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    • 8. 发明授权
    • Caphalosporin compounds having at position-7 an .alpha.-etherified
hydroxyiminoarylacetamido group
    • 在位置-7处具有α-乙酰化羟基亚氨基芳基乙酰胺基的咖啡糊精化合物
    • US4208517A
    • 1980-06-17
    • US855080
    • 1977-11-28
    • Michael W. FoxtonGordon I. GregoryDavid M. Rogers
    • Michael W. FoxtonGordon I. GregoryDavid M. Rogers
    • C07D307/54C07D501/32C07D501/34A61K31/545
    • C07D307/54
    • 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 wth the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; R.sup.c and R.sup.d, which may be the same or different, each represents a hydrogen atom or a substituting group e.g. an alkyl group or substituted alkyl group; or R.sup.c and R.sup.d together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring which contains 5-7 ring members and which may contain additional hetero atoms, and may be substituted by lower alkyl; R.sup.e represents hydrogen or C.sub.1-4 alkyl; m and n are each 0 or 1 such that the sum of m and n is 0 or 1 and Y is selected from various oxygen and sulphur nucleophiles] and non-toxic derivatives thereof.
    • 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, 或者R a和R b一起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; R c和R d可以相同或不同,表示氢原子或取代基团。 烷基或取代的烷基; 或Rc和Rd与它们所连接的氮原子一起形成饱和或不饱和的杂环,其含有5-7个环成员并且可以含有另外的杂原子,并且可以被低级烷基取代; Re表示氢或C 1-4烷基; m和n各自为0或1,使得m和n的和为0或1,Y选自各种氧和硫亲核试剂]及其无毒的衍生物。
    • 10. 发明授权
    • 7 2-(Aminocarbonylalkoxyimino)acetamido! derivatives of cephalosporin
    • 7 {8 2-(氨基羰基烷氧基亚氨基)乙酰氨基{9 {头孢菌素衍生物
    • US4074047A
    • 1978-02-14
    • US694465
    • 1976-06-09
    • Michael W. FoxtonGordon I. GregoryDavid M. Rogers
    • Michael W. FoxtonGordon I. GregoryDavid M. Rogers
    • A61K31/545A61K31/546A61P31/04C07D307/54C07D333/24C07D501/20C07D501/26C07D501/32C07D501/34
    • C07D501/20C07D307/54C07D333/24
    • Cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## (WHERE R is phenyl, thienyl or furyl; R.sup.a and R.sup.b 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, aminocarbonyl, N-substituted aminocarbonyl 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; R.sup.c is hydrogen or C.sub.1-4 alkyl; and m and n are each 0 or 1 such that the sum of m and n is 0 or 1) exhibit broad spectrum antibiotic activity characterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases. The compounds, which are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer, have particularly good activity against Proteus organisms including indole positive strains and, especially when both R.sup.a and R.sup.b are other than hydrogen, against Pseudomonas organisms.
    • 头孢菌素抗生素,其中7β-酰胺基具有结构(其中R是苯基,噻吩基或呋喃基; R a和R b各自选自氢,C 1-4烷基,C 2-4链烯基,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,氨基羰基,N-取代的氨基羰基和氰基,或者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; R c是 氢或C 1-4烷基; m和n各自为0或1,使得m和n的和为0或1)表现出广谱抗生素活性,其特征在于对革兰氏阴性微生物特别高的活性,包括产生β- 内酰胺酶 作为syn异构体的化合物或含有至少90%的顺式异构体的合成和反异构体的混合物的化合物对包括吲哚阳性菌株在内的变形杆菌生物具有特别好的活性,特别是当Ra和Rb都不是氢时, 针对假单胞菌生物。