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16 条记录 (耗时 0.024 秒)

    Substituted 5-benzyl-2,4-diaminopyrimidines
    1.
    发明授权
    Substituted 5-benzyl-2,4-diaminopyrimidines 失效
    取代的5-苄基-2,4-二氨基嘧啶

    公开(公告)号：US06821980B1

    公开(公告)日：2004-11-23

    申请号：US10129461

    申请日：2002-07-18

    申请人： Philippe Guerry ,  Peter Mohr ,  Marc Muller ,  Werner Mueller ,  Philippe Pflieger

    发明人： Philippe Guerry ,  Peter Mohr ,  Marc Muller ,  Werner Mueller ,  Philippe Pflieger

    IPC分类号： A61K31505

    CPC分类号： C07D239/49 ,  A61K31/505

    摘要： The invention relates to substituted 5-benzyl-2,4-diaminopyrimidines of general formula (A) wherein R1 is C2-C3 alkyl an R2 is heterocyclyl, phenyl or naphthyl, bonded by one of its C-atoms and R3 is C2-C6 alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfamoyl, heterocyclysylfonyl, heterocyclylalkylsulfonyl or dialkylsulfamoyl; wherein alkyl, cycloalkyl and alyenyl can carry up to 6 carbon atoms alone or in compositions and can carry up to 6 ring members heterocyclically, alone, or in compositions and the groups R2 and R3 can be substituted; and to acid addition salts of compounds. The invention also relates to a method for producing the above 5-benzyl-2,4-diaminopyrimidines, to the intermediate. products that are produced, to corresponding medicaments and to the use of 5-benzyl-2,4-diaminopyrimidines as medicinal preparations. The products have antibiotic properties and are useful for combating or preventing infectious diseases.

    摘要翻译： 本发明涉及通式（A）的取代的5-苄基-2,4-二氨基嘧啶，其中R 1是C 2 -C 3烷基，R 2是其一个C原子键合的杂环基，苯基或萘基， R 3为C 2 -C 6烷基，烯基，环烷基，环烷基烷基，杂环基烷基，烷基磺酰基，环烷基磺酰基，环烷基烷基氨磺酰基，杂芳基磺酰基，杂环基烷基磺酰基或二烷基氨磺酰基。 其中烷基，环烷基和亚烯基可以单独或组合物中携带多达6个碳原子，并且可以单独携带多达6个环成员，或者在组合物中并且基团R 2和R 3可以被取代; 和化合物的酸加成盐。 本发明还涉及制备上述5-苄基-2,4-二氨基嘧啶的方法。 生产的产品，相应的药物和使用5-苄基-2,4-二氨基嘧啶作为药物制剂。 该产品具有抗生素特性，可用于对抗或预防传染病。

    Substituted 2,4-diaminopyrimidines
    6.
    发明授权
    Substituted 2,4-diaminopyrimidines 失效
    取代的2,4-二氨基嘧啶

    公开(公告)号：US5866583A

    公开(公告)日：1999-02-02

    申请号：US842459

    申请日：1997-04-24

    申请人： Philippe Guerry ,  Henri Stalder ,  Pierre-Charles Wyss

    发明人： Philippe Guerry ,  Henri Stalder ,  Pierre-Charles Wyss

    IPC分类号： A61K31/00 ,  A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P31/00 ,  A61P31/04 ,  C07D217/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14

    CPC分类号： C07D401/04 ,  C07D217/06 ,  C07D401/10 ,  C07D401/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14

    摘要： Compounds of formula I ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is bromine, lower-alkoxy or hydroxy, R.sup.3 is hydrogen, lower-alkyl, cycloalkyl, aryl, heterocyclyl, aralkyl, heterocyclyl-lower-alkyl or cyano, R.sup.4 and R.sup.5 each independently are hydrogen, lower-alkyl, lower-alkoxy, halogen, hydroxy, amino, di(lower alkyl)amino, cyano or nitro and Q is ethynylene or vinylene, or pharmaceutically usable salts thereof, the use of these compounds and their salts as therapeutically active substances; medicaments based on these substances and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula I and their pharmaceutically acceptable salts and intermediates for their manufacture.

    摘要翻译： 式I的化合物其中R 1是低级烷氧基，R 2是溴，低级烷氧基或羟基，R 3是氢，低级烷基，环烷基，芳基，杂环基，芳烷基，杂环基 - 低级 - 烷基或氰基，R 4 和R 5各自独立地为氢，低级烷基，低级烷氧基，卤素，羟基，氨基，二（低级烷基）氨基，氰基或硝基，Q为亚乙炔基或亚乙烯基或其药学上可用的盐，使用这些化合物和 其盐作为治疗活性物质; 基于这些物质及其生产的药物; 使用这些物质作为药物和生产抗菌活性药物; 以及式I化合物及其药学上可接受的盐和其制备中间体的制备。

    Substituted aminoalkyl biphenyl compounds and method of treating fungal infections
    7.
    发明授权
    Substituted aminoalkyl biphenyl compounds and method of treating fungal infections 失效
    取代的氨基胆碱化合物和治疗真菌感染的方法

    公开(公告)号：US5177067A

    公开(公告)日：1993-01-05

    申请号：US718495

    申请日：1991-06-19

    申请人： Philippe Guerry ,  Synese Jolidon

    发明人： Philippe Guerry ,  Synese Jolidon

    IPC分类号： A61K31/135 ,  A61P31/04 ,  A61P31/10 ,  C07C215/30 ,  C07C217/48 ,  C07C225/16 ,  C07C255/58 ,  C07D295/10

    CPC分类号： C07C225/16 ,  C07C215/30 ,  C07C255/58

    摘要： Antimycotically-active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-7 -alkyl or C.sub.2-7 -alkenyl or together are a straight chain C.sub.2-4 -alkylene; R.sup.3 and R.sup.4 each independently are hydrogen or C.sub.1-7 -alkyl; R.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, nitro, cyano, C.sub.1-7 -alkoxy or C.sub.1-7 -alkyl; and Q is an unsubstituted or substituted phenyl or naphthyl group, wherein the substituents are at least one of halogen, trifluoromethyl, cyano, nitro, C.sub.1-7 -alkyl, C.sub.1-7 -alkoxy; C.sub.2-10 -alkenyl; or a substituted or unsubstituted C.sub.1-10 -alkyl group wherein said substituents are at least one hydroxy group; andpharmaceutically acceptable acid addition salts thereof.

    摘要翻译： 式IMA的抗真菌活性化合物，其中R 1和R 2各自独立地为氢，C 1-7 - 烷基或C 2-7 - 烯基或一起为直链C 2-4 - 亚烷基; R 3和R 4各自独立地为氢或C 1-7 - 烷基; R 5和R 6各自独立地为氢，卤素，三氟甲基，硝基，氰基，C 1-7 - 烷氧基或C 1-7 - 烷基; Q为未取代或取代的苯基或萘基，其中取代基为卤素，三氟甲基，氰基，硝基，C 1-7 - 烷基，C 1-7 - 烷氧基， C2-10-烯基; 或取代或未取代的C 1-10 - 烷基，其中所述取代基是至少一个羟基; 及其药学上可接受的酸加成盐。

    Substituted aminoalkyl biphenyl compounds
    10.
    发明授权
    Substituted aminoalkyl biphenyl compounds 失效
    取代的氨基烷基联苯化合物

    公开(公告)号：US5239084A

    公开(公告)日：1993-08-24

    申请号：US943268

    申请日：1992-09-10

    申请人： Philippe Guerry ,  Synese Jolidon

    发明人： Philippe Guerry ,  Synese Jolidon

    IPC分类号： C07C215/30 ,  C07C225/16 ,  C07C255/58

    CPC分类号： C07C225/16 ,  C07C215/30 ,  C07C255/58

    摘要： Antimycotically-active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-7 -alkyl or C.sub.2-7 -alkenyl or together are a straight chain C.sub.2-4 -alkylene; R.sup.3 and R.sup.4 each independently are hydrogen or C.sub.1-7 -alkyl; R.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, nitro, cyano, C.sub.1-7 -alkoxy or C.sub.1-7 -alkyl; and Q is an unsubstituted or substituted phenyl or naphthyl group, wherein the substituents are at least one of halogen, trifluoromethyl, cyano, nitro, C.sub.1-7 -alkyl, C.sub.1-7 -alkoxy; C.sub.2-10 -alkenyl; or a substituted or unsubstituted C.sub.1-10 -alkyl group wherein said substituents are at least one hydroxy group; andpharmaceutically acceptable acid addition salts thereof.

    摘要翻译： 式IMA的抗真菌活性化合物，其中R 1和R 2各自独立地为氢，C 1-7 - 烷基或C 2-7 - 烯基或一起为直链C 2-4 - 亚烷基; R 3和R 4各自独立地为氢或C 1-7 - 烷基; R 5和R 6各自独立地为氢，卤素，三氟甲基，硝基，氰基，C 1-7 - 烷氧基或C 1-7 - 烷基; Q为未取代或取代的苯基或萘基，其中取代基为卤素，三氟甲基，氰基，硝基，C 1-7 - 烷基，C 1-7 - 烷氧基， C2-10-烯基; 或取代或未取代的C 1-10 - 烷基，其中所述取代基是至少一个羟基; 及其药学上可接受的酸加成盐。