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    1-Carba(dethia)caphalosporin antibiotics
    1.
    发明公开
    1-Carba(dethia)caphalosporin antibiotics 失效
    1-卡巴（去硫）头孢菌素Antibiotika。

    公开(公告)号：EP0445925A1

    公开(公告)日：1991-09-11

    申请号：EP91301058.3

    申请日：1991-02-11

    申请人： ELI LILLY AND COMPANY

    发明人： Hornback, William Joseph ,  Munroe, John Edwin

    IPC分类号： C07D463/00 ,  A61K31/435

    CPC分类号： C07D463/18 ,  C07D463/06 ,  C07D463/20 ,  C07D463/22

    摘要： 1-Carba(1-dethia)cephem antibacterial compounds possessing a 3-(substituted or unsubstituted)thiazolo group are provided. Further provided is a method for treating bacterial infections in man and other animals and a pharmaceutical formulation utilizing said 1-carba(1-dethia)cephems. The compounds are of formula

    wherein
    X is a group selected from amino, halo, cyano, hydrogen, nitro, C₁-C₆ alkyl, C₁-C₆ substituted alkyl, a C₃ to C₆ heterocyclic ring containing 1, 2, or 3 nitrogen atoms and 0 or 1 sulfur or oxygen atoms, said ring optionally substituted by one or more groups selected from halo, nitro, hydroxy, C₁-C₆ alkyl or C₁-C₆ substituted alkyl; phenyl, substituted phenyl, or an acyl group of the formula

    wherein R˝ is C₁-C₆ alkyl, C₁-C₆ substituted alkyl, phenyl, or substituted phenyl;
    R³ is hydrogen, C₁-C₄ alkoxy, or a group of the formula -NHCHO; and
    R¹ is an acyl group of the formula

    wherein R² is hydrogen; C₁-C₆ alkyl, C₁-C₆ alkyl substituted by cyano, carboxy, halogen, amino, C₁-C₄ alkoxy, C₁-C₄ alkylthio, or trifluoromethylthio; a phenyl or substituted phenyl group represented by the formula

    wherein a and a′ independently are hydrogen, halogen, hydroxy, C₁-C₄ alkoxy, C₁-C₄ alkanoyloxy, C₁-C₄ alkyl, C₁-C₄ alkylthio, amino, mono- or di(C₁-C₄ alkyl)amino, C₁-C₄ alkanoylamino, C₁-C₄ alkylsulfonylamino, carboxy, carbamoyl, hydroxymethyl, aminomethyl, or carboxymethyl;
    a group represented by the formula

    wherein a and a′ have the same meanings as defined above, Z is 0 or S, and m is 0 or 1;
    a heteroarylmethyl group represented by the formula

            R₁-CH₂-


    wherein R₁ is thienyl, furyl, benzothienyl, benzofuryl, indolyl, triazolyl, tetrazolyl, oxazolyl, thiazolyl, oxadiazolyl, thiadiazolyl, and such heteroaryl groups substituted by amino, hydroxy, halogen, C₁-C₄ alkyl, C₁-C₄ alkoxy, or C₁-C₄ alkylsulfonylamino;
    a substituted methyl group represented by the formula

    wherein R₂ is cyclohex-1,4-dienyl, or a phenyl group or substituted phenyl group represented by the formula

    wherein a and a′ have the above defined meanings, or R₂ is R₁ as defined above, and Q is hydroxy, C₁-C₄ alkanoyloxy, carboxy, sulfo, or amino;
    or R² is a keto group or an oximino-substituted group represented by the formulae

    wherein R₃ is R₁ or R₂ as defined above and R₄ is hydrogen, C₁-C₄ alkyl, or a group represented by the formula

    wherein b and b′ independently are hydrogen, or C₁-C₃ alkyl, and b and b′ when taken together with the carbon to which they are bonded form a 3- to 6-membered carbocyclic ring, R₅ is hydroxy, C₁-C₄ alkoxy, amino, C₁-C₄ alkylamino, or di(C₁-C₄ alkyl)amino; and n is 0, 1, 2, or 3;
    or a pharmaceutically acceptable salt thereof.

    摘要翻译： 提供了具有3-（取代或未取代）噻唑基的1-卡巴（1-脱氢）头孢菌素抗菌化合物。 还提供了一种用于治疗人和其他动物中的细菌感染的方法，以及利用所述1-碳（1-脱硫）头孢克的药物制剂。 化合物是式CHEM，其中X是选自氨基，卤素，氰基，氢，硝基，C 1 -C 6烷基，C 1 -C 6取代的烷基，含有1,2或3个氮的C 3至C 6杂环的基团 原子和0或1个硫或氧原子，所述环任选被一个或多个选自卤素，硝基，羟基，C 1 -C 6烷基或C 1 -C 6取代的烷基的基团取代; 苯基，取代的苯基或式CHEM的酰基，其中R sec是C 1 -C 6烷基，C 1 -C 6取代的烷基，苯基或取代的苯基; R 3是氢，C 1 -C 4烷氧基或式-NHCHO的基团; 并且R 1是式CHEM的酰基，其中R 2是氢; C 1 -C 6烷基，被氰基，羧基，卤素，氨基，C 1 -C 4烷氧基，C 1 -C 4烷硫基或三氟甲硫基取代的C 1 -C 6烷基; 其中a和min分别独立地为氢，卤素，羟基，C 1 -C 4烷氧基，C 1 -C 4烷酰氧基，C 1 -C 4烷基，C 1 -C 4烷硫基，氨基， 或二（C 1 -C 4烷基）氨基，C 1 -C 4烷酰基氨基，C 1 -C 4烷基磺酰基氨基，羧基，氨基甲酰基，羟甲基，氨基甲基或羧甲基; 由式CHEM表示的基团，其中a和min具有与上述相同的含义，Z为0或S，m为0或1; 由式R 1 -CH 2 - 表示的杂芳基甲基，其中R 1是噻吩基，呋喃基，苯并噻吩基，苯并呋喃基，吲哚基，三唑基，四唑基，恶唑基，噻唑基，恶二唑基，噻二唑基和被氨基，羟基，卤素， C4烷基，C1-C4烷氧基或C1-C4烷基磺酰基氨基; 由式（CHEM）表示的取代甲基，其中R2是环己-1,4-二烯基，或苯基或由式CHEM表示的取代苯基，其中a和min具有上述定义，或R2 是如上定义的R 1，Q是羟基，C 1 -C 4烷酰氧基，羧基，磺基或氨基; 或R 2是由式CHEM表示的酮基或肟基取代基，其中R 3是如上定义的R 1或R 2，R 4是氢，C 1 -C 4烷基或由式CHEM 其中b和b min独立地是氢或C 1 -C 3烷基，b和b min与它们所键合的碳一起形成3至6元碳环，R 5是羟基，C 1 -C 4 烷氧基，氨基，C 1 -C 4烷基氨基或二（C 1 -C 4烷基）氨基; 并且n为0,1,2或3; 或其药学上可接受的盐。