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公开(公告)号：JPS6335578A
公开(公告)日：1988-02-16
申请号：JP18116586
申请日：1986-07-31
发明人： YAMANE TAKEHIKO , KONDO HIDEO , HASHIZUME TAKUSHI , YAMASHITA KATSUJI , HOSOE KAZUNORI , WATANABE KIYOSHI
IPC分类号： C07D498/18 , A61K31/535 , A61K31/54 , A61P31/04 , C07D265/00 , C07D273/00 , C07D279/00 , C07D307/00
摘要： NEW MATERIAL:The compound of formula I (n is 1-5; X is O or S; R and R are H, 1-4C alkyl or 1-4C hydroxyalkyl) and its salt. USE:A medicine. An antibacterial agent. It is a solid having dark red color, soluble in a number of organic solvents, exhibiting strong antibacterial activity against Gram-positive bacteria and acid-fast bacteria and having low toxicity. It can be used as a production raw material for novel rifamycin derivative of formula II having strong antibacterial activity. It is administered at a rate of 10mg-10g of the active component daily for adult. PREPARATION:The compound of formula I can be produced by reacting a rifamycin derivative of formula III with an amine of formula IV in an organic solvent such as methanol in the presence of a reducing agent such as sodium cyanoborohydride at room temperature for 30min - about 1 month, thereby effecting reductive amination reaction.
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公开(公告)号：JPS6239558A
公开(公告)日：1987-02-20
申请号：JP17835685
申请日：1985-08-13
发明人： SHIRAISHI TADAYOSHI , DOMOTO TAKASHI , SHIMADA YOSHIO , IMAI NAOHIRO , KONDO HIDEO , KATSUMI IKUO , HIDAKA TAKAYOSHI , WATANABE KIYOSHI
IPC分类号： C07F15/02 , A61K31/275 , A61P31/04 , A61P35/00 , A61P43/00 , B01J31/00 , B01J31/02 , C07B61/00 , C07C67/00 , C07C253/00 , C07C255/41 , C12N9/99
摘要： NEW MATERIAL:A compound expressed by formula I [R is substituted phenyl or ferrocenyl expressed by formula II (both R and R are OH or at least either one of R and R is phenoxy)]. USE:An antimicrobial agent, tyrosine kinase inhibitor, having possibility of being useful as a carcinostatic agent and carcinogenic inhibitor and useful as a synthetic intermediate for many organic compounds. PREPARATION:An aldehyde expressed by the formula R -CHO and alpha- cyanoacetamide are subjected to the Knoevenagel reaction using a basic catalyst, e.g. piperidine or ammonium acetate, to afford the aimed compound expressed by formula I. Alternatively, the aldehyde expressed by the formula R -CHO is condensed with the alpha-cyanoacetamide on the absence or presence of an acid or base catalyst, e.g. sulfuric acid or pyridine, to give the aimed compound expressed by formula I.
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公开(公告)号：JPH0276883A
公开(公告)日：1990-03-16
申请号：JP15549689
申请日：1989-06-16
发明人： KANO FUMIHIKO , YAMANE TAKEHIKO , KONDO HIDEO , HASHIZUME TAKUSHI , YAMASHITA KATSUJI , HOSOE KAZUNORI , KUZE FUMIYUKI , WATANABE KIYOSHI
IPC分类号： C07D498/18 , A61K31/535 , A61P31/04
摘要： NEW MATERIAL:A compound of formula I [A is formula II (R and R are 1-3C alkyl, 2-6C aminoalkyl, etc.), formula III (a is 2-7; R is H; amino, 1-4C monoalkylamino, etc.), etc.; X is 1-6C alkoxyl, 2-6C alkenyloxy, 1-6C alkylthio, 1-6C acyl, etc.; X is H, 1-6C alkyl or halogen] (including the compound of formula I wherein A is formula IV of the 5' position; X is -OCH3, -CN, etc., at the 4 position; X is H). EXAMPLE:3',5'-Dimethoxybenzoxazinorifamycin. USE:An antibiotic. PREPARATION:A rifamycin derivative of formula V (X is H, 1-6C alkoxy, halogen or nitro) is reacted with an amino of a formula AH.
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公开(公告)号：JPH0138085B2
公开(公告)日：1989-08-11
申请号：JP17994981
申请日：1981-11-09
发明人： KATSUMI IKUO , KONDO HIDEO , YAMASHITA KATSUJI , HIDAKA TAKAYOSHI , HOSOE KAZUNORI , ARIKI YUTAKA , YAMASHITA TOSHIAKI , WATANABE KYOSHI
IPC分类号： A61K31/045 , A61K31/05 , A61K31/10 , A61K31/12 , A61K31/13 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/27 , A61K31/275 , A61P25/04 , A61P29/00 , C07C49/248 , C07C59/52 , C07C69/732
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公开(公告)号：JPS63233987A
公开(公告)日：1988-09-29
申请号：JP6833187
申请日：1987-03-23
发明人： KANO FUMIHIKO , YAMANE TAKEHIKO , KONDO HIDEO , YAMASHITA KATSUJI , HOSOE KAZUNORI , WATANABE KIYOSHI
IPC分类号： C07D498/18 , A61K31/535 , A61P31/04 , C07D265/00 , C07D273/00 , C07D307/00
摘要： NEW MATERIAL:The compound of formula I, formula II and their salt. USE:An antibacterial agent. It is administered in a dose of 3mg-1g daily for adult. PREPARATION:The compound of formula I or II can be produced by reacting rifamycin O or S with 2-amino-4-tert-butylphenol. The reaction is carried out preferably in a polar solvent (e.g. methanol and ethanol) when rifamycin O is used as the starting raw material or in a nonpolar solvent (e.g. benzene and toluene) when rifamycin S is used as the starting raw material.
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公开(公告)号：JPS6324498B2
公开(公告)日：1988-05-20
申请号：JP17994881
申请日：1981-11-09
发明人： KATSUMI IKUO , KONDO HIDEO , YAMASHITA KATSUJI , HIDAKA TAKAYOSHI , HOSOE KAZUNORI , ARIKI YUTAKA , YAMASHITA TOSHIAKI , WATANABE KYOSHI
IPC分类号： C07C69/02 , A61K31/12 , A61K31/365 , A61K31/415 , A61P7/02 , A61P25/04 , A61P29/00 , C07C45/00 , C07C49/587 , C07C67/00 , C07D233/96 , C07D307/58
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公开(公告)号：JPS6330490A
公开(公告)日：1988-02-09
申请号：JP17322286
申请日：1986-07-23
发明人： YAMANE TAKEHIKO , YAMASHITA KATSUJI , HASHIZUME TAKUSHI , KONDO HIDEO , HOSOE KAZUNORI , WATANABE KIYOSHI
IPC分类号： C07D498/18 , A61K31/535 , A61P31/04 , C07D265/00 , C07D267/00 , C07D307/00
摘要： NEW MATERIAL:A compound shown by formula I {A is group shown by formula N(R )R [R is !-5C alkyl, 3-8C cycloalkyl, etc; R is 6-20C alkyl, -(CH2)a-R (R is -CH=CH2, etc.; a is 1-4), etc.], group shown by formula II (group shown by formula III is 2-7C three- - eight-membered cyclic amino; R is H or halogen; R is 1-3C alkoxy, etc.), group shown by formula IV (c is 2-6; d is 1-4; e is 1-7), etc.} and a salt thereof. USE:An antibacterial agent against Gram-positive and Gram-negative bacteria. PREPARATION:Benzoxazinorifamycin shown by formula V is reacted with an amine shown by formula AH in a reaction solvent such as pyridine, DMF, etc., at -5-50 deg.C.
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公开(公告)号：JPS62242687A
公开(公告)日：1987-10-23
申请号：JP8651686
申请日：1986-04-15
发明人： YAMANE TAKEHIKO , KONDO HIDEO , HASHIZUME TAKUSHI , YAMASHITA KATSUJI , HOSOE KAZUNORI , WATANABE KIYOSHI
IPC分类号： C07D498/18 , A61K31/535 , A61K31/54 , A61P31/04 , C07D265/00 , C07D273/00 , C07D307/00 , C07D513/18
摘要： NEW MATERIAL:A compound of formula I or formula II [X is O or S; R is OH, 1-3C alkoxy, group of formula III-V (R is H or 1-3C alkoxy; R is H, 1-3C alkyl or phenyl; R is 1-3C alkyl, phenyl, -CH2CF3, etc.; R is H, 1-3C alkyl or carboxyl), etc.] and its salt. USE:An antibacterial agent having low toxicity. PREPARATION:The objective compound can be produced by using a rifamycin derivative of formula VI or VII as a starting raw material, reacting the derivative with a compound of formula H2N-R in an organic solvent such as methanol at a temperature between -20 deg.C and the boiling point of the solvent in the presence of an acid such as acetic acid for 10min-1 week, removing the reagent and reaction solvent, etc., from the reaction product and purifying the obtained crude product by column chromatography, etc.
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公开(公告)号：JPS6128667B2
公开(公告)日：1986-07-01
申请号：JP17190479
申请日：1979-12-28
IPC分类号： C07D277/06 , C07D207/16 , C07D263/04
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公开(公告)号：JPH0414670B2
公开(公告)日：1992-03-13
申请号：JP17881984
申请日：1984-08-28
发明人： KATSUMI IKUO , KONDO HIDEO , YAMASHITA KATSUJI , HIDAKA TAKAYOSHI , HOSOE KAZUNORI , YAMASHITA TOSHIAKI , WATANABE KYOSHI
IPC分类号： C09K3/00 , A61K31/365 , A61P7/02 , C07D307/33 , C07D307/58
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