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102 条记录 (耗时 0.04 秒)

    Substituted aminoalkyl biphenyl compounds
    62.
    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。

    Method of treating fungal infections
    63.
    发明授权
    Method of treating fungal infections 失效
    治疗真菌感染的方法

    公开(公告)号：US5137920A

    公开(公告)日：1992-08-11

    申请号：US533605

    申请日：1990-06-05

    申请人： Philippe Guerry ,  Synese Jolidon ,  Rene Zurfluh

    发明人： Philippe Guerry ,  Synese Jolidon ,  Rene Zurfluh

    IPC分类号： A61K31/135 ,  A61K31/275 ,  A61K31/40 ,  A61P31/04 ,  C07C215/28 ,  C07C217/48 ,  C07C225/16 ,  C07C253/30 ,  C07C255/58 ,  C07D295/10 ,  C07D295/108

    CPC分类号： C07D295/108 ,  C07C215/28 ,  C07C217/48 ,  C07C225/16 ,  C07C255/58

    摘要： Compunds having the formula ##STR1## wherein each of R.sup.1 and R.sup.2 individually is hydrogen, lower alkyl, or lower alkenyl, R.sup.3 is hydrogen, halogen or lower alkyl, Q is alkylene with 2 to 11 carbon atoms and at least 2 carbon atoms between the two free valencies or alkenylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies and each of Y and Y' individually is a direct bond, the group R.sup.1 R.sup.2 --N--Q--CH.sub.2 -- is attached to the 3- or 4-position of ring A and the symbol R represents that the ring to which it is attached is unsubstituted or is substituted with at least one of halogen, trifluoromethyl, cyano, nitro, lower alkyl or lower alkoxy, and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties. In particular, they have a pronounced antifungal activity and can be used as medicaments, especially for the control or prevention of topical or systemic infections which are caused by pathogenic fungi.

    摘要翻译： 具有式“IMAGE”I的组合物，其中R 1和R 2各自独立地为氢，低级烷基或低级烯基，R 3为氢，卤素或低级烷基，Q为具有2至11个碳原子的亚烷基和至少2个碳原子 两个自由价之间具有4至11个碳原子和至少4个碳原子的两个自由价或亚烯基，Y和Y'各自独立地为直接键，R1R2-NQ-CH2-基团连接到3- 或环A的4位，符号R表示其所连接的环是未取代的或被至少一个卤素，三氟甲基，氰基，硝基，低级烷基或低级烷氧基取代的化合物及其药学上可接受的酸加成 盐具有宝贵的药理性质。 特别地，它们具有显着的抗真菌活性，并且可以用作药物，特别是用于控制或预防由病原真菌引起的局部或全身感染。

    Use of substituted aminoalkoxybenzene derivatives in the control or prevention of fungal infections
    64.
    发明授权
    Use of substituted aminoalkoxybenzene derivatives in the control or prevention of fungal infections 失效
    在控制或预防真菌感染中使用取代的氨基甲苯苯衍生物

    公开(公告)号：US5106878A

    公开(公告)日：1992-04-21

    申请号：US556241

    申请日：1990-07-20

    申请人： Philippe Guerry ,  Synese Jolidon ,  Rene Zurfluh

    发明人： Philippe Guerry ,  Synese Jolidon ,  Rene Zurfluh

    IPC分类号： A61K31/13 ,  A61K31/135 ,  A61K31/395 ,  A61P31/04 ,  C07C43/205 ,  C07C49/84 ,  C07C213/02 ,  C07C213/08 ,  C07C217/18 ,  C07C217/20 ,  C07C217/22 ,  C07C217/46 ,  C07D205/04 ,  C07D207/08 ,  C07D295/08 ,  C07D295/092

    CPC分类号： C07D295/088 ,  C07C217/18 ,  C07C217/20 ,  C07C217/22 ,  C07C217/46 ,  C07D205/04

    摘要： The compound of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 individually is hydrogen, lower alkyl or lower alkenyl or together signify straight-chain alkylene with 2 or 4 carbon atoms, R.sup.3 is hydrogen, halogen or lower alkyl, Q is alkylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies or alkenylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies and each of Y and Y' individually is a direct bond or the group --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--, the group R.sup.1 R.sup.2 N--Q--O-- is attached to the 3- or 4-position of ring A and the symbol R designates that the ring to which it is attached is unsubstituted or is substituted with at least one substituent selected from the group consisting of halogen, trifluoromethyl, cyano, nitro, lower alkyl and lower alkoxy, and their pharmaceutically acceptable acid addition salts can be used for the control or prevention of fungal infections, especially of topical or systemic infections which are caused by pathogenic fungi, and for the manufacture of antifungally-active medicaments. The compounds of formula I have not only a pronounced antifungal activity, but they also exhibit synergistic effects in combination with other known antifungally-active substances which inhibit sterol biosynthesis such as ketoconazole and terbinafine.

    摘要翻译： 式Ⅰ化合物，其中R 1和R 2各自独立地为氢，低级烷基或低级烯基或一起表示具有2或4个碳原子的直链亚烷基，R 3为氢，卤素或低级烷基，Q为亚烷基 在两个自由价之间具有4至11个碳原子和至少4个碳原子，在两个自由价之间具有4至11个碳原子和至少4个碳原子的亚烯基，Y和Y'各自独立地是直接键合或 基团-CH 2 - ， - CH 2 CH 2 - ， - CH = CH-或-C 3BOND C-，基团R 1 R 2 N-QO-连接到环A的3-或4-位，符号R表示环 其连接是未取代的或被至少一个选自卤素，三氟甲基，氰基，硝基，低级烷基和低级烷氧基的取代基取代，并且其药学上可接受的酸加成盐可用于控制或预防真菌 感染，特别是局部或全身感染 由致病真菌引起的离子和用于制造抗真菌药物的离子。 式I化合物不仅具有显着的抗真菌活性，而且还与抑制甾醇生物合成的其它已知的抗真菌活性物质如酮康唑和特比萘芬组合显示协同效应。

    Process for the production of 4-(trialkylammonium)-acetoacetarylides
    66.
    发明授权
    Process for the production of 4-(trialkylammonium)-acetoacetarylides 失效
    制备4-（三烷基铵） - 乙酰乙酰胺的方法

    公开(公告)号：US4558158A

    公开(公告)日：1985-12-10

    申请号：US501898

    申请日：1983-06-07

    申请人： Leander Tenud ,  Synese Jolidon

    发明人： Leander Tenud ,  Synese Jolidon

    IPC分类号： C07C231/00 ,  C07C67/00 ,  C07C231/12 ,  C07C237/04 ,  C09B44/02 ,  C07C91/42

    CPC分类号： C09B44/02

    摘要： Process for the production of 4-(trialkylammonium)-acetoacetarylides having the formula: ##STR1## wherein R is H, a lower alkyl, --OCH.sub.3, --OC.sub.2 H.sub.5, --Cl, --Br, --NO.sub.2, --NHCOCH.sub.3 or an anilated heterocyclic ring; n is 1 to 3; R.sup.1, R.sup.2 and R.sup.3 each is an alkyl having 1 to 18 C atoms; and X is Cl or Br. Such arylide is prepared by reacting a corresponding trialkylamine with a corresponding 4-haloacetoacetarylide at a low temperature in the presence of an organic solvent.

    摘要翻译： 制备具有下式的4-（三烷基铵） - 乙酰乙酰基化合物的方法：其中R是H，低级烷基，-OCH 3，-OC 2 H 5，-Cl，-Br，-NO 2，-NHCOCH 3或被杂环的杂环 ; n为1〜3; R1，R2和R3各自为具有1至18个C原子的烷基; X为Cl或Br。 在有机溶剂存在下，通过使相应的三烷基胺与相应的4-卤代乙酰基乙酰胺在低温下反应来制备。