发明名称 PYRIDINE DERIVATIVES SUBSTITUTED BY HETEROCYCLIC AND PHOSPHONOAMINO GROUP, AND ANTI-FUNGAL AGENT CONTAINING SAME
摘要 An antifungal agent that has an excellent antifungal activity and excels in not only properties, especially solubility in water but also safety. Ther e are disclosed compounds of the formula (I) and salts thereof. [in the form ula, R1 is a hydrogen atom, halogen atom, amino, R11-NH- (R11 is a C1-C6 alk yl, hydroxylated C1-C6 alkyl, C1-C6 alkoxylated C1-C6 alkyl or C1-C6 alkoxyc arbonylated C1-C6 alkyl), R12-(CO)-NH- (R12 is a C1-C6 alkyl or C1-C6 alkoxy lated C1-C6 alkyl), C1-C6 alkyl, hydroxylated C1-C6 alkyl, cyano C1-C6 alkyl , C1-C6 alkoxy, C1-C6 alkoxylated C1-C6 alkyl or phosphonoamino; R2 is a hyd rogen atom, C1-C6 alkyl, amino, di-(C1-C6 alkylamino) or phosphonoamino; eit her X or Y is a nitrogen atom while the other is a nitrogen atom or oxygen a tom; the ring A is a 5- or 6-membered heteroaryl ring or benzene ring option ally having one or two C1-C6 alkyls or halogen atoms; Z is a single bond, me thylene,ethylene, oxygen atom, sulfur atom, -CH2O-, -OCH2-, -NH-, -CH2NH-, - NHCH2-, -CH2S- or -SCH2-; R3 is a hydrogen atom, halogen atom, or optionally monosubstituted or disubstituted C1-C6 alkyl, C3-C8 cycloalkyl, C6-C10 aryl , 5- or 6-membered heteroaryl or 5- or 6-membered nonaromatic heterocycle; a nd R4 is a hydrogen atom or halogen atom, provided that either R1 or R2 is p hosphonoamino].
申请公布号 CA2684503(A1) 申请公布日期 2008.11.13
申请号 CA20082684503 申请日期 2008.04.23
申请人 EISAI R&D MANAGEMENT CO., LTD. 发明人 WATANABE, NAOAKI;YAMAMOTO, EIICHI;TANAKA, KEIGO
分类号 C07F9/6558;A61K31/664;A61P31/10 主分类号 C07F9/6558
代理机构 代理人
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