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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
发明人: YAMAHARA JOJI , TORIHARA MASAHIRO , TAMAI HIRONOBU
IPC分类号: A61K31/35 , A61K31/352 , A61P19/10 , A61P43/00 , C07D311/36
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.
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公开(公告)号:JPH0421670B2
公开(公告)日:1992-04-13
申请号:JP26612585
申请日:1985-11-28
申请人: TSUMURA KK , KOSUGE TAKUO
发明人: KOSUGE TAKUO , ISHIDA KINJI , KITADA ZENZO
IPC分类号: C07H17/07 , C07D311/36 , C07D311/56
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公开(公告)号:JPH0411545B2
公开(公告)日:1992-02-28
申请号:JP20558182
申请日:1982-11-25
IPC分类号: C07C69/92 , A61K31/352 , A61P35/00 , C07C45/00 , C07C45/64 , C07C45/68 , C07C49/825 , C07C49/84 , C07C65/21 , C07C67/00 , C07C67/307 , C07C67/31 , C07D311/22 , C07D311/30 , C07D311/36 , C07D405/04 , C07D407/04 , C07D409/04 , C07D409/06
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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
发明人: JOKURA YOJI , ISHIKAWA SHINJI , NISHIZAWA YOSHINORI , YOSHIMURA KOICHI , KITAHARA TAKASHI , HATTORI MICHIHIRO
IPC分类号: C07D311/36 , A61K8/00 , A61K8/49 , A61K31/35 , A61K31/352 , A61P35/00 , A61P43/00 , A61Q5/00 , A61Q7/00 , A61Q15/00
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.
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公开(公告)号:JPS62201882A
公开(公告)日:1987-09-05
申请号:JP27151886
申请日:1986-11-14
发明人: ITO TOKUKI , OGAWARA HIROSHI , WATANABE SHUNICHI
IPC分类号: C07D311/24 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/425 , A61K31/435 , A61K31/535 , A61P35/00 , A61P37/06 , A61P43/00 , C07D311/36
摘要: NEW MATERIAL:A compound expressed by formula I [R is a group expressed by formula II (A is lower alkylene; R and R are H, alkyl, cycloalkyl, heterocyclic group, etc.), -CONHR (R is H, alkyl, etc.), etc.; R is OH, alkoxy or acyloxy] and salt thereof. EXAMPLE:Ethyl-4'-ethoxalyloxy-5,7-dihydroxy-2-isoflavoncarboxylate. USE:A carcinostatic agent and immunosuppressive agent. PREPARATION:A compound expressed by formula III (X is halogen or organic sulfonic acid residue) is reacted with an amine expressed by formula IV in the presence of a base, e.g. pyridine or potassium carbonate, in an organic solvent to afford the aimed compound expressed by formula I (R is a group expressed by formula II), etc.
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公开(公告)号:JPS62145016A
公开(公告)日:1987-06-29
申请号:JP28458485
申请日:1985-12-18
申请人: MITSUBISHI CHEM IND
发明人: NISHINO CHIKAO , KOBAYASHI KOJI
IPC分类号: C07D311/32 , A61K31/35 , A61K31/352 , A61P3/06 , C07D311/36 , C07D311/60
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.
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公开(公告)号:JPS60132976A
公开(公告)日:1985-07-16
申请号:JP24278083
申请日:1983-12-21
发明人: YAMAZAKI IWAO , SAWA YOUICHI
IPC分类号: A61K31/35 , A61K31/352 , A61P3/00 , C07D311/36
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.
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公开(公告)号:JPS5946217A
公开(公告)日:1984-03-15
申请号:JP15710382
申请日:1982-09-09
申请人: Rikagaku Kenkyusho
发明人: ISONO KIYOSHI , ASAHI KENICHI
IPC分类号: C07D311/30 , A61K31/35 , A61K31/352 , A61P35/00 , C07D311/32 , C07D311/36
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。
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公开(公告)号:JPS593998B2
公开(公告)日:1984-01-27
申请号:JP11599477
申请日:1977-09-27
发明人: RASURO FUOIAA , MIHARII NOGURADEI , AGUNESU GOTSUTOSHIIGEN , BORUBARA BERUMESU , YAANOSU SUTORERISUKII , ANDORASU BORUFUNAA , ROORANTO FUARUKASU , SANDORU ANTASU , MARIA KOBAKUSU
IPC分类号: A23K1/16 , A23K1/18 , A61K31/35 , A61K31/352 , A61P1/00 , A61P3/00 , C07D311/36
CPC分类号: C07D311/36 , A23K20/121 , A23K20/137 , A23K50/30
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50.
公开(公告)号:JPS5896082A
公开(公告)日:1983-06-07
申请号:JP20558282
申请日:1982-11-25
申请人: LIPHA
IPC分类号: A61K31/35 , A61K31/352 , A61K31/38 , A61K31/535 , A61P35/00 , C07D311/22 , C07D311/30 , C07D311/32 , C07D311/36 , C07D407/04 , C07D409/04 , C07D409/06
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