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1.
公开(公告)号:US20080015202A1
公开(公告)日:2008-01-17
申请号:US11574946
申请日:2005-09-08
Applicant: Takayuki Inoue , Takashi Tojo , Masataka Morita
Inventor: Takayuki Inoue , Takashi Tojo , Masataka Morita
IPC: A61K31/426 , A61K31/445 , A61K31/497 , A61P27/02 , C07D411/00
CPC classification number: C07D417/10 , C07D277/46 , C07D417/06 , C07D417/12
Abstract: A compound of the formula (I): U-V-W-X-Y-Z (I) wherein U is lower alkyl; V is —CONH— or —NR1CO— wherein R1 is a hydrogen or lower alkyl; W is a bond or lower alkylene; X is a bivalent residue derived from optionally substituted thiazole; Y is a bond or lower alkylene; and Z is a group of the formula: wherein R2 is a group of the formula: -A-B-D-E-F-G wherein A is a bond or lower alkylene; B is a bond, —NH— or D is a bond, —CS— or —CO—; E is a bond or —NH—; F is a bond, —CO—, —O— or —SO2—; and G is lower alkyl, optionally protected amino, —OH, phenyl, R3 is lower alkyl, provided that when Z is a group of the formula: then G should not be amino, when Z is a group of the formula: then G should not be when Z is a group of the formula: and G is optionally protected amino, then D should be —CS—, or then A should be lower alkylene, B or E should be —NH— and F should be —CO—; or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor as well as a pharmaceutical composition and a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a subject, and the like.
Abstract translation: 式(I)的化合物:<?in-line-formula description =“In-line Formulas”end =“lead”?> UVWXYZ(I)<?in-line-formula description =“In-line Formulas” end =“tail”?>其中U是低级烷基; V是-CONH-或-NR 1 CO-,其中R 1是氢或低级烷基; W是键或低级亚烷基; X是衍生自任选取代的噻唑的二价残基; Y是键或低级亚烷基; 并且Z是下式的基团:其中R 2是下列基团:-A-B-D-E-F-G其中A是键或低级亚烷基; B是键,-NH-或D是键,-CS-或-CO-; E是键或-NH-; F是键,-CO - , - O-或-SO 2 - 。 并且G为低级烷基,任意保护的氨基,-OH,苯基,R 3为低级烷基,条件是当Z为下式基团时,则G不应为氨基,当Z为 组式为:那么G不应该是当Z是下式的基团时:G是任意保护的氨基,那么D应该是-CS-,或者A应该是低级亚烷基,B或E应该是-NH- 而F应为-CO-; 或其药学上可接受的盐可用作血管粘附蛋白-1(VAP-1)抑制剂,以及用于预防或治疗VAP-1相关疾病,特别是黄斑水肿的药物组合物和方法,该方法包括施用有效的 化合物或其药学上可接受的盐对受试者的量等。
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公开(公告)号:US06331521B1
公开(公告)日:2001-12-18
申请号:US09423654
申请日:1999-12-01
Applicant: Yasuhiro Hori , Yasuhisa Tsurumi , Shigehiro Takase , Hiroshi Hatanaka , Kazutoshi Sakamoto , Seiji Hashimoto , Hidenori Ohki , Takashi Tojo , Keiji Matsuda , Kohji Kawabata
Inventor: Yasuhiro Hori , Yasuhisa Tsurumi , Shigehiro Takase , Hiroshi Hatanaka , Kazutoshi Sakamoto , Seiji Hashimoto , Hidenori Ohki , Takashi Tojo , Keiji Matsuda , Kohji Kawabata
IPC: A61K3800
Abstract: 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.
Abstract translation: 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。
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公开(公告)号:US08163767B2
公开(公告)日:2012-04-24
申请号:US11995445
申请日:2006-07-13
Applicant: Takayuki Inoue , Takashi Tojo , Masataka Morita , Yutaka Nakajima , Keiko Hatanaka , Shohei Shirakami , Hiroshi Sasaki , Akira Tanaka , Fumie Takahashi , Koichiro Mukoyoshi , Yasuyuki Higashi , Akira Okimoto , Takeshi Hondo , Hitoshi Sawada
Inventor: Takayuki Inoue , Takashi Tojo , Masataka Morita , Yutaka Nakajima , Keiko Hatanaka , Shohei Shirakami , Hiroshi Sasaki , Akira Tanaka , Fumie Takahashi , Koichiro Mukoyoshi , Yasuyuki Higashi , Akira Okimoto , Takeshi Hondo , Hitoshi Sawada
IPC: A61K31/44 , C07D471/14
CPC classification number: C07D471/14 , C07D519/00
Abstract: The invention relates to compound of the formula (I) or its salt, wherein —R1, —R2, —R3, —R4, —R5, -M-, —X— and —Y═ are as defined in the description, their use of as, medicament, the process for their preparation and use for the treatment of JAK3 mediated diseases.
Abstract translation: 本发明涉及式(I)化合物或其盐,其中-R1,-R2,-R3,-R4,-R5,-M-,-X-和-Y =如说明书中所定义,它们 使用as,药物,其制备方法和用于治疗JAK3介导的疾病。
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公开(公告)号:US07442715B2
公开(公告)日:2008-10-28
申请号:US11505321
申请日:2006-08-17
Applicant: Akira Nagashima , Takayuki Inoue , Mitsuru Ohkubo , Kousei Yoshihara , Takashi Tojo , Masataka Morita
Inventor: Akira Nagashima , Takayuki Inoue , Mitsuru Ohkubo , Kousei Yoshihara , Takashi Tojo , Masataka Morita
IPC: A61K31/427
CPC classification number: C07D417/06 , C07D277/46 , C07D277/48 , C07D277/56 , C07D417/12
Abstract: A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a mammal, and the like.
Abstract translation: 式(I)化合物:其中各符号如说明书中所定义,或其药学上可接受的盐可用作血管粘附蛋白-1(1R) VAP-1)抑制剂,药物组合物,预防或治疗VAP-1相关疾病,尤其是黄斑水肿的方法,该方法包括将有效量的化合物或其药学上可接受的盐给予哺乳动物等 。
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5.
公开(公告)号:US20070254931A1
公开(公告)日:2007-11-01
申请号:US11572772
申请日:2005-07-27
Applicant: Takayuki Inoue , Takashi Tojo , Masataka Morita
Inventor: Takayuki Inoue , Takashi Tojo , Masataka Morita
IPC: A61K31/426 , A61P19/02 , A61P19/08 , A61P3/10 , A61P9/10 , C07D277/46
CPC classification number: C07D277/46
Abstract: A compound of the formula (I), (II), (III) or (IV): wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a subject, and the like.
Abstract translation: 式(I),(II),(III)或(IV)的化合物:其中每个符号如说明书中所定义,或其药学上可接受的盐可用作血管粘附蛋白-1(VAP-1) 抑制剂,药物组合物,预防或治疗VAP-1相关疾病,特别是黄斑水肿的方法,该方法包括向受试者施用有效量的化合物或其药学上可接受的盐等。
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公开(公告)号:US07125901B2
公开(公告)日:2006-10-24
申请号:US10764529
申请日:2004-01-27
Applicant: Takayuki Inoue , Takashi Tojo , Masataka Morita , Mitsuru Ohkubo , Kousei Yoshihara , Akira Nagashima
Inventor: Takayuki Inoue , Takashi Tojo , Masataka Morita , Mitsuru Ohkubo , Kousei Yoshihara , Akira Nagashima
IPC: A61K31/427 , C07D277/44
CPC classification number: C07D417/06 , C07D277/46 , C07D277/48 , C07D277/56 , C07D417/12
Abstract: A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a mammal, and the like.
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公开(公告)号:US20050171350A1
公开(公告)日:2005-08-04
申请号:US10498018
申请日:2002-12-16
Applicant: Kazuhiko Take , Chiyoshi Kasahara , Shinji Shigenaga , Yoshiteru Eikyu , Takashi Tojo
Inventor: Kazuhiko Take , Chiyoshi Kasahara , Shinji Shigenaga , Yoshiteru Eikyu , Takashi Tojo
IPC: A61K31/4985 , A61K31/506 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P11/06 , A61P11/10 , A61P17/00 , A61P17/04 , A61P19/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P27/02 , A61P27/14 , A61P27/16 , A61P29/00 , A61P35/00 , A61P43/00 , C07D403/06 , C07D403/12 , C07D403/14 , C07D487/04 , C07D487/02 , C07D43/02
CPC classification number: C07D403/14 , C07D403/06 , C07D487/04
Abstract: A compound of the formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined in the description, or a salt thereof. The object compound of the present invention has pharmacological activities such as Tachykinin antagonism, and is useful for manufacture of a medicament for treating or preventing Tachykinin-mediated diseases.
Abstract translation: 式(I)的化合物:其中R 1,R 2,R 3,R 4, R 5,R 6,R 7,R 8和R 9, 各自如说明书中所定义,或其盐。 本发明的目的化合物具有速激肽拮抗作用等药理活性,可用于制备治疗或预防速激肽介导的疾病的药物。
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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
Applicant: 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
Inventor: 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
Abstract: 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.
Abstract translation: 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:US06507345B1
公开(公告)日:2003-01-14
申请号:US08829424
申请日:1997-03-31
Applicant: Takashi Tojo
Inventor: Takashi Tojo
IPC: G09G500
CPC classification number: G06F3/04812
Abstract: An apparatus and method for creating graphics in which an image pattern to be pasted is displayed on the screen of a display unit through a display content VRAM, by inputting an operation command from an operator for pasting the image pattern on the display screen of a display unit from an input unit, referring to pattern data to be pasted and also referring to animation information data, obtaining information on how the form and color temporarily change when the pattern is pasted, creating the display data, and displaying the display data on the screen of the display unit.
Abstract translation: 一种用于创建图形的装置和方法,其中通过显示内容VRAM在显示单元的屏幕上显示要粘贴的图像图案的图形,通过从操作者输入用于将图像图案粘贴在显示器的显示屏幕上的操作命令 单元,参考要粘贴的图案数据,并且还参考动画信息数据,获取当图案被粘贴时形式和颜色如何暂时改变的信息,创建显示数据,以及在屏幕上显示显示数据 的显示单元。
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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
Applicant: Hidenori Ohki , Kenji Murano , Takashi Tojo , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Hiroaki Mizuno , David Barrett , Keiji Matsuda , Kohji Kawabata
Inventor: Hidenori Ohki , Kenji Murano , Takashi Tojo , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Hiroaki Mizuno , David Barrett , Keiji Matsuda , Kohji Kawabata
IPC: A61K3812
Abstract: 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.
Abstract translation: 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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