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    • 8. 发明授权
    • N,N'-substituted imidodicarbonimidic diamides derived from hydroxylamines
    • 衍生自羟胺的N,N'-取代的亚氨基二甲酰胺二酰胺
    • US5322858A
    • 1994-06-21
    • US837258
    • 1992-02-14
    • Craig CanfieldDavid P. JacobusNeil J. Lewis
    • Craig CanfieldDavid P. JacobusNeil J. Lewis
    • A61K31/155A61K31/16A61P31/04A61P33/00A61P33/06C07C279/26C07C321/28C07C323/10C07C323/13
    • C07C279/26C07C323/13Y10S514/895
    • There are provided compounds of the formula ##STR1## wherein R.sup.1 is a substituted or unsubstituted divalent aliphatic group of 1 to 16 carbon atoms; wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, aryl and arlkyl, R.sup.3 is selected from the group consisting of same group of values as R.sup.5, R.sup.5 is selected from the group consisting of substituted and unsubstituted alkyl of 1-10 carbon atoms, aryl, cycloalkyl and heterocycloalkyl of 3-8 carbon atoms, wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, cycloalkyl of 3-8 carbon atoms, lower alkenyl, lower alkynyl, nitro, lower alkoxy, lower alkoxycarbonyl, phenyl loweralkyl, phenyl, mono and polyhalophenyl, phenoxy, mono and polyhalophenoxy, R.sup.6 and R.sup.7 may be the same or different and are hydrogen, alkanoyl or alkoxyalkanoyl, R.sup.7 may also have the same value as R.sup.5, Y is oxygen or sulfur, m is 0 or 1, q is 0 or 1, wherein the prefix alk designates moieties which are straight chain or branched chain, and the term lower designates 1-6 carbon atoms and the unmodified term alk signifies 1-24 carbon atoms, the respective tautomers thereof, the pharmaceutically acceptable salts and addition salts thereof and the hydrates of said salts and addition salts. There are further provided methods of protecting subjects liable thereto from infections caused by an organism of the group Plasmodium sp., Mycobacterium sp. and Pneumocystis carinii by administering to a subject liable to such infection, a prophylactically effective amount of a compound of the foregoing formula. These compounds will also reduce the level of infection where said subjects have already been infected.
    • 提供式IMA的化合物,其中R 1是1至16个碳原子的取代或未取代的二价脂族基团; 其中所述取代基是单取代或多取代的,并且选自低级烷基,芳基和烷基,R 3选自与R 5相同的值组,R 5选自取代和未取代的烷基 1-10个碳原子,3-8个碳原子的芳基,环烷基和杂环烷基,其中取代基是单或多,并且选自低级烷基,3-8个碳原子的环烷基,低级烯基,低级炔基, 硝基,低级烷氧基,低级烷氧基羰基,苯基低级烷基,苯基,单和多卤代苯基,苯氧基,单和多卤代苯氧基,R6和R7可以相同或不同,为氢,烷酰基或烷氧基烷酰基,R7也可具有与R5相同的值, Y为氧或硫,m为0或1,q为0或1,其中前缀alk表示直链或支链的部分,术语“低级”表示1-6个碳原子,未修饰的术语“ 24碳 原子,其各自的互变异构体,其药学上可接受的盐和加成盐以及所述盐和加成盐的水合物。 进一步提供了保护受益于其的受试者的方法,所述受体是由疟原虫属,分枝杆菌属(Mycobacterium sp。)组成的生物引起的感染引起的。 和卡氏肺囊虫,通过给予易感染的受试者,预防有效量的上述化合物。 这些化合物还将降低所述受试者已被感染的感染水平。