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154 条记录 (耗时 0.018 秒)

    Enteric coated oral dosage form
    64.
    发明授权
    Enteric coated oral dosage form 失效
    肠溶包衣口服剂型

    公开(公告)号：US4525339A

    公开(公告)日：1985-06-25

    申请号：US434452

    申请日：1982-10-15

    申请人： Charanjit Behl ,  George Beskid ,  Navnit Shah ,  Jacques Tossounian ,  Joel Unowsky

    发明人： Charanjit Behl ,  George Beskid ,  Navnit Shah ,  Jacques Tossounian ,  Joel Unowsky

    IPC分类号： C07D477/00 ,  A61K9/36 ,  A61K9/48 ,  A61K9/62 ,  A61K31/397 ,  A61K31/40 ,  A61K31/43 ,  A61K31/535 ,  A61K31/545 ,  A61K47/14 ,  A61K47/26 ,  C07D499/46 ,  C07D499/64 ,  C07D499/68 ,  C07D499/893 ,  C07D499/897

    CPC分类号： A61K47/14 ,  A61K31/40 ,  A61K31/43 ,  A61K31/545 ,  A61K9/4891

    摘要： There is presented a method, in the form of a dosage formulation, for transforming substantially orally inactive .beta.-lactam antibiotics or their pharmaceutically acceptable salts or the esters, ethers, or hydrates of said antibiotics or their salts into orally active compounds by combination of the chosen .beta.-lactam antibiotic with an enhancer comprising an aliphatic, preferably a C.sub.2 to C.sub.18, straight- or branched-chain, saturated or unsaturated, fatty acid or an aliphatic, preferably a C.sub.2 to C.sub.12, straight- or branched-chain, saturated or unsaturated, fatty acid mono-, di- or triglyceride or mixtures thereof, partial or total esters of propylene glycol, polyethylene glycol and carbohydrates of C.sub.2 to C.sub.12 fatty acids, as well as the pharmaceutically acceptable esters and ethers of said glycerides. The antibiotic and enhancer mixture may be administered orally as a solid dosage form with the .beta.-lactam antibiotic above or, optionally, with the enhancer protected by an enteric coating.

    摘要翻译： 呈现剂型制剂形式的方法，用于将基本上口服无活性的β-内酰胺抗生素或其药学上可接受的盐或所述抗生素或其盐的酯，醚或水合物转化为口服活性化合物，通过 选择的具有增强剂的β-内酰胺抗生素，其包含脂族，优选C2至C18直链或支链饱和或不饱和脂肪酸或脂族，优选C2至C12直链或支链饱和或 不饱和脂肪酸单 - ，二 - 或甘油三酸酯或其混合物，丙二醇，聚乙二醇和C2至C12脂肪酸的碳水化合物的部分或全部酯，以及所述甘油酯的药学上可接受的酯和醚。 抗生素和增强剂混合物可以作为固体剂型口服施用，其中β-内酰胺抗生素在上面，或任选地与由肠溶衣保护的增强剂一起使用。

    .beta.-Lactam antibiotics and their medicinal use
    67.
    发明授权
    .beta.-Lactam antibiotics and their medicinal use 失效
    β-内酰胺抗生素及其药用

    公开(公告)号：US4386089A

    公开(公告)日：1983-05-31

    申请号：US276762

    申请日：1981-06-24

    申请人： Hans-Bodo Konig ,  Karl G. Metzger ,  Michael Preiss

    发明人： Hans-Bodo Konig ,  Karl G. Metzger ,  Michael Preiss

    IPC分类号： C07D499/70 ,  A61K31/43 ,  A61P31/04 ,  C07D233/38 ,  C07D277/20 ,  C07D277/48 ,  C07D499/00 ,  C07D499/46 ,  C07D499/64 ,  C07D501/20 ,  C07D501/34 ,  C07D501/36 ,  A61K31/545

    CPC分类号： C07D277/20 ,  C07D233/38 ,  C07D277/48 ,  C07D499/00

    摘要： .beta.-Lactam compounds of the formula ##STR1## in which B denotes an optionally substituted heterocyclic 5-membered or 6-membered ring or an optionally substituted phenyl ring,Z denotes a hydrogen atom or a C.sub.1 to C.sub.4 alkoxy group, ##STR2## Y, E.sub.1 and E.sub.2 independently of one another denote a divalent organic radical andR.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently of one another denote a hydrogen atom or an alkyl, alkenyl, alkinyl, alkadienyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, aryl or heterocyclyl radical, it also being possible for the above-mentioned radicals, with the exception of hydrogen, to be substituted, or an acyl radical,are antibacterial agents with a broad antibacterial spectrum and are useful as agents for promoting growth and for improving feed utilization in animals and as antioxidants.

    摘要翻译： 式（I）的β-内酰胺化合物，其中B表示任选取代的杂环5元或6元环或任选取代的苯环，Z表示氢原子或C1至C4烷氧基， Y，E1和E2彼此独立地表示二价有机基团，R 1，R 2，R 3和R 4彼此独立地表示氢原子或烷基，烯基，炔基，链烯基，环烷基，环烯基 ，环链二烯基，芳基或杂环基，除了氢被取代以外，上述基团也可以是酰基，是具有广谱抗菌谱的抗菌剂，并且可用作促进生长的试剂 并提高动物和抗氧化剂的饲料利用率。

    2-Carbamoyloxymethyl-penicillin derivatives
    68.
    发明授权
    2-Carbamoyloxymethyl-penicillin derivatives 失效
    2-羧甲氧基甲基 - 青霉素衍生物

    公开(公告)号：US4322347A

    公开(公告)日：1982-03-30

    申请号：US893092

    申请日：1978-04-03

    申请人： Robert L. Cundall ,  Derek Walker

    发明人： Robert L. Cundall ,  Derek Walker

    IPC分类号： A61K31/43 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D499/00 ,  C07D499/21 ,  C07D499/42 ,  C07D499/44 ,  C07D499/46 ,  C07D499/60 ,  C07D499/64 ,  C07D499/68 ,  C07D499/74 ,  C07D499/76 ,  C07D499/78 ,  C07D499/80 ,  C07D501/14 ,  C07D501/18 ,  C07D501/22 ,  C07D501/59 ,  C07D519/06 ,  C07D499/32 ,  A61K31/38

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： Penicillin sulfoxide esters are reacted with an isocyanate to produce the corresponding (substituted)-2-carbamoyloxymethylpenam, the corresponding (substituted)-3-carbamoyloxycepham or the corresponding 3-methylcephem. The 6- or 7-side-chain of these products may be cleaved to give the corresponding 6-amino (penams) or 7-amino (cephams and cephems) compounds, and the latter may be reacylated to produce different 6-acyl-2-carbamoyloxymethyl penams, 7-acyl-3-carbamoyloxy cephams and 7-acyl-3-methylcephems. The substituent groups may be removed from the (substituted)-2-carbamoyloxypenams or the (substituted)-3-carbamoyloxycephams to give the corresponding free 2-carbamoyloxymethylpenams or 3-carbamoyloxycephams, respectively.

    摘要翻译： 将青霉素亚砜酯与异氰酸酯反应以产生相应的（取代的）-2-氨基甲酰氧基甲基氨基钠，相应的（取代的）-3-氨基甲酰氧基头孢烯或相应的3-甲基头孢烯。 这些产物的6-或7-侧链可能被切割，得到相应的6-氨基（半阴离子）或7-氨基（cephams和cephems）化合物，后者可以被再酰化以产生不同的6-酰基-2 - 氨基甲酰氧基甲基半阴离子，7-酰基-3-氨基甲酰氧基Cephams和7-酰基-3-甲基头孢烯。 取代基可以从（取代的）-2-氨基甲酰氧基草酸或（取代的）-3-氨基甲酰氧基头孢中除去，分别得到相应的游离的2-氨基甲酰氧基甲基氨基或3-氨基甲酰氧基头孢。

    6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acid, antibacterial compositions thereof and method of use thereof
    69.
    发明授权
    6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acid, antibacterial compositions thereof and method of use thereof 失效
    6-氨基螺[penam-2,4'-哌啶] -3-羧酸，其抗菌组合物及其使用方法

    公开(公告)号：US4271173A

    公开(公告)日：1981-06-02

    申请号：US162615

    申请日：1980-06-24

    申请人： Ludovic Rodriguez ,  Jacques Leclercq ,  Pierre Ykman ,  Eric Cossement

    发明人： Ludovic Rodriguez ,  Jacques Leclercq ,  Pierre Ykman ,  Eric Cossement

    IPC分类号： C07D499/46 ,  A61K31/43 ,  A61K31/431 ,  A61P31/04 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/74 ,  C07D499/76 ,  C07D499/80 ,  C07D499/90 ,  C07D499/32 ,  A61K31/425

    CPC分类号： C07D499/00

    摘要： 6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acid derivatives having the formula ##STR1## wherein R is a methyl, phenyl or benzyl radical, Z.sub.1 is a hydrogen atom and Z.sub.2 is a radical selected from those known from penicillin chemistry and is preferably a 2-phenylacetyl, 2-amino-2-phenylacetyl, 5-methyl-3-phenyl-4-isoxazolecarbonyl or 2,6-dimethoxybenzoyl radical, or Z.sub.1 and Z.sub.2 together represent a bivalent radical Z.sub.3 and preferably a (hexahydro-1H-azepin-1-yl)methylene radical, as well as the pharmaceutically acceptable non-toxic salts thereof and process for preparing the same.These compounds have valuable antibacterial properties and are useful as therapeutic agents in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria.

    摘要翻译： 6-氨基螺[penam-2,4'-哌啶] -3-羧酸衍生物，其结构式为：其中R为甲基，苯基或苄基，Z1为氢原子，Z2为选自 由青霉素化学已知的那些，优选2-苯基乙酰基，2-氨基-2-苯基乙酰基，5-甲基-3-苯基-4-异恶唑羰基或2,6-二甲氧基苯甲酰基，或Z 1和Z 2一起代表二价基团Z 3 并且优选为（六氢-1H-吖庚因-1-基）亚甲基，以及其药学上可接受的无毒盐及其制备方法。 这些化合物具有有价值的抗菌性质，可用作治疗由革兰氏阳性菌和革兰氏阴性菌引起的传染病的治疗剂。