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公开(公告)号:US20050261177A1
公开(公告)日:2005-11-24
申请号:US10469233
申请日:2002-03-07
申请人: Ayako Toda , Hiroaki Mizuno , Takahiro Matsuya , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Hitomi Ogino , Keiji Matsuda
发明人: Ayako Toda , Hiroaki Mizuno , Takahiro Matsuya , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Hitomi Ogino , Keiji Matsuda
摘要: This invention relates to new polypeptide compound represented by the following general formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-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: 本发明涉及由以下通式(I)表示的新的多肽化合物:其中R 1,R 2,R 3,R 3, SUP> 4,R 5和R 6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)的抑制活性 β-1,3-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,包括卡氏肺囊虫感染(例如肺孢子虫卡氏肺炎) 人类或动物。
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公开(公告)号:US06884774B2
公开(公告)日:2005-04-26
申请号:US10030161
申请日:2001-02-20
申请人: Ayako Toda , Takahiro Matsuya , Hiroaki Mizuno , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Keiji Matsuda
发明人: Ayako Toda , Takahiro Matsuya , Hiroaki Mizuno , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Keiji Matsuda
IPC分类号: A61K38/00 , A01N43/90 , A61J1/03 , A61K38/12 , A61P31/00 , A61P31/10 , C07K1/113 , C07K7/54 , C07K7/56 , C07K5/00
摘要: This invention relates to new polypeptide compound represented by the general formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-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 Pneumocystic 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,R 2,R 3,R 3, 4,R 5和R 6如描述中所定义,或其盐具有抗微生物活性(特别是抗真菌活性),对β的抑制活性 -1,3-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,包括人类卡氏肺囊虫感染(例如肺孢子虫卡氏肺炎) 或动物。
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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:US06884868B1
公开(公告)日:2005-04-26
申请号:US09926385
申请日:2000-04-25
申请人: Takashi Tojo , Hidenori Ohki , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Keiji Matsuda , Masaharu Ichihara , Norio Hashimoto , Atsushi Kanda , Atsushi Ohigashi
发明人: Takashi Tojo , Hidenori Ohki , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Keiji Matsuda , Masaharu Ichihara , Norio Hashimoto , Atsushi Kanda , Atsushi Ohigashi
摘要: This invention relates to new polypeptide compound represented by general formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-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R 1,R 2,R 3,R 3, 4,R 5和R 6如描述中所定义,或其盐具有抗微生物活性(特别是抗真菌活性),对β的抑制活性 -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,所述传染病包括人类卡氏肺囊虫感染(例如肺孢子虫卡氏肺炎) 或动物。
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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: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: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:US5939413A
公开(公告)日:1999-08-17
申请号:US952112
申请日:1997-11-24
申请人: Masaaki Matsuo , Daijiro Hagiwara , Takashi Manabe , Nobukiyo Konishi , Shinji Shigenaga , Kenji Murano , Hiroshi Matsuda , Hiroshi Miyake
发明人: Masaaki Matsuo , Daijiro Hagiwara , Takashi Manabe , Nobukiyo Konishi , Shinji Shigenaga , Kenji Murano , Hiroshi Matsuda , Hiroshi Miyake
IPC分类号: A61K31/495 , A61K31/55 , A61P1/00 , A61P11/00 , A61P25/00 , A61P27/02 , A61P29/00 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14
CPC分类号: C07D401/14 , C07D403/04 , C07D403/06
摘要: This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or Tachykinin-mediated diseases in human beings or animals.
摘要翻译: PCT No.PCT / JP96 / 01334 Sec。 371日期:1997年11月24日 102(e)1997年11月24日PCT PCT 1996年5月21日PCT公布。 WO96 / 37488 PCT公开号 日期:1996年11月28日本发明涉及下式的哌嗪衍生物:其中每个符号如说明书中所定义,及其药学上可接受的盐,其制备方法,包含其的药物组合物,以及使用 相同的治疗或速激肽介导的疾病在人类或动物。
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公开(公告)号:US5670505A
公开(公告)日:1997-09-23
申请号:US348176
申请日:1994-11-28
申请人: Masaaki Matsuo , Daijiro Hagiwara , Takashi Manabe , Nobukiyo Konishi , Shinji Shigenaga , Kenji Murano , Hiroshi Matsuda , Hiroshi Miyake
发明人: Masaaki Matsuo , Daijiro Hagiwara , Takashi Manabe , Nobukiyo Konishi , Shinji Shigenaga , Kenji Murano , Hiroshi Matsuda , Hiroshi Miyake
IPC分类号: A61K31/495 , A61K31/496 , A61K31/55 , A61P9/00 , A61P11/00 , A61P11/08 , A61P17/00 , A61P25/04 , A61P25/06 , A61P27/02 , A61P27/14 , A61P27/16 , A61P29/00 , A61P37/08 , A61P43/00 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D417/06 , C07D417/14
CPC分类号: C07D401/06 , C07D241/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/06 , C07D417/06 , C07D417/14
摘要: A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl; Y is a direct bond or lower alkylene; and R.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein. The compounds are advantageously used as Tachykinin antagonists in the treatment of respiratory diseases, ophthalmic diseases and inflammatory diseases, for example.
摘要翻译: 下式的哌嗪化合物:其中:X为羰基或磺酰基; Y是直接键或低级亚烷基; 并且R 1,R 2,R 3,R 4如本文所定义。 该化合物例如有利地用作速激肽拮抗剂用于治疗呼吸系统疾病,眼科疾病和炎性疾病。
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公开(公告)号:US5883098A
公开(公告)日:1999-03-16
申请号:US884039
申请日:1997-06-27
申请人: Masaaki Matsuo , Daijiro Hagiwara , Takashi Manabe , Nobukiyo Konishi , Shinji Shigenaga , Kenji Murano , Hiroshi Matsuda , Hiroshi Miyake
发明人: Masaaki Matsuo , Daijiro Hagiwara , Takashi Manabe , Nobukiyo Konishi , Shinji Shigenaga , Kenji Murano , Hiroshi Matsuda , Hiroshi Miyake
IPC分类号: C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/06 , C07D417/06 , C07D417/14 , A61K31/495
CPC分类号: C07D401/06 , C07D241/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/06 , C07D417/06 , C07D417/14
摘要: A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl;Y is a direct bond or lower alkylene; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein. The compounds are advantageously used as Tachykinin antagonists in the treatment of respiratory diseases, ophthalmic diseases and inflammatory diseases, for example.
摘要翻译: 下式的哌嗪化合物:其中:X为羰基或磺酰基; Y是直接键或低级亚烷基; 并且R 1,R 2,R 3,R 4如本文所定义。 该化合物例如有利地用作速激肽拮抗剂用于治疗呼吸系统疾病,眼科疾病和炎性疾病。
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