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    N-acetylcarboxymethylchitosan derivatives and process for preparation thereof
    2.
    发明授权
    N-acetylcarboxymethylchitosan derivatives and process for preparation thereof 失效

    公开(公告)号：US5463022A

    公开(公告)日：1995-10-31

    申请号：US969307

    申请日：1993-02-16

    申请人： Kazuhiro Inoue ,  Teruomi Ito ,  Satoshi Okuno ,  Katsutoshi Aono

    发明人： Kazuhiro Inoue ,  Teruomi Ito ,  Satoshi Okuno ,  Katsutoshi Aono

    IPC分类号： A61K47/48 ,  C08B37/08 ,  A61K38/00 ,  C07G17/00 ,  C07K9/00 ,  C08B37/00

    CPC分类号： C08B37/003

    摘要： N-acetylcarboxymethylchitosan derivatives are provided by the present invention. They are represented by the following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 individually mean H or carboxymethyl group; P denotes a group R.sub.3 CO--, a group R.sub.4 NH-- or a group R.sub.5 O-- with assuming that R.sub.3 COOH denotes a compound having carboxyl group, R.sub.4 NH.sub.2 denotes a compound having amino group and R.sub.5 OH denotes an alcohol compound; Q stands for H or a group --OH; X represents a peptide chain containing same or different, one to ten amino acids; a.sub.1 and a.sub.2 individually represent zero or a positive integer, provided that both of a.sub.1 and a.sub.2 are not zero at the same time, and b stands for a positive integer; and having the following characteristic values (1)-(4):______________________________________ (1) carboxymethylation degree: 0.5-1.2 (2) molecular weight (as measured 3,000-300,000 by gel filtration method): (3) a/(a + b): 0.01-1 [provided that a = a.sub.1 + a.sub.2 ] (4) P/X ratio (molar ratio): 0.1-1 ______________________________________ P in the formula (I) can be the residue of a pharmaceutical compound. In this case, the substances of the formula (I) are derivatives of the pharmaceutical compound, which derivatives have been improved in the properties such as organotropism in vivo.P in the formula (I) can also be protective groups. In this case, removal of the protective groups from the substances of the formula (I) by deprotection makes it possible to provide such N-acetylcarboxymethylchitosan derivative which is useful as carrier for pharmaceutical compounds and which has the terminals of the so deprotected peptide chains capable of being linked with a pharmaceutical compound.There are further obtained such derivatives of the substances of the formula (I), in which derivatives some of the N-acetylcarboxymethylglucosamine units have been replaced by units having a high solubility in water.

    Carboxymethylmannoglucans and derivatives thereof
    3.
    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。

    Formamido and carboxyamido compounds which can be retained in brain
    5.
    发明授权
    Formamido and carboxyamido compounds which can be retained in brain 失效
    可以保留在脑中的甲酰氨基和羧酰氨基化合物

    公开(公告)号：US5580904A

    公开(公告)日：1996-12-03

    申请号：US211304

    申请日：1994-06-24

    申请人： Toyoaki Ishikura ,  Teruomi Ito ,  Takashi Kato ,  Kazutoshi Horie ,  Hiroshi Ishihara ,  Takashi Senou

    发明人： Toyoaki Ishikura ,  Teruomi Ito ,  Takashi Kato ,  Kazutoshi Horie ,  Hiroshi Ishihara ,  Takashi Senou

    IPC分类号： A61K47/20 ,  A61K47/22 ,  A61K47/48 ,  C07C323/41 ,  C07C327/30 ,  C07D207/16 ,  C07D239/42 ,  C07D295/12 ,  C07D295/13 ,  C07D405/12 ,  A61K31/16 ,  C07C233/01

    CPC分类号： C07D239/42 ,  A61K47/48023 ,  A61K47/48061 ,  A61K47/48215 ,  C07C323/41 ,  C07C327/30 ,  C07D207/16 ,  C07D295/13 ,  C07D405/12 ,  C07C2101/14

    摘要： According to the present invention, a novel compound group which can pass through blood-brain barrier (BBB) with carrying a drug thereon and stay within brain to release the drug and a well-known compound group having the properties described above are provided.The compound represented by the general formula ##STR1## wherein, R.sup.1 represents C.sub.1-6 alkyl which may be substituted by a group selected from hydroxyl, carboxyl, amino group which may be substituted by C.sub.1-6 alkyl, and a five- to seven-membered saturated heterocyclic ring,R.sup.2 represents hydrogen or C.sub.1-6 alkyl,R.sup.3 represents hydrogen or C.sub.1-6 alkyl which may be substituted by hydroxyl,R.sup.4 represents hydrogen or C.sub.1-6 alkyl,R.sup.5 represents an amino acid residue, or --S--R.sup.6 or --CO--R.sup.6 wherein R.sup.6 represents C.sub.1-14 alkyl which may be substituted by a five- to seven-membered saturated ring; C.sub.2-6 alkenyl; aryl; or a five- to seven-membered saturated ring; or the group represented by the general formula (IVa): ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the same meanings as defined above, and.multidot..multidot..multidot..multidot..multidot..multidot..multidot..multidot..multidot. represents a single bond or a double bondprovided that at least one of R.sup.1, R.sup.3 and R.sup.5 contains hydroxyl, carboxyl or amino, and a salt thereof.

    摘要翻译： PCT No.PCT / JP93 / 01075 Sec。 371日期：1994年6月24日 102（e）1994年6月24日PCT 1993年7月30日PCT公布。 公开号WO94 / 03424 日本1994年2月17日根据本发明，可以通过血脑屏障（BBB）携带药物并保持在脑内以释放药物的新型化合物组和具有所述性质的公知化合物组 提供以上。 由通式（Ia）表示的化合物，其中，R 1表示可被选自羟基，羧基，可被C 1-6烷基取代的氨基的基团取代的C 1-6烷基， 至7元饱和杂环，R 2表示氢或C 1-6烷基，R 3表示氢或可被羟基取代的C 1-6烷基，R 4表示氢或C 1-6烷基，R 5表示氨基酸残基，或 - S-R6或-CO-R6，其中R6表示可被5至7元饱和环取代的C 1-14烷基; C 2-6烯基; 芳基; 或五至七元饱和环; 或由通式（IVa）表示的基团：其中R 1，R 2，R 3和R 4具有与上述相同的含义，并且+ E，uns xxxxxxxxx + EE表示单键或双键 条件是R 1，R 3和R 5中的至少一个含有羟基，羧基或氨基，及其盐。