会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明授权
    • Substituted aminoalkoxybenzene anti-fungicidal compositions and use
    • 取代氨基烷氧基苯类杀真菌剂及用途
    • US5214046A
    • 1993-05-25
    • US832190
    • 1992-02-06
    • Philippe GuerrySynese JolidonRene Zurfluh
    • Philippe GuerrySynese JolidonRene Zurfluh
    • C07C217/18C07C217/20C07C217/22C07C217/46C07D205/04C07D295/092
    • C07D295/088C07C217/18C07C217/20C07C217/22C07C217/46C07D205/04
    • 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 to 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 substitutent 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.
    • 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至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-CB 3 -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,特别是局部或全身疾病 由致病真菌引起的作用和用于制造抗真菌药物。 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。
    • 5. 发明授权
    • Substituted aminoalkyl biphenyl compounds
    • 取代的氨基烷基联苯化合物
    • US5239084A
    • 1993-08-24
    • US943268
    • 1992-09-10
    • Philippe GuerrySynese Jolidon
    • Philippe GuerrySynese Jolidon
    • C07C215/30C07C225/16C07C255/58
    • C07C225/16C07C215/30C07C255/58
    • 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.
    • 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。
    • 6. 发明授权
    • Method of treating fungal infections
    • 治疗真菌感染的方法
    • US5137920A
    • 1992-08-11
    • US533605
    • 1990-06-05
    • Philippe GuerrySynese JolidonRene Zurfluh
    • Philippe GuerrySynese JolidonRene Zurfluh
    • A61K31/135A61K31/275A61K31/40A61P31/04C07C215/28C07C217/48C07C225/16C07C253/30C07C255/58C07D295/10C07D295/108
    • C07D295/108C07C215/28C07C217/48C07C225/16C07C255/58
    • 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.
    • 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。
    • 7. 发明授权
    • Use of substituted aminoalkoxybenzene derivatives in the control or
prevention of fungal infections
    • 在控制或预防真菌感染中使用取代的氨基甲苯苯衍生物
    • US5106878A
    • 1992-04-21
    • US556241
    • 1990-07-20
    • Philippe GuerrySynese JolidonRene Zurfluh
    • Philippe GuerrySynese JolidonRene Zurfluh
    • A61K31/13A61K31/135A61K31/395A61P31/04C07C43/205C07C49/84C07C213/02C07C213/08C07C217/18C07C217/20C07C217/22C07C217/46C07D205/04C07D207/08C07D295/08C07D295/092
    • C07D295/088C07C217/18C07C217/20C07C217/22C07C217/46C07D205/04
    • 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.
    • 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。
    • 10. 发明授权
    • Substituted 5-benzyl-2,4-diaminopyrimidines
    • 取代的5-苄基-2,4-二氨基嘧啶
    • US06821980B1
    • 2004-11-23
    • US10129461
    • 2002-07-18
    • Philippe GuerryPeter MohrMarc MullerWerner MuellerPhilippe Pflieger
    • Philippe GuerryPeter MohrMarc MullerWerner MuellerPhilippe Pflieger
    • A61K31505
    • C07D239/49A61K31/505
    • 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.
    • 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。