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。

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。

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。

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。

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。

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。

公开(公告)号：US5376634A

公开(公告)日：1994-12-27

申请号：US715961

申请日：1991-06-17

申请人： Toshiro Iwamoto ,  Akihiko Fujie ,  Kumiko Nitta ,  Yasuhisa Tsurumi ,  Nobuharu Shigematsu ,  Chiyoshi Kasahara ,  Motohiro Hino ,  Masakuni Okuhara ,  Kazuo Sakane ,  Kohji Kawabata ,  Hidenori Ohki

发明人： Toshiro Iwamoto ,  Akihiko Fujie ,  Kumiko Nitta ,  Yasuhisa Tsurumi ,  Nobuharu Shigematsu ,  Chiyoshi Kasahara ,  Motohiro Hino ,  Masakuni Okuhara ,  Kazuo Sakane ,  Kohji Kawabata ,  Hidenori Ohki

IPC分类号： A61K38/00 ,  A61K38/12 ,  A61P31/04 ,  A61P31/10 ,  C07C309/43 ,  C07K1/06 ,  C07K7/56 ,  C07K7/64 ,  C12P21/04 ,  C12R1/645 ,  C07K5/12 ,  A61K37/02 ,  C07K7/06

CPC分类号： C07K7/56 ,  A61K38/00

摘要： A polypeptide compound having antimicrobial activity of the following general formula: ##STR1## wherein R.sup.1 is hydrogen or acyl group, R.sup.2 is hydroxy or acyloxy,R.sup.3 is hydroxysulfonyloxy, andR.sup.4 is hydrogen or carbamoyl,with proviso thatR.sup.1 is not palmitoyl, when R.sup.2 is hydroxy,R.sup.3 is hydroxysulfonyloxy andR.sup.4 is carbamoyl,and a pharmaceutically acceptable salt thereof.

摘要翻译： 具有以下通式的抗微生物活性的多肽化合物：其中R1是氢或酰基，R2是羟基或酰氧基，R3是羟基磺酰氧基，R4是氢或氨基甲酰基，条件是R1不是棕榈酰基，当R2 是羟基，R3是羟基磺酰氧基，R4是氨基甲酰基，及其药学上可接受的盐。

公开(公告)号：US06399567B1

公开(公告)日：2002-06-04

申请号：US09308218

申请日：1999-06-16

申请人： Ryuichi Kanasaki ,  Shigehiro Takase ,  Michizane Hashimoto ,  Hiroshi Hatanaka ,  Kazutoshi Sakamoto ,  Seiji Hashimoto ,  Nobuyuki Shiraishi ,  Hidenori Ohki ,  Kohji Kawabata

发明人： Ryuichi Kanasaki ,  Shigehiro Takase ,  Michizane Hashimoto ,  Hiroshi Hatanaka ,  Kazutoshi Sakamoto ,  Seiji Hashimoto ,  Nobuyuki Shiraishi ,  Hidenori Ohki ,  Kohji Kawabata

IPC分类号： A61K3812

CPC分类号： C07K7/56 ,  A61K38/00

摘要： This invention relates to new polypeptide compounds represented by the following formula (I): wherein R1 is as defined in the description or a 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： 本发明涉及由下式（I）表示的新多肽化合物：其中R1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-1,3-葡聚糖合酶的抑制活性， 涉及其制备方法，包含其的药物组合物，以及用于预防和/或治疗人或动物中包括卡氏肺囊虫感染（例如卡氏肺囊虫肺炎）的感染性疾病的方法。

公开(公告)号：US06331521B1

公开(公告)日：2001-12-18

申请号：US09423654

申请日：1999-12-01

申请人： Yasuhiro Hori ,  Yasuhisa Tsurumi ,  Shigehiro Takase ,  Hiroshi Hatanaka ,  Kazutoshi Sakamoto ,  Seiji Hashimoto ,  Hidenori Ohki ,  Takashi Tojo ,  Keiji Matsuda ,  Kohji Kawabata

发明人： Yasuhiro Hori ,  Yasuhisa Tsurumi ,  Shigehiro Takase ,  Hiroshi Hatanaka ,  Kazutoshi Sakamoto ,  Seiji Hashimoto ,  Hidenori Ohki ,  Takashi Tojo ,  Keiji Matsuda ,  Kohji Kawabata

IPC分类号： A61K3800

CPC分类号： C07K7/56 ,  A61K38/00

摘要： The invention relates to new polypeptide compounds represented by the following formula [I]: wherein R1 is hydrogen, etc, R2 is hydrogen, etc, R3 is hydrogen, etc, and R4 is hydrogen, etc, or a 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 diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.

摘要翻译： 本发明涉及由下式[I]表示的新的多肽化合物：其中R 1为氢等，R 2为氢等，R 3为氢等，R 4为氢等，或其具有抗微生物活性的盐 ，抗真菌活性），对β-1,3-葡聚糖合酶的抑制活性，其制备方法，包含其的药物组合物，以及用于预防和/或治疗感染性疾病包括卡氏肺囊虫感染的方法 （例如卡氏肺囊虫肺炎）在人或动物中。

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

CPC分类号： C07K7/56 ,  A61K38/00

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。