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1. 发明专利

JPH0753372A ANTI-MRSA COMPOSITION 失效
公开(公告)号：JPH0753372A
公开(公告)日：1995-02-28
申请号：JP20232393
申请日：1993-08-16
申请人： MEIJI SEIKA KAISHA , BIO MATERIAL KK
发明人： YONEDA TOSHIO , FUJII NAOYUKI , OOISHI MAKI , IINUMA KATSUHARU , SATO ATSUYUKI , YASUDA KIMIAKI
IPC分类号： A01N43/50 , A61K31/415 , A61L31/16 , A61P31/04 , C07D233/60 , C07D233/64 , D06M13/352 , D06M16/00 , D06N3/00 , D21H21/36
摘要： PURPOSE:To obtain an anti-MRSA composition containing a specific imidazole compound, having anti-MRSA (methicillin resistant Staphylococcus aureus) activity, effective for preventing the MRSA infection and useful for applying to textile products such as bed sheet, operating gown, sanitary gown and mask. CONSTITUTION:This anti-MRSA composition is produced by dissolving 2'- chloroacetophenone expressed by the formula I in dioxane, dropping Br2 to the solution under ice cooling to form o-chlorophenacyl bromide, reacting the bromide with imidazole, adding fuming nitric acid to the reaction mixture, separating the precipitated crystal by filtration, reducing the crystal to obtain a compound of the formula II, reacting with p-chlorobenzyl chloride, etc., to obtain an imidazole compound expressed by the formula III (R to R are each H or a halogen), mixing the compound with a liquid or solid carrier and optionally an auxiliary agent such as dispersing agent and emulsifying agent and forming the obtained mixture in the form of pharmaceutical preparation such as wettable powder, emulsifiable concentrate, powder or granule.

2. 发明专利

JPH07233068A THERAPEUTIC AGENT FOR HYPERCHOLESTEROLEMIA, HYPERLIPEMIA OR ARTERIOSCLEROSIS 失效
公开(公告)号：JPH07233068A
公开(公告)日：1995-09-05
申请号：JP32416894
申请日：1994-12-27
申请人： MEIJI SEIKA KAISHA
发明人： IINUMA KATSUHARU , INOUE KEIZO , ARAI HIROYOSHI , YONEDA TOSHIO , KAJII KENZO , UOTANI KAZUMICHI , OUCHI SHOKICHI , SHIOTANI MASAHARU , KONNO FUKIO , MAKABE OSAMU
IPC分类号： C07D273/00 , A61K31/395 , A61K31/535 , A61P9/00 , A61P9/10
摘要： PURPOSE:To obtain a therapeutic agent for hypercholesterolemia, hyperlipemia or arteriosclerosis, comprising PF1022 substance and its analog or its salt as an active ingredient. CONSTITUTION:This therapeutic agent contains a compound of the formula (R1 and R2 each is H, OH, an 1-8C alkoxy, an aryloxy, nitro, morpholino, trityloxy or 2-tetrahydropyranyloxy) or its salt as an active ingredient. The compound of the formula suppresses formation of cholesterol by macrophage and also inhibits formation of triglyceride. The compound can be pharmaceutically manufactured for oral, parenteral or local administration and a dose is 0.1-1,000mg per adult daily.

3. 发明专利

JPH06184126A CYCLIC DEPSIPEPTIDE AND ITS PRODUCTION 失效
公开(公告)号：JPH06184126A
公开(公告)日：1994-07-05
申请号：JP27909492
申请日：1992-10-19
申请人： MEIJI SEIKA KAISHA
发明人： OYAMA MAKOTO , OKADA YUMIKO , NAKAGAWA KOJI , TAKAGI MASAYUKI , OKADA TADAAKI , MURAI YASUSHI , YONEDA TOSHIO , IINUMA KATSUHARU
IPC分类号： C07D273/00 , C12P17/14 , C12R1/645
摘要： PURPOSE:To provide a new depsipeptide obtained by culturing a mold. CONSTITUTION:PF 1022 strain belonging to asporogenic imperfect fungi is cultured in a culture medium containing nutritive components capable of being incorporated by general microorganisms. From the resultant cultured material, the objective substance, PF 1022E can be isolated by using the solvent extraction method, the silica gel column chromatography method, etc. This substance is a new cyclic depsipeptide having a molecular formula of C52H76N4O13 and represented by the formula.

4. 发明专利

JPH0641145A CEPHALOSPORIN DERIVATIVE 失效
公开(公告)号：JPH0641145A
公开(公告)日：1994-02-15
申请号：JP19396792
申请日：1992-07-21
申请人： MEIJI SEIKA KAISHA
发明人： OKADA YUMIKO , MURAI YASUSHI , YONEDA TOSHIO , IINUMA KATSUHARU , SATO ATSUYUKI
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/04 , C07D501/06 , C07D501/24
摘要： PURPOSE:To provide a new cephalosporin derivative useful as an intermediate for an aminothiazol cephalosporin derivative having an excellent antibacterial activity and being a medicine for various bacterial infections. CONSTITUTION:The derivative is a cephalosporin derivative expressed by formula 1 (X is an eliminable group; R is a (lower alkyl substituted) thiazolyl; R is H or a carboxyl protecting group) or its salt, e.g. p- methoxybenzyl-7beta-[(Z)-4-2-(4-methylthiazol-5-yl)ethenyl]-3-cephem-4 -carboxylate. The compound of formula 1 can be obtained by subjecting a compound of formula 2 or its salt to reaction with a compound of formula 3, its reactive derivative or its salt and, if needed, eliminating a carboxyl protecting group. Further, the compound of formula 1 is subjected to reaction with a compound of formula 4 and, if necessary, to eliminate a protecting group, to obtain a cephalosporin antibiotic compound by a short and simple process and in good yield.

5. 发明专利

JPH05320148A SYNTHESIS OF CYCLIC DEPSIPEPTIDE PF1022 SUBSTANCE 失效
公开(公告)号：JPH05320148A
公开(公告)日：1993-12-03
申请号：JP13113992
申请日：1992-05-22
申请人： MEIJI SEIKA KAISHA
发明人： OYAMA MAKOTO , YONEDA TOSHIO , IINUMA KATSUHARU , OKADA TADAAKI
IPC分类号： A61K31/395 , A61P33/10 , C07D273/00
摘要： PURPOSE:To obtain a cyclic depsipeptide PF1022 substance useful as an anthelmintic drug from phenyllactic acid, lactic acid and leucine. CONSTITUTION:The objective compound of formula can be produced by cyclizing the compound of the formula L-N-CH3.Leu-D-lac-L-N-CH3-Leu-D-phe.lac-L-N- CH3.Leu-D-lac-L-CH3-Leu-D-phe.lac-OH (lac is lactic acid; N-CH3-Leu is N- methylleucine; phe-lac is phenyllactic acid; Leu is leucine). The cyclization is carried out by dicyclohexylcarbodiimide (DCC) process or water-soluble DCC+ additive (e.g. N-hydroxysuccinimide) process in a solvent (e.g. THF-DMF) at 0-50 deg.C.

6. 发明专利

JPH0551361A AZETIDINONE DERIVATIVE 失效
公开(公告)号：JPH0551361A
公开(公告)日：1993-03-02
申请号：JP21239491
申请日：1991-08-23
申请人： MEIJI SEIKA KAISHA
发明人： WASHIMI SHINJIRO , YASUDA SHOHEI , YAMAMOTO YUICHI , SAKANAKA OSAMU , MATSUHASHI IWAO , YONEDA TOSHIO , IINUMA KATSUHARU , NISHIHATA TAKESHI
IPC分类号： C07D205/095 , C07D501/04 , C07D501/08
摘要： PURPOSE:To obtain a new compound useful as a synthetic intermediate for cephalosporin-based antibiotic substances. CONSTITUTION:A compound expressed by formula I (R' is H or protecting group of carboxylic acid; R is aryl, arylmethyl, H or 1-10C alkyl; Ar is aryl), e.g. p-methoxybenzyl 2-[3-(3,5-dichlorosalicylideneamino)-4-benzenesulf onylthio-2- azetidinon-1-yl]-3-methyl-3-butenoate. The compound expressed by formula I is obtained by reacting a compound expressed by formula II with an aldehyde expressed by the formula R -CHO in an inert solvent (e.g. methylene chloride) at -30 to +100 deg.C. The compound expressed by formula I can readily be converted into 3-cephem derivatives by its treatment with a base.

7. 发明专利

JPH02229116A CARCINOSTATIC AGENT COMPOSITION 失效
公开(公告)号：JPH02229116A
公开(公告)日：1990-09-11
申请号：JP4848889
申请日：1989-03-02
申请人： MEIJI SEIKA KAISHA , MICROBIAL CHEM RES FOUND
发明人： HOSOI KAORU , ISHIZAWA TAKAYUKI , OKADA MAKOTO , YONEDA TOSHIO , MURATA SHINJIRO , FUKATSU SHUNZO , TSUCHIYA OSAMU
IPC分类号： C07H15/252 , A61K9/00 , A61K9/19 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K47/26 , A61P35/00
摘要： PURPOSE:To obtain a carcinostatic composition, containing an anbthracycline- based compound FAD-104 and lactose in a specific proportion, excellent in stability and preservable at ambient temperature. CONSTITUTION:A carcinostatic agent composition, containing (8S,10S)-8-(7- carboxyheptanoyloxyacetyl) -10- [2,6-dideoxy-2-fluoro-alpha-L-talopyranosyl)oxy] -7,8,9,10-tetrahydro-6,8,11-trihydroxy-1-methoxy-5,12-naphthacenedione expressed by the formula or a nontoxic salt thereof as an active ingredient and obtained by blending 1 pt.wt. afore-mentioned compound with 0.5-0 pts.wt., preferably 1-4 pts.wt. lactose. The composition is preferably in the form of a freeze-dried product prepared by suspended or dissolving the compound which is the active ingredient and lactose in a suitable proportion within the above-mentioned range, together with a pH adjuster and freeze-drying the resultant suspension or solution regulated to a pH between 5 and 7.

8. 发明专利

JPH03264069A ANTIBACTERIAL DEODORIZING WORKING AGENT AND WORKING METHOD 失效
公开(公告)号：JPH03264069A
公开(公告)日：1991-11-25
申请号：JP7323790
申请日：1990-03-26
申请人： SAKAI ENG KK , MEIJI SEIKA KAISHA
发明人： KATAYAMA MATSUKO , YASUDA KIMIAKI , TAKEBE HIDEAKI , IINUMA KATSUHARU , YONEDA TOSHIO
IPC分类号： A61L2/26 , A61L9/01
摘要： PURPOSE:To provide the antibacterial and deodorizing effect to a working processed product, suppress the breeding of the harmful microorganisms on the product and prevent the deterioration of the product which is caused by the harmful microorganisms by applying the amino glycoside group antibacterial substance to the antibacterial deodorizing work for a fiber product, in particular, for a fiber product having a hydrophobic surface. CONSTITUTION:The reduction substance of the derivative in which the amino group of the amino glycoside group antibacterial substance is Schiff's base-formed sufficiently endures in the actual use, through the durability for washing slightly reduces, also in the conventional using method. As for the Schiff's base derivative of the amino glycoside group antibacterial substance, though the substance having the superior crystalline performance among the derivative in which all the amino groups are Schiff's base-formed can be isolated and the physical properties can be confirmed, isolation of each or a specific substance of a plurality of derivatives which are formed by using the aldehyde in the quantity which is insufficient for Schiff's formation of the derivative other than the above-described derivative, in particular, of all the amino groups is impossible in consideration of the stability of the Schiff's base.

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