ISOFLAVONE COMPOUND AND THERAPEUTIC AGENT FOR OSTEOPOROSIS

    公开(公告)号:JPH04356479A

    公开(公告)日:1992-12-10

    申请号:JP15790191

    申请日:1991-06-01

    申请人: KURARAY CO

    摘要: PURPOSE:To provide the subject new compound useful as a therapeutic agent for osteoporosis. CONSTITUTION:The compound of formula I (R is 6-10C alkyl 1,5-disubstituted with lower alkyl), e.g. 7-(1,5-dimethylhexyl)-3-phenyl-4H-1-benzopyranone. The compound of formula I can be produced by using a compound of formula II (R1 is lower alkyl) as a starting raw material, protecting the hydroxyl group with a protection group R2, introducing 4-substituted 5-9C alkyl side chain by Grignard reaction to obtain a compound of formula III, eliminating the protection group and removing the hydroxyl group by dehydration, reducing the double bond of the formed compound by hydrogenation reaction, bonding the obtained phenol derivative to a phenyl acetyl halide by Friedel-Crafts reaction and subjecting the obtained deoxybenzoin compound of formula IV to cyclization reaction.

    5ALPHA-REDUCTASE INHIBITOR
    44.
    发明专利

    公开(公告)号:JPH02193920A

    公开(公告)日:1990-07-31

    申请号:JP1348289

    申请日:1989-01-23

    申请人: KAO CORP

    摘要: PURPOSE:To provide the subject inhibitor having an excellent 5alpha-reductase- inhibiting activity and high safety and effective for the therapy of prostatic hypertroply, etc., caused by the action of androgenic hormone by containing an inflavone compound as an active ingredient. CONSTITUTION:A 5alpha-reductase inhibitor contains an isoflavone compound of the formula (R , R and R are H, chain or alicyclic hydrocarbon or 1-6C alkoxyl; A, B, C and D are H, hydroxyl or methoxyl, but R and C are simultaneously not H) as an active ingredient. The 5alpha-reductase inhibitor may be administered not only as such but also in the form of tablets, powder, etc. When the inhibitor is used e.g. in the form of a solid preparation, the solid preparation may contain an inert diluent such as lactose or mannitol, a lubricant such as magnesium stearate, a disintegrator such as cellulose or calcium gluconate, etc.

    ANTIBACTERIAL AGENT
    46.
    发明专利

    公开(公告)号:JPS62145016A

    公开(公告)日:1987-06-29

    申请号:JP28458485

    申请日:1985-12-18

    摘要: PURPOSE:To provide an antibacterial agent containing a specific flavonoid compound as an active component and exhibiting suppressing effect against indigenous dermatic bacteria. CONSTITUTION:A flavonoid compound selected from 5,7-dihydroxy-4'- methoxyisoflavone, 3'4',5,7-tetrahydroxyflavanone and l-epigallocatechin is used as an active component of the objective antibacterial agent at an amount of 0.01-1wt% of the whole composition. The compound is used together with proper base, diluent, etc. It is effective against Staphylococcus epidermis which is an indigenous dermatic bacterium. The agent is useful for the prevention and remedy of dermatic diseases such as acne vulgaris (pimple). The base and additive are e.g. oil, water, surfactant, alcohol, chelating agent, antioxidant, thickener, pigment, antiseptic, etc., and the agent is used in the form of solution, emulsion, powder, dispersion, etc.

    NOVEL 3-PHENYL-4H-1-BENZOPYRAN-4-ONE DERIVATIVE

    公开(公告)号:JPS60132976A

    公开(公告)日:1985-07-16

    申请号:JP24278083

    申请日:1983-12-21

    摘要: NEW MATERIAL:The 3-phenyl-4H-1-benzopyran-4-one derivative of formula I (R is H or OH; R is lower alkyl). EXAMPLE:7-(1-Ethoxycarbonylethyl)oxy-3-phenyl-4H-1-benzopyran-4-one. USE:Useful as a remedy for osteoporosis. It acts directly to the bone and exhibits excellent bone resorption suppressing effect. It is used for example to the symptoms such as the fracture of the huckle- and backbone, centrum of vertebra, collum femoris, costa, collum humeri, etc. PREPARATION:The compound of formula I can be produced by reacting the hydroxyl compound of formula II with the 2-halogenoalkanecarboxylic acid of formula III (X is halogen; R is H or lower alkyl) or its ester, and if necessary, hydrolyzing the reaction product.

    Carcinostatic agent
    48.
    发明专利
    Carcinostatic agent 失效
    致癌剂

    公开(公告)号:JPS5946217A

    公开(公告)日:1984-03-15

    申请号:JP15710382

    申请日:1982-09-09

    摘要: PURPOSE: To provide a low-toxic carcinostatic agent having differentiation inducing activity to the tumor cell of animal, and exhibiting excellent carcinostatic activity, by using a flavonoid or an isoflavonoid as an active component.
    CONSTITUTION: The objective agent contains the compound of formula I or formula II [R
    1 WR
    4 are OH or OCH
    3 ; R
    5 and R
    6 are group of formula III (R
    7 W R
    9 are H, OH or OCH
    3 ), H, OH or OCH
    3 ], e.g. genistein (4',5,7-trihydroxyisoflavone) as an active component. The agent can be administered orally or parenterally. Dose: 0.01W100mg/kg, preferably ≤10mg/kg daily for adult for oral administration, and preferably ≤2mg/kg for parenteral administration.
    COPYRIGHT: (C)1984,JPO&Japio

    摘要翻译: 目的:通过使用类黄酮或异黄酮作为活性成分,提供具有对动物肿瘤细胞的分化诱导活性并具有优异的制癌活性的低毒制剂。 构成:目标剂含有式I或式II化合物[R1-R4是OH或OCH3; R5和R6是式III的基团(R7-R9是H,OH或OCH3),H,OH或OCH3],例如 染料木素(4',5,7-三羟基异黄酮)作为活性成分。 该试剂可以口服或肠胃外给药。 剂量:口服给药成人每天0.01-100mg / kg,优选<= 10mg / kg,优选肠胃外给药<= 2mg / kg。