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    Erythromycin a 11,12-carbonate 9-oxime derivatives
    3.
    发明授权
    Erythromycin a 11,12-carbonate 9-oxime derivatives 失效
    红霉素a 11,12-碳酸酯9-肟衍生物

    公开(公告)号：US4921839A

    公开(公告)日：1990-05-01

    申请号：US158543

    申请日：1988-02-22

    申请人： Edward G. Brain ,  Eric Hunt ,  Andrew K. Forrest

    发明人： Edward G. Brain ,  Eric Hunt ,  Andrew K. Forrest

    IPC分类号： C07H17/08

    CPC分类号： C07H17/08

    摘要： Antibacterially active 11,12-carbonate derivatives of erythromycin 9-(optionally substituted)oxime and 9-imino compounds and their pharmaceutically acceptable ester or acid addition salt thereof: ##STR1## wherein R.sup.1 denotes an oxime group, a substituted oxime group, or an imino group;R.sup.3 denotes a hydrogen atom or an unsubstituted or substituted alkyl group;R.sup.7 denotes hydrogen or methyl;one of R.sup.8 and R.sup.9 denotes hydrogen, hydroxy, alkoxy, alkanoyloxy, amino, substituted amino, or a group of the formula R.sup.A --SO.sub.2 --O--, in which R.sup.A denotes an organic group, and the other of R.sup.8 and R.sup.9 denotes hydrogen, orR.sup.8 and R.sup.9 together denote an oxo group, an oxime group, or a substituted oxime group.

    9,11-O-methylene derivatives of 9-dihydroerythromycin
    8.
    发明授权
    9,11-O-methylene derivatives of 9-dihydroerythromycin 失效
    9-二氢红霉素的9,11-O-亚甲基衍生物

    公开(公告)号：US4743593A

    公开(公告)日：1988-05-10

    申请号：US806026

    申请日：1985-12-06

    申请人： Eric Hunt

    发明人： Eric Hunt

    IPC分类号： C07H17/08 ,  A61K31/70

    CPC分类号： C07H17/08

    摘要： An antibacterially active 9,11-O-methylene derivative of 9-dihydroerythromycin wherein the methylene group is optionally substituted by one or two hydrocarbon groups. In particular, compounds of formula I and their pharmaceutically acceptable esters and acid addition salts: ##STR1## wherein: R.sup.1 and R.sup.2 are each H, optionally substituted hydrocarbon, or optionally substituted 5 or 6-membered O or S heterocyclyl, orR.sup.1 +R.sup.2 is optionally substituted divalent hydrocarbon,R.sup.3 is H or OH;R.sup.4 is H, F or OH;R.sup.5 and R.sup.6 are each H of CH.sub.3 ;one of R.sup.7 and R.sup.8 is H, OH, alkoxy, alkanoyloxy optionally substituted NH.sub.2, or R.sup.9 --SO.sub.2 --O--, and the other of R.sup.7 and R.sup.8 is H, orR.sup.7 +R.sup.8 is oxo, oxime or substituted oxime; and R.sup.9 is organic.

    摘要翻译： 9-二氢红霉素的抗菌活性9,11-O-亚甲基衍生物，其中亚甲基任选被一个或两个烃基取代。 特别地，式I化合物及其药学上可接受的酯和酸加成盐：其中：R 1和R 2各自为H，任选取代的烃，或任选取代的5或6元O或S杂环基，或R 1 + R2是任选取代的二价烃，R3是H或OH; R4是H，F或OH; R5和R6各自为CH3的H; R 7和R 8中的一个是H，OH，烷氧基，烷酰氧基任选取代的NH 2或R 9 -SO 2 -O-，R 7和R 8中的另一个是H，或者R 7 + R 8是氧代，肟或取代的肟; R9是有机的。

    Clavulanic acid derivatives their preparation and use
    9.
    发明授权
    Clavulanic acid derivatives their preparation and use 失效
    克拉维酸衍生物的制备和用途

    公开(公告)号：US4372946A

    公开(公告)日：1983-02-08

    申请号：US167378

    申请日：1980-07-09

    申请人： Thomas T. Howarth ,  Eric Hunt

    发明人： Thomas T. Howarth ,  Eric Hunt

    IPC分类号： C07C271/22 ,  C07D205/085 ,  C07D503/00 ,  A61K35/00

    CPC分类号： C07C271/22 ,  C07D205/085 ,  C07D503/00

    摘要： Compounds of the formula (I): ##STR1## and salts and esters thereof, wherein R.sub.1 is a hydrogen atom or a lower alkyl, aryl or aralkyl group, R.sub.2 and R.sub.3 are independently hydrogen, aryl, aralkyl, lower alkyl or substituted lower alkyl, or R.sub.3 is joined to R.sub.1 to form a 4-, 5-, or 6- membered ring or is joined to R.sub.2 to form a 5- or 6- membered ring with the proviso that when R.sub.2 is hydrogen, R.sub.1 is not hydrogen and R.sub.1 and R.sub.3 are not joined to form a group of the sub-formula (a) wherein R.sub.4 is a hydrogen atom or a NH.CO.R.sub.5 group wherein R.sub.5 is a lower alkyl, lower alkoxy lower alkyl, aryl, aralkyl, aryloxyalkyl; lower alkoxy or aryloxy group have .beta.-lactamase inhibitory and anti-bacterial properties.

    摘要翻译： 式（I）化合物：其中R 1为氢原子或低级烷基，芳基或芳烷基，R 2和R 3独立地为氢，芳基，芳烷基，低级烷基或 取代的低级烷基，或R 3与R 1连接形成4-，5-或6-元环，或连接至R 2以形成5-或6-元环，条件是当R 2为氢时，R 1为 不是氢并且R1和R3不连接形成一个子式（a）的基团，其中R4是氢原子或NH.CO.R5基团，其中R5是低级烷基，低级烷氧基低级烷基， 芳基，芳烷基，芳氧基烷基; 低级烷氧基或芳氧基具有β-内酰胺酶抑制和抗菌性质。

    Decarboxyclavulanic acid thio ethers, their preparation and use
    10.
    发明授权
    Decarboxyclavulanic acid thio ethers, their preparation and use 失效
    十二烷基硫酸钠，它们的制备和用途

    公开(公告)号：US4275067A

    公开(公告)日：1981-06-23

    申请号：US932489

    申请日：1978-08-10

    申请人： Eric Hunt

    发明人： Eric Hunt

    IPC分类号： A61K31/42 ,  A61P31/04 ,  A61P31/10 ,  C07D503/00 ,  C07D498/04

    CPC分类号： C07D503/00

    摘要： Compounds of the formula (II): ##STR1## wherein X is S, SO or SO.sub.2 ; and R is (a) an alkyl group of up to 4 carbon atoms, (b) an alkyl group of up to 4 carbon atoms substituted by an OR.sup.1, NHR.sup.1, NH.CO.R.sup.1 or CO.sub.2 R.sup.2 group wherein R.sup.1 is a hydrogen atoms, an alkyl group of up to 4 carbon atoms or benzyl group, and R.sup.2 is a moiety such that CO.sub.2 R.sup.2 is a carboxyl, salted carboxyl or esterified carboxyl group, (c) an aryl group or (d) an aralkyl group are useful for their anti-fungal and .beta.-lactamase inhibitory properties.

    摘要翻译： 式（II）的化合物：其中X是S，SO或SO 2; 并且R是（a）至多4个碳原子的烷基，（b）由OR 1，NHR 1，NH.CO.R 1或CO 2 R 2基团取代的至多4个碳原子的烷基，其中R 1是氢原子， 最多4个碳原子的烷基或苄基，R2是CO 2R2是羧基，盐化羧基或酯化羧基的部分，（c）芳基或（d）芳烷基可用于其抗 - 真菌和β-内酰胺酶抑制性质。