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1. 发明专利

JPS60114199A NOVEL MONACOLINS 失效
公开(公告)号：JPS60114199A
公开(公告)日：1985-06-20
申请号：JP22119883
申请日：1983-11-24
申请人： NIPPON KAYAKU KK , NIPPON SHINYAKU CO LTD , ENDO AKIRA
发明人： NAKAMURA TSUNEROU , KUNISHIMA AOI , MASUDA MINORU , ENDOU AKIRA
IPC分类号： C12P7/42 , C12P7/62 , C12P17/06 , C12R1/645
摘要： PURPOSE:To prepare a novel monacolin having lowering action on cholestrol in the blood, by cultivating a microorganism belonging to the genus Monascus. CONSTITUTION:A strain FERM P-4822 of Monascus raber is varied to give a variant FERM P-7203, which is cultivated at 20-30 deg.C at 6-8pH under aerobic conditions, and a monacolin shown by the formula I (R is group shown by the formula II or formula III; M is H, monovalent metal, ammonium, quaternay amine, or 1-4C alkyl) is collected from the culture solution.

2. 发明专利

JPS57146587A NEW PHYSIOLOGICALLY ACTIVE SUBSTANCE MUTASTEIN AND PREPARATION THEREOF 失效
公开(公告)号：JPS57146587A
公开(公告)日：1982-09-10
申请号：JP3198581
申请日：1981-03-06
申请人： ENDO AKIRA
发明人： ENDOU AKIRA
IPC分类号： A61K36/06 , A61P1/02 , C07G99/00 , C12P1/02 , C12R1/66
摘要： PURPOSE:To prepare a new physiologically active substance mutastein having inhibitory action on the dextran synthesis, preventing and remedial action on carious teeth, etc., by cultivating a microorganism belonging to the genus Aspergillus. CONSTITUTION:A microorganism, e.g. Aspergillus terreus M3328 (FERM-P No. 5891), belonging to the genus Aspergillus, and having the ability to produce mutastein is inoculated into a nutrient culture medium and cultivated at 20-30 deg.C under aerobic conditions to collect the new physiologically active substance mutastein having a molecular weight >=200,000, an ultraviolet absorption spectrum shown in Fig. 1, an infrared absorption spectrum shown in Fig. 2 and properties of proteins from the resultant culture fluid.

3. 发明专利

JPS57146586A PREPARATION OF NEW PHYSIOLOGICALLY ACTIVE SUBSTANCE TOMASTACHIN 失效
公开(公告)号：JPS57146586A
公开(公告)日：1982-09-10
申请号：JP3198481
申请日：1981-03-06
申请人： ENDO AKIRA
发明人： ENDOU AKIRA
IPC分类号： C12P21/00 , A61K36/06 , A61P3/08 , C07G99/00 , C12P1/02 , C12R1/645
摘要： PURPOSE:To prepare a new physiologically active substance tomastachin having the hypoglycemic action, by cultivating a microorganism belonging to the genus Caldosporium. CONSTITUTION:A microorganism, e.g. Cladosporium cladosporioides M3573 (FERM-P No.5892), belonging to the genus Cladosporium, and having the ability to produce tomastachin is inoculated into a nutrient culture medium and cultivated at 20-30 deg.C under aerobic conditions to collect the new physiologically active substance tomastachin having a molecular weight of about 25,000 measured by the gel filtration method, an ultraviolet absorption spectrum shown in Fig. 1, an infrared absorption spectrum shown in Fig. 2 and the properties of proteins from the resultant culture fluid.

4. 发明专利

JPS55139396A MONACOLIN J* NEW TYPE OF PHYSIOLOGICALLY ACTICE SUBSTANCE* AND ITS PREPARATION 失效
公开(公告)号：JPS55139396A
公开(公告)日：1980-10-31
申请号：JP4424979
申请日：1979-04-13
申请人： ENDO AKIRA
发明人： ENDOU AKIRA
IPC分类号： C07D309/30 , A61K31/351 , A61K31/355 , A61K31/365 , A61K36/06 , A61P3/06 , C07G99/00 , C12P1/02 , C12P17/06 , C12R1/645
摘要： NEW MATERIAL:Monacolin J, a physiologically active substance of the formula with following physical and chemical properties: elementary analysis, C: 71.54%, H: 8.65%, 0: 19.90%; molecular weight (measured by mass analysis), 320; molecular formula, C19H28O4; sobubility, soluble in methanol, acetone, chloroform, benzen, insoluble in hexane, petroleum ether; a neutral white powder; it can be detected as a spot by thin layer chromatography. USE:Antihyperlipemia and antiarteriosclerotic. PREPARATION:A bacteria capable of producing monacolin J, e.g., Monascus ruber No.1005 (FERM-P No.4822) is aerobically cultured at 20-35 deg.C.

5. 发明专利

JPS57174589A SAFE REFUGE APPARATUS FROM HIGH PLACE 失效
公开(公告)号：JPS57174589A
公开(公告)日：1982-10-27
申请号：JP6048981
申请日：1981-04-20
申请人： ENDO AKIRA
发明人： ENDOU AKIRA
IPC分类号： E06C1/56 , A62B5/00 , E06C9/14

6. 发明专利

JPS57146570A KOJI 失效
公开(公告)号：JPS57146570A
公开(公告)日：1982-09-10
申请号：JP3351281
申请日：1981-03-09
申请人： ENDO AKIRA
发明人： ENDOU AKIRA
IPC分类号： C12N1/14 , A61K36/06 , A61P3/06 , A61P3/08
摘要： PURPOSE:To obtain a koji having an action of lowering cholesterol and bloodsugar, by cultivating a mold belonging to the genus Monascus. CONSTITUTION:A mold such as Monascus paxii, M. pilosus, M. pubigerus, M. vitreus, M. ruber (FERM-P 4822) belonging to the genus Monascus is cultivated in a medium using rice, wheat, beans, maize, other grain, as a nutritive source aerobically, to give a koji. Using this koji, SAKE, MIRIN ( a sweet SAKE used as a seasoning), AMAZAKE (a sweet dring made from fermented rice), miso, soy sauce, and other food are prepared. When the koji is medicated to a rabbit or rat, the reduction in the bloodsugar value and the concentration of cholesterol in the serum is observed.

7. 发明专利

JPS56150013A PREVENTIVE AND REMEDY FOR CANCER 失效
公开(公告)号：JPS56150013A
公开(公告)日：1981-11-20
申请号：JP5262480
申请日：1980-04-21
申请人： ENDO AKIRA
发明人： ENDOU AKIRA
IPC分类号： A61K31/05 , A61K31/12 , A61K31/19 , A61K31/22 , A61P35/00
摘要： PURPOSE:A preventive and remedy for cancer having also improved cholesterol lowering actions, comprising monacolin K or ML-236B or their derivatives as an active ingredient. CONSTITUTION:A preventive and remedy for cancer comprising monacolin K shown by the formula I or ML-236B shown by the formula II or their derivatives (e.g., monachloline K carboxylic acid shown by the formula III, ML-236B carboxylic acid shown by the formula IV, etc.), formed with a proper excipient into a drug form, e.g., powder, capsule, tablet, injection, etc. It can be administered orally or into the cavum abdominis or to the vein, and its dose is 0.5-1000mg/kg/day.

8. 发明专利

JPS58172310A PREVENTIVE AND REMEDY FOR DENTAL CARIES 失效
公开(公告)号：JPS58172310A
公开(公告)日：1983-10-11
申请号：JP5508382
申请日：1982-04-02
申请人： ENDO AKIRA
发明人： ENDOU AKIRA
IPC分类号： A61K8/00 , A61K8/21 , A61K8/40 , A61K8/41 , A61K8/43 , A61K8/66 , A61Q11/00
摘要： PURPOSE:A preventive and remedy for dental caries having synergistically enhanced anticaries action, by using both a substance for inhibiting the formation of dental calculi and a substance for dissolving dental calculi. CONSTITUTION:A preventive and remedy for caries (dental caries) containing (A) a substance for inhibiting the formation of dental calculi such as (i) a substance for inhibiting the synthesis of insoluble glucan caused by bacteria in the oral cavity, (ii) a substance for inhibiting the growth of bacteria in the oral cavity, or (iii) a substance selected from a fluorine compound, bis-biguanide compound, quaternary ammonium salt, fatty amine and an anionic surface active agent and (B) a substance for dissolving dental calculi such as enzyme for hydrolyzing the alpha-1,3-bond and/or alpha-1,6-bond of insoluble glucan synthesized by bacteria in the oral cavity in a weight ratio of preferably A:B=(1:50)-(50:1). The preventive and remedy can be administered orally or to the abdominal cavity or intravenously, oral administration is preferable, and especially oral administration of 1-100mg/day is preferable.

9. 发明专利

JPS56115717A PREVENTIVE AND REMEDY FOR PROSTATOMEGALY 失效
公开(公告)号：JPS56115717A
公开(公告)日：1981-09-11
申请号：JP1938680
申请日：1980-02-19
申请人： ENDO AKIRA
发明人： ENDOU AKIRA
IPC分类号： A61K31/365 , A61K31/22 , A61P13/02 , A61P15/00 , C07C69/30 , C07D309/30
摘要： PURPOSE:To provide a preventive and remedy for prostatomegaly, having extremely low toxicity and excellent cholesterol-lowering activity, by using monacholin K or ML-236B or their derivatives as effective component. CONSTITUTION:Monacholin K of formula I, ML-236B of formula II or their derivatives [e.g. the carboxylic acid of formula III, a component of formula IV (M is metal element; n is valency of said element)] are used as effective components of a preventive and remedy for prostatomegaly. The above effective component can be administered singly or as a preparation in the form of powder, capsule, tablet, injection, etc. in combination with proper diluent, by oral administration, peritoneal infusion, intravenous injection, etc. Dose: 0.5-1,000mg/kg daily.

10. 发明专利

JPS60188066A NOVEL COLLAGENASE DISCOLYSIN AND ITS PREPARATION 失效
公开(公告)号：JPS60188066A
公开(公告)日：1985-09-25
申请号：JP4529284
申请日：1984-03-09
申请人： ENDO AKIRA
发明人： ENDOU AKIRA
IPC分类号： A61K38/00 , C12N9/52 , C12R1/465
摘要： PURPOSE:To produce a novel collagenase, discolysin, capable of solubilizing insoluble collagen, by culturing a microbial strain belonging to Streptomyces genus. CONSTITUTION:A microbial strain belonging to Streptomyces genus and capable of producing discolysin, e.g. Streptomyces C-51 strain (FERM-P No.7469), is cultured in a nutrient medium under aerobic condition at 25-35 deg.C, and the objective discolysin is separated from the cultured product.

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