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    • 2. 发明授权
    • Water soluble azoles as broad-spectrum antifungals
    • 水溶性唑类作为广谱抗真菌剂
    • US06384030B1
    • 2002-05-07
    • US09700251
    • 2000-11-09
    • Lieven MeerpoelLeo Jacobus Jozef BackxLouis Jozef Elisabeth Van der VekenJan HeeresFrank Christopher Odds
    • Lieven MeerpoelLeo Jacobus Jozef BackxLouis Jozef Elisabeth Van der VekenJan HeeresFrank Christopher Odds
    • C07D40514
    • C07D249/08C07D231/12C07D233/56C07D249/12
    • The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein L represent a radical of formula wherein each Alk independently represents an optionally substituted C1-6alkanediyl; is 1, 2 or 3; Y is O, S or NR2; R1 represents hydrogen, aryl, Het1, or an optionally substituted C1-6alkyl; each R2 independently represents hydrogen or C1-6alkyl; or in case R1 and R2 are attached to the same nitrogen atom, they may be taken together to form a heterocyclic radical; or they may be taken together to form an azido radical; each R3 independently represents hydrogen, hydroxy or C1-4alkyloxy; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; Het1 represents an optionally substituted monocyclic or bicyclic heterocyclic radical; Het2 is the same as Het1 and may also be piperazinyl, homopiperazinyl, 1,4-dioxanyl, morpholinyl, thiomorpholinyl; R6 represents hydrogen or C1-4alkyl; R7 represents hydrogen or C1-4alkyl; or R6 and R7 taken together form a bivalent radical of formula —N═CH— (i), —CH═N— (ii), —CH═CH— (iii), —CH2—CH2 (iv), wherein one hydrogen atom in the radicals (i) and (ii) may be replaced with a C1-4alkyl radical and one or more hydrogen atoms in radicals (iii) and (iv) may be replaced by a C1-4alkyl radical; D represents a trisubstituted 1,3-dioxolane derivative; as antifungals; their processes for preparation, compositions containing them and their use as a medicine.
    • 本发明涉及配制N-氧化物形式的新化合物,其药学上可接受的加成盐和立体化学异构形式,其中L代表甲酰基的基团,每个Alk独立地表示任选取代的C 1-6烷二基; 是1,2或3; Y是O,S或NR2; R 1表示氢,芳基,Het1或任选取代的C 1-6烷基; 每个R 2独立地表示氢或C 1-6烷基; 或者在R1和R2连接到相同的氮原子的情况下,它们可以一起形成杂环基; 或者它们可以一起形成叠氮基; 每个R 3独立地表示氢,羟基或C 1-4烷氧基; 芳基表示苯基,萘基,1,2,3,4-四氢 - 萘基,茚基或茚满基; 每个所述芳基可任选被取代; Het1表示任选取代的单环或双环杂环基; Het2与Het1相同,也可以是哌嗪基,高哌嗪基,1,4-二氧杂环己基,吗啉基,硫代吗啉基; R6代表氢或C1-4烷基; R7代表氢或C1-4烷基; 或者R 6和R 7一起形成式-N = CH-(ⅰ),-CH = N-(ⅱ),-CH = CH-(ⅲ),-CH 2 -CH 2(ⅳ)的二价基团,其中一个氢 基团(i)和(ii)中的原子可以被C 1-4烷基取代,并且基团(iii)和(iv)中的一个或多个氢原子可被C 1-4烷基取代; D表示三取代的1,3-二氧戊环衍生物; 作为抗真菌剂; 其制备方法,含有它们的组合物及其作为药物的用途。