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71. 发明专利

DE3782430D1 未知
公开(公告)号：DE3782430D1
公开(公告)日：1992-12-03
申请号：DE3782430
申请日：1987-07-30
申请人： MAEDA HIROSHI , FUJI OIL CO LTD
发明人： MAEDA HIROSHI , MATSUMURA YASUHIRO , TAKAMATSU KIYOHARU , SHIMODA TADAHISA
IPC分类号： A61K38/55 , A61K36/00 , A61K36/48 , A61K38/00 , A61K45/06 , A61K47/00 , A61K47/48 , A61P35/00 , A61P37/08 , A61P43/00 , A61K37/64
摘要： Cancerous thoractic fluid contains, as active ingredient soybean Kunitz trypsine inhibitor. The soybean Kunitz trypsine inhibitor can be isolated by any conventional process. For example, a soy bean raw material is extracted with a polar solvent (e.g. ethanol) and purified by membrane sepn., isoelectric point sedimentation, salting out, etc.. The crude prod. is further purified by gel filtration, ion exchange and other physical or chemical absorption. As the active ingredient, the isolated soybean Kunitz trypsine inhibitor (activity 1.502.5 units/mg) is administered in an amt. of 1-3000 mg/60kg (weight) for intra-abdominal injection or 1-300 kg/60 kg (weight) for intravenous injection.

72. 发明专利

CA1283359C COMPOSITIONS OF NEOCARZINOSTATIN DERIVATIVE FOR NON-INJECTION ADMINISTRATION 未知
公开(公告)号：CA1283359C
公开(公告)日：1991-04-23
申请号：CA543429
申请日：1987-07-30
申请人： YAMANOUCHI PHARMA CO LTD , MAEDA HIROSHI , KURARAY CO , KAYAKU ANTIBIOTIC RESEARCH CO
发明人： MAEDA HIROSHI , SUZUKI FUJIO , OKA KIICHIRO , TANAKA SHOHEI
IPC分类号： A61K38/00 , A61K9/10 , A61K9/107 , A61K31/785 , A61K47/00 , A61K47/10 , A61K47/14 , A61K47/48 , A61P35/00 , G03C1/06 , G03C1/485 , A61K37/02
摘要： COMPOSITIONS OF NEOCARZINOSTATIN DERIVATIVE FOR NON-INJECTION ADMINISTRATION A composition for non-injection administration comprises a neocarzinostatin derivative and medium to long chain fatty acid glycerides and may orally, intrarectally, intrathoracically or intraperitoneally be administered to cancer patients.

73. 发明专利

CA1241640A NEOCARZINOSTATIN DERIVATIVES AND A PROCESS FOR MANUFACTURING THE SAME 未知
公开(公告)号：CA1241640A
公开(公告)日：1988-09-06
申请号：CA459768
申请日：1984-07-26
申请人： KURARAY CO , YAMANOUCHI PHARMA CO LTD , KAYAKU ANTIBIOTIC RESEARCH CO , MAEDA HIROSHI
发明人： MAEDA HIROSHI , KANAMARU RYUNOSUKE , ISHIDA NAKAO , YOSHITAKE TOSHIHIKO , UEDA MINORU
IPC分类号： A61K38/00 , A61P35/00 , C07K1/107 , C07K1/113 , C07K14/00 , C07K14/195 , C07K14/41 , C07K17/08 , C08F8/00 , C08F222/08
摘要： Neocarzinostatin derivatives having excellent anticancer activity, which have the following formula (A) (SMA)-(NCS)-(SMA) (A) wherein (NCS) represents divalent neocarzinostatin residue in which one hydrogen atom is removed from each of the primary amino group in alanine residue at the N-terminal of neocarzinostatin and that in lysine residue at 20th position from the N-terminal of neocarzinostatin and (SMA) represents monovalent styrene-maleic acid copolymeric residue having a weightaverage molecular weight of 800?2,500 and consisting of structural units of styrene residue (a) ; maleic acid residue (b) ; and a residue (c) having the following formula in which a hydroxyl group of one carboxyl group in the maleic acid residue is removed and link to be bonded to neocarzinostatin residue wherein the linkage of carbon atom in carbonyl group bonds to the neocarzinostatin residue. Said neocarzinostatin derivative is manufactured by reacting neocarzinostatin in an aqueous medium with a large molar excess of powdery partially hydrolyzed styrene-maleic anhydride copolymer consisting of styrene residue; maleic acid residue; and maleic anhydride residue and having the particularly defined weight average molecular weight and number average molecular weight, and then subjecting the reaction product to gel filtration to isolate neocarzinostatin derivative.

75. 发明专利

DE2813017A1 未知
公开(公告)号：DE2813017A1
公开(公告)日：1978-10-05
申请号：DE2813017
申请日：1978-03-23
申请人： MAEDA HIROSHI , ISHIDA NAKAO
发明人： MAEDA HIROSHI , KANAMARU RYUNOSUKE , ISHIDA NAKAO , SENDAI MIYAGI
IPC分类号： C08F8/00 , A61K38/00 , A61P35/00 , C07K1/113 , C07K14/36 , C07K14/37 , C07K14/41 , C07K17/08 , C08F8/30 , C08F8/32 , C07G17/00 , A61K37/02
摘要： Neocarzinostatin derivatives having the formula; wherein N represents a neocarzinostatin residue, and R1+R2 represents a residue of polystyrene-maleic acid copolymer having a molecular weight of 2,500 to 80,000. These neocarzinostatin derivatives are prepared by reacting neocarzinostatin with a polystyrene-maleic acid copolymer containing at least one maleic anhydride residue per molecule. The neocarzinostatin derivatives exhibit anticarcinogenic activity.

76. 发明授权

US5389366A Neocarzinostatin derivative composition for oral administration 失效
标题翻译：用于口服给药的新辅佐星素衍生物组合物
公开(公告)号：US5389366A
公开(公告)日：1995-02-14
申请号：US061338
申请日：1993-05-17
申请人： Hiroshi Maeda , Fujio Suzuki , Kiichiro Oka , Shohei Tanaka
发明人： Hiroshi Maeda , Fujio Suzuki , Kiichiro Oka , Shohei Tanaka
IPC分类号： A61K47/48 , A61K31/74
CPC分类号： A61K47/48176
摘要： A composition for oral administration to cancer patients includes a neocarzinostatin derivative and from 0.1 and 100 ml per mg of the neocarzinostatin derivative of at least one fatty acid glyceride which has from 6 to 20 carbon atoms and which is noniodized. The composition is effective in the treatment of cancer by oral administration, including a solid cancerous tumor.
摘要翻译：用于癌症患者的口服给药组合物包括新碳青霉调节素衍生物，和0.1至100ml每毫克含有6至20个碳原子并被非碘化的至少一种脂肪酸甘油酯的新碳青霉素抑制素衍生物。该组合物通过口服给药治疗癌症是有效的，包括固体癌性肿瘤。

77. 发明授权

US4844897A Anti-tumor protease preparations 失效
标题翻译：抗肿瘤蛋白酶制剂
公开(公告)号：US4844897A
公开(公告)日：1989-07-04
申请号：US906240
申请日：1986-09-12
申请人： Hiroshi Maeda , Yasuhiro Matsumura , Osamu Asami , Hideyuki Tanaka , Ikuharu Sasaki
发明人： Hiroshi Maeda , Yasuhiro Matsumura , Osamu Asami , Hideyuki Tanaka , Ikuharu Sasaki
IPC分类号： A61K38/00 , C12N9/52 , C12N9/54 , C12N9/96
CPC分类号： C12N9/54 , C12N9/52 , C12N9/96 , A61K38/00
摘要： Method of treating a tumor in a mammal comprises administering to said mammal an effective anti-tumor amount of proteases originating from microorganisms.Method of treating a tumor in a mammal comprises administering to said mammal an effective anti-tumor amount of a protease originating from a microorganism which protease is chemically modified by one of the following procedures:(a) coupling with a saccharide,(b) introduction of a hydrophobic polymeric group,(c) alteration of electric charge of the protein surface,(d) conjugation with a low molecular weight anti-tumor agent of molecular weight less than 2,000,(e) formation of dimer or oligomer by cross-linking of protease molecules,(f) conjugation with a synthetic polycation,(g) conjugation with a synthetic polyanion, and(h) combination of the above-mentioned procedures.Microorganism protease is chemically modified by one of the following procedures:(a) coupling with a saccharide,(b) introduction of a hydrophobic polymeric group,(c) alteration of electric charge of the protein surface,(d) conjugation with a low molecular weight anti-tumor agent of molecular weight less than 2,000,(e) formation of dimer or oligomer by cross-linking of protease molecules,(f) conjugation with a synthetic polycation,(g) conjugation with a synthetic polyanion, and(h) combination of the above-mentioned procedures.
摘要翻译：治疗哺乳动物肿瘤的方法包括向所述哺乳动物施用有效的抗肿瘤量的源于微生物的蛋白酶。治疗哺乳动物肿瘤的方法包括向所述哺乳动物施用有效的抗肿瘤量的来自微生物的蛋白酶，所述蛋白酶通过以下方法之一进行化学修饰：（a）与糖的偶联，（b）引入的疏水性聚合物组，（c）蛋白质表面电荷的改变，（d）与分子量小于2,000的低分子量抗肿瘤剂缀合，（e）通过交联形成二聚体或低聚物的蛋白酶分子，（f）与合成聚阳离子的缀合，（g）与合成聚阴离子的缀合，和（h）上述步骤的组合。微生物蛋白酶通过以下方法之一进行化学修饰：（a）与糖的偶联，（b）引入疏水聚合基团，（c）改变蛋白质表面的电荷，（d）与低分子（e）通过蛋白酶分子的交联形成二聚体或寡聚体，（f）与合成聚阳离子的缀合，（g）与合成聚阴离子的缀合，和（h）分子量小于2000的重量抗肿瘤剂，组合上述程序。

78. 发明授权

US4782113A Neocarzinostatin derivatives and method of producing the same 失效
标题翻译：新卡诺他汀衍生物及其制备方法
公开(公告)号：US4782113A
公开(公告)日：1988-11-01
申请号：US911454
申请日：1986-09-25
申请人： Hiroshi Maeda , Ryunosuke Kanamaru , Nakao Ishida , Toshihiko Yoshitake , Minoru Ueda
发明人： Hiroshi Maeda , Ryunosuke Kanamaru , Nakao Ishida , Toshihiko Yoshitake , Minoru Ueda
IPC分类号： C08F8/00 , A61K31/00 , A61K31/785 , A61K38/00 , A61P35/00 , C07K1/113 , C07K14/00 , C07K14/195 , C07K14/41 , C07K17/08 , C08F8/32 , C08F212/08 , C08F222/02
CPC分类号： C07K14/00 , Y10S260/47
摘要： Substantially pure neocarzinostatin anticancer agents have the formula (A):(SMA)--(NCS)--(SMA) (A)wherein (NCS) is a divalent neocarzinostatin residue and (SMA) comprises the monovalent residue of a partially half-esterified styrene-maleic acid copolymer having a weight-average molecular weight of from 800 to 2,500, said (NCS) residue being bonded to said (SMA) residues via amide linkages formed between primary amino groups of the neocarzinostatin molecule and carbonyl groups of the partially half-esterified styrene-maleic acid copolymer.
摘要翻译：基本上纯的新碳青霉素抑制剂具有式（A）：（SMA） - （NCS） - （SMA）（A），其中（NCS）是二价新碳青霉素抑制素残基，（SMA）包含部分半酯化苯乙烯 - 马来酸共聚物，其重均分子量为800至2,500，所述（NCS）残基通过酰胺键与所述（SMA）残基相连，所述酰胺键是在新碳纳托杆菌素分子的伯氨基和部分半胱氨酸的羰基之间形成的，酯化苯乙烯 - 马来酸共聚物。

79. 发明专利

CA2977873C POLYMER-TYPE FLUORESCENT MOLECULE PROBE 未知
公开(公告)号：CA2977873C
公开(公告)日：2020-05-12
申请号：CA2977873
申请日：2012-09-05
申请人： MAEDA HIROSHI
发明人： MAEDA HIROSHI , HASHIZUME MAKOTO , FANG JUN , NAKAMURA HIDEAKI , QIN HAIBO , HACKBARTH STEFFEN , MURATA MASAHARU
IPC分类号： A61K49/00 , A61K47/56 , A61K47/69 , A61P35/00
摘要： The present invention provides a fluorescent molecule probe for efficient fluorescent detection (visualization) of tumors or for implementing fluorescent detection and photodynamic therapy; more specifically, the present invention provides a polymer-type fluorescent molecule probe for fluorescent detection of tumors, the probe including a composite comprising a fluorescent molecule and a biocompatible polymer.

80. 发明专利

CA2851344C POLYMER-TYPE FLUORESCENT MOLECULE PROBE 未知
公开(公告)号：CA2851344C
公开(公告)日：2017-10-03
申请号：CA2851344
申请日：2012-09-05
申请人： MAEDA HIROSHI
发明人： MAEDA HIROSHI , HASHIZUME MAKOTO , FANG JUN , NAKAMURA HIDEAKI , QIN HAIBO , HACKBARTH STEFFEN , MURATA MASAHARU
IPC分类号： A61K49/00 , A61B1/00 , A61K41/00 , G01N21/64
摘要： The present invention provides a fluorescent molecular probe for efficient fluorescent detection (visualization) of tumors or for implementing fluorescent detection and photodynamic treatment, more specifically, the present invention provides a macromolecular fluorescent molecular probe for fluorescent detection of tumor, comprising a complex comprising a fluorescent molecule and a biocompatible macromolecule.

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