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21. 发明专利

JPS5951291A Oxadethiacephalosporin intermediate and its preparation 失效
标题翻译： OXADETHIACEPHALOSPORIN中间体及其制备
公开(公告)号：JPS5951291A
公开(公告)日：1984-03-24
申请号：JP15954882
申请日：1982-09-16
申请人： Meiji Seika Kaisha Ltd , Merck & Co Inc
发明人： OKONOGI TSUNEO , MURAI YASUSHI , SHIBAHARA MASAYUKI , FUKATSU SHIYUNZOU , NIIDA TAROU , WAKAZAWA TADASHI
IPC分类号： A61K31/535 , A61P31/04 , C07D205/085 , C07D403/12 , C07D505/00 , C07F9/568
CPC分类号： C07D403/12 , C07D205/085 , C07D505/00 , C07F9/5683 , Y02P20/55
摘要： NEW MATERIAL:The compound of formula I [R1 is H or OCH3; R2 is lower alkyl; R3 is CH3, halomethyl, or -CH2S-Het (Het is heterocyclic group which may have substitutent group); A is H or COOH-protecting group]. EXAMPLE:7beta-Amino -7alpha- methoxy-2alpha-methyl -3-(1-methyl-1H-tetrazol-5-yl) thiomethyl-1-oxa-1-dethia-3-cephem-4-carboxylic acid. USE:A synthetic intermediate of 7beta-acyl-2-alkyl-1-oxa-1-dethia-cephalosporin compound which is a strong antibacterial agent. PROCESS:The compound of formula I can be prepared by (1) cyclizing the novel azetidinone compound of formula II (RCO- is acyl; ph is phenyl; A' is COOH- protecting group), (2) eliminating the RCO-group from the resultant compound of formula III, (3) reacting the product with an aromatic aldehyde to obtain the compound of formula IV (R4 is aromatic group), and (4) carrying out the steric inversion of the 7alpha-NH2.
摘要翻译：新材料：式I化合物[R1是H或OCH3; R2是低级烷基; R3是CH3，卤甲基或-CH2S-Het（Het是可以具有取代基的杂环基）; A为H或COOH保护基]。实施例：7β-氨基-7α-甲氧基-2α-甲基-3-（1-甲基-1H-四唑-5-基）硫甲基-1-氧杂-1-脱硫-3-头孢烯-4-羧酸。用途：作为强抗菌剂的合成中间体，其为β-二酰基-2-烷基-1-氧杂-1-脱氢头孢菌素化合物。方法：式I化合物可以通过（1）环化式II的新的氮杂环丁酮化合物（RCO-是酰基; ph是苯基; A'是COOH-保护基）来环化，（2）消除RCO- 所得到的式III化合物，（3）使产物与芳族醛反应，得到式IV化合物（R4为芳族基团），和（4）进行7α-NH 2的空间倒置。

22. 发明专利

JPS5726690A New preparation of cephamycin derivative 失效
标题翻译： CEPHAMYCIN衍生物的新制备
公开(公告)号：JPS5726690A
公开(公告)日：1982-02-12
申请号：JP10060380
申请日：1980-07-24
申请人： Meiji Seika Kaisha Ltd
发明人： SAITOU TOSHINORI , FUKATSU SHIYUNZOU , NISHIHATA TAKESHI , SHIBAHARA MASAYUKI
IPC分类号： C07D501/04 , C07D501/57
CPC分类号： Y02P20/55
摘要： PURPOSE: To obtain the titled compound useful as an antimicrobial agent, etc. in high yield, by treating a specific amide group-containing cephem carboxylic acid with a halogenating agent, followed by imino etherification with a lower alcohol, treatment with an acylating agent, and removal of protecting group.
CONSTITUTION: A compound shown by the formula I (R
1 is amino-protecting group; R
2 is H or amino-protecting group; R
3 and R
4 are carboxyl-protecting group) is treated with a halogenating agent in the presence of a base to give an imino halide derivative, which is reacted with a lower alcohol to give an imino ether derivative shown by the formula II (R
5 is lower alkyl). This compound is reacted with an acylating agent to give a compound shown by the formula III [R
6 is X
2 CH (X
2 is halogen), etc.], the carboxyl-protecting group R
4 is removed and the resulting compound is reacted with cysteine, etc., to give 7β-(2D-2-amino-2-carboxyl) eth ethyl-thioacetamido-7α-methoxy-3-( 1-methyl-1H-tetrazole-5-yl )thiomethyl-3-cephem-4-carboxylic acid shown by the formula IV or its salt.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：目的：通过用卤化剂处理含有特定酰胺基的头孢霉酸，然后用低级醇进行亚氨基醚化，用酰化剂处理，以高产率获得用作抗微生物剂等的标题化合物，并除去保护基。构成：式I化合物（R 1为氨基保护基; R 2为H或氨基保护基; R 3和R 4为羧基保护基）的化合物用卤化剂在碱存在下反应，得到亚氨基卤化物衍生物，其与低级醇反应，得到式II所示的亚氨基醚衍生物（R 5为低级烷基）。该化合物与酰化剂反应，得到式III所示的化合物[R 6为X 2 CH（X 2为卤素）等]，羧基保护基R 4，并将所得化合物与半胱氨酸等反应，得到7beta-（2D-2-氨基-2-羧基）乙基 - 乙酰基氨基-7α-甲氧基-3-（1-甲基-1H-四唑-5 - 基）硫代甲基-3-头孢烯-4-羧酸或其盐。

23. 发明专利

JPH09104694A ACIC ADDITION SALT OF ARBEKACIN WITH (-)-CIS-1,2-EPOXYPROPYLPHOSPHONIC ACID, ITS PRODUCTION AND ANTIMICROBIAL AGENT 失效
公开(公告)号：JPH09104694A
公开(公告)日：1997-04-22
申请号：JP26182295
申请日：1995-10-09
申请人： MICROBIAL CHEM RES FOUND , MEIJI SEIKA KAISHA
发明人： SHIBAHARA MASAYUKI , USUI TAKAYUKI , NIISATO TETSUTARO , SHINEI YOSHIHIDE , GOMI SHUICHI , INOUE SHIGEHARU , KONDO SHINICHI , TAKEUCHI TOMIO
IPC分类号： C07H1/00 , A61K31/665 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H15/234 , C07H15/26 , C07H17/04
摘要： PROBLEM TO BE SOLVED: To produce the subject new acid addition salt having high antimicrobial activities and low nephrotoxicity by reacting arbekacin with (-)-cis-1,2-epoxypropylphosphonic acid in an aqueous solution and then freeze- drying the aqueous layer of the reactional solution. SOLUTION: This new acid addition salt of an arbekacin represented by formula I [one to five of five groups X are groups, added to amino groups of the arbekacin and represented by formula II (M is H, Na , K , ammonium cation, etc.)] with (-)-cis-1,2-epoxypropylphosphonic acid (salt). Since the acid addition salt has high antimicrobial activities and low nephrotoxicity, it is useful as an antimicrobial agent, etc. The new acid addition salt is obtained by reacting a free salt of the arbekacin with a hemi-amine salt of (-)-cis-1,2- epoxypropylphosphonic acid in an amount of 1-5mol hemi-amine salt of the epoxypropylphosphonic acid, described above and based on 1mol arbekacin in an aqueous medium, producing the acid addition salt and then freeze-drying or concentrating and evaporating the aqueous layer after the reaction to dryness.

24. 发明专利

JPH07165761A NEW PHYSIOLOGICALLY ACTIVE SUBSTANCE SF2771 COMPOUND AND ITS PRODUCTION 失效
公开(公告)号：JPH07165761A
公开(公告)日：1995-06-27
申请号：JP30893893
申请日：1993-12-09
申请人： MEIJI SEIKA KAISHA
发明人： SUZUKI KAZUO , KAWAI MAYUMI , HOTSUTA KUNIMOTO , HATSU MASAHIRO , SHIMIZU AKIRA , AMANO SHOICHI , IMAI SATOSHI , SHIBAHARA MASAYUKI
IPC分类号： C12P17/18 , A61K31/495 , A61P35/00 , C07D487/04 , C12R1/465
摘要： PURPOSE:To obtain the subject compound inducing a promotive activity by neutrophils against tumor cells, useful as an immunoenhancing agent and as a material for obviating the interaction between tumor cells and phagocytes such as neutrophils, by taking from a cultured product obtained by culturing specific bacteria belonging to Streptomyces. CONSTITUTION:This compound of the formula is obtained from a cultured product obtained by culturing SF2771 substance-productive bacteria belonging to Streptomyces (FERM P-13884). The physicochemical properties of the compound of the formula are as follows: color an appearance: colorless needlelike crystal; melting point: 178-180 deg.C; molecular formula: C9H12N2O2; molecular weight: 180; specific rotatory power: [alpha] D=109.6 deg. (c=1.0, methanol); solubility: readily soluble in water, methanol, ethyl acetate, acetone and chloroform, sparingly soluble in hexane; color reaction: positive to molybdic acid and iodine, negative to ninhydrin; the Rf value in silica gel thin-layer chromatography: butanol:(acetic acid:water(4:1:2)) 0.85.

25. 发明专利

JPH06234772A NEW CEPHALOSPORIN DERIVATIVE 失效
公开(公告)号：JPH06234772A
公开(公告)日：1994-08-23
申请号：JP19240393
申请日：1993-08-03
申请人： MEIJI SEIKA KAISHA
发明人： TSUSHIMA MASAKI , KANOU YUUKO , IWAMATSU KATSUYOSHI , TAMURA ATSUSHI , SHIBAHARA MASAYUKI
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D519/06 , C07D519/00
摘要： PURPOSE:To obtain a new compound useful for treating bacterial infection diseases, and having a broad antibacterial spectrum. CONSTITUTION:The subject compound is expressed by the formula I [X is carbon or N; Y is S, O, (low alkyl substituted) N; R is H or (substituted) low alkyl; R is (substmtuted) low alkyl or (substituted) low alkylene; A ring is an unsaturated 6-membered heterocycle having >=1 N]. E.g., 7-{(Z)-2-(2- aminothiazol-4-yl)-2-methoxyiminoacetamid}-3-(5-methylthiazolo[4,5- C]pyridinium-2-yl)thiomethyl-3-cephem-4-carboxylate. Here, the compound of the formula I can be obtained by removing a protecting group of a compound of the formula IV, is an amino-protecting group; R is R , etc.; R is a carboxylprotecting group) to react with a compound of the formula III (W is halogen, etc.).

26. 发明专利

JPH0687865A NEW 1-OXA-1-DETHIACEPHEM COMPOUND 失效
公开(公告)号：JPH0687865A
公开(公告)日：1994-03-29
申请号：JP708493
申请日：1993-01-20
申请人： MEIJI SEIKA KAISHA , MERCK & CO INC
发明人： SHIBAHARA MASAYUKI , OKONOGI TSUNEO , MURAI YASUSHI , FUKATSU SHUNZO , NIIDA TARO , WAKAZAWA TADASHI , BAATON JII KURISUTENSEN
IPC分类号： C07D493/00 , A61K31/535 , A61P31/04 , C07D498/04 , C07D505/00 , C07D498/053

27. 发明专利

JPH05310773A 失效
公开(公告)号：JPH05310773A
公开(公告)日：1993-11-22
申请号：JP11181692
申请日：1992-04-30
申请人： MEIJI SEIKA KAISHA
发明人： AJITO KEIICHI , SHIBAHARA MASAYUKI , USUI TAKAYUKI , KAKINUMA KAZUYO , IIDA MAIKO
IPC分类号： C07H15/224 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/26
摘要： PURPOSE:To obtain a new compound containing 2-deoxystreptamine as an ingredient and being an intermediate for 5,3',4'-trideoxyneamin useful as an antimicrobial agent. CONSTITUTION:A compound of the formula [R is monovalent amino protecting group; R is H or (substituted) OH, R is H, (substituted) OH or halogen; R is same as R , with the proviso that either one of R and R is H], e.g. 1,6-N, O-benzylidene-1,3,2'6'-tetra-N -BOC-3',4'-dideoxyneamin. This compound of the formula is obtained by reacting, e.g. a bicyclic amine glycoside containing 2- deoxystreptamine modified with a monovalent amine protecting group as an ingredient with benzaldehyde dimethylacetal in the presence of a catalytic amount of p-toluenesulfonic acid pyridine salt and selectively subjecting an amino at 1st position and OH at 6th position to benzylidenation.

28. 发明专利

JPH05117292A NEW 16-MEMBERED RING MACROLIDE DERIVATIVE AND ITS PRODUCTION 失效
公开(公告)号：JPH05117292A
公开(公告)日：1993-05-14
申请号：JP27740191
申请日：1991-10-24
申请人： MEIJI SEIKA KAISHA
发明人： AJITO KEIICHI , SHIMIZU AKIRA , USUI TAKAYUKI , SHIBAHARA MASAYUKI , NAGAOKA KOZO , INOUE SHIGEHARU
IPC分类号： C07H17/08 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04
摘要： PURPOSE:To obtain the subject new compound useful as antibacterial agent against Gram-positive bacteria and an intermediate for various kinds of valuable compounds. CONSTITUTION:A compound of formula I [R is O or (OR )2 (R is 1-4C straight- chain alkyl or benzyl), etc.; R is H, 4-O-propionylmycarose residue, etc.; R is H or COR (R is 1-3C straight-chain alkyl)] or a salt thereof such as a compound of formula II showing the following properties. Appearance: colorless solid. Molecular formula: C30H40NO11. Melting point: 105-111 deg.C. Solubility: soluble in chloroform, acetone, etc., insoluble in neutral and alkali water. The compound of formula II is obtained by oxidizing leucomycin A7 of formula III by a method of reacting the compound with pyridinium chlorochromate preferably in an inert organic solvent at -10 to 50 deg.C and subjecting formed 9-dehydroleucomycin A7 to acidolysis by a method of treating 9-dehydroleucomycin A7 with an acid catalyst composed of p-toluenesulfonic acid in the presence of preferably ethylene glycol.

29. 发明专利

JPH03204885A NEW CEPHALOSPORIN BASED COMPOUND 失效
公开(公告)号：JPH03204885A
公开(公告)日：1991-09-06
申请号：JP34416389
申请日：1989-12-28
申请人： MEIJI SEIKA KAISHA
发明人： SAKAGAMI KENJI , IWAMATSU KATSUYOSHI , ATSUMI KUNIO , SHIBAHARA MASAYUKI , KAWAHARAJIYOU KATSUMI , INOUE SHIGEHARU
IPC分类号： C07D501/36 , A61K31/545 , A61K31/546 , A61P31/04
摘要： NEW MATERIAL:A compound expressed by formula I [R1 and R2 are H or (protected) carboxyl; A is nucleophilic residue; n and m are 0-3]. EXAMPLE:7-[2-(2-Tolytylaminothiazol-4-yl)-2-(3-diphenylmethoxy-4-pyrid on-1-yl) ethoxyiminoacetamido]-3-(1,2,3-thiadiazol-5-yl)thiomethyl-3-cephem-4-c arboxylic acid p-methoxybenzyl ester. USE:A antimicrobial agent. PREPARATION:A compound expressed by formula II (R3 is H or carboxyl protecting group) or reactive derivative in amino group thereof or salt thereof is reacted with a compound expressed by formula III (R4 is H or amino protecting group; R5 is H or OH protecting group) or reactive derivative in carboxyl group thereof or salt thereof.

30. 发明专利

JPS61158985A NOVEL 1-OXA-1-DETHIACEPHALOSPORIN COMPOUND AND ANTIBACTERIALCONTAINING SAME 失效
公开(公告)号：JPS61158985A
公开(公告)日：1986-07-18
申请号：JP29367185
申请日：1985-12-28
申请人： MEIJI SEIKA KAISHA , MERCK & CO INC
发明人： SHIBAHARA MASAYUKI , OKONOGI TSUNEO , MURAI YASUSHI , FUKATSU SHUNZO , NIIDA TARO , WAKAZAWA TADASHI , BAATON JII KURISUTENSEN
IPC分类号： C07D493/00 , A61K31/535 , A61P31/04 , C07D498/04 , C07D505/00

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