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

IPC分类号： A61K38/00 ,  A61P31/00 ,  A61P31/10 ,  A61P43/00 ,  C07K7/56 ,  C07K7/50

CPC分类号： C07K7/56 ,  A61K38/00

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。

公开(公告)号：US06455726B2

公开(公告)日：2002-09-24

申请号：US09782291

申请日：2001-02-14

申请人： Masaharu Ichihara ,  Norio Hashimoto ,  Atsushi Kanda ,  Kooji Kagara

发明人： Masaharu Ichihara ,  Norio Hashimoto ,  Atsushi Kanda ,  Kooji Kagara

IPC分类号： C07C22900

CPC分类号： C07C227/06 ,  C07C229/38 ,  C07C229/34

摘要： A compound of the following formula (II) and a process for preparing of the compound of the following formula (I) its preparation wherein R1 is carboxy or protected carboxy; R2 is lower alkoxy or higher alkoxy; A1 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane; and A2 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane, or a salt thereof. The process comprises, reacting a compound of the formula (III): wherein R1, R2, A1 and A2 are each as defined above or a salt thereof, with an acid ammonium salt to give a compound of the formula (II).

摘要翻译： 下式（II）的化合物及其制备方法，其中R1为羧基或被保护的羧基; R2为低级烷氧基或高级烷氧基; A1为二价芳环，二价杂环 基团或二价环（低级）烷烃; 和A 2是二价芳环，二价杂环基或二价环（低级）烷烃或其盐。 该方法包括使式（III）化合物：其中R1，R2，A1和A2各自如上定义，或其盐与酸性铵盐反应，得到式（II）化合物。

公开(公告)号：US06291680B1

公开(公告)日：2001-09-18

申请号：US09446359

申请日：1999-12-20

申请人： Masaharu Ichihara ,  Norio Hashimoto ,  Atsushi Kanda ,  Kooji Kagara

发明人： Masaharu Ichihara ,  Norio Hashimoto ,  Atsushi Kanda ,  Kooji Kagara

IPC分类号： C07D261106

CPC分类号： C07C227/06 ,  C07C229/38 ,  C07C229/34

摘要： A compound of formula (1) or a salt thereof: wherein R1 is a carboxy or a protected carboxy; R2 is a lower alkoxy or a higher alkoxy; A1 is a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane; and A2 a divalent aromatic ring, a divalent heterocyclic group or a divalent cyclo(lower)alkane; is prepared by reacting a compound of formula (III) or a salt thereof with acid ammonium salt: wherein R1, R2, A1 and A2 are each as defined above; to give a compound of formula (II) or a salt thereof which is further reacted with a salt of hydroxylamine: wherein R1, R2, A1 and A2 are each as defined above.

摘要翻译： 式（1）的化合物或其盐：其中R1是羧基或被保护的羧基; R2是低级烷氧基或高级烷氧基; A1是二价芳环，二价杂环基或二价环（低级）烷烃; 和A2为二价芳环，二价杂环基或二价环（低级）烷烃; 通过使式（III）的化合物或其盐与酸性铵盐反应制备：其中R1，R2，A1和A2各自如上所定义; 得到与羟胺盐进一步反应的式（II）化合物或其盐：其中R1，R2，A1和A2各自如上所定义。