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1. 发明授权

US4174318A Alkylative cleavage of azetidinone disulfides 失效
标题翻译：氮杂环丁烷二硫化物的烷基化裂解
公开(公告)号：US4174318A
公开(公告)日：1979-11-13
申请号：US726425
申请日：1976-09-22
申请人： Derek H. R. Barton , Peter G. Sammes , Graham Hewitt , Brian E. Looker , William G. E. Underwood
发明人： Derek H. R. Barton , Peter G. Sammes , Graham Hewitt , Brian E. Looker , William G. E. Underwood
IPC分类号： C07D205/095 , C07D499/00 , C07D205/08
CPC分类号： C07D499/00 , C07D205/095
摘要： Novel semisynthetic 4-thio-azetidin-2-one derivatives of use in the production of cephalosporins, penicillins and related .beta.-lactam antibiotic compounds are provided by cleavage reactions involving the corresponding 4-dithio-azetidin-2-one derivative or a suitable thiazoline derivative, which starting materials may be obtained from penicillins without changing the configuration of the .beta.-lactam structure desired in the final product.
摘要翻译：用于生产头孢菌素，青霉素和相关β-内酰胺抗生素化合物的新型半合成4-硫代 - 氮杂环丁烷-2-酮衍生物通过涉及相应的4-二硫代氮杂环丁-2-酮衍生物或合适的噻唑啉衍生物，其起始材料可以从青霉素获得，而不改变最终产物中所需的β-内酰胺结构的构型。

2. 发明授权

US4193917A Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US4193917A
公开(公告)日：1980-03-18
申请号：US713649
申请日：1976-08-12
申请人： Derek H. R. Barton , Alan G. Long , Brian E. Looker , Edward M. Wilson , William G. Elphinstone
发明人： Derek H. R. Barton , Alan G. Long , Brian E. Looker , Edward M. Wilson , William G. Elphinstone
IPC分类号： C07D205/095 , C07D205/06
CPC分类号： C07D205/095
摘要： Novel semisynthetic .beta.-lactam intermediates of use in the production of cephalosporins, penicillins and related .beta.-lactam antibiotic compounds are provided. The novel compounds are prepared from .beta.-lactams obtained by cleavage of the 1,2-sulphur-carbon bond of a penicillin 1-oxide (with subsequent internal or external trapping of the sulphur atom to leave a residual substituent as the .beta.-lactam nitrogen) by removal of the said residual substituent by an oxidative cleavage reaction.
摘要翻译：提供了用于生产头孢菌素，青霉素和相关β-内酰胺抗生素化合物的新型半合成β-内酰胺中间体。新化合物由通过切割青霉素1-氧化物的1,2-硫 - 碳键获得的β-内酰胺制备（随后硫原子的内部或外部捕获而留下残余取代基作为β-内酰胺氮）通过氧化裂解反应除去所述残留取代基。

3. 发明授权

US4665167A Manufacture of antibiotics 失效
公开(公告)号：US4665167A
公开(公告)日：1987-05-12
申请号：US666544
申请日：1984-10-30
申请人： Brian E. Looker
发明人： Brian E. Looker
IPC分类号： C07D277/20 , C07D277/40 , C07D277/42
CPC分类号： C07D277/587
摘要： The invention provides crystalline (Z)-2-(2-t-butoxycarbonyl-prop-2-oxyimino)-2-(2-triphenylmethylaminothiazol-4-yl)acetic acid in association with dioxan and its crystalline ethyl ester in association with methanol. The compounds are of value as intermediates in the preparation of .beta.-lactam antibiotics such as ceftazidime or azthreonam.

4. 发明授权

US4943631A Process for cephem compounds 失效
标题翻译：头孢烯化合物的方法
公开(公告)号：US4943631A
公开(公告)日：1990-07-24
申请号：US141192
申请日：1988-01-06
申请人： Brian E. Looker
发明人： Brian E. Looker
IPC分类号： A61K20060101 , A61K31/545 , C07D501/04 , C07D501/24 , C07D501/46
CPC分类号： C07D501/46 , Y02P20/55
摘要： The present invention provides compounds of general formula (III) ##STR1## [wherein R is an amino or protected amino group;R.sup.2a is a straight or branched chain alkyl group containing from 1 to 4 carbon atoms, an allyl, but-2-enyl or but-3-enyl group, or is a group of formula ##STR2## (wherein each of R.sup.3 and R.sup.4 is independently a hydrogen atom or a methyl or ethyl group, or R.sup.3 and R.sup.4 taken together with the carbon atom to which they are attached may be a cycloalkylidene group containing from 3 to 5 carbon atoms, and R.sup.5 is a hydrogen atom or a carboxyl blocking group);Y represents a 1-methyl-1-pyrrolidinium group andR.sup.7 represents the group --COO.sup.- or --COOR.sup.6, where R.sup.6 is a hydrogen atom or a carboxyl blocking group] and salts thereof.
摘要翻译：本发明提供通式（III）的化合物：其中R是氨基或被保护的氨基; R2a是含有1至4个碳原子的直链或支链烷基，烯丙基，丁-2-烯基或丁-3-烯基，或者是式（IMAGE）的基团（其中R3和R4各自为独立地是氢原子或甲基或乙基，或者R 3和R 4与它们所连接的碳原子一起可以是含有3至5个碳原子的亚环烷基，R5是氢原子或羧基封端基）; Y表示1-甲基-1-吡咯烷鎓基，R 7表示-COO-或-COOR 6基团，其中R 6表示氢原子或羧基封端基]及其盐。

5. 发明授权

US4497956A Manufacture of antibiotics 失效
公开(公告)号：US4497956A
公开(公告)日：1985-02-05
申请号：US441250
申请日：1982-11-12
申请人： Brian E. Looker
发明人： Brian E. Looker
IPC分类号： C07D277/20 , C07D277/40 , C07D277/42
CPC分类号： C07D277/587
摘要： The invention provides crystalline (Z)-2-(2-t-butoxycarbonyl-prop-2-oxyimino-2-(2-triphenylmethylaminothiazol-4-yl)acetic acid in association with dioxan and its crystalline ethyl ester in association with methanol. The compounds are of value as intermediates in the preparation of .beta.-lactam antibiotics such as ceftazidime or azthreonam.

6. 发明授权

US5043334A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US5043334A
公开(公告)日：1991-08-27
申请号：US441612
申请日：1989-11-27
申请人： Richard Bell , Michael W. Foxton , Brian E. Looker
发明人： Richard Bell , Michael W. Foxton , Brian E. Looker
IPC分类号： A61K31/545 , A61P31/04 , C07D277/20 , C07D501/20 , C07D501/24
CPC分类号： C07D277/587 , Y02P20/55
摘要： Compounds of general formula (I) ##STR1## (where R.sup.1 is a carboxyl group, a group COO.sup..crclbar. or a blocked carboxyl group;R.sup.2 is an amino or protected amino group; andR is hydrogen or a group of the formula CH.sub.2 X, where X represents a halogen atom, a hydroxyl group, an acetoxy group; a group of the formula O.CO.NHR.sup.3, where R.sup.3 is hydrogen, a C.sub.1-4 alkyl group optionally substituted by 1 to 3 halogen atoms or an N-protecting group; a group of the formula OR.sup.4, where R.sup.4 is a C.sub.1-4 alkyl group optionally substituted by halogen or a C.sub.1-4 alkoxy group; or a pyridinium, 3-carbamoyl-pyridinium or 4-carbamoyl-pyridinium group;B is --S-- or --SO-- (.alpha.- or .beta.-); and the dotted line bridging the 2-, 3- and 4- positions indicates that the compound is a ceph-2-em or ceph-3-em compound) and salts thereof, the compounds of formula (I) being associated with an anion when X represents a pyridinium, 3-carbamoylpyridinium group or a 4-carbamoylpyridinium group and R.sup.1 is other than COO.sup..crclbar.) are disclosed.Processes for their preparation and pharmaceutical compositions containing them are also disclosed.
摘要翻译：通式（I）的化合物（Ⅰ）（其中R1是羧基，COO（ - ）或封端羧基; R2是氨基或被保护的氨基; R是氢或一个式CH 2 X，其中X表示卤素原子，羟基，乙酰氧基;式O.CO.NHR 3的基团，其中R 3是氢，任选被1至3个卤素原子取代的C 1-4烷基或 N-保护基;式OR4的基团，其中R4是任选被卤素或C 1-4烷氧基取代的C 1-4烷基;或吡啶鎓，3-氨基甲酰基 - 吡啶鎓或4-氨基甲酰基 - 吡啶鎓基 ; B是-S-或-SO-（α-或β-）;桥接2-，3-和4-位的虚线表示该化合物是ceph-2-em或ceph-3-em 化合物）及其盐，当X表示吡啶鎓，3-氨基甲酰基吡啶鎓基或4-氨基甲酰基吡啶基且R 1不同于COO（ - ）时，式（I）的化合物与阴离子缔合。还公开了其制备方法和含有它们的药物组合物。

7. 发明授权

US4560683A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US4560683A
公开(公告)日：1985-12-24
申请号：US509043
申请日：1983-06-29
申请人： Brian E. Looker
发明人： Brian E. Looker
IPC分类号： C07D277/20 , C07D501/24 , C07D501/34 , A61K31/545
CPC分类号： C07D277/587
摘要： Cephalosporin antibiotics of general formula ##STR1## (wherein R.sup.1 represents a hydrogen atom or a methyl or 2-chloroethyl group) and non-toxic salts and non-toxic metabolically labile esters thereof. The compounds exhibit broad spectrum antibiotic activity and have high activity against both Gram-positive and Gram-negative organisms, including many .beta.-lactamase producing strains. Processes for the preparation of the compounds and pharmaceutical compositions containing them are described.
摘要翻译：通式为（IMA）（I）（其中R1表示氢原子或甲基或2-氯乙基）的头孢菌素抗生素及其无毒的盐和无毒的代谢不稳定的酯。该化合物表现出广谱抗生素活性，并且对革兰氏阳性和革兰氏阴性生物（包括许多β-内酰胺酶生产菌株）具有高活性。描述了制备化合物和含有它们的药物组合物的方法。

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