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1. 发明授权

US4427675A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US4427675A
公开(公告)日：1984-01-24
申请号：US306729
申请日：1981-09-29
申请人： Barry E. Ayres , Cynthia H. O'Callaghan , David G. H. Livermore , Christopher E. Newall
发明人： Barry E. Ayres , Cynthia H. O'Callaghan , David G. H. Livermore , Christopher E. Newall
IPC分类号： A61K20060101 , A61K31/545 , A61K31/55 , C07D20060101 , C07D501/38 , C07D501/46 , C07D501/56
CPC分类号： C07D501/46
摘要： Cephalosporin antibiotics of general formula ##STR1## (wherein R.sup.a and R.sup.b, which may be the same or different, each represent a C.sub.1-4 alkyl group, or together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene group). These compounds exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms.Particularly effective compounds of formula (I) are (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimino)acetamio]-3-(pyridazinium-1-ylmethyl)ceph-3-em-4-carboxylate and (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(t-carboxycyclobut-1-oxyimino)acetamido]-3-(pyridazinium-1-ylmethyl)ceph-3-em-4-carboxylate. The invention also includes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I), compositions containing the antibiotic compounds of the invention and a method of combatting bacterial infection utilizing the antibiotics.
摘要翻译：通式（I）（I）的头孢菌素抗生素（其中可以相同或不同的R a和R b各自表示C 1-4烷基，或与它们所连接的碳原子一起形成C3-7 环亚烷基）。这些化合物表现出广谱抗生素活性，对于革兰氏阴性生物体如假单胞菌属生物菌株，其活性异常高。特别有效的式（I）化合物是（6R，7R）-7 - [（Z）-2-（2-氨基噻唑-4-基）-2-（2-羧基-2-氧亚氨基）乙酰胺] -3 - （哒嗪鎓-1-基甲基）头孢-3-烯-4-羧酸酯和（6R，7R）-7 - [（Z）-2-（2-氨基噻唑-4-基）-2-（叔 - 羧基环 - -1-乙酰氨基）乙酰氨基] -3-（哒嗪鎓-1-基甲基）头孢-3-烯-4-羧酸酯。本发明还包括式（I）化合物的无毒盐和无毒代谢不稳定酯，含有本发明抗生素化合物的组合物和利用抗生素对抗细菌感染的方法。

2. 发明授权

US4621081A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US4621081A
公开(公告)日：1986-11-04
申请号：US423555
申请日：1982-09-27
申请人： Cynthia H. O'Callaghan , Barry E. Ayres , David G. H. Livermore , Christopher E. Newall , Niall G. Weir
发明人： Cynthia H. O'Callaghan , Barry E. Ayres , David G. H. Livermore , Christopher E. Newall , Niall G. Weir
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D501/24 , C07D501/36
CPC分类号： C07D277/20 , C07D277/587
摘要： Cephalosporin antibiotics of general formula: ##STR1## (wherein R.sup.a and R.sup.b, which may be the same or different, each represent a C.sub.1-4 alkyl group or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene group, and Y.sup..sym. represents a C-linked 5- or 6-membered heterocyclic ring containing at least one C.sub.1-4 alkyl-substituted quaternary nitrogen atom, which ring may also contain one or more sulphur atoms) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms.A particular antibiotic compound of formula (I) possessing excellent antibacterial activity against strains of Pseudomonas organisms, as well as other valuable therapeutic properties, is (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxycyclobut-1-oxyimino)acetamido]-3-[(1-methylpyridinium-4-yl)-thiomethyl]ceph-3-em-4-carboxylate. The invention also includes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I). Also described are compositions containing the antibiotics of the invention and processes for the preparation of the antibiotics.
摘要翻译：具有以下通式的头孢菌素抗生素：其中可以相同或不同的R a和R b各自代表C 1-4烷基或R a和R b与它们所连接的碳原子一起形成 C 3-7亚环烷基，Y（+）表示含有至少一个C 1-4烷基取代的季氮原子的C连接的5-或6-元杂环，该环也可含有一个或多个硫原子）广谱抗生素活性，对革兰氏阴性生物体（如假单胞菌属生物菌株）的活性异常高。（6R，7R）-7 - [（Z）-2-（2-氨基噻唑-4-基） - 苯并噻唑-4-基] - 对于具有优异的抗假单胞菌菌株抗菌活性的其它有价值的治疗性质的式（I）吡啶-4-基）-2-（1-羧基环丁-1-氧亚氨基）乙酰氨基] -3 - [（1-甲基吡啶鎓-4-基） - 硫代甲基]环丙-3-烯-4-羧酸甲酯。本发明还包括式（I）化合物的无毒盐和无毒代谢不稳定的酯。还描述了含有本发明的抗生素和制备抗生素的方法的组合物。

3. 发明授权

US4464368A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US4464368A
公开(公告)日：1984-08-07
申请号：US285966
申请日：1981-07-23
申请人： Cynthia H. O'Callaghan , Barry E. Ayres , Christopher E. Newall , David G. H. Livermore , Derek R. Sutherland
发明人： Cynthia H. O'Callaghan , Barry E. Ayres , Christopher E. Newall , David G. H. Livermore , Derek R. Sutherland
IPC分类号： C07D277/20 , C07D501/46 , C07D501/38 , A61K31/425
CPC分类号： C07D277/587
摘要： Cephalosporin antibiotics of general formula ##STR1## (wherein R.sup.a and R.sup.b, which may be the same or different, each represent a C.sub.1-4 alkyl group, or together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene group and R.sup.1 represents a C.sub.1-4 alkyl group) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms.Particularly effective compounds of formula (I) are (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimino)acetamido]-3-(2-methylpyrazolium-1-ylmethyl)ceph-3-em-4-carboxylate and (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-[(1-carboxycyclobut-1-oxyimino)acetamido]-3-(2-methylpyrazolium-1-ylmethyl)]ceph-3-em-4-carboxylate. The invention also includes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I), compositions containing the antibiotic compounds of the invention, and methods for combatting bacterial infections utilizing the antibiotics.
摘要翻译：通式（I）（I）的头孢菌素抗生素（其中可以相同或不同的R a和R b各自表示C 1-4烷基，或与它们所连接的碳原子一起形成C3-7 环烷叉基，R 1表示C 1-4烷基）表现出广谱抗生素活性，对革兰氏阴性生物如假单胞菌属生物体的活性异常高。特别有效的式（I）化合物是（6R，7R）-7 - [（Z）-2-（2-氨基噻唑-4-基）-2-（2-羧基-2-氧亚氨基）乙酰氨基] -3 - （2-甲基吡唑-1-基甲基）头孢-3-烯-4-羧酸酯和（6R，7R）-7 - [（Z）-2-（2-氨基噻唑-4-基）-2 - [（1 - 羧基环丁-1-氧基咪唑o）乙酰氨基] -3-（2-甲基吡唑鎓-1-基甲基）]头孢-3-烯-4-羧酸乙酯。本发明还包括式（I）化合物的无毒盐和无毒代谢不稳定的酯，含有本发明的抗生素化合物的组合物，以及利用抗生素对抗细菌感染的方法。

4. 发明授权

US4504477A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US4504477A
公开(公告)日：1985-03-12
申请号：US285492
申请日：1981-07-21
申请人： Cynthia H. O'Callaghan , Barry E. Ayres , David G. H. Livermore , Christopher E. Newall , Niall G. Weir
发明人： Cynthia H. O'Callaghan , Barry E. Ayres , David G. H. Livermore , Christopher E. Newall , Niall G. Weir
IPC分类号： C07D501/56 , A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/36 , C07D501/46
CPC分类号： C07D501/36
摘要： Cephalosporin antibiotics of general formula ##STR1## (wherein Y.sup..sym. represents a C-attached 1-C.sub.1-4 alkylpyridinium group) exhibit broad spectrum antibiotic activity with unusually high activity against strains of Pseudomonas organisms as well as high activity against various members of the Enterobacteriaceae. The invention also includes the non-toxic salts, non-toxic metabolically labile esters and 1-oxides of compounds of formula (I). Also described are compositions containing the antibiotics of the invention and processes for the preparation of the antibiotics.
摘要翻译：具有通式（I）（其中Y（+）表示C-连接的1-C 1-4烷基吡啶基）的头孢菌素抗生素表现出广谱抗生素活性，对假单胞菌生物体的菌株具有异常高的活性，以及对各种肠杆菌科的成员。本发明还包括式（I）化合物的无毒盐，无毒代谢不稳定的酯和1-氧化物。还描述了含有本发明的抗生素和制备抗生素的方法的组合物。

5. 发明授权

US4168309A Cephalosporins having a 7-(carboxy substituted .alpha.-etherified oximinoarylacetamido) group 失效
标题翻译：头孢菌素具有7-（羧基取代的{60-乙酰肟基芳基乙酰胺基）基团
公开(公告)号：US4168309A
公开(公告)日：1979-09-18
申请号：US838366
申请日：1977-09-30
申请人： Barry E. Ayres
发明人： Barry E. Ayres
IPC分类号： C07D501/44 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/38 , C07D501/40 , C07D501/46 , C07D501/60
CPC分类号： C07D501/38
摘要： Antibiotic compounds of the general formula ##STR1## [wherein R is a phenyl, thienyl or furyl group; R.sup.a and R.sup.b which may be the same or different, are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl and cyano, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; m or n are each 0 or 1 such that the sum of m and n is 0 or 1; and R.sup.1 together with the nitrogen atom to which it is attached form a saturated or partially saturated 4-10 membered heterocyclic ring which may contain one or more further heteroatoms selected from 0,N and S and which may be substituted by a lower alkyl, lower alkoxy, lower acyloxy, lower alkoxycarbonyl, hydroxy, carboxy, amino, acylamino, substituted or unsubstituted carbamoyl or aryl group, or such a heterocyclic ring fused with a benzene ring] and non-toxic derivatives thereof, the compounds being syn isomers or existing as mixtures of syn and anti isomers.
摘要翻译：通式（I）的抗生素化合物[其中R是苯基，噻吩基或呋喃基; R a和R b可以相同或不同，各自选自氢，C 1-4烷基，C 2-4烯基，C 3-7环烷基，苯基，萘基，噻吩基，呋喃基，羧基，C 2-5烷氧基羰基和氰基，或 R a和R b与它们所连接的碳原子一起形成C 3-7亚环烷基或亚环烯基; m或n各自为0或1，使得m和n的和为0或1; 并且R 1与其连接的氮原子一起形成饱和或部分饱和的4-10元杂环，其可以含有一个或多个另外的选自O，N和S的杂原子，并且其可以被低级烷基取代，低级烷基烷氧基，低级酰氧基，低级烷氧基羰基，羟基，羧基，氨基，酰氨基，取代或未取代的氨基甲酰基或芳基，或与苯环稠合的杂环]及其无毒衍生物，所述化合物为顺式异构体或存在顺式和反式异构体的混合物。

6. 发明授权

US4985407A Dipeptide compounds, processes for their preparation and compositions containing them 失效
标题翻译：二肽化合物，其制备方法和含有它们的组合物
公开(公告)号：US4985407A
公开(公告)日：1991-01-15
申请号：US280330
申请日：1988-12-06
申请人： Michael W. Foxton , Barry E. Ayres , Anthony W. J. Cooper
发明人： Michael W. Foxton , Barry E. Ayres , Anthony W. J. Cooper
IPC分类号： C12N9/99 , A61K38/55 , A61P5/38 , A61P9/00 , A61P9/10 , A61P9/12 , A61P27/02 , A61P27/06 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81
CPC分类号： C07K5/0227 , C07K5/0207 , Y10S530/86
摘要： There are described new compounds of formula (1) ##STR1## wherein R.sup.1 represents an acyl group;X.sup.1 represents phenylalanine or p-methoxyphenylalanine bonded N-terminally to R.sup.1 and C-terminally to X.sup.2 ;X.sup.2 represents histidine or N-methylhistidine bonded N-terminally to X.sup.1 and C-terminally to the group --NH--;R.sup.2 represents a C.sub.4-6 cycloalkyl group;R.sup.3 represents a group CHR.sup.6 R.sup.7 is a hydrogen atom and R.sup.7 is a phenyl group, or R.sup.6 is a methyl group and R.sup.7 is a hydrogen atom or a methyl or ethyl group;X.sup.3 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl groups;R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or NR.sup.4 R.sup.5 may form a 5- or 6- membered polymethylenimine ring;and salts and solvates thereof.The new compounds have been found to exhibit activity as renin inhibitors, combining good duration of action with significant oral potency.Compositions containing the compounds of formula (1) and processes for preparing the compounds are also described.

7. 发明授权

US4315005A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US4315005A
公开(公告)日：1982-02-09
申请号：US132644
申请日：1980-03-21
申请人： Barry E. Ayres , Niall G. Weir
发明人： Barry E. Ayres , Niall G. Weir
IPC分类号： C07D213/20 , C07D501/36 , A61K31/545 , C07D501/56
CPC分类号： C07D213/20
摘要： Cephalosporin antibiotics of general formula ##STR1## (wherein R.sup.1 and R.sup.b, which may be the same or different, each represent a C.sub.1-2 alkyl group, or together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkylidene group and Y.sup..sym. represents a 1-carbamoylmethylpyridinium group) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms.Particularly effective compounds of formula (I) are (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimino)acetamido]-3-[(1-carbamoylmethylpyridinium-4-yl)thiomethyl]ceph-3-em-4-carboxylate and (6R,7R)-[(Z)-2-(2-aminothiazol-4-yl)-2-[(1-carboxycyclobut-1-oxyimino)acetamido]-3-[(1-carbamoylmethylpyridinium-4-yl)thiomethyl]-ceph-3-em-4-carboxylate. The invention also includes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I), compositions containing the antibiotic compounds of the invention and processes for the preparation of the antibiotics.
摘要翻译：通式为（IMA）（I）的头孢菌素抗生素（其中R 1和R b可以相同或不同，各自表示C1-2烷基，或与它们所连接的碳原子一起形成C 3-6 环亚烷基和Y（+）表示1-氨基甲酰基甲基吡啶基）表现出广谱抗生素活性，对革兰氏阴性生物如假单胞菌生物体的活性异常高。特别有效的式（I）化合物是（6R，7R）-7 - [（Z）-2-（2-氨基噻唑-4-基）-2-（2-羧基-2-氧亚氨基）乙酰氨基] -3 - [（1-氨基甲酰基甲基吡啶鎓-4-基）硫代甲基]头孢-3-烯-4-羧酸酯和（6R，7R） - [（Z）-2-（2-氨基噻唑-4-基）-2- [ （1-羧基环丁-1-氧亚氨基）乙酰氨基] -3 - [（1-氨基甲酰基甲基吡啶鎓-4-基）硫代甲基] - 头孢-3-烯-4-羧酸乙酯。本发明还包括式（I）化合物的无毒盐和无毒代谢不稳定的酯，含有本发明的抗生素化合物的组合物和制备抗生素的方法。

8. 发明授权

US5057496A Dipeptide compounds containing histidine or N-methyl histidine processes for their preparation and compositions containing them 失效
标题翻译：含有它们的制备和组合物的HISTIDINE或N-甲基苯乙烯过程的化合物
公开(公告)号：US5057496A
公开(公告)日：1991-10-15
申请号：US280495
申请日：1988-12-06
申请人： Peter C. Cherry , Michael W. Foxton , Barry E. Ayres , Andrew D. Searle
发明人： Peter C. Cherry , Michael W. Foxton , Barry E. Ayres , Andrew D. Searle
IPC分类号： C12N9/99 , A61K38/55 , A61P5/38 , A61P9/00 , A61P9/10 , A61P9/12 , A61P27/02 , A61P27/06 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81
CPC分类号： C07K5/0227 , C07K5/0207
摘要： There are described new compounds of formula (1) ##STR1## wherein R.sup.1 represents an acyl group;X.sup.1 represents phenylalanine or p-methoxyphenylalanine bonded N-terminally to R.sup.1 and C-terminally to X.sup.2 ;X.sup.2 represents histidine or N-methylhistidine bonded N-terminally to X.sup.1 and C-terminally to the group --NH--;R.sup.2 represents a C.sub.4-6 cycloalkyl group;R.sup.3 represents a group CHR.sup.6 R.sup.7 (where R.sup.6 is a hydrogen atom or a hydroxyl group and R.sup.7 is a pyridinyl ring);X.sup.3 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl groups;R.sup.4, and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or NR.sup.4 R.sup.5 may form a 5- or 6- membered polymethylenimine ring;and salts and solvates thereof.The new compounds have been found to exhibit activity as renin inhibitors, combining good duration of action with significant oral potency.Compositions containing the compounds of formula (1) and processes for preparing the compounds are also described.

9. 发明授权

US4192871A Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US4192871A
公开(公告)日：1980-03-11
申请号：US907915
申请日：1978-05-22
申请人： Gordon H. Phillipps , Peter J. May , Barry E. Ayres
发明人： Gordon H. Phillipps , Peter J. May , Barry E. Ayres
IPC分类号： C07J3/00 , C07J5/00 , C07J7/00 , C07J13/00 , C07J17/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J63/00 , C07J71/00
CPC分类号： C07J13/005 , C07J17/00 , C07J3/005 , C07J31/006 , C07J41/0088 , C07J41/0094 , C07J43/003 , C07J5/0015 , C07J63/00 , C07J7/003 , C07J71/001
摘要： Pregnanes and androstanes are described which essentially possess a 3.alpha.-hydroxy group, a 5.alpha.-hydrogen atom or a 4.5- or 5,6-double bond, a 17.alpha.-hydrogen atom and an 11.beta.-aminoester group. Other optional substituents or double bonds may be present. The compounds have anaesthetic activity.
摘要翻译：描述了基本上具有3α-羟基，5α-氢原子或4.5-或5,6-双键，17α-氢原子和11β-氨基酯基团的孕烷和雄甾烷基。可以存在其它任选的取代基或双键。该化合物具有麻醉活性。

10. 发明授权

US4132849A Process for the preparation of 3-hydroxymethyl cephalosporins 失效
标题翻译： 3-羟甲基头孢菌素的制备方法
公开(公告)号：US4132849A
公开(公告)日：1979-01-02
申请号：US840249
申请日：1977-10-07
申请人： Barry E. Ayres
发明人： Barry E. Ayres
IPC分类号： C07D20060101 , C07D501/04 , C07D501/26 , C07D501/60
CPC分类号： C07D501/04
摘要： A process for the preparation of a 3-hydroxymethyl cephalosporin compound which comprises selectively hydrolyzing a 3-formyloxymethyl cephalosporin compound under acidic conditions in the presence of a protic solvent whereby a 3-hydroxymethyl cephalosporin is produced.
摘要翻译：一种制备3-羟甲基头孢菌素化合物的方法，其包括在酸性条件下在质子溶剂存在下选择性水解3-甲氧基甲基头孢菌素化合物，由此产生3-羟甲基头孢菌素。

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