专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明专利

JPH0543545A NEW AZA-SACCHARIDE DERIVATIVE 失效
公开(公告)号：JPH0543545A
公开(公告)日：1993-02-23
申请号：JP20520791
申请日：1991-08-15
申请人： MEIJI SEIKA KAISHA
发明人： ISHII YOSHIYUKI , USUI TAKAYUKI , SHIBAHARA MASAYUKI , NAGAOKA KOZO , INOUE SHIGEHARU
IPC分类号： A61K31/445 , A61P31/12 , A61P31/18 , C07D211/46
摘要： PURPOSE:To obtain a new aza-saccharide derivative capable of increasing beta- glycosidase inhibitory activity and exhibiting a wide range of antiviral activity. CONSTITUTION:A deoxynorimycin derivative expressed by formula I [R is H or 1-6C lower alkyl; mark $ indicates that the absolute configuration is (R) or (S)], e.g. 1,5-imino-1,5,7-trideoxy-D glycero-D-gluco-heptitol. A compound expressed by formula II which is a compound expressed by formula I (R is H) is obtained by protecting amino group of, e.g. deoxynojirimycin as a starting material with benzyl group, etc., then protecting hydroxyl groups at the 2-and 3-positions with a cyclic acetal type protecting group, providing a compound expressed by formula III (Bn is benzyl; TBDMS is tert-butyldimethylsilyl), subsequently passing the resultant compound through compounds expressed by formulas IV, V and VI and successively deprotecting the prepared compounds.

42. 发明专利

JPS63154622A ANTIMICROBIAL AGENT CONTAINING CEPHALOSPORIN DERIVATIVE AS ACTIVE INGREDIENT FOR MAMMAL 失效
公开(公告)号：JPS63154622A
公开(公告)日：1988-06-27
申请号：JP30293286
申请日：1986-12-18
申请人： MEIJI SEIKA KAISHA , MIHASHI SUSUMU
发明人： SHIBAHARA MASAYUKI , OKONOGI TSUNEO , MURAI YASUSHI , KUDO TOSHIAKI , YOSHIDA TAKASHI , NISHIHATA TAKESHI , KONDO SHINICHI
IPC分类号： A61K31/435 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36
摘要： PURPOSE:To obtain the titled antimicrobial agent, containing a cephalorsporin derivative as an active ingredient and effective against bacteria including a wide range of resistant germs. CONSTITUTION:An antimicrobial agent for mammals, containing a compound expressed by the formula (n is 1-4), e.g. monosodium (6R,7R)-7-[(Z)-2-(2- aminothiazol-4-yl)-2-{(1S)-carboxyethoxyimino}acetamido]-3-(1-ethylpyr idinium-4- ylthiomethyl)-ceph-3-em-4-carboxylate, or salt thereof as an active ingredient. The compound expressed by the formula has low toxicity and is rapidly migrated into blood and internal organs by intramuscular or intravenous administration and has sufficient persistence in a concentration sufficient to produce antimicrobial action. The dose thereof is 0.5-3g/day, preferably 1-2g/day and administered in one or several divided portions. The above-mentioned antimicrobial agent has antimicrobial action on a wide range of germs from Gram-positive bacteria, e.g. Staphylococcus aureus, etc., to Gram-negative bacteria, e.g. Escherichia coli, etc.

43. 发明专利

JPS625961A PYRIDOTHIONE COMPOUND HAVING ACIDIC GROUP AND NOVEL CEPHALOSPORIN DERIVATIVE DERIVED FROM SAID COMPOUND 失效
公开(公告)号：JPS625961A
公开(公告)日：1987-01-12
申请号：JP14548985
申请日：1985-07-01
申请人： MEIJI SEIKA KAISHA
发明人： SHIBAHARA MASAYUKI , KUDO TOSHIAKI , OKONOGI TSUNEO , MURAI YASUSHI , TAKAHASHI SACHIKO , NISHIHATA TAKESHI , KONDO SHINICHI
IPC分类号： C07D213/70 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/56
摘要： NEW MATERIAL:The compound of formula I [R1 is H or CH3; R2' is carboxyl, carboxymethyl, their protected groups, sulfonyl or sulfomethyl; the steric configuration of the symbol * represents optically active (R) or (S) isomer or optically inactive (R, S) isomer], the compound of formula II (R3 is methyl, allyl, carboxymethyl, etc.), and their nontoxic salt and nontoxic ester. EXAMPLE:(6R, 7R)-7-[( Z )-2-(2-aminothiazol-4-yl)-2-(methoxyimino)- acetamido]-3- {1-(1-sulfomethyl)pyridinium-4-ylthiomethyl}-ceph-3-em-4-carboxylate. USE:Antibiotic substance. PREPARATION:The compound of formula III is made to react with the compound of formula IV to obtain the compound of formula I having sulfonic acid group at the side chain. The compound of formula II can be produced by introducing the compound of formula I to the 3'-position of cephalosporin.

44. 发明专利

JPS61183291A NOVEL 7-AMINOCEPHALOSPORIN DERIVATIVE AND NOVEL N-FLUOROETHYLPYRIDOTHIONE COMPOUND 失效
公开(公告)号：JPS61183291A
公开(公告)日：1986-08-15
申请号：JP2418485
申请日：1985-02-09
申请人： MEIJI SEIKA KAISHA
发明人： KUDO TOSHIAKI , MURAI YASUSHI , OKONOGI TSUNEO , SHIBAHARA MASAYUKI , FUKATSU SHUNZO
IPC分类号： C07D213/68 , C07D213/70 , C07D501/18 , C07D501/36
摘要： NEW MATERIAL:A compound shown by the formula I (n is O or 1; n is 0-2; when n is O, n is 3, when n is 1, n is 2, and when n is 2, n is 1; A is carboxylic acid-protecting group; X is Cl , I , CH3CO 2, etc.). EXAMPLE:Diphenylmethyl 3-[{1-(2-fluoroethyl)pyridinium}-4-ylthiomethyl]-7-ami n-o-3- cephem-4-carboxylate iodide. USE:A compound useful as an antibacterial agent, suitable for production on industrial scale. PREPARATION:For example, a cephalosporin compound shown by the formula II is reacted with a compound shown by the formula III [e.g., 1-(2-fluoroethyl)-4- pyridothione, etc.] in an inert solvent(preferably DMF, etc.), preferably in the presence of NaI at 10-80 deg.C. the compound shown by the formula III is a novel compound, and obtained by reacting a compound shown by the formula IV with fluoroethylamine hydrochloride, and reacting the reaction product with phosphorus sulfide.

45. 发明专利

JPS5946287A Novel 1-oxa-1-dethia-cephalosporin derivative 失效
标题翻译：新型1-OXA-1-DETHIA-CEPHALOSPORIN衍生物
公开(公告)号：JPS5946287A
公开(公告)日：1984-03-15
申请号：JP12757482
申请日：1982-07-23
申请人： Meiji Seika Kaisha Ltd , Merck & Co Inc
发明人： SHIBAHARA MASAYUKI , OKONOGI TSUNEO , MURAI YASUSHI , 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 {R is group of formula II (R1 is 2- or 3-thienyl; R2 is H or carboxy) or formula III [R3 is H or (carboxy)-lower alkyl]; R4 is H or methoxy; R5 is lower alkyl; R6 is group of formula IV [Het is (substituted) heterocyclic group]}. EXAMPLE:7-( 2-Thienylacetamido )-2alpha-methyl-4-( 1-methyl-1H-tetrazol-5-yl )-thiomethyl-1-oxa-1-dethia-3-cephem-4-carboxylic acid. USE:Antibacterial agent. Antibiotic substance useful for the remedy and prevention of bacterial infectious diseases. PROCESS:The objective compound can be prepared by condensing the compound of formula V (A is carboxyl-protecting group) with a carboxylic acid (or its reactive derivative) in an organic solvent (e.g. methylene chloride), and eliminating the protecting group e.g. with an acid. The compound of formula V is a novel substance, which can be synthesized e.g. from the compound of formula VIvia several steps.
摘要翻译：新物质：式Ⅰ化合物（R为式Ⅱ的基团（R1为2-或3-噻吩基; R2为H或羧基）或式Ⅲ[R3为H或（羧基） - 低级烷基]; R4是H或甲氧基; R5是低级烷基; R6是式IV的基团[Het是（取代的）杂环基]]。实施例7-（2-噻吩乙酰氨基）-2α-甲基-4-（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：抗菌剂。用于治疗和预防细菌感染性疾病的抗生素物质。方法：目标化合物可以通过在有机溶剂（例如二氯甲烷）中将式V化合物（A为羧基保护基）与羧酸（或其反应性衍生物）缩合而制备，并除去保护基团。与酸。式V化合物是一种新型物质，其可以合成例如由式VI化合物通过几个步骤。

46. 发明专利

JPS5910591A 1-oxadethiacephalosporin compound and antibacterial agent containing the same 失效
标题翻译： 1-OXADETHIACEPHALOSPORIN化合物和含有它的抗菌剂
公开(公告)号：JPS5910591A
公开(公告)日：1984-01-20
申请号：JP11863782
申请日：1982-07-09
申请人： Meiji Seika Kaisha Ltd
发明人： SHIBAHARA MASAYUKI , OKONOGI TSUNEO , MURAI YASUSHI , FUKATSU SHIYUNZOU , NIIDA TAROU , WAKAZAWA TADASHI
IPC分类号： C07D498/04 , A61K31/535 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36 , C07D505/00
CPC分类号： C07D505/00 , Y02P20/55
摘要： NEW MATERIAL:The compound of formula I {R
1 is 1W4C alkyl; R
2 is group of formula II (R
3 is H or carboxyl), or formula III [R
4 is H or amino; R
5 is 1W 4C alkyl or group of formula IV (R
6 and R
7 are H or 1W4C alkyl)]}, its salt and its ester.
EXAMPLE: 7-( 2- Thienylacetamido)1-oxa- 1-dethia-3- methylthio- 3-cephem- 4-carboxylic acid of formula V.
USE: Antibacterial agent which can be administered orally as well as parenterally. It has excellent antibacterial activites not only to Gram-positive bacteria but also to Gram-negative bacteria.
PROCESS: The objective compound is prepared, e.g. by reacting (acylating) the 7- amino group of the 1-oxadethia-3-alkylthio-7-aminocephem compound of formula VI(R
8 is H or carboxyl-protecting group) with the thienyl compound of formula VII[ R
9 is H or (protected) carboxyl; -COR
10 is carboxyl or its reactive derivative group], and if necessary, eliminating the protecting group.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I化合物{R1为1-4C烷基; R2是式II的基团（R3是H或羧基）或式III [R4是H或氨基; R5为1-4C烷基或式IV基团（R6和R7为H或1-4C烷基）]}，其盐及其酯。实施例：具有式V的7-（2-噻吩乙酰氨基）1-氧杂-1-脱硫-3-甲硫基-3-头孢烯-4-羧酸。用途：可以口服和肠胃外给药的抗菌剂。它具有优异的抗菌活性，不仅对革兰氏阳性菌，而且对革兰氏阴性细菌。方法：目标化合物如通过使式VI（R 8为H或羧基保护基）的1-恶嗪-3-烷硫基-7-氨基头孢烯化合物的7-氨基与式VII的噻吩基化合物反应（酰化）[R 9为H或（保护）羧基; -COR10是羧基或其反应性衍生物基团]，如果需要，除去保护基。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式