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1. 发明申请

US20090041670A1 Near Infrared Fluorescent Contrast Agent And Method For Fluorescence Imaging 审中-公开
标题翻译：近红外荧光对比剂和荧光成像方法
公开(公告)号：US20090041670A1
公开(公告)日：2009-02-12
申请号：US12147717
申请日：2008-06-27
申请人： Masayuki Kawakami , Hiroshi Kitaguchi , Kai Licha , Christin Perlitz , Hiroaki Eguchi , Natsuko Tsuda , Kazuhiro Aikawa
发明人： Masayuki Kawakami , Hiroshi Kitaguchi , Kai Licha , Christin Perlitz , Hiroaki Eguchi , Natsuko Tsuda , Kazuhiro Aikawa
IPC分类号： A61K49/00
CPC分类号： A61K49/0032 , A61K49/0052
摘要： A near infrared fluorescent contrast agent which is excellent in permeability in a living tissue and enables specific imaging of tumor and/or blood vessel, comprising a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R7, and R8 represent a C1-C10 alkyl group or the like; R3, R4, R5, R6, R9, R10, R11, and R12 represent a hydrogen atom, a C1-C6 alkyl group, an aryl group or the like; X1 and X2 represent a C1-C15 alkyl group or an aryl group and X1 and X2 in total have 0 to 4 carboxyl groups; m1, m2, and m3 represents 0 or 1; L1 to L7 independently represent a methine group; M represents a hydrogen atom, a metal, or a quaternary ammonium salt; and n represents an integer of 1 to 7 necessary for neutralizing charge.
摘要翻译： 1.一种近红外荧光造影剂，其特征在于，在生物体组织中的透过性优异，能够对肿瘤和/或血管进行特异性成像，其特征在于，含有式（I）表示的化合物或其药学上可接受的盐，其中R1，R2，R7，并且R 8表示C 1 -C 10烷基等; R3，R4，R5，R6，R9，R10，R11和R12表示氢原子，C1-C6烷基，芳基等; X1和X2表示C1-C15烷基或芳基，X1和X2总共具有0至4个羧基; m1，m2，m3表示0或1; L1至L7独立地表示次甲基; M表示氢原子，金属或季铵盐; n表示中和电荷所需的1〜7的整数。

2. 发明申请

US20080045574A1 Anti-Trypanosomiasis Agent 有权
标题翻译：抗锥虫病药
公开(公告)号：US20080045574A1
公开(公告)日：2008-02-21
申请号：US11576426
申请日：2005-09-29
申请人： Masataka Ihara , Kiyosei Takasu , Khanitha Pudhom , Hiroshi Kitaguchi , Masayuki Kawakami , Kozo Sato
发明人： Masataka Ihara , Kiyosei Takasu , Khanitha Pudhom , Hiroshi Kitaguchi , Masayuki Kawakami , Kozo Sato
IPC分类号： A61K31/426 , A61P33/00
CPC分类号： C07D417/14 , A61K31/428 , A61K31/4439 , A61K31/4709 , Y02A50/414
摘要： The present invention is to provide an anti-trypanosomiasis agent having a high selective toxicity, and high preventing or treating effect against trypanosomiasis, comprising a compound shown by the following general formula (1) as an active ingredient (wherein R1 and R2 each independently represents a hydrogen atom, halogen atom, hydroxyl group, oxygen atom, C1-5 alkyl group, C1-5 alkoxy group, C5-8 aryl group, C5-8 aryloxy group, C2-6 alkoxycarbonyl group or C2-6 alkylaminocarbonyl group, and may be bound to each other; R3, R4, and R5 each independently represents a C1-5 alkyl group or C5-8 aryl group; R6 and R7 each independently represents a hydrogen atom, halogen atom, hydroxyl group, oxygen atom, C1-8 alkyl group, C1-5 alkoxy group, C5-8 aryl group, C5-8 aryloxy group, or C2-6 alkoxycarbonyl group, and may be bound to each other; Y and Z each independently represents an atom group necessary to form a 5- or 6-membered heterocycle; m and n each represent 0 or 1; Q represents a physiologically acceptable anion; k represents an integer of 0 to 2, necessary to make the electric charge of the whole molecule 0).
摘要翻译：本发明提供具有高选择性毒性和对锥虫病的高预防或治疗作用的抗锥虫病药，其包含由以下通式（1）表示的化合物作为活性成分（其中R 1， / O 2和R 2各自独立地表示氢原子，卤素原子，羟基，氧原子，C 1-5烷基，C 1-5 C 5〜8芳基，C 5〜8芳氧基，C 2-6烷氧基羰基或C 2-6个亚烷基氨基羰基，并且可以彼此结合; R 3，R 4和R 5 >各自独立地表示C 1-5烷基或C 5-8芳基; R 6和R 7， SUP各自独立地表示氢原子，卤素原子，羟基，氧原子，C 1-8烷基，C 1-5烷氧基，C 1〜 5-8芳基，C 5-8芳氧基，或C 1〜并且可以相互结合; Y和Z各自独立地表示形成5-或6-元杂环所必需的原子团; m和n各自表示0或1; Q表示生理上可接受的阴离子; k表示0〜2的整数，使整个分子的电荷为0）。

3. 发明授权

US07795285B2 Anti-trypanosomiasis agent 有权
标题翻译：抗锥虫病药
公开(公告)号：US07795285B2
公开(公告)日：2010-09-14
申请号：US11576426
申请日：2005-09-29
申请人： Masataka Ihara , Kiyosei Takasu , Khanitha Pudhom , Hiroshi Kitaguchi , Masayuki Kawakami , Kozo Sato
发明人： Masataka Ihara , Kiyosei Takasu , Khanitha Pudhom , Hiroshi Kitaguchi , Masayuki Kawakami , Kozo Sato
IPC分类号： A01N43/78
CPC分类号： C07D417/14 , A61K31/428 , A61K31/4439 , A61K31/4709 , Y02A50/414
摘要： The present invention is to provide an anti-trypanosomiasis agent having a high selective toxicity, and high preventing or treating effect against trypanosomiasis, comprising a compound shown by the following general formula (1) as an active ingredient (wherein R1 and R2 each independently represents a hydrogen atom, halogen atom, hydroxyl group, oxygen atom, C1-5 alkyl group, C1-5 alkoxy group, C5-8 aryl group, C5-8 aryloxy group, C2-6 alkoxycarbonyl group or C2-6 alkylaminocarbonyl group, and may be bound to each other; R3, R4, and R5 each independently represents a C1-5 alkyl group or C5-8 aryl group; R6 and R7 each independently represents a hydrogen atom, halogen atom, hydroxyl group, oxygen atom, C1-8 alkyl group, C1-5 alkoxy group, C5-8 aryl group, C5-8 aryloxy group, or C2-6 alkoxycarbonyl group, and may be bound to each other; Y and Z each independently represents an atom group necessary to form a 5- or 6-membered heterocycle; m and n each represent 0 or 1; Q represents a physiologically acceptable anion; k represents an integer of 0 to 2, necessary to make the electric charge of the whole molecule 0).
摘要翻译：本发明提供具有高选择性毒性和对锥虫病的高预防或治疗作用的抗锥虫病药，其包含由以下通式（1）表示的化合物作为活性成分（其中R 1和R 2各自独立地表示氢原子，卤素原子，羟基，氧原子，C 1-5烷基，C 1-5烷氧基，C 5-8芳基，C 5-8芳氧基，C 2-6烷氧基羰基或C 2-6烷基氨基羰基，可以相互结合; R3，R4和R5各自独立地表示C1-5烷基或C5-8芳基; R6和R7各自独立地表示氢原子，卤素原子，羟基，氧原子，C1- 8个烷基，C 1-5烷氧基，C 5-8芳基，C 5-8芳氧基或C 2-6烷氧基羰基，并且可以彼此结合; Y和Z各自独立地表示形成 5-或6-元杂环; m和n各自表示0或1; Q表示物理生理上可接受的阴离子 k表示0〜2的整数，使整个分子的电荷为0）。

4. 发明申请

US20100113789A1 MEDICINAL COMPOSITION FOR PREVENTION OR TREATMENT OF PARASITIC PROTOZOAN INFECTION 有权
标题翻译：用于预防或治疗PARASITIC PROTOZOAN感染的药物组合物
公开(公告)号：US20100113789A1
公开(公告)日：2010-05-06
申请号：US11576429
申请日：2005-09-30
申请人： Masataka Ihara , Kiyosei Takasu , Khanitha Pudhom , Hiroshi Kitaguchi , Masayuki Kawakami , Kozo Sato
发明人： Masataka Ihara , Kiyosei Takasu , Khanitha Pudhom , Hiroshi Kitaguchi , Masayuki Kawakami , Kozo Sato
IPC分类号： C07D417/14
CPC分类号： C07D277/84 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/4709 , C07D277/64 , C07D417/14 , Y02A50/409 , Y02A50/411 , Y02A50/414
摘要： The present invention is to provide a medicinal composition for preventing or treating parasitic protozoan infections, having a high selective toxicity against parasitic protozoan infection, and a superior preventive or treating effect. A medicinal composition for preventing or treating parasitic protozoan infections comprises a compound shown by the following general formula (1) as an active ingredient (wherein R represents an alkyl group, aryl group or heterocyclic group; A and B each independently represents a 5- or 6-membered ring containing at least one hetero atom, or a condensation ring wherein 1 or more 3- to 8-membered ring is condensed thereto; Y represents S, O, Se, or —NR1— (R1 represents an alkyl group, aryl group or heterocyclic group); L1, L2, L3, L4 and L5 each independently represents a methine group; Q represents a physiologically acceptable anion; k represents an integer of 0 to 2, necessary to make the electric charge of the whole molecule 0; p and q each represents an integer of 0 to 3, wherein the sum of p and q is 1 or more, and 6 or less.)
摘要翻译：本发明提供一种用于预防或治疗对寄生原虫感染具有高选择性毒性的寄生原虫感染的药物组合物，以及优异的预防或治疗效果。用于预防或治疗寄生原生动物感染的药物组合物包含由以下通式（1）表示的化合物作为活性成分（其中R表示烷基，芳基或杂环基; A和B各自独立地表示5-或含有至少一个杂原子的6元环或其中1个以上3〜8元环稠合的缩合环; Y表示S，O，Se或-NR1-（R1表示烷基，芳基基团或杂环基）; L1，L2，L3，L4和L5各自独立地表示次甲基; Q表示生理上可接受的阴离子; k表示使整个分子0的电荷所必需的0至2的整数; p和q各自表示0〜3的整数，p和q的和为1以上6以下）

5. 发明申请

US20050226815A1 Near infrared fluorescent contrast agent and method for fluorescence imaging 失效
标题翻译：近红外荧光造影剂及荧光成像方法
公开(公告)号：US20050226815A1
公开(公告)日：2005-10-13
申请号：US10506819
申请日：2003-03-07
申请人： Masayuki Kawakami , Hiroshi Kitaguchi , Kai Licha , Christin Perlitz , Hiroaki Eguchi , Natsuko Tsuda , Kazuhiro Aikawa
发明人： Masayuki Kawakami , Hiroshi Kitaguchi , Kai Licha , Christin Perlitz , Hiroaki Eguchi , Natsuko Tsuda , Kazuhiro Aikawa
IPC分类号： C07D409/14 , A61B1/00 , A61B3/10 , A61B3/14 , A61K49/00 , C07D209/14 , C07D209/60 , G01N21/64 , A61B10/00 , A61B5/00 , A61B8/00
CPC分类号： A61K49/0032 , A61K49/0052
摘要： A near infrared fluorescent contrast agent which is excellent in permeability in a living tissue and enables specific imaging of tumor and/or blood vessel, comprising a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R7, and R8 represent a C1-C10 alkyl group or the like; R3, R4, R5, R6, R9, R10, R11, and R12 represent a hydrogen atom, a C1-C6 alkyl group, an aryl group or the like; X1 and X2 represent a C1-C15 alkyl group or an aryl group and X1 and X2 in total have 0 to 4 carboxyl groups; m1, m2, and m3 represents 0 or 1; L1 to L7 independently represent a methine group; M represents a hydrogen atom, a metal, or a quaternary ammonium salt; and n represents an integer of 1 to 7 necessary for neutralizing charge.
摘要翻译：一种近红外荧光造影剂，其在生物体组织中的渗透性优异，能够进行肿瘤和/或血管的特异性成像，其包含式（I）表示的化合物或其药学上可接受的盐，其中R 1， R 2，R 7，R 8和R 8表示C 1 -C 3烷基， 10烷基等; R 3，R 4，R 5，R 6，R 9， R 10，R 11和R 12代表氢原子，C 1 -C 12烷基， 6个烷基，芳基等; X 1和X 2代表C 1 -C 15烷基或芳基，X ^{1和X 2共有0至4个羧基; m 1，m 2，m 3，O 3表示0或1; L 1至L 7独立地表示次甲基; M表示氢原子，金属或季铵盐; n表示中和电荷所需的1〜7的整数。}

6. 发明授权

US06939975B2 Cyanine dyes 失效
标题翻译：花青染料
公开(公告)号：US06939975B2
公开(公告)日：2005-09-06
申请号：US10344273
申请日：2001-08-03
申请人： Masayuki Kawakami , Hiroshi Kitaguchi
发明人： Masayuki Kawakami , Hiroshi Kitaguchi
IPC分类号： C09B23/01 , C09B23/08 , G03C1/12 , G03C1/14 , G03C1/20
CPC分类号： C09B23/0041 , C09B23/0033 , C09B23/0066 , C09B23/086 , G03C1/127 , G03C1/14 , G03C1/20
摘要： A compound represented by the following formula (I) or a salt thereof: wherein R1 and R2 represent an alkyl group or an aryl group; R3 to R6 represent hydrogen atom, an alkyl group, an aryl group, a heteroaryl group, a halogen atom, cyano group, carboxyl group or sulfo group; X1 and X2 represent an alkyl group having 1 to 15 carbon atoms or an aryl group, and the total number of carboxyl groups existing in X1 and X2 is 4 or less; m1 to m3 represents 0 or 1; L1 to L7 represent a methine group; M represents hydrogen atom, a metal or a quaternary ammonium salt; Y represents nonmetallic elements required to form a 5- to 10-membered heterocyclic ring; and n represents an integer of 1 to 7 required to neutralize charge, which is useful for manufacture of silver halide photographic light-sensitive materials.
摘要翻译：由下式（I）表示的化合物或其盐：其中R 1和R 2代表烷基或芳基; R 3至R 6代表氢原子，烷基，芳基，杂芳基，卤素原子，氰基，羧基或磺基; X 1和X 2代表具有1至15个碳原子的烷基或芳基，并且存在于X 1中的羧基的总数 SUP>和X <2>为4以下; m 1至m 3表示0或1; L 1至L 7表示次甲基; M表示氢原子，金属或季铵盐; Y表示形成5至10元杂环所需的非金属元素; n表示中和电荷所需的1〜7的整数，可用于制造卤化银照相感光材料。

7. 发明授权

US08193224B2 Medicinal composition for prevention or treatment of parasitic protozoan infection 有权
标题翻译：用于预防或治疗寄生原生动物感染的药物组合物
公开(公告)号：US08193224B2
公开(公告)日：2012-06-05
申请号：US11576429
申请日：2005-09-30
申请人： Masataka Ihara , Kiyosei Takasu , Khanitha Pudhom , Hiroshi Kitaguchi , Masayuki Kawakami , Kozo Sato
发明人： Masataka Ihara , Kiyosei Takasu , Khanitha Pudhom , Hiroshi Kitaguchi , Masayuki Kawakami , Kozo Sato
IPC分类号： A61K31/427 , A61K31/428 , C07D277/66 , C07D277/04 , C07D277/84
CPC分类号： C07D277/84 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/4709 , C07D277/64 , C07D417/14 , Y02A50/409 , Y02A50/411 , Y02A50/414
摘要： The present invention is to provide a medicinal composition for preventing or treating parasitic protozoan infections, having a high selective toxicity against parasitic protozoan infection, and a superior preventive or treating effect. A medicinal composition for preventing or treating parasitic protozoan infections comprises a compound shown by the following general formula (1) as an active ingredient (wherein R represents an alkyl group, aryl group or heterocyclic group; A and B each independently represents a 5- or 6-membered ring containing at least one hetero atom, or a condensation ring wherein 1 or more 3- to 8-membered ring is condensed thereto; Y represents S, O, Se, or —NR1— (R1 represents an alkyl group, aryl group or heterocyclic group); L1, L2, L3, L4 and L5 each independently represents a methine group; Q represents a physiologically acceptable anion; k represents an integer of 0 to 2, necessary to make the electric charge of the whole molecule 0; p and q each represents an integer of 0 to 3, wherein the sum of p and q is 1 or more, and 6 or less).
摘要翻译：本发明提供一种用于预防或治疗对寄生原虫感染具有高选择性毒性的寄生原虫感染的药物组合物，以及优异的预防或治疗效果。用于预防或治疗寄生原生动物感染的药物组合物包含由以下通式（1）表示的化合物作为活性成分（其中R表示烷基，芳基或杂环基; A和B各自独立地表示5-或含有至少一个杂原子的6元环或其中1个以上3〜8元环稠合的缩合环; Y表示S，O，Se或-NR1-（R1表示烷基，芳基基团或杂环基）; L1，L2，L3，L4和L5各自独立地表示次甲基; Q表示生理上可接受的阴离子; k表示使整个分子0的电荷所必需的0至2的整数; p和q各自表示0〜3的整数，p和q的和为1以上且6以下）。

8. 发明申请

US20090076067A1 PHARMACEUTICAL COMPOSITION COMPRISING AZARHODACYANINE COMPOUND AS ACTIVE INGREDIENT 审中-公开
标题翻译：包含作为活性成分的阿拉伯糖胺化合物的药物组合物
公开(公告)号：US20090076067A1
公开(公告)日：2009-03-19
申请号：US11915286
申请日：2006-06-05
申请人： Masataka Ihara , Kiyosei Takasu , Kanitha Pudhom , Masayuki Kawakami , Hiroshi Kitaguchi , Kouzou Satou
发明人： Masataka Ihara , Kiyosei Takasu , Kanitha Pudhom , Masayuki Kawakami , Hiroshi Kitaguchi , Kouzou Satou
IPC分类号： A61K31/437 , C07D417/14 , A61K31/444
CPC分类号： C07D417/14 , A61K31/426 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4709 , C07D498/04 , C07D513/04 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415 , Y02A50/421
摘要： The object of the invention is to provide pharmaceutical composition that can be used as a therapeutic and/or prophylactic agent. Particularly, the pharmaceutical composition of the invention has significant therapeutic effect and survival benefit for the disease caused by parasitic protozoa, and selective toxicity against the causative protozoa. The pharmaceutical composition comprises a compound represented by general formula (1). Particularly, the invention relates to a composition that is an effective therapeutic/prophylactic agent for malaria, leishmania, African sleeping sickness, Chagas disease, toxoplasmosis lymphatic filariasis, babesiosis, and coccidiosis, and a novel compound contained therein.
摘要翻译：本发明的目的是提供可用作治疗和/或预防剂的药物组合物。特别地，本发明的药物组合物对由寄生原虫引起的疾病和对致病原生动物的选择性毒性具有显着的治疗效果和生存益处。药物组合物包含由通式（1）表示的化合物。特别地，本发明涉及作为疟疾，利什曼原虫，非洲睡眠病，恰加斯病，弓形体病，淋巴丝虫病，贝氏菌病和球虫病的有效治疗/预防剂及其中所含的新化合物的组合物。

9. 发明申请

US20090036437A1 PHARMACEUTICAL COMPOSITION COMPRISING PHENOXAZINIUM COMPOUND AS AN ACTIVE INGREDIENT 审中-公开
标题翻译：包含酚氧化合物作为活性成分的药物组合物
公开(公告)号：US20090036437A1
公开(公告)日：2009-02-05
申请号：US11815394
申请日：2006-02-07
申请人： Masataka Ihara , Kiyosei Takasu , Masayuki Kawakami , Hiroshi Kitaguchi , Kouzou Satou
发明人： Masataka Ihara , Kiyosei Takasu , Masayuki Kawakami , Hiroshi Kitaguchi , Kouzou Satou
IPC分类号： C07D265/38 , A61K31/538 , C07D413/10 , A61P33/02
CPC分类号： A61K31/538 , C07D265/38 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415
摘要： The purpose of the present invention is therefore to provide a pharmaceutical composition, especially that for the treatment and/or prevention of parasitic infection by protozoa, which has a high therapeutic effect and selective toxicity or a life-prolongation effect for the parasitic infection by protozoa. The present invention is therefore related to a pharmaceutical composition comprising the compound represented by the following general formula (1) as an active ingredient, especially to those for the treatment and/or prevention of parasitic infection by protozoa
摘要翻译：因此，本发明的目的是提供一种药物组合物，特别是用于治疗和/或预防原生动物寄生虫感染的药物组合物，其对原生动物的寄生虫感染具有高治疗效果和选择性毒性或延长寿命。因此，本发明涉及包含由以下通式（1）表示的化合物作为活性成分的药物组合物，特别是用于治疗和/或预防原生动物寄生虫感染的药物组合物

10. 发明授权

US07473415B2 Near infrared fluorescent contrast agent and method for fluorescence imaging 失效
标题翻译：近红外荧光造影剂及荧光成像方法
公开(公告)号：US07473415B2
公开(公告)日：2009-01-06
申请号：US10506819
申请日：2003-03-07
申请人： Masayuki Kawakami , Hiroshi Kitaguchi , Kai Licha , Christin Perlitz , Hiroaki Eguchi , Natsuko Tsuda , Kazuhiro Aikawa
发明人： Masayuki Kawakami , Hiroshi Kitaguchi , Kai Licha , Christin Perlitz , Hiroaki Eguchi , Natsuko Tsuda , Kazuhiro Aikawa
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K49/0032 , A61K49/0052
摘要： A near infrared fluorescent contrast agent which is excellent in permeability in a living tissue and enables specific imaging of tumor and/or blood vessel, comprising a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R7, and R8 represent a C1-C10 alkyl group or the like; R3, R4, R5, R6, R9, R10, R11, and R12 represent a hydrogen atom, a C1-C6 alkyl group, an aryl group or the like; X1 and X2 represent a C1-C15 alkyl group or an aryl group and X1 and X2 in total have 0 to 4 carboxyl groups; m1, m2, and m3 represents 0 or 1; L1 to L7 independently represent a methine group; M represents a hydrogen atom, a metal, or a quaternary ammonium salt; and n represents an integer of 1 to 7 necessary for neutralizing charge.
摘要翻译： 1.一种近红外荧光造影剂，其特征在于，在生物体组织中的透过性优异，能够对肿瘤和/或血管进行特异性成像，其特征在于，含有式（I）表示的化合物或其药学上可接受的盐，其中R1，R2，R7，并且R 8表示C 1 -C 10烷基等; R3，R4，R5，R6，R9，R10，R11和R12表示氢原子，C1-C6烷基，芳基等; X1和X2表示C1-C15烷基或芳基，X1和X2总共具有0至4个羧基; m1，m2，m3表示0或1; L1至L7独立地表示次甲基; M表示氢原子，金属或季铵盐; n表示中和电荷所需的1〜7的整数。

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