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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：US6013653A
公开(公告)日：2000-01-11
申请号：US43121
申请日：1998-04-21
申请人： Kooji Kagara , Nobutaka Kawai , Takashi Nakamura , Shigeru Ieda , Koji Machiya , Atsushi Ohigashi
发明人： Kooji Kagara , Nobutaka Kawai , Takashi Nakamura , Shigeru Ieda , Koji Machiya , Atsushi Ohigashi
IPC分类号： C07D471/04 , A61K31/44 , A61K31/435 , C07D221/06
CPC分类号： C07D471/04 , Y02P20/55
摘要： A process for producing pyridiondole derivatives represented by general formula (III) or their salts (wherein R.sup.1 represents hydrogen, lower alkyl or lower alkenyl; R.sup.2 represents hydrogen, lower alkyl or halogeno; and R.sup.3 represents optionally substituted imidazolyl), which comprises reacting a compound represented by general formula (I) or its salt (wherein R.sup.1 and R.sup.2 are each as defined above) with a compound represented by general formula (II) or its salt (wherein R.sup.3.sub.a represents optionally substituted imidazolyl having an imino protecting group; and X represents halogeno), followed by a reaction for eliminating the imino protecting group); and a process for producing optically active pyridoindole derivatives represented by general formula (IV) or their salts: which comprises reacting a racemic mixture of the pyridoindole derivative represent by formula (III) or its salt with (1R)-(-)-10-camphorsulfonic acid.
摘要翻译： PCT No.PCT / JP96 / 02692 Sec。 371日期：1998年4月21日 102（e）1998年4月21日PCT PCT 1996年9月18日PCT公布。 出版物WO97 / 11074 日本1997年3月27日制备通式（III）表示的吡啶并衍生物或其盐（其中R1表示氢，低级烷基或低级烯基; R2表示氢，低级烷基或卤代; R3代表任意取代的咪唑基）的方法， 其包括使通式（I）表示的化合物或其盐（其中R 1和R 2各自如上定义）与通式（II）表示的化合物或其盐（其中R 3a表示任选取代的具有亚氨基保护的咪唑基） 基团，X表示卤代），然后进行反应，除去亚氨基保护基）。 以及由通式（IV）表示的光学活性吡啶并吲哚衍生物或其盐的方法，其包括使式（III）表示的吡啶并吲哚衍生物的外消旋混合物或其盐与（1R） - （ - ） - 樟脑磺酸。
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公开(公告)号：US20120022271A1
公开(公告)日：2012-01-26
申请号：US13259640
申请日：2010-04-13
申请人： Atsushi Ohigashi , Takashi Kikuchi
发明人： Atsushi Ohigashi , Takashi Kikuchi
IPC分类号： C07C253/30 , C07D207/08 , C07D207/16
CPC分类号： C07D207/12 , C07B53/00 , C07C253/30 , C07D207/16 , C07C255/24
摘要： [Object]A novel method for producing an optically active pyrrolidine compound, which is useful as a production intermediate of a pharmaceutical, and a production intermediate thereof, is provided.[Means for Solution]According to the production method of the present invention, a chloro compound that is a key intermediate can be produced efficiently industrially by subjecting a mixture of regioisomers obtained by reacting an optically active epoxy compound substituted with aryl, which is easily available, with an amine compound, to chlorination. Furthermore, an optically active pyrrolidine compound can be produced industrially efficiently with the key intermediate.[Selected Figure] None
摘要翻译： 本发明提供了可用作药物的生产中间体的光学活性吡咯烷化合物及其制备中间体的新方法。 [解决方案]根据本发明的制造方法，作为关键中间体的氯化合物可以通过使由易于获得的光取代的芳基取代的光学活性环氧化合物反应获得的区域异构体的混合物在工业上有效地制造 与胺化合物进行氯化反应。 此外，光学活性吡咯烷化合物可以用关键中间体在工业上有效地制备。 [已选图]无
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公开(公告)号：US20050227914A1
公开(公告)日：2005-10-13
申请号：US10522622
申请日：2003-08-04
IPC分类号： C07D261/08 , C07D413/12 , C07K1/08 , C07K7/54 , C07K7/56 , A61K38/12 , C07D261/02 , C07K5/12
CPC分类号： C07K7/56 , C07D261/08
摘要： The present invention relates to a process for preparing a pharmaceutical starting compound compound by hydrolyzing a compound of the general formula (II): Wherein R1 is protected carboxy, R2 is lower alkoxy or higher alkoxy, A1 is an aromatic bivalent group, heterocyclic bivalent group or cyclo(lower)alkane bivalent group, and A2 is an aromatic bivalent group, heterocyclic bivalent group or cyclo(lower)alkane bivalent group, with aqueous potassium hydroxide and by treating with hydrochloric acid.
摘要翻译： 本发明涉及通过水解通式（II）的化合物来制备药物起始化合物的方法：其中R 1是保护的羧基，R 2是 低级烷氧基或高级烷氧基，A 1是芳族二价基团，杂环二价基团或环（低级）烷烃二价基团，A 2是芳族二价基团，杂环基 二价基团或环（低级）烷烃二价基团，与氢氧化钾水溶液一起，并用盐酸处理。
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公开(公告)号：US07199248B2
公开(公告)日：2007-04-03
申请号：US10522622
申请日：2003-08-04
IPC分类号： C07D261/08 , C07D487/12
CPC分类号： C07K7/56 , C07D261/08
摘要： The present invention relates to a process for preparing a pharmaceutical starting compound compound by hydrolyzing a compound of the general formula (II): Wherein R1 is protected carboxy, R2 is lower alkoxy or higher alkoxy, A1 is an aromatic bivalent group, heterocyclic bivalent group or cyclo (lower) alkane bivalent group, and A2 is an aromatic bivalent group, heterocyclic bivalent group or cyclo (lower) alkane bivalent group, with aqueous potassium hydroxide and by treating with hydrochloric acid.
摘要翻译： 本发明涉及通过水解通式（II）的化合物来制备药物起始化合物的方法：其中R 1是保护的羧基，R 2是 低级烷氧基或高级烷氧基，A 1是芳族二价基团，杂环二价基团或环（低级）烷烃二价基团，A 2是芳族二价基团，杂环基 二价基团或环（低级）烷烃二价基团，与氢氧化钾水溶液一起，并用盐酸处理。
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