发明名称 WATER SOLUBLE AZOLES AS BROAD-SPECTRUM ANTIFUNGALS
摘要 The present invention concerns novel compounds of formula the i(N)-oxide forms, the pharmaceutically acceptable addition salts and steriochemically isomeric forms thereof, wherein L represents a radical of formula wherein each Alk independently represents an optionally substituted C1-6alkenediyl; n is 1, 2 or 3; Y is O. S or NR2; R1 represents hydrogen, aryl, Het1, or optionally substituted C16alkyl; 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 C1-4alkoxy; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; eachof said aryl group 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, 1,4-dioxanyl, morpholinyl, thiomorpholinyl; R6 represents hydrogen or C1-4alkyl; R7 represents hydrogen or C1-4alkyl; or R6 and R7 taken together for 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 aC1-4alkyl radical; D represents a trisubstituted 1,3-dioxolane derivative; as antifungals; their processes for preparation, composition containing them and their use as a medicine.
申请公布号 BG64954(B1) 申请公布日期 2006.10.31
申请号 BG20000104933 申请日期 2000.11.09
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 MEERPOEL LIEVEN;BACKX LEO JACOBUS JOZEF;VAN DER VEKEN LOUIS;ODDS FRANK CHRISTOPHER;HEERES JAN
分类号 C07D405/14;A61K31/495;A61K31/496;A61K31/497;A61K31/5377;A61K31/541;A61P31/04;A61P31/10;C07D249/00;C07D249/12;C07D295/00;C07D319/00;C07D405/06;C07D405/12;C07D413/14;C07D417/14;C07D521/00 主分类号 C07D405/14
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