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1. 发明专利

JP2003246792A ANTI-INFLUENZA-VIRAL COMPOUND 审中-公开
公开(公告)号：JP2003246792A
公开(公告)日：2003-09-02
申请号：JP2002046170
申请日：2002-02-22
申请人： MEIJI MILK PROD CO LTD , KITASATO INST
发明人： YAMADA HARUKI , NAGAI TAKAYUKI , FURUHATA KIMIO , AJISAKA KATSUMI
IPC分类号： A23L1/30 , A61K31/7048 , A61P31/16 , C07H15/26 , C07H17/07
摘要： PROBLEM TO BE SOLVED: To provide a compound which is formed by bonding a sialic acid derivative or a KDN derivative to a flavone derivative, decreases the amount of the influenza virus, improves the viability of cells infected by the influenza virus, and is useful as a medicine for preventing or curing influenza and also as a food for preventing or curing influenza. SOLUTION: This compound is represented by formula (1) (wherein R 1 and R 7 are each independently H, Na or K; R 2 , R 3 , R 4 , R 5 , R 8 , R 9 , R 10 , and R 11 are each independently H, a sulfuric acid group or an acetyl group; R 6 and R 12 are each independently H or an acetyl, methyl, ethyl, n-propyl, n-butyl, n-octyl, benzyl or allyl group; X and Y are each independently an acetoamino, glycolylamino, hydroxyl or acetyloxy group; and A and B are each independently O or S). COPYRIGHT: (C)2003,JPO

2. 发明专利

JPH0418019A SIALIDASE INHIBITOR 失效
公开(公告)号：JPH0418019A
公开(公告)日：1992-01-22
申请号：JP11974290
申请日：1990-05-11
申请人： TSUMURA & CO , KITASATO INST
发明人： YAMADA AKISHIRO , NAGAI TAKAYUKI , TOMIMORI TAKESHI
IPC分类号： C12N9/24 , A61K31/00 , A61K31/35 , A61K31/352 , A61K31/353 , A61P31/00 , A61P31/12 , A61P31/16 , A61P43/00 , C07D311/30 , C12N9/99
摘要： PURPOSE:To obtain an antiviral agent useful for treating viral diseases such as influenza, having inhibitory activity against sialidase, comprising a flavone contained in a certain crude drug. CONSTITUTION:A sialidase inhibitor comprising a compound shown by the formula (R is H, OH or methoxyl) as an active ingredient. The compound shown by the formula is obtained by extracting Scutellariae Radix, Scutellariae Hderba or an original plnat thereof with an organic solvent such as a lower alcohol or chloroform or water, distilling away the solvent and subjecting the residue to silica gel column chromatography. A dose of the compound is 50mg to 1g per adult dividely several times daily in the case of oral agent. In the case of a parenteral agent, a dose is 0.1mg to 1g and properly administered by intravenous injection, intravenous drip, hypodermic injection or intramuscular injection.

3. 发明专利

JPH1160599A NEW GLYCOPROTEIN AND ANTIVIRAL AGENT COMPOSED OF THE GLYCOPROTEIN 失效
公开(公告)号：JPH1160599A
公开(公告)日：1999-03-02
申请号：JP22917897
申请日：1997-08-26
申请人： KITASATO INST
发明人： YAMADA HARUKI , NAGAI TAKAYUKI , SAKURAI MASUMI
IPC分类号： A61K38/00 , A61K36/18 , A61P31/12 , A61P31/16 , C07K14/415 , A61K35/78
摘要： PROBLEM TO BE SOLVED: To provide a new glycoprotein consisting of a glycoprotein having respectively specific contents of carbohydrate and chlorine ion and a specific molecular weight, having antiviral activity, free from side action and useful for the prophylaxis, treatment, etc., of the infection with virus such as influenza virus. SOLUTION: This new glycoprotein contains about 17.5 wt.% of carbohydrates, about 21.5 wt.% of proteins and about 28.6 wt.% of chlorine ion and has a molecular weight of about 7×10 wherein the mol.% of the constituent sugars are about 71.8 for glucose, about 11.0 for galacturonic acid, about 8.1 for glucuronic acid, about 3.9 for galactose, about 2.6 for mannose, about 1.4 for arabinose and about 1.3 for rhamnose. It is useful e.g. as an agent having antiviral action, free from side effect and effective for the treatment and prophylaxis of infection with virus such as influenza virus. The glycoprotein can be produced by adding refined water to Banrankon (root of Isatis tinctoria, etc.), decocting for about 3 hr, filtering the product, concentrating the filtrate, adding ethanol to the concentrated filtrate, filtering the formed precipitate, drying the precipitate, dissolving the dried material in an aqueous solution of Nail and purifying by gel-filtration.

4. 发明专利

JPH02101095A NOVEL COMPOUND AND SACCHARIDE CHAIN METABOLISM-INHIBITING AGENT CONTAINING SAME COMPOUND AS ACTIVE INGREDIENT 失效
公开(公告)号：JPH02101095A
公开(公告)日：1990-04-12
申请号：JP25093088
申请日：1988-10-06
申请人： TSUMURA & CO , KITASATO INST
发明人： YAMADA HARUKI , NAGAI TAKAYUKI , KIYOHARA HIROAKI , OTSUKA TAKAO
IPC分类号： C12N9/99 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7042 , A61K31/7048 , A61K36/18 , A61P31/12 , A61P37/04 , A61P43/00 , C07H15/203 , C07H17/07
摘要： NEW MATERIAL:(+ or -)-Plantagocide. USE:A mannosidase-inhibiting agent or glucosidase-inhibiting agent useful as a drug for immunological disorders, etc. PREPARATION:Plantaginis Semen, a seed of Plantago asiatica L., is extracted with mixed solvents of water, acetone, etc., and the extracted solution is subjected to the removal of the solvents and subsequently to the application of a silica gel column chromatography using methanol, etc., as an elution solvent to fractionate the objective substance.

5. 发明专利

JPS6442427A SIALIDASE INHIBITOR 失效
公开(公告)号：JPS6442427A
公开(公告)日：1989-02-14
申请号：JP19819487
申请日：1987-08-10
申请人： TSUMURA & CO , KITASATO INST
发明人： YAMADA AKISHIRO , CHIYOU SOUTETSU , OTSUKA TAKAO , NAGAI TAKAYUKI , SAKAKIBARA IWAO , MIHASHI HIROSHI
IPC分类号： A61K31/35 , A61K31/352 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P29/00 , A61P43/00 , C07D311/60 , C07H17/07
摘要： PURPOSE:To obtain a sialidase inhibitor, containing formononetin, luteolin or luteolin-7-O-glucoside as active ingredients, applicable to medicines, such as anti-inflammatory agent and having high safety with low toxicity. CONSTITUTION:A sialidase inhibitor obtained by extracting Dalbergia odorifera T. CHEN which is heart wood of dried root of a leguminous plant or Chrysanthemum indicum L. which is a dried flower part of a composite plant as a raw material with a solvent, such as methanol, by heating at 0 deg.C- the boiling point temperature of the solvent or using ultrasonic waves to provide an extract solution, directly or concentrating or drying the extract solution and subjected the resultant substance to column chromatography with an adsorbent, such as silica gel, to afford a fraction, recrystallizing the obtained fraction from a solvent, such as water or methanol, to afford the aimed compound which is an active ingredient. The resultant substance can be prepared in the form of a pharmaceutical by a conventional method and the dose thereof as an oral agent is 100-450mg in several divided portion a day for an adult.

6. 发明专利

JPH11236402A NEW POLYSACCHARIDE, AND ANTIVIRUS AGENT AND ADJUVANT AGENT OF THE POLYSACCHARIDE 失效
公开(公告)号：JPH11236402A
公开(公告)日：1999-08-31
申请号：JP4167998
申请日：1998-02-24
申请人： KITASATO INST
发明人： YAMADA HARUKI , NAGAI TAKAYUKI , SAKURAI MASUMI
IPC分类号： A61K31/715 , A61K36/18 , A61P31/12 , A61P43/00 , C08B37/00 , A61K35/78
摘要： PROBLEM TO BE SOLVED: To obtain a polysaccharide having antivirus activities useful for treatment and prevention of virus infection, and adjuvant activities for a vaccine, and further to obtain an antivirus agent and an adjuvant agent of the polysaccharide. SOLUTION: This polysaccharide comprises >=90 mol.% glucose as a constituent saccharide, comprising 1,4-bonded glucose, terminal glucose, 1,6-bonded glucose and 1,4,6-branched glucose as the coupling scheme, and has about 8×10 or about 6×10 molecular weight.

7. 发明专利

JPH09227373A ANTI-INFLUENZA VIRUS AGENT 失效
公开(公告)号：JPH09227373A
公开(公告)日：1997-09-02
申请号：JP3368296
申请日：1996-02-21
申请人： TEIJIN LTD , KITASATO INST
发明人： NISHIBE YOSHIHISA , MAKINO YUJI , YAMADA HARUKI , NAGAI TAKAYUKI
IPC分类号： C07D311/30 , A61K9/08 , A61K9/14 , A61K9/72 , A61K31/35 , A61K31/352 , A61K31/715 , A61P31/12 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To obtain an anti-influenza virus agent strengthened in an activity against influenza viruses and capable of being applied to a wide virus subtype spectrum. SOLUTION: This anti-influenza virus agent contains a flavonoid compound and a cellulose ether compound as active ingredients. The flavonoid compound includes 5,7,4'-trihydroxy-8-methoxyflavone, and the cellulose ether compound includes hydroxypropyl cellulose. The flavonoid compound and the cellulose ether compound are administered in a ratio of 1:(0.01-100) in the case of a liquid medicine, and also in a ratio of 1:(0.1-1000) in the case of a powder medicine. When administered into an airway consisting of a nasal cavity, the anti-influenza virus agent is administered in the form of a nasal drop, an aerosol, etc. When administered into an airway consisting of a lung (including a trachea and bronchi), the anti-influenza virus agent is administered in the form of an insufflation. The flavonoid compound in the anti-influenza virus agent is administered at a daily dose of 0.1-500mg/kg once to three times a day as a therapeutic agent, and also administered at a daily dose of 0.01-100mg/kg once to three times as a preventing agent.

8. 发明专利

JPH07173069A AGENT HAVING ADJUVANT ACTION 失效
公开(公告)号：JPH07173069A
公开(公告)日：1995-07-11
申请号：JP34330193
申请日：1993-12-17
申请人： TSUMURA & CO , KITASATO INST
发明人： YAMADA HARUKI , NAGAI TAKAYUKI
IPC分类号： A61K39/145 , A61K36/00 , A61K39/39 , A61P31/12 , A61P31/16 , A61P43/00 , A61K35/78
摘要： PURPOSE:To obtain a pharmaceutical agent containing SHOSEIRYUTO or its extract as an active component and having adjuvant action, etc., an influenza virus vaccine. CONSTITUTION:This agent contains SHOSEIRYUTO [a Chinese herb drug containing HANGE (rhizome of Pinellia ternata), KANZOU (root of Glycyrrhiza glabra), KEIHI (bark of Cinnamomum cassia), GOMISHI (fruit of Schizandra chinensis), SAISHIN (rhizome of Asiasarum sieboldi), SHAKUYAKU (root of Paeonia albiflora), MAOU (stalk of Ephedra sinica), KANKYOU (rhizome of Zingiber officinale), etc.] or its extract as an active component. It is prepared in the form of tablet, powder, granule, solution, injection, drip, etc. The daily dose of the agent for adult is 1-10g of the dried extract of SHOSEIRYUTO in 1-3 divided doses in the case of oral administration. The adjuvant action agent containing SHOSEIRYUTO as an active component has an effect to promote the action of vaccine against influenza, etc., and low side effect to enable safe administration.

9. 发明专利

JPH04208264A NEW ALKALOID AND GLUCOSIDASE INHIBITOR COMPRISING THE SAME ALKALOID AS ACTIVE INGREDIENT 失效
公开(公告)号：JPH04208264A
公开(公告)日：1992-07-29
申请号：JP33052290
申请日：1990-11-30
申请人： TSUMURA & CO , KITASATO INST
发明人： YAMADA HARUKI , NAGAI TAKAYUKI , ABAYOMI SOFUOORA , OTANI IZUMI
IPC分类号： A61K31/40 , A61K31/403 , A61K36/81 , A61P31/12 , A61P35/00 , A61P37/00 , A61P43/00 , C07D209/52
摘要： NEW MATERIAL:An alkaloid shown by the formula (R1 to R3 are H or OH). EXAMPLE:2,4,5,6,7-Pentahydroxytetrahydrocyclopenta[6]pyrrolidine. USE:A glucosidase inhibitor. Usable as an antiviral agent, an immunomodulator, a cancer metastasis inhibitor, etc. PREPARATION:JIKOTSUPI, root skin of Lycium chinense MILL of the family Solanaceae, is extracted with water and/or an alcohol, a supernatant liquid obtained after removal of the extracted solution is precipitated by adding ethanol, the supernatant liquid is subjected to column chromatography or high- performance liquid chromatography for collection once or more times, eluted with water, ammonia, acetonitrile, methanol, acetone, etc., as an eluting solvent and fractioned while confirming the objective component by thin layer chromatography.

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