ESTROGEN RECEPTOR BETA-ISOFORM ACTIVATOR

    公开(公告)号:JPH11292872A

    公开(公告)日:1999-10-26

    申请号:JP9029698

    申请日:1998-04-02

    摘要: PROBLEM TO BE SOLVED: To obtain a new compound having selective estrogenic activity on estrogen receptor β-isoform, and useful as a therapeutic agent for diseases associated with blood estrogen level drop such as osteoporosis. SOLUTION: This new compound is shown by formula I (R1 is H or the like; R2 and R3 are each H or the like; (n) is 0-2), e.g. 4-hydroxy-3-(4- hydroxyphenyl)benzo[b]thiophene. The compound of formula I is obtained by the following procedure: a compound of formula II (R18 is a phenolic hydroxyl group-protecting group) (e.g. 3-methoxybenzenethiol) is reacted with a 2-bromo-4'- alkoxyacetophenone (e.g. 2-bromo-4'-methoxyacetophenone) under heating reflux in pyridine to form a compound which, in turn, is cyclized in polyphosphoric acid pref. at room temperature to 120 deg.C to form an isomer mixture which is subsequently separated/purified by chromatography using e.g. silica gel, and as necessary, iodine is introduced onto the 2-position of the resulting purified substance followed by further introducing substituent(s) onto the substance.

    PRODUCTION OF ISOFLAVONE COMPOUND
    92.
    发明专利

    公开(公告)号:JPH11263786A

    公开(公告)日:1999-09-28

    申请号:JP6686798

    申请日:1998-03-17

    摘要: PROBLEM TO BE SOLVED: To provide a method for producing an isoflavone compound, capable of purifying and producing the isoflavone compound from soybean embryo buds as a raw material in a large amount at a low cost. SOLUTION: This method for producing an isoflavone compound comprises subjecting soybean embryo buds obtained to an extraction treatment in a process for producing soybean protein, fermented soybeans, etc., as a raw material with a water-soluble organic solvent or a water-containing organic solvent, concentrating the extract solution, subjecting the concentrated product to a liquid-liquid distribution using a hydrophobic organic solvent, removing lipophilic components into the hydrophobic organic solvent layer, again concentrating the left aqueous solution layer, distilling off the organic solvent, passing the residue through a synthetic adsorption resin to allow the resin to adsorb the isoflavone compound, washing the isoflavone-adsorbed resin with water or water containing a small amount of an organic solvent to remove impurities, eluting the isoflavone compound from the resin with an organic solvent or its mixture with water, concentrating the elusion solution and subsequently drying the concentrate. The method for producing the isoflavone compound may comprise further concentrating the concentrate to distill off the organic solvent in stead of the above-described liquid-liquid distribution using the organic solvent, removing the generated emulsified solid products by a centrifugal separation method, passing the residue through the synthetic adsorption resin, and further treating the adsorbed isoflavone compound by the same method.

    DRINK CONTAINING ISOFLAVONE COMPOUND AND ITS PRODUCTION

    公开(公告)号:JPH11243928A

    公开(公告)日:1999-09-14

    申请号:JP5550898

    申请日:1998-03-06

    申请人: NICHIMO KK

    摘要: PROBLEM TO BE SOLVED: To obtain a drink containing an isoflavone compound, having an increased internal absorption rate, having excellent anticancer and immunosuppression activities, and useful as a food, a medicine or the like by formulating a specific isoflavone compound, a suspending agent and the like. SOLUTION: This drink containing an isoflavone compound is obtained by formulating the isoflavone compound such as isoflavone aglycone, obtained from the isoflavone compound obtained by hydrolyzing a plant of the bean family or the material containing the precursor thereof, a suspending agent such as a xanthan gum and a gelatin, and optionally an arbitrary component.

    HELICOBACTER PYLORI INHIBITOR
    95.
    发明专利

    公开(公告)号:JPH1112172A

    公开(公告)日:1999-01-19

    申请号:JP16094797

    申请日:1997-06-18

    申请人: YAKULT HONSHA KK

    摘要: PROBLEM TO BE SOLVED: To obtain the subject inhibitor having excellent antibacterial activity against Helicobacter pylori, also high in safety by using, as active ingredient, a specific compound afforded by soybean or processed products thereof. SOLUTION: This Helicobacter pylori inhibitor contains, as active ingredient, an isoflavone or saponin. The isoflavone may be either of glycoside type or hydrolyzed aglycone portion, for example, daidzin, daidzein, genistin; while the saponin may be either of glycoside type or sapogenin as an aglycone. For the isoflavone or saponin, a combination of one or more kinds thereof can be used. Because these active ingredients are rich in soybean or processed products thereof, these foods can be used directly. The daily effective amount of this inhibitor is 0.01-100 mg per adult in terms of the isoflavone or saponin.

    PRODUCTION OF WATER-SOLUBLE SOYBEAN ISOFLAVONE

    公开(公告)号:JPH10298175A

    公开(公告)日:1998-11-10

    申请号:JP11385897

    申请日:1997-05-01

    申请人: SUNSTAR INC

    发明人: MIZUTANI KENICHI

    IPC分类号: C07D311/36

    摘要: PROBLEM TO BE SOLVED: To produce a water-soluble soybean isoflavone high in water-solubility, capable of manifesting a good stability with the passage of time when dissolving the one by mixing a crude extract of a soybean with cyclodextrin in an aqueous solution, and removing an insoluble material therefrom. SOLUTION: (A) A crude extract obtained from a soybean raw material (preferably soybean hypocotyl, etc., having high content of the isoflavone) is mixed with (B) cyclodextrin in an aqueous solution, and an insoluble material is removed from the obtained mixture to provide the objective water-soluble soybean isoflavone in the method for producing the water-soluble soybean isoflavone. Preferably, the pH of the aqueous solution when mixing the components A with B is regulated so as to be 2-8, and the temperature is regulated so as to be 5-40 deg.C. The aqueous solution preferably includes no organic solvent. A method such as a centrifugation and a filtration can be used for the removal of the impurity. The objective soybean isoflavone useful for prevention, etc., of osteoporosis is cheaply and readily produced.

    THERAPEUTIC AGENT FOR SKIN MULTIPLICATION DISEASE

    公开(公告)号:JPH10226642A

    公开(公告)日:1998-08-25

    申请号:JP4855297

    申请日:1997-02-18

    申请人: KIKKOMAN CORP

    摘要: PROBLEM TO BE SOLVED: To obtain a secure excellent agent for preventing and treating skin mutiplication disease and a cosmetic material by formulating a genistein active ingredient with a therapeutic agent for skin disease and a cosmetic material. SOLUTION: Genistein used is obtainable by synthesis, extraction from soy lees and soy oil, fermentation using microorganisms and also extraction from beans such as soybean and the like. As therapeutic agents for psoriasis, ichthyosis, keratosis and dandruff disease caused by excess multiplication of skin, 0.01-5 w/w% may be applied when administrated to a lesion part as an ointment, and about 20-1000mg may be at once administrated several times a day for adult when used as a peroral drug. When used as a cosmetic material, if there is no obstacle in use, even the low concentration product extracted from soybeans and soy lees in place of pure genistein is usable.

    COMPOSITION FOR PROMOTING LIPOLYSIS IN ADIPOCYTE

    公开(公告)号:JPH1087486A

    公开(公告)日:1998-04-07

    申请号:JP26377396

    申请日:1996-09-13

    发明人: SEKIYA KEIZO

    摘要: PROBLEM TO BE SOLVED: To obtain the subject composition containing isoflavones in an amount effective for promoting the lipolysis in adipocyte, having safety and usable in cosmetics, pharmaceuticals, etc., having slimming effect. SOLUTION: This composition contains an active amount of isoflavones. The isoflavones are components of leguminous plants such as soybean and preferably one or more compounds selected from daidzein, daidzin, genistein and genistin. The active amount of the isoflavone is e.g. 0.05-1,000,000μg/mL(g) as a pharmaceutical agent for injection or infusion and 5-1,000mg/mL(g) as a food, pharmaceutical agent, etc., having the form of solid, liquid, powder, etc., and administered by oral or transcutaneous administration. The agent is safely utilizable in the field of pharmaceuticals, cosmetics, functional foods, etc., exhibiting slimming effect.