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1. 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。

2. 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。

3. 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。

4. 发明专利

JPH0564956B2 失效
公开(公告)号：JPH0564956B2
公开(公告)日：1993-09-16
申请号：JP29367185
申请日：1985-12-28
申请人： MEIJI SEIKA CO , 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

5. 发明专利

JPS61251685A NOVEL 1-OXA-1-DETHIACEPHALOSPORIN COMPOUND AND ANTIBACTERIALCONTAINING SAME 失效
公开(公告)号：JPS61251685A
公开(公告)日：1986-11-08
申请号：JP4185486
申请日：1986-02-28
申请人： MEIJI SEIKA KAISHA , MERCK & CO INC
发明人： SHIBAHARA MASAYOSHI , OKONOGI TSUNEO , MURAI YASUSHI , FUKATSU SHUNZO , NIIDA TARO , WAKAZAWA TADASHI , BAATON JII KURISUTENSEN
IPC分类号： A61K31/535 , A61P31/04 , C07D498/04 , C07D505/00

6. 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

7. 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

8. 发明专利

JPS60105682A 2-ALKYL-3'-NOR-OXACEPHALOSPORIN DERIVATIVE 失效
公开(公告)号：JPS60105682A
公开(公告)日：1985-06-11
申请号：JP21318283
申请日：1983-11-15
申请人： MEIJI SEIKA CO , MERCK & CO INC
发明人： OKONOGI TSUNEO , SHIBAHARA MASAYUKI , MURAI YASUSHI , FUKATSU SHIYUNZOU , NIIDA TAROU , WAKAZAWA TADASHI , BAATON JI KURISUTENSEN
IPC分类号： C07D505/00 , A61K31/535 , A61P31/04 , C07D498/04

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