制备方法,涉及包含其的药物组合物,以及用于预防和/或治疗感染性疾病的方法,包括卡介菌肺炎卡介菌感染(例如卡氏肺囊虫肺炎)在人中 正在或动物。
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