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公开(公告)号:US4081443A
公开(公告)日:1978-03-28
申请号:US806882
申请日:1977-06-15
申请人: Shoichiro Uyeo , Hikaru Itani , Tsutomu Aoki , Teruji Tsuji , Wataru Nagata
发明人: Shoichiro Uyeo , Hikaru Itani , Tsutomu Aoki , Teruji Tsuji , Wataru Nagata
IPC分类号: C07D499/00 , C07D499/44
CPC分类号: C07D499/00
摘要: Compounds of the formula: ##STR1## (where COB is carboxy or protected carboxy and X is hydrogen or nucleophilic group)preparable by oxidation of the corresponding N-nitrosopenicillin derivatives are useful as starting materials for synthesizing known and useful cephalosporins.
摘要翻译: 下式的化合物:其中COB为羧基或被保护的羧基,X为氢或亲核基团)可通过氧化相应的N-亚硝基青霉素衍生物制备可用作合成已知和有用的头孢菌素的起始原料。
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公开(公告)号:US4138486A
公开(公告)日:1979-02-06
申请号:US780183
申请日:1977-03-22
申请人: Masayuki Narisada , Wataru Nagata
发明人: Masayuki Narisada , Wataru Nagata
IPC分类号: C07D505/00 , A61K31/535 , A61K31/5365 , A61P31/00 , A61P31/04 , C07D205/00 , C07D265/00 , C07D498/02 , C07D498/04 , C07D505/06 , C07D505/18 , C07D505/20 , A61K27/00 , A61K31/555 , A61K31/695
CPC分类号: C07D498/04 , A61K31/535 , C07D205/00 , C07D265/00 , C07D505/00
摘要: Antibacterial 1-oxadethiacephalosporins of the formula: ##STR1## [wherein Ar is ##STR2## (in which Acyl is organic or inorganic acyl); COB.sup.1 and COB.sup.2 each is carboxy or protected carboxy; Het is ##STR3## (in which COB.sup.3 is carboxy or protected carboxy); AND Y is hydrogen or methoxy;And when COB.sup.1, COB.sub.2, and/or COB.sup.3 is carboxy, pharmaceutically acceptable salts thereof are included,But with a proviso that when Y is methoxy, Het is ##STR4## a pharmaceutical or veterinary composition comprising the said 1-oxadethiacephalosporins and pharmaceutical carrier, and a method for treating or preventing human or veterinary infectious diseases comprising administering the said 1-oxadethiacephalosporin.
摘要翻译: 下式的抗菌1-恶二硫醚孢子:其中Ar是有机或无机酰基;其中Ar是有机或无机酰基; COB1和COB2各自为羧基或保护的羧基; Het是
(其中COB 3是羧基或被保护的羧基); 且Y为氢或甲氧基; 当COB1,COB2和/或COB3为羧基时,包括其药学上可接受的盐,但是当Y为甲氧基时,Het为包含所述1-恶二硫醚类和药物载体的药物或兽用组合物, 以及用于治疗或预防人或兽传染性疾病的方法,包括施用所述1-恶二硫醚类。 -
公开(公告)号:US4539148A
公开(公告)日:1985-09-03
申请号:US523414
申请日:1983-08-16
申请人: Sadao Yamamoto , Hikaru Itani , Hiromi Takahashi , Teruji Tsuji , Wataru Nagata
发明人: Sadao Yamamoto , Hikaru Itani , Hiromi Takahashi , Teruji Tsuji , Wataru Nagata
IPC分类号: C07D205/08 , C07C51/00 , C07C59/21 , C07C67/00 , C07C241/00 , C07C245/18 , C07D205/085 , C07D261/02 , C07D309/12 , C07D498/00 , C07D505/00 , C07F7/08 , C07F7/10 , C07F7/18 , C07D487/04 , C07D403/12
CPC分类号: C07F7/1852 , C07C245/18 , C07C51/00 , C07C59/21 , C07D205/085 , C07D309/12 , C07D505/00 , C07F7/0892 , C07F7/10 , Y02P20/55
摘要: Useful intermediates, 7.alpha.-acylamino-3-(oxo or exomethylene)-1-dethia-1-oxacepham-4.alpha.-carboxylates, are produced by the intramolecular carbenoid insertion of a 2-diazo-3-(oxo or exomethylene)-4-(3.alpha.-acylamino-2-oxoazetidin-4.beta.-yl)oxybutyrate prepared in several steps from the corresponding oxazolinoazetidinone and diketone.
摘要翻译: 有用的中间体7α-酰基氨基-3-(氧代或异亚甲基)-1-脱氢-1-氧乙脒-β-α-羧酸盐是通过分子内碳氢化合物插入2-重氮-3-(氧代或异亚甲基) - 4-(3α-酰基氨基-2-氧代氮杂环丁烷-4β-基)氧基丁酸酯,由相应的恶唑啉氮杂环丁酮和二酮在几步中制备。
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公开(公告)号:US4323567A
公开(公告)日:1982-04-06
申请号:US156872
申请日:1980-06-05
申请人: Masayuki Narisada , Wataru Nagata
发明人: Masayuki Narisada , Wataru Nagata
IPC分类号: C07D505/00 , A61K31/535 , A61K31/5365 , A61P31/00 , A61P31/04 , C07D205/00 , C07D265/00 , C07D498/02 , C07D498/04 , C07D505/06 , C07D505/18 , C07D505/20 , C07D413/14 , A61K31/41 , C07D413/12
CPC分类号: C07D498/04 , A61K31/535 , C07D205/00 , C07D265/00 , C07D505/00
摘要: Antibacterial 1-oxadethiacephalosporins of the formula: ##STR1## wherein Ar is ##STR2## (in which Acyl is organic or inorganic acyl); COB.sup.1 and COB.sup.2 each is carboxy or protected carboxy;Het is ##STR3## (in which COB.sup.3 is carboxy or protected carboxy); and Y is hydrogen or methoxy;and when COB.sup.1 and COB.sup.2, and/or COB.sup.3 is carboxy, pharmaceutically acceptable salts thereof are included, but with a proviso that when Y is methoxy, Het is ##STR4## a pharmaceutical or veterinary composition comprising the said 1-oxadethiacephalosporins and pharmaceutical carrier, and a method for treating or preventing human or veterinary infectious diseases comprising administering the said 1-oxadethiacephalosporin.Also disclosed are epimers of the compounds of formula (I) wherein the asymmetric carbon of the malonic methine is in the D(R)- or L(S)- configuration. The individual epimers are separable by column chromatography and/or crystallization. The bactericidal activity of the D-epimers is greater than that of the L-epimers or the mixtures of the epimers.
摘要翻译: 其中Ar是有机或无机酰基的酰基;其中Ar是有机或无机酰基;其中Ar是有机或无机酰基。 COB1和COB2各自为羧基或被保护的羧基; Het是
(其中COB 3是羧基或被保护的羧基); Y为氢或甲氧基; 并且当COB1和COB2和/或COB3为羧基时,包括其药学上可接受的盐,但条件是当Y为甲氧基时,Het为包含所述1-恶二硫醚类和药物载体的药物或兽用组合物, 以及用于治疗或预防人或兽传染性疾病的方法,包括施用所述1-恶二硫醚类。 还公开了式(I)化合物的差向异构体,其中丙二酸次甲基的不对称碳为D(R) - 或L(S) - 构型。 单独的差向异构体可通过柱色谱和/或结晶分离。 D-差向异构体的杀菌活性大于L-差向异构体或差向异构体的混合物的杀菌活性。 -
公开(公告)号:US4203982A
公开(公告)日:1980-05-20
申请号:US819931
申请日:1977-07-28
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36 , C07D501/56 , C07D501/57 , C07D501/60
CPC分类号: C07D501/36 , C07D501/57
摘要: Antibacterial 7.beta.-arylmalonamido-7.alpha.-methoxy-3-heterocyclic thiomethyl-3-cephem-4-carboxylic acids of the formula: ##STR1## wherein Ar is a heterocyclic group or p-oxysubstituted phenyl; COB.sup.1 and COB.sup.2 are each a carboxy or protected carboxy group; and Het is an unsubstituted or substituted heterocyclic group. These compounds are prepared from, e.g., 7.beta.-amino-7.alpha.-methoxy-3-heterocyclic thiomethyl-3-cephem-4-carboxylic acid derivatives by acylation with arylmalonic acid or reactive derivatives thereof. They are useful as an active ingredient in antibacterial pharmaceutical preparations.
摘要翻译: 其中Ar是杂环基或对 - 氧代取代的苯基的抗菌7β-芳基丙二酰氨基-7α-甲氧基-3-杂环硫代甲基-3-头孢烯-4-羧酸。 COB1和COB2各自为羧基或被保护的羧基; 并且Het是未取代或取代的杂环基。 这些化合物通过用芳基丙二酸或其活性衍生物进行酰化由例如7β-氨基-7α-甲氧基-3-杂环硫代甲基-3-头孢烯-4-羧酸衍生物制备。 它们作为抗菌药物制剂中的活性成分是有用的。
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公开(公告)号:US4201782A
公开(公告)日:1980-05-06
申请号:US936506
申请日:1978-08-24
申请人: Masayuki Narisada , Wataru Nagata
发明人: Masayuki Narisada , Wataru Nagata
IPC分类号: C07D505/06 , A61K31/535 , A61K31/5365 , A61P31/00 , A61P31/04 , C07D505/00 , C07D505/20 , A61K31/41 , C07D413/02 , C07D413/14
CPC分类号: C07D505/00
摘要: Antibacterial 7.beta.-arylmalonamido-7.alpha.-methoxy-3-optionally alkylated thiadiazolylthiomethyl-1-oxadothiacephalosporins of the following formula: ##STR1## (wherein Ar is 2-thienyl, 3-thienyl, phenyl, p-hydroxyphenyl, p-acyloxyphenyl or p-protected hydroxyphenyl;COB.sup.1 and COB.sup.2 each is carboxy, protected carboxy or a carboxylate salt; andR is hydrogen or lower alkyl),processes for preparing said compounds, a pharmaceutical or veterinary composition comprising the said compounds and pharmaceutical carrier and a method for treating or preventing human or veterinary infectious diseases comprising administering the said compound.
摘要翻译: 具有下式的抗菌7β-芳基丙酰胺基-7α-甲氧基-3-任选的烷基化噻二唑基硫代甲基-1-氧代硫代头孢菌素:其中Ar是2-噻吩基,3-噻吩基,苯基,对羟基苯基,对 - 酰氧基苯基或 对保护的羟基苯基; COB1和COB2各自为羧基,保护的羧基或羧酸盐; R为氢或低级烷基),制备所述化合物的方法,包含所述化合物和药物载体的药物或兽医组合物和 治疗或预防人或兽医感染性疾病,包括给予所述化合物。
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公开(公告)号:US4197402A
公开(公告)日:1980-04-08
申请号:US15180
申请日:1979-02-26
申请人: Yoshio Hamashima , Wataru Nagata
发明人: Yoshio Hamashima , Wataru Nagata
IPC分类号: C07D505/00 , C07D498/00
CPC分类号: C07D505/00
摘要: 1-Oxa-cephalosporin analogues of the formula: ##STR1## [wherein X is 3-thienylmalonyl, phenylmalonyl, 4-hydroxyphenylmalonyl, or 2-fluoro-4-hydroxyphenylmalonyl;Y is hydrogen or methoxy; andR is hydrogen, alkali metal, or alkaline earth metal]and the preparation thereof.
摘要翻译: 具有下式的1-氧杂 - 头孢菌素类似物:其中X是3-噻吩基丙二酰基,苯基丙二酸,4-羟基苯基丙二酸或2-氟-4-羟基苯基丙二酰基; Y是氢或甲氧基; 和R是氢,碱金属或碱土金属]及其制备。
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公开(公告)号:US4180571A
公开(公告)日:1979-12-25
申请号:US959784
申请日:1978-11-13
申请人: Masayuki Narisada , Wataru Nagata
发明人: Masayuki Narisada , Wataru Nagata
IPC分类号: A61K31/535 , C07D205/00 , C07D265/00 , C07D498/04 , C07D505/00 , A61K31/41 , C07D498/00
CPC分类号: A61K31/535 , C07D205/00 , C07D265/00 , C07D498/04 , C07D505/00
摘要: Antibacterial 1-oxadethiacephalosporins of the formula: ##STR1## [wherein Ar is ##STR2## (in which Acyl is organic or inorganic acyl); COB.sup.1 and COB.sup.2 each is carboxy or protected carboxy;Het is ##STR3## (in which COB.sup.3 is carboxy or protected carboxy); and Y is hydrogen or methoxy;and when COB.sup.1, COB.sup.2, and/or COB.sup.3 is carboxy, pharmaceutically acceptable salts thereof are included, but with a proviso that when Y is methoxy, Het is ##STR4## a pharmaceutical or veterinary composition comprising the said 1-oxadethiacephalosporins and pharmaceutical carrier, and a method for treating or preventing human or veterinary infectious diseases comprising administering the said 1-oxadethiacephalosporin.
摘要翻译: 下式的抗菌1-恶二硫醚孢子:其中Ar是有机或无机酰基;其中Ar是有机或无机酰基; COB1和COB2各自为羧基或被保护的羧基; Het是
(其中COB 3是羧基或被保护的羧基); Y为氢或甲氧基; 并且当COB1,COB2和/或COB3为羧基时,包括其药学上可接受的盐,但条件是当Y为甲氧基时,Het为包含所述1-恶二硫醚类和药物载体的药物或兽用组合物, 以及用于治疗或预防人或兽传染性疾病的方法,包括施用所述1-恶二硫醚类。 -
公开(公告)号:US4254119A
公开(公告)日:1981-03-03
申请号:US74811
申请日:1979-09-11
申请人: Yoshio Hamashima , Wataru Nagata
发明人: Yoshio Hamashima , Wataru Nagata
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D501/20
CPC分类号: C07D277/587 , Y02P20/55
摘要: Antibacterial compounds represented by the following formula including their pharmaceutically acceptable salts and esters; process for preparing them; pharmaceutical preparation comprising them; and method for combating infections by administering them: ##STR1## (wherein Hal is halogen;R.sup.1 is hydrogen or an amino-protecting group;R.sup.2 is alkyl; andR.sup.3 is hydrogen or a carboxy-protecting group.)
摘要翻译: 由下式表示的抗菌化合物包括其药学上可接受的盐和酯; 准备工作的过程; 包含它们的药物制剂; 以及通过施用它们来对抗感染的方法:其中Hal是卤素; R1是氢或氨基保护基; R2是烷基; R3是氢或羧基保护基。
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公开(公告)号:US4705852A
公开(公告)日:1987-11-10
申请号:US876976
申请日:1986-06-20
申请人: Wataru Nagata , Tsutomu Aoki , Yasuhiro Nishitani
发明人: Wataru Nagata , Tsutomu Aoki , Yasuhiro Nishitani
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36 , C07D501/57 , C07D505/00 , C07D205/08 , A61K31/535
CPC分类号: C07D505/00 , Y02P20/55
摘要: An antibacterial cephalosporin hydroxamic acid derivative represented by the following formula (I), processes for its preparation, compositions containing the same as an active ingredient, and a method for killing bacteria by contacting with said compound. ##STR1## (wherein, R is acyl; R.sup.1 is hydrogen or methoxy; R.sup.2 is alkylene; R.sup.3 is hydrogen, aliphatic group or a hydroxy-protecting group; R.sup.4 is hydrogen or amino-protecting group; R.sup.5 is hydrogen, light metal atom or carboxy-protecting group; and X is oxygen, sulfur, or sulfinyl).
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