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    Camptothecin derivatives
    1.
    发明授权
    Camptothecin derivatives 失效
    喜树碱衍生物

    公开(公告)号：US06617456B1

    公开(公告)日：2003-09-09

    申请号：US09624012

    申请日：2000-07-21

    申请人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    发明人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    IPC分类号： C07D49800

    CPC分类号： C08B37/0018 ,  A61K47/61 ,  A61K47/65 ,  C08B37/0021

    摘要： A camptothecin derivative comprising a compound of the formula [I]: wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is —Xn-Alkm-R6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by —Xn-Alkm-R6, and the remaining three groups are H, alkyl or a halogen, and one or two —CH2— of the alkylene in (A) or (B) may optionally be replaced by —O—, —S— or —NH—, X is —O— or —NH—, Alk is alkylene, or —OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects and are useful as a medicament.

    摘要翻译： 包含式[I]化合物的喜树碱衍生物：其中R1，R2，R3，R4和R5是（A）相邻的两个基团结合形成亚烷基，或两者都是H，其余三个基团之一是-Xn -Alkm-R6，另外两个为H，烷基或卤素，或（B）相邻的两个基团结合形成亚烷基，所述亚烷基的一个碳原子被-Xn-Alkm-R6取代，并且 剩余的三个基团是H，烷基或卤素，并且（A）或（B）中的一个或两个亚烷基的-CH 2可以任选地被-O - ， - S-或-NH-替代，X是-O - 或-NH-，Alk为亚烷基或-OH，m和n均为0或1，或m为1，n为0，喜树碱化合物通过氨基酸或肽与具有羧基的多糖结合 ，或其药学上可接受的盐。 所述喜树碱衍生物显示出增强的抗肿瘤活性，但副作用很少，可用作药物。

    Camptothecin derivatives
    2.
    发明授权
    Camptothecin derivatives 失效
    喜树碱衍生物

    公开(公告)号：US06512118B1

    公开(公告)日：2003-01-28

    申请号：US09227158

    申请日：1999-01-08

    申请人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    发明人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    IPC分类号： C07D47100

    CPC分类号： C08B37/0018 ,  A61K47/61 ,  A61K47/65 ,  C08B37/0021

    摘要： A camptothecin derivative comprising a compound of the formula [I] is disclosed: wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is —Xn-Alkm-R6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by —Xn-Alkm-R6, and the remaining three groups are H, alkyl or a halogen, and one or two —CH2— of the alkylene in (A) or (B) may optionally be replaced by —O—, —S— or —NH—, X is —O— or —NH—, Alk is alkylene, R6 is —NH2, or —OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects and are useful as a medicament.

    摘要翻译： 公开了包含式[I]化合物的喜树碱衍生物：其中R1，R2，R3，R4和R5是（A）相邻的两个基团结合形成亚烷基，或两者都是H，其余三个基团之一是 -Xn-Alkm-R6，另外两个为H，烷基或卤素，或（B）相邻的两个基团结合形成亚烷基，所述亚烷基的一个碳原子被-Xn-Alkm-R6取代， 并且其余三个基团是H，烷基或卤素，并且（A）或（B）中亚烷基的一个或两个-CH 2可以任选地被-O - ， - S-或-NH-代替，X是 -O-或-NH-，Alk为亚烷基，R6为-NH2或-OH，m和n均为0或1，或m为1，n为0，喜树碱化合物与具有羧基的多糖结合 通过氨基酸或肽，或其药学上可接受的盐。 所述喜树碱衍生物显示出增强的抗肿瘤活性，但副作用很少，可用作药物。

    Camptothecin derivatives
    3.
    发明授权
    Camptothecin derivatives 失效
    喜树碱衍生物

    公开(公告)号：US5837673A

    公开(公告)日：1998-11-17

    申请号：US689018

    申请日：1996-07-30

    申请人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    发明人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    IPC分类号： A61K9/00 ,  A61K31/4745 ,  A61K38/00 ,  A61K47/48 ,  A61P35/00 ,  C07D491/22 ,  C07K5/065 ,  C07K5/103 ,  C07K9/00 ,  A61K31/00 ,  A61K38/14

    CPC分类号： C07D491/22 ,  A61K47/4823 ,  A61K47/48338 ,  C07K5/06078 ,  C07K5/1008 ,  C07K9/003 ,  A61K38/00

    摘要： A camptothecin derivative comprising a compound of the formula �I!: ##STR1## wherein R.sup.1 is a substituted or unsubstituted lower alkyl group, X.sup.1 is a group of the formula: --NHR.sup.2 (R.sup.2 is a hydrogen atom or a lower alkyl group) or a group of --OH, and Alk is a straight chain or branched chain alkylene group having optionally an oxygen atom in the chain thereof, bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects unlike conventional anticancer agents, and hence, these compounds are extremely useful as a medicament.

    摘要翻译： 包含式[I]化合物的喜树碱衍生物：其中R1是取代或未取代的低级烷基，X1是下式的基团：-NHR2（R2是氢原子或低级烷基 基团）或一组-OH，Alk是其链中任选具有氧原子的直链或支链亚烷基，经由氨基酸或肽与具有羧基的多糖结合，或其药学上可接受的盐 其中。 所述喜树碱衍生物显示增强的抗肿瘤活性，但与常规抗癌剂不同​​的副作用很少，因此这些化合物作为药物是非常有用的。

    Camptothecin derivatives
    4.
    发明授权
    Camptothecin derivatives 失效
    喜树碱衍生物

    公开(公告)号：US5892043A

    公开(公告)日：1999-04-06

    申请号：US773182

    申请日：1996-12-27

    申请人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    发明人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    IPC分类号： A61K47/48 ,  C08B37/00 ,  C08B37/02 ,  C07D471/00

    CPC分类号： C08B37/0018 ,  A61K47/4823 ,  A61K47/48338 ,  C08B37/0021

    摘要： A camptothecin derivative comprising a compound of the formula �I!: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is --X.sub.n --Alk.sub.m --R.sup.6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by --X.sub.n --Alk.sub.m --R.sup.6, and the remaining three groups are H, alkyl or a halogen, and one or two --CH.sub.2 -- of the alkylene in (A) or (B) may optionally be replaced by --O--, --S-- or --NH--, X is --O-- or --NH--, Alk is alkylene, R.sup.6 is --NH.sub.2, ##STR2## or --OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects and are useful as a medicament.

    摘要翻译： 包含式[I]化合物的喜树碱衍生物：其中R 1，R 2，R 3，R 4和R 5是（A）相邻的两个基团结合形成亚烷基，或两者都是H，并且其中之一 其余三个为-Xn-Alkm-R6，另外两个为H，烷基或卤素，或（B）相邻的两个基团结合形成亚烷基，所述亚烷基的一个碳原子被-Xn- Al-C-R6，其余三个基团是H，烷基或卤素，并且（A）或（B）中亚烷基的一个或两个-CH 2可以任选地被-O - ， - S-或-NH - ，X为-O-或-NH-，Alk为亚烷基，R6为-NH2，或IMA为-OH，m和n均为0或1，或m为1，n为0，喜树碱化合物为 通过氨基酸或肽或其药学上可接受的盐与具有羧基的多糖结合。 所述喜树碱衍生物显示出增强的抗肿瘤活性，但副作用很少，可用作药物。

    Carboxymethylmannoglucans and derivatives thereof
    7.
    发明授权
    Carboxymethylmannoglucans and derivatives thereof 失效
    羧甲基甘露糖葡聚糖及其衍生物

    公开(公告)号：US5863908A

    公开(公告)日：1999-01-26

    申请号：US689095

    申请日：1996-07-30

    申请人： Kazuhiro Inoue ,  Teruomi Ito ,  Takayuki Kawaguchi ,  Katsutoshi Aono ,  Satoshi Okuno ,  Toshiro Yano

    发明人： Kazuhiro Inoue ,  Teruomi Ito ,  Takayuki Kawaguchi ,  Katsutoshi Aono ,  Satoshi Okuno ,  Toshiro Yano

    IPC分类号： A61K47/36 ,  A61K47/48 ,  C08B15/00 ,  C08B37/00 ,  A61K31/725 ,  A61K31/715 ,  A61K31/72

    CPC分类号： C08B37/0087 ,  A61K47/4823

    摘要： A carboxymethylmannoglucan comprising tetrasaccharide units represented by the following general formula (I) and salt thereof. Further, the invention discloses a carboxymethylmannoglucan derivative and salt thereof produced by subjecting part or the whole of mannose of the tetrasaccharide units to ring opening and subjecting part or the whole of glucose which constitute the main chain but have no mannose as a branch ##STR1## wherein R.sup.1 to R.sup.12 each represent a hydrogen atom or a carboxymethyl group.The compounds are useful as carrier for delaying the disappearance of a drug in the blood and for enhancing the organotropism of the drug for a carcinoma.

    摘要翻译： 包含由以下通式（I）表示的四糖单元及其盐的羧甲基甘露糖葡聚糖。 此外，本发明公开了通过使四糖单元的一部分或全部甘露糖开环并使构成主链但不具有甘露糖的部分或全部葡萄糖作为分支而制备的羧甲基葡萄糖聚糖衍生物及其盐。 （I）其中R 1至R 12各自表示氢原子或羧甲基。 这些化合物可用作延迟药物在血液中消失并用于增强癌症药物的有机性的载体。

    Polysaccharide derivatives and drug carriers
    9.
    发明授权
    Polysaccharide derivatives and drug carriers 失效
    多糖衍生物和药物载体

    公开(公告)号：US5688931A

    公开(公告)日：1997-11-18

    申请号：US325296

    申请日：1994-12-28

    申请人： Hideo Nogusa ,  Hiroshi Hamana ,  Toshiro Yano ,  Masahiro Kajiki ,  Keiji Yamamoto ,  Satoshi Okuno ,  Shuichi Sugawara ,  Nobukazu Kashima ,  Kazuhiro Inoue

    发明人： Hideo Nogusa ,  Hiroshi Hamana ,  Toshiro Yano ,  Masahiro Kajiki ,  Keiji Yamamoto ,  Satoshi Okuno ,  Shuichi Sugawara ,  Nobukazu Kashima ,  Kazuhiro Inoue

    IPC分类号： A61K47/48 ,  C08B37/00 ,  C08B37/02 ,  C07H13/02 ,  C07K5/00 ,  C08B37/08

    CPC分类号： C08B37/0063 ,  A61K47/48338 ,  C08B37/00 ,  C08B37/0006

    摘要： A novel polysaccharide derivative, a drug carrier comprising a novel polysaccharide derivative, and a drug complex are disclosed. The polysaccharide derivative according to the present invention comprises a polysaccharide having a carboxyl group in which a peptide chain is introduced at a part or all of the carboxyl groups of the polysaccharide. The peptide chain comprises 1-8 amino acids which may be the same or different. A part or all of the amino groups in the peptide chain which are not involved in the linkages with the carboxyl groups of the polysaccharide or the carboxyl groups in the peptide chain may form an acid amide linkage or an ester linkage with a carboxyl group, an amino group or a hydroxyl group of a third compound such as drugs. The polysaccharide derivative has a property of accumulating in a high amount at a tumor, and thus can deliver efficiently a drug which has a side-effect or a limited sustainment of the drug efficacy to the tumor.

    摘要翻译： PCT No.PCT / JP94 / 00322 Sec。 371日期1994年12月28日第 102（e）日期1994年12月28日PCT 1994年2月28日PCT PCT。 第WO94 / 19376号公报 日期1994年9月1日公开了一种新型多糖衍生物，包含新型多糖衍生物的药物载体和药物复合物。 本发明的多糖衍生物含有在多糖的一部分或全部羧基上引入肽链的具有羧基的多糖。 肽链包含1-8个氨基酸，其可以相同或不同。 不参与与肽链中的多糖或羧基的羧基的连接的肽链中的一部分或全部氨基可以与羧基形成酸酰胺键或酯键， 氨基或第三化合物如药物的羟基。 多糖衍生物具有在肿瘤中高度积累的性质，因此能够有效地递送对肿瘤具有药效的副作用或有限维持性的药物。

    Video camera device
    10.
    发明授权
    Video camera device 有权
    摄像机设备

    公开(公告)号：US06707619B1

    公开(公告)日：2004-03-16

    申请号：US09442918

    申请日：1999-11-18

    申请人： Satoshi Okuno

    发明人： Satoshi Okuno

    IPC分类号： G02B1514

    CPC分类号： G08B13/19632 ,  G03B37/00 ,  G08B13/19619 ,  G08B13/1963 ,  H04N7/18

    摘要： The invention is aimed to miniaturize an angle adjustment mechanism of a mirror barrel and simplify the structure thereof. A ball joint mechanism in which a spherical portion provided to the base end of a mirror barrel is joined to a spherical portion support table provided to a main chassis by a joint ring is constructed, and the rotation of the mirror barrel in three axial directions around the center of the spherical portion can be performed.

    摘要翻译： 本发明的目的在于使镜筒的角度调节机构小型化并简化其结构。 一种球接头机构，其中设置在镜筒的基端的球形部分通过接合环接合到设置在主底架上的球形支撑台，并且镜筒在三个轴向方向上的旋转 可以执行球形部分的中心。