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    .alpha.-(4-Biphenylyl)-benzyl-azolium salts and their use for combating micro-organisms
    6.
    发明授权
    .alpha.-(4-Biphenylyl)-benzyl-azolium salts and their use for combating micro-organisms 失效
    α-（4-联苯基） - 苄基 - 唑烷鎓盐及其用于抗微生物的用途

    公开(公告)号：US4243670A

    公开(公告)日：1981-01-06

    申请号：US14783

    申请日：1979-02-23

    申请人： Erik Regel ,  Wilfried Draber ,  Karl H. Buchel ,  Manfred Plempel

    发明人： Erik Regel ,  Wilfried Draber ,  Karl H. Buchel ,  Manfred Plempel

    IPC分类号： C08G69/48 ,  A61K31/41 ,  A61K31/415 ,  A61P31/04 ,  A61P31/10 ,  C07D233/56 ,  C07D233/58 ,  C07D233/60 ,  C07D249/08 ,  C07D521/00 ,  C08G69/00 ,  A01N43/26 ,  A01N43/28

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The present invention relates to novel .alpha.-(4-biphenylyl)-benzyl-azolium salts of the general formula ##STR1## in which A represents the CH group or a N atomR.sup.1 and R.sup.2 are identical or different and each represents hydrogen, alkyl or optionally substituted phenyl,R.sup.3 represents hydrogen, alkyl, or an optionally substituted phenyl, phenylalkyl, phenylcarbonyl or phenylcarbonylalkyl group,X represents halogen, alkyl, halogenoalkyl, alkoxy, alkylthio, nitro or cyano,Y represents X or optionally substituted phenyl,m and n each represents 0 or an integer from1 to 5 andZ represents the anion of an inorganic or organic acid.The invention also includes processes for the preparation of the compounds and, in addition includes compositions containing the compounds and methods for their use. The compounds of the invention exhibit antimicrobial activity and sporicidal activity.

    摘要翻译： 本发明涉及其中A表示CH基团或N原子R1和R2相同或不同并且各自表示氢的通式为“IMA”（I）的新型α-（4-联苯基） - 苄基 - ，烷基或任选取代的苯基，R 3表示氢，烷基或任选取代的苯基，苯基烷基，苯基羰基或苯基羰基烷基，X表示卤素，烷基，卤代烷基，烷氧基，烷硫基，硝基或氰基，Y表示X或任选取代的苯基， m和n各自表示0或1至5的整数，Z表示无机或有机酸的阴离子。 本发明还包括制备化合物的方法，并且还包括含有这些化合物的组合物及其使用方法。 本发明的化合物显示出抗微生物活性和杀孢子活性。

    Antimicrobial agents
    10.
    发明授权
    Antimicrobial agents 失效
    抗微生物剂

    公开(公告)号：US4215131A

    公开(公告)日：1980-07-29

    申请号：US21295

    申请日：1979-03-16

    申请人： Wolfgang Kramer ,  Karl H. Buchel ,  Manfred Plempel ,  Ingo Haller

    发明人： Wolfgang Kramer ,  Karl H. Buchel ,  Manfred Plempel ,  Ingo Haller

    IPC分类号： C07D249/08 ,  A61K31/41 ,  A61P31/04 ,  A61P31/10 ,  C07D233/60 ,  C07D521/00 ,  A01N9/00 ,  A01N9/22

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： Pharmaceutical compositions free from pathogenic microorganisms which could be harmful to warm-blooded animals, are provided containing, as an active ingredient, an antimicrobially effective amount of at least one compound of the formula ##STR1## in which R represents hydrogen, --CO--R.sup.1 or --SO.sub.2 --R.sup.2, whereinR.sup.1 represents optionally substituted alkyl, alkenyl or alkinyl, optionally substituted phenyl, optionally substituted phenoxyalkyl, phenylalkyl, cycloalkyl, alkylamino, dialkylamino or optionally substituted phenylamino,R.sup.2 represents alkyl or optionally substituted phenyl,A represents a keto group or a --CH(OH)-- grouping,X represents hydrogen or an --OR grouping, whereinR is as defined above,X.sup.1 represents alkyl or optionally substituted phenyl,Y represents --CH-- or a nitrogen atom,Z represents halogen, alkyl, halogenoalkyl, cycloalkyl, alkoxy, alkythio, alkoxycarbonyl, optionally substituted phenyl, optionally substituted phenoxy, optionally substituted phenylalkyl, amino, cyano or nitro andn represents 0 or an integer from 1 to 5, or a salt thereof, in admixture with a sterile pharmaceutical carrier, such as a solid or liquefied gaseous diluent, or with a liquid diluent other than a solvent of molecular weight less than 200 (preferably 300) except in the presence of a surface-active agent.The compositions of the invention are useful as antimycotic agents.Also included in the invention is the provision of the compositions of the invention in unit dosage form as well as the provision of methods of treatment wherein the compositions of the invention are administered to warm-blooded animals.

    摘要翻译： 提供了不含可能对温血动物有害的致病微生物的药物组合物，其含有抗微生物有效量的至少一种下式化合物（Ⅰ），其中R表示氢， - CO-R1或-SO2-R2，其中R1表示任选取代的烷基，烯基或炔基，任选取代的苯基，任选取代的苯氧基烷基，苯基烷基，环烷基，烷基氨基，二烷基氨基或任选取代的苯基氨基，R 2表示烷基或任选取代的苯基，A表示 酮基或-CH（OH） - 基，X表示氢或-OR基团，其中R如上定义，X​​ 1表示烷基或任选取代的苯基，Y表示-CH-或氮原子，Z表示卤素 烷基，卤代烷基，环烷基，烷氧基，链烯基，烷氧基羰基，任选取代的苯基，任选取代的苯氧基，任选取代的苯基烷基，氨基，氰基 或硝基，n代表0或1至5的整数，或其盐与无菌药物载体（例如固体或液化气体稀释剂）混合，或与分子量小于 200（优选300），除了在表面活性剂的存在下。 本发明的组合物可用作抗真菌剂。 本发明还包括以单位剂量形式提供本发明的组合物以及提供治疗方法，其中将本发明的组合物施用于温血动物。