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公开(公告)号：EP0916348B1
公开(公告)日：2004-08-18
申请号：EP97924325.0
申请日：1997-06-05
发明人： INOUE, Kazuhiro, Daiichi Pharmaceutical Co., Ltd. , SUSAKI, Hiroshi, Daiichi Pharmaceutical Co., Ltd. , IKEDA, Masahiro, Daiichi Pharmaceutical Co., Ltd. , KUGA, Hiroshi, Daiichi Pharmaceutical Co., Ltd. , KUMAZAWA, Eiji, Daiichi Pharmaceutical Co., Ltd. , TOGO, Akiko, Daiichi Pharmaceutical Co., Ltd.
IPC分类号： A61K47/48
CPC分类号： A61K47/61
摘要： Drug complexes wherein a carboxy (C1-4)alkyldextran polyalcohol, which has been treated under such conditions as to allow the substantially complete formation of the polyalcohol, is bonded to the residue of a medicinal compound such as an antitumor agent via a spacer consisting of one amino acid or a spacer consisting of two to eight amino acids bonded to each other via peptide bonds. The complexes are excellent in the tumor site selectivity and thus can exhibit a high antitumor effect with relieved expression of toxicity.
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公开(公告)号：EP0544000B1
公开(公告)日：1997-05-02
申请号：EP91914632.4
申请日：1991-08-16
发明人： INOUE, Kazuhiro, 5-6-6, Matsugaoka , ITO, Teruomi, 6-89-104, Shinmatsudo , OKUNO, Satoshi, 8-5-18, Waseda , AONO, Katsutoshi,
CPC分类号： C08B37/003
摘要： A novel N-acetylcarboxymethylchitosan derivative represented by general formula (I) and having the following properties (1) to (4): (1) degree of carboxymethylation: 0.5 - 1.2, (2) molecular weight (according to gel filtration): 3,000 - 300,000, (3) a/(a+b): 0.01 - 1 wherein a = a1 + a2, (4) P/X (by mole): 0.1 - 1. Formula (I), wherein R1 and R2 represent each hydrogen or carboxymethyl; P represents R3CO, R4NH or R5O; Q represents hydrogen or hydroxy; X represents a peptide chain containing 1 to 10 same or different amino acid residues; R3COOH, R4NH2 and R5OH represent carboxylic acid, amine and alcohol compounds, respectively; a1 and a2 represent each 0 or a positive integer except for the case where both of them are 0 at the same time; and b represents a positive integer. When the P group in the formula (I) represents a group derived from a pharmaceutical compound, the substance of the formula (I) is useful as a drug improved in the directivity toward a target organ.
摘要翻译： （1）〜（4）所示的新型N-乙酰羧甲基壳聚糖衍生物：（1）羧甲基化度：0.5〜1.2，（2）分子量（根据凝胶过滤）：3,000 式（I）中，R 1和R 2分别表示 - （ - ） - 300,000，（3）a /（a + b）：0.01-1其中a = a1 + a2，（4）P / 氢或羧甲基; P表示R3CO，R4NH或R5O; Q代表氢或羟基; X代表含有1至10个相同或不同氨基酸残基的肽链; R 3 COOH，R 4 NH 2和R 5 OH分别代表羧酸，胺和醇化合物; 除了两者同时为0的情况之外，a1和a2分别表示0或正整数; b表示正整数。 当式（I）中的P基团表示来源于药物化合物的基团时，式（I）的物质可用作改善靶器官指向性的药物。
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公开(公告)号：EP0725145A1
公开(公告)日：1996-08-07
申请号：EP95909993.8
申请日：1995-02-27
发明人： SATO, Haruya , YAMAMOTO, Keiji , SUZUKI, Kokichi , IKEDA, Masahiro , SAKAGAMI, Masahiro , TANIGUCHI, Makoto
摘要： A physiologically active protein (including a fused protein comprising the same and a peptide bonded thereto through an amide linkage) is improved in the adaptability to a medicine by modifying the protein through the action of a transglutaminase on the same and an amino group donor having a polyethylene glycol, polysaccharide, polyamino acid or branched saccharide derivative portion without detriment to the inherent physiological activity.
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公开(公告)号：EP0544000A4
公开(公告)日：1993-08-04
申请号：EP91914632
申请日：1991-08-16
发明人： INOUE, KAZUHIRO, 5-6-6, MATSUGAOKA , ITO, TERUOMI, 6-89-104, SHINMATSUDO , OKUNO, SATOSHI, 8-5-18, WASEDA , AONO, KATSUTOSHI,
CPC分类号： C08B37/003
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公开(公告)号：EP0544000A1
公开(公告)日：1993-06-02
申请号：EP91914632.4
申请日：1991-08-16
发明人： INOUE, Kazuhiro, 5-6-6, Matsugaoka , ITO, Teruomi, 6-89-104, Shinmatsudo , OKUNO, Satoshi, 8-5-18, Waseda , AONO, Katsutoshi,
CPC分类号： C08B37/003
摘要： A novel N-acetylcarboxymethylchitosan derivative represented by general formula (I) and having the following properties (1) to (4): (1) degree of carboxymethylation: 0.5 - 1.2, (2) molecular weight (according to gel filtration): 3,000 - 300,000, (3) a/(a+b) : 0.01 - 1 wherein a = a₁ + a₂ , (4) P/X (by mole): 0.1 - 1. Formula (I), wherein R₁ and R₂ represent each hydrogen or carboxymethyl; P represents R₃CO, R₄NH or R₅O; Q represents hydrogen or hydroxy; X represents a peptide chain containing 1 to 10 same or different amino acid residues; R₃COOH, R₄NH₂ and R₅OH represent carboxylic acid, amine and alcohol compounds, respectively; a₁ and a₂ represent each 0 or a positive integer except for the case where both of them are 0 at the same time; and b represents a positive integer. When the P group in the formula (I) represents a group derived from a pharmaceutical compound, the substance of the formula (I) is useful as a drug improved in the directivity toward a target organ.
摘要翻译： （1）〜（4）所示的新型N-乙酰羧甲基壳聚糖衍生物：（1）羧甲基化度：0.5〜1.2，（2）分子量（根据凝胶过滤）：3,000 式（I）中，R 1和R 2分别代表各自独立的碳原子数为1〜3的（a），（b）， 氢或羧甲基; P代表R 3 CO，R 4 NH或R 5 O; Q代表氢或羟基; X代表含有1至10个相同或不同氨基酸残基的肽链; R 3 COOH，R 4 NH 2和R 5 OH分别代表羧酸，胺和醇化合物; a 1和a 2分别代表0或正整数，除了它们两者同时为0的情况; b表示正整数。 当式（I）中的P基团表示来源于药物化合物的基团时，式（I）的物质可用作改善靶器官指向性的药物。
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公开(公告)号：EP0526649B1
公开(公告)日：1998-05-20
申请号：EP92905093.8
申请日：1992-02-21
发明人： INOUE, Kazuhiro 5-6-6, Matsugaoka , ITO, Teruomi 6-89-104, Shin-Matsudo , KAWAGUCHI, Takayuchi 1-15-2-406, Sugamo , AONO, Katsutoshi , OKUNO, Satoshi 8-5-18, Waseda , YANO, Toshiro 3-1-8-410, Akebono
CPC分类号： C08B37/0087 , A61K47/61
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公开(公告)号：EP0489162A4
公开(公告)日：1993-09-29
申请号：EP91904345
申请日：1991-02-25
CPC分类号： C07H15/14 , A61K9/1272 , C07H15/04
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公开(公告)号：EP0489162A1
公开(公告)日：1992-06-10
申请号：EP91904345.5
申请日：1991-02-25
CPC分类号： C07H15/14 , A61K9/1272 , C07H15/04
摘要： A derivative of a glycolipid containing a sialic acid of general formula (I), a process for the production thereof, and a particulate carrier containing the derivative as the constituent. In formula (I), the symbol represents either an α or β linkage; R¹ represents hydrogen or acetyl; R² represents hydrogen, C₁ to C₄ lower alkyl or alkali metal ion; X represents oxygen, sulfur, or a residue represented by the following formula (II) or (III): -O(CH₂) m NHCO- (II), wherein m is an integer of 1 to 10, -O(CH₂)mCONH- (III) and Y represents a group of formula (IV); wherein A represents a C₁₀ to C₄₀ linear or branched acylamino or the like, B represents hydrogen, carboxyl or a group of formula (V), and n and n' are each an integer of 0 to 3.
摘要翻译： 含有通式（I）的唾液酸的糖脂的衍生物，其制造方法以及含有该衍生物作为构成成分的颗粒状载体。 在式（I）中，符号代表α或β键; R 1代表氢或乙酰基; R 2代表氢，C 1 -C 4低级烷基或碱金属离子; X代表氧，硫或下式（Ⅱ）或（Ⅲ）代表的残基：-O（CH 2）mNHCO-（Ⅱ），其中m为1至10的整数，-O（CH 2）m CONH- （III）且Y代表式（IV）的基团; A代表C 10 -C 40直链或支链酰氨基等，B代表氢，羧基或式（V）基团，n和n'各自为0-3的整数。
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公开(公告)号：EP0614886A1
公开(公告)日：1994-09-14
申请号：EP93916247.5
申请日：1993-07-30
发明人： ISHIKURA, Toyoaki, A-202, Heights-Edogawadai , ITO, Teruomi, 104, Lion's Mansion Shin-Matsudo , KATOH, Takashi , HORIE, Kazutoshi, 207, Bell-Clair Edogawadai , ISHIHARA, Hiroshi , SENOU, Takashi
IPC分类号： C07C323/41 , C07C327/30 , C07D295/18 , C07D207/16 , A61K47/48 , C07D295/12
CPC分类号： C07D239/42 , A61K47/54 , A61K47/545 , A61K47/60 , C07C323/41 , C07C327/30 , C07C2601/14 , C07D207/16 , C07D295/13 , C07D405/12
摘要： A group of novel compounds which can pass through the blood-brain barrier (BBB) with a drug carried thereon and reside in the brain to release the drug and a group of known compounds having the above characteristics. More specifically, a compound represented by general formula (Ia) and a salt thereof, wherein R¹ represents hydroxy, carboxy, amino which may be substituted by C₁-C₆ alkyl, or C₁-C₆ alkyl which may be substituted by a 5-to 7-membered saturated heterocyclic group, R² represents hydrogen or C₁-C₆ alkyl, R³ represents hydrogen or C₁-C₆ alkyl which may be hydroxylated, R⁴ represents hydrogen or C₁-C₆ alkyl, R⁵ represents amino acid residue, or -S-R⁶ or -CO-R⁶ (wherein R⁶ represents C₁-C₁₄ alkyl which may be substituted by a 5- to 7-membered saturated heterocyclic group, C₁-C₁₄ alkyl, C₂-C₆ alkenyl, aryl or a 5- to 7-membered saturated ring group), or a group represented by general formula (IVa), wherein R¹, R², R³ and R⁴ are each as defined above, and symbol ......... represents either a single or a double bond, provided that at least one of R¹, R³ and R⁵ represents hydroxy, carboxy or amino.
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公开(公告)号：EP0526649A4
公开(公告)日：1993-09-08
申请号：EP92905093
申请日：1992-02-21
发明人： INOUE, KAZUHIRO 5-6-6, MATSUGAOKA , ITO, TERUOMI 6-89-104, SHIN-MATSUDO , KAWAGUCHI, TAKAYUCHI 1-15-2-406, SUGAMO , AONO, KATSUTOSHI , OKUNO, SATOSHI 8-5-18, WASEDA , YANO, TOSHIRO 3-1-8-410, AKEBONO
CPC分类号： C08B37/0087 , A61K47/61
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