Cephalosporins
    2.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号:US4880795A

    公开(公告)日:1989-11-14

    申请号:US21293

    申请日:1987-03-03

    IPC分类号: A61K31/545 C07D501/46

    CPC分类号: C07D501/46

    摘要: Novel cephalosporins of the formula ##STR1## in which R.sup.1 is an aliphatic or cycloaliphatic hydrocarbyl radical of up to 6 carbon atoms which is optionally substituted by a carboxyl group, ##STR2## R.sup.2 and R.sup.3 each independently is an optionally substituted aliphatic or cycloaliphatic hydrocarbyl radical of up to 6 carbon atoms, but is not unsubstituted methyl,or pharmaceutically acceptable salts thereof, are effective antibacterially and promote the growth of animals.

    摘要翻译: 式(IMAGE)的新型头孢菌素,其中R 1是至多6个碳原子的脂族或脂环族烃基,任选被羧基取代,R 2和R 3各自独立地是任选取代的 最多6个碳原子的脂族或脂环族烃基,但不是未取代的甲基或其药学上可接受的盐是有效的抗菌活性并促进动物的生长。

    Cephalosporins
    3.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号:US4626535A

    公开(公告)日:1986-12-02

    申请号:US566975

    申请日:1983-12-30

    CPC分类号: C07D285/08 C07D417/06

    摘要: Novel antibacterially active cephalosporins of the formula ##STR1## in which R.sup.1 denotes hydrogen, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, a polycyclic aromatic ring or an optionally substituted heterocyclic 5- or 6-member ring having 1-4 heteroatoms,R.sup.2 represents hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkenyl, halogen, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, hydroxymethyl, formyloxymethyl, C.sub.1 -C.sub.4 -alkylcarbonyloxymethyl, aminocarbonyloxymethyl, pyridiniummethyl, 4-carbamoylpyridiniummethyl, 4-sulphonylethylpyridiniummethyl, 4-carboxylmethylpyridiniummethyl or heterocyclylthiomethyl, heterocyclyl representing a radical of the formula ##STR2## wherein R.sup.8 denotes hydrogen, methyl, 2-dimethylaminoethyl, carboxymethyl, sulphomethyl, carboxyethyl or sulphoethyl andR.sup.9 denotes hydrogen or methyl,or pharmaceutically tolerated salts or esters thereof.

    摘要翻译: 式中,R1表示氢,任选取代的烷基,取代或未取代的苯基环,多环芳环或具有1-4个杂原子的任选取代的杂环的5-或6-元环的新型抗菌活性头孢菌素,R2 表示氢,C 1 -C 4 - 烷基,C 1 -C 4 - 烯基,卤素,C 1 -C 4 - 烷氧基,C 1 -C 4 - 烷硫基,羟甲基,甲酰氧基甲基,C 1 -C 4 - 烷基羰氧基甲基,氨基羰基氧基甲基,吡啶鎓甲基,4-氨基甲酰基吡啶鎓甲基,4-磺基乙基吡啶鎓甲基 ,4-羧基甲基吡啶鎓甲基或杂环硫基甲基,代表下式基团的杂环基,其中R8表示氢,甲基,2-二甲基氨基乙基,羧甲基,磺基甲基,羧乙基或磺基,R9表示氢或甲基, 或其药学上可耐受的盐或酯。

    Cephalosporins
    5.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号:US4767754A

    公开(公告)日:1988-08-30

    申请号:US926027

    申请日:1986-10-30

    CPC分类号: C07D501/46

    摘要: Antibacterially effective cephalosporins of the formula ##STR1## in which R.sup.1 denotes C.sub.1 -C.sub.6 -alkyl, phenyl or halogen-substituted phenyl andA represents a nitrogen-containing, positively charged heterocyclic 5-membered to 7-membered ring which is bonded via N and can contain a total of up to 4 hetero-atoms from the group comprising N, O and S, and onto which up to two further rings can be fused, and which can optionally be substituted, with the proviso that, if the ring is a 6-membered ring, A does not represent an unsubstituted pyridine ring or a pyridine ring which is mono- or di-substituted by identical or different substituents from the group comprising C.sub.1 -C.sub.4 -alkyl, chlorine, bromine, carbamoyl or N-C.sub.1 -C.sub.4 -alkylcarbamoyl, or pharmaceutically acceptable salts thereof or esters thereof which can be split under physiological conditions.

    摘要翻译: 式中,R1表示C1-C6-烷基,苯基或卤素取代的苯基,A表示通过N键合的含氮带正电的杂环的5元至7元环,其具有式“IMAGE”的抗菌有效头孢菌素 可以包含总共多达4个来自包含N,O和S的基团的杂原子,并且其上可以稠合至多两个另外的环,并且其可以任选地被取代,条件是如果环是 6元环,A不表示未被取代的吡啶环或吡啶环,其被包含C 1 -C 4 - 烷基,氯,溴,氨基甲酰基或N-C 1 -C 6烷基的相同或不同取代基单取代或二取代 C4-烷基氨基甲酰基,或其药学上可接受的盐或其酯,其可在生理条件下分裂。

    Novel .beta.-lactam antibiotics
    7.
    发明授权
    Novel .beta.-lactam antibiotics 失效
    新型β-内酰胺抗生素

    公开(公告)号:US4632918A

    公开(公告)日:1986-12-30

    申请号:US730979

    申请日:1985-05-06

    CPC分类号: C07D501/46 C07D501/18

    摘要: Novel .beta.-lactam antibiotics of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3, which may be identical or different, denote a substituted or unsubstituted alkyl radical or a monocyclic or bicyclic, optionally substituted, carbocyclic or heterocyclic ring, orR.sup.1 represents an optionally substituted alkyl radical or a monocyclic or bicyclic, substituted or unsubstituted, carbocyclic or heterocyclic ring, andR.sup.2 and R.sup.3, together with the N.sup..sym. atom, form an optionally substituted monocyclic or polycyclic ring which can be saturated or unsaturated and can contain oxygen, sulphur and nitrogen as other hetero atoms, orR.sup.1, R.sup.2 and R.sup.3, together with the N.sup..sym. atom, form a bridged, optionally substituted polycyclic ring which can be saturated or unsaturated and can contain oxygen, sulphur and nitrogen as other hetero atoms, andR.sup.4 represents hydrogen or optionally substituted alkyl, aryl or heterocyclyl or hydroxycarbonyl, lower alkoxycarbonyl, halogen, pseudohalogen or a group of the formula ##STR2## in which n denotes 0, 1 or 2, andB represents a direct bond, oxygen or a group ##STR3## and A and W, independently of one another, represent hydrogen or optionally substituted alkyl, aryl or heterocyclyl, or together form an optionally substituted carbocyclic or heterocyclic ring.

    摘要翻译: 新颖的具有式“IMAGE”的β-内酰胺抗生素,其中R1,R2和R3可以相同或不同,表示取代或未取代的烷基或单环或双环,任选取代的碳环或杂环,或R 1表示 任选取代的烷基或单环或双环,取代或未取代的碳环或杂环,并且R 2和R 3与N(+)原子一起形成可以是饱和或不饱和的任选取代的单环或多环, 含有氧,硫和氮作为其它杂原子,或者R 1,R 2和R 3与N(+)原子一起形成可以是饱和或不饱和的并且可以含有氧,硫和氮的桥连的任选取代的多环, 其它杂原子,R 4表示氢或任选取代的烷基,芳基或杂环基或羟基羰基,低级烷氧基羰基,卤素,假卤素或式IMAG E>其中n表示0,1或2,B表示直接键,氧或基团,且A和W彼此独立地表示氢或任选取代的烷基,芳基或杂环基,或一起形成 任选取代的碳环或杂环。