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1. 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。

2. 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。}

3. 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。

4. 发明授权

US07008614B2 Liposome containing hydrophobic iodine compound and X-ray contrast medium for radiograph comprising the liposome 失效
标题翻译：含有疏水碘化合物的脂质体和包含脂质体的放射线的X射线造影剂
公开(公告)号：US07008614B2
公开(公告)日：2006-03-07
申请号：US10223461
申请日：2002-08-20
申请人： Hiroshi Kitaguchi , Kazuhiro Aikawa
发明人： Hiroshi Kitaguchi , Kazuhiro Aikawa
IPC分类号： A61K49/00 , A61K9/127
CPC分类号： A61K49/0466
摘要： A liposome containing a hydrophobic iodine compound represented by the following general formula (I) as a membrane component: R1—CO2—R2 wherein R1 represents a substituted or unsubstituted 2,3,5-triiodophenyl group or a substituted or unsubstituted 3,4,5-triiodophenyl group; and R2 represents a hydrocarbon group having 10 or more carbon atoms, and an X-ray contrast medium, which comprises said liposome which is used for radiography of a vascular disease.
摘要翻译：含有由以下通式（I）表示的疏水性碘化合物作为膜组分的脂质体：<？in-line-formula description =“In-line formula”end =“lead”？> R＆lt; 1＆其中R 1 =“尾”→>其中R 1，R 2，R 2，R 2，代表取代或未取代的2,3,5-三碘苯基或取代或未取代的3,4,5-三碘苯基; R 2表示具有10个或更多个碳原子的烃基，X射线造影剂包含用于血管疾病的放射摄影的所述脂质体。

5. 发明授权

US07264790B2 1,3-glyceride compound having two iodophenyl groups 失效
标题翻译：具有两个碘苯基的1,3-甘油酯化合物
公开(公告)号：US07264790B2
公开(公告)日：2007-09-04
申请号：US10487319
申请日：2002-08-22
申请人： Kazunobu Takahashi , Hiroshi Kitaguchi , Kazuhiro Aikawa
发明人： Kazunobu Takahashi , Hiroshi Kitaguchi , Kazuhiro Aikawa
IPC分类号： A61K49/00 , C07C53/00 , C07C57/00 , C07C59/00 , C08G63/48 , A61K49/04
CPC分类号： C07C233/83 , A61K49/0433 , A61K49/0466 , C07C69/66 , C07C69/712 , C07C69/736 , C07C233/18 , C07C237/20 , C07C323/52
摘要： A compound represented by the following general formula (I) or a salt thereof: wherein Ar1 and Ar2 independently represent a substituted or unsubstituted aryl group having at least one iodine atom as a substituent; L1 and L2 independently represent a divalent bridging group of which main chain consists of 7 or more atoms at least one of which is a heteroatom; and X represents —CH(OH)— or —CO—, which is suitable for an iodine-containing contrast medium containing liposomes.
摘要翻译：由以下通式（I）表示的化合物或其盐：其中Ar 1和Ar 2独立地表示具有至少一个碘原子的取代或未取代的芳基作为取代基; L 1和L 2独立地表示二价桥连基团，其主链由7个或更多个原子组成，其中至少一个是杂原子; X表示-CH（OH） - 或-CO-，适用于含有脂质体的含碘造影剂。

6. 发明授权

US07101532B2 Liposome containing hydrophobic iodine compound 有权
标题翻译：含有疏水性碘化合物的脂质体
公开(公告)号：US07101532B2
公开(公告)日：2006-09-05
申请号：US10258801
申请日：2001-04-26
申请人： Kazuhiro Aikawa , Hiroshi Kitaguchi
发明人： Kazuhiro Aikawa , Hiroshi Kitaguchi
IPC分类号： A61K49/04
CPC分类号： A61K9/127 , A61K49/0438 , A61K49/0466
摘要： A liposome containing a hydrophobic iodine compound such as a 1,3,5-triiodobenzene derivative having at least one substituent containing 18 or more carbon atoms as a membrane component, and an X-ray contrast medium containing the liposome for use in radiography of a vascular disease and the like.
摘要翻译：含有疏水性碘化合物的脂质体，例如具有至少一个含有18个或更多个碳原子的取代基的1,3,5-三碘苯衍生物作为膜组分，以及含有用于放射线照相术的脂质体的X射线造影剂血管疾病等。

7. 发明授权

US07371877B2 Glycerol ester derivative 失效
标题翻译：甘油酯衍生物
公开(公告)号：US07371877B2
公开(公告)日：2008-05-13
申请号：US10507486
申请日：2003-03-27
申请人： Kazunobu Takahashi , Hiroshi Kitaguchi , Kazuhiro Aikawa
发明人： Kazunobu Takahashi , Hiroshi Kitaguchi , Kazuhiro Aikawa
IPC分类号： C07F9/02 , A61K51/04
CPC分类号： C07D295/15 , A61K49/0466 , A61K51/1234 , C07C69/712 , C07C233/05 , C07C275/14 , C07F9/10 , C07F9/117
摘要： A compound represented by the following general formula (IA) or a salt thereof: wherein Ar1 represents hydrogen atom or an aryl group having at least one iodine atom as a substituent; Ar2 represents an aryl group having at least one iodine atom as a substituent; L1 and L2 independently represent a divalent bridging group of which main chain contains 6 or more carbon atoms; L3 represents a single bond or a divalent bridging group of which main chain contains 1 to 6 carbon atoms and one oxygen atom; X represents a functional group containing at least one heteroatom, provided that, when L3 is a single bond, X represents a functional group other than hydroxyl group. The compound can be used as a membrane component of liposomes, and the liposomes can be used as a contrast medium for X-ray radiography.
摘要翻译：由以下通式（IA）表示的化合物或其盐：其中Ar 1表示氢原子或具有至少一个碘原子作为取代基的芳基; Ar 2表示具有至少一个碘原子作为取代基的芳基; L 1和L 2独立地表示主链含有6个或更多个碳原子的二价桥连基团; L 3表示主链含有1〜6个碳原子和1个氧原子的单键或二价桥连基团; X表示含有至少一个杂原子的官能团，条件是当L 3为单键时，X表示除羟基以外的官能团。该化合物可以用作脂质体的膜组分，并且脂质体可以用作X射线照相术的造影剂。

8. 发明申请

US20060062726A1 Glycerol ester derivative 失效
标题翻译：甘油酯衍生物
公开(公告)号：US20060062726A1
公开(公告)日：2006-03-23
申请号：US10507486
申请日：2003-03-27
申请人： Kazunobu Takahashi , Hiroshi Kitaguchi , Kazuhiro Aikawa
发明人： Kazunobu Takahashi , Hiroshi Kitaguchi , Kazuhiro Aikawa
IPC分类号： A61K51/00 , C07F5/00 , C07F9/12
CPC分类号： C07D295/15 , A61K49/0466 , A61K51/1234 , C07C69/712 , C07C233/05 , C07C275/14 , C07F9/10 , C07F9/117
摘要： A compound represented by the following general formula (IA) or a salt thereof: wherein Ar1 represents hydrogen atom or an aryl group having at least one iodine atom as a substituent; Ar2 represents an aryl group having at least one iodine atom as a substituent; L1 and L2 independently represent a divalent bridging group of which main chain contains 6 or more carbon atoms; L3 represents a single bond or a divalent bridging group of which main chain contains 1 to 6 carbon atoms and one oxygen atom; X represents a functional group containing at least one heteroatom, provided that, when L3 is a single bond, X represents a functional group other than hydroxyl group. The compound can be used as a membrane component of liposomes, and the liposomes can be used as a contrast medium for X-ray radiography.
摘要翻译：由以下通式（IA）表示的化合物或其盐：

9. 发明申请

US20050002864A1 1,3-glyceride compound having two iodophenyl groups 失效
标题翻译：具有两个碘苯基的1,3-甘油酯化合物
公开(公告)号：US20050002864A1
公开(公告)日：2005-01-06
申请号：US10487319
申请日：2002-08-22
申请人： Kazunobu Takahashi , Hiroshi Kitaguchi , Kazuhiro Aikawa
发明人： Kazunobu Takahashi , Hiroshi Kitaguchi , Kazuhiro Aikawa
IPC分类号： A61K49/04 , C07C69/66 , C07C69/712 , C07C69/736 , C07C233/18 , C07C233/83 , C07C237/20 , C07C323/52 , C07C69/76
CPC分类号： C07C233/83 , A61K49/0433 , A61K49/0466 , C07C69/66 , C07C69/712 , C07C69/736 , C07C233/18 , C07C237/20 , C07C323/52
摘要： A compound represented by the following general formula (I) or a salt thereof: wherein Ar1 and Ar2 independently represent a substituted or unsubstituted aryl group having at least one iodine atom as a substituent; L1 and L2 independently represent a divalent bridging group of which main chain consists of 7 or more atoms at least one of which is a heteroatom; and X represents —CH(OH)— or —CO—, which is suitable for an iodine-containing contrast medium containing liposomes.
摘要翻译：由以下通式（I）表示的化合物或其盐：其中Ar 1和Ar 2独立地表示具有至少一个碘原子作为取代基的取代或未取代的芳基; L 1和L 2独立地表示二价桥连基团，其主链由7个或更多个原子组成，其中至少一个是杂原子; X表示-CH（OH） - 或-CO-，适用于含有脂质体的含碘造影剂。

10. 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）。

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