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NEW DERIVATIVES OF AZOL OR TRIAZOL, ITS PREPARATION PROCEDURE AND ITS APPLICATION AS ANTI-FUNGICAL MEDICINES.

机译:偶氮或三唑的新衍生物,其制备方法及其在抗真菌药物中的应用。

摘要

The compounds of formula (I) in which: - X is a nitrogen atom or a CH group, - Ar1 represents a carbocyclic or heterocyclic aryl unsubstituted or substituted by one or more radicals R2, R3 or R4, - A represents a hydrogen atom or represents a CH2 group that forms, with R1 a cyclic carbon carbon bond, in order to obtain a 6-link cycle fused with the phenyl, - Ar3 represents a carbocyclic or heterocyclic aryl unsubstituted or substituted by one or more radicals R8, R9 or R10 - R2, R3, R4, R5, R6 R7, R8, R9 or R10 identical or different, represent fluorine, chlorine, bromine, cyano, mono40 bi- or trihalogen (C1-C8) alkyl, mono-bi - or trihalogen (C1-C8) -alkyloxy, hydroxy, nitro, carboxyl, formyl, -SO3H, -OSO3H, (R11O) 2P (O) -, (R11O) 2P (O) -O-, amino, (C1- C8) -alkylamino, di ((C1-C8) alkyl) amino, (C5-C14) aryl (C1-C6) alkylemino or (C5-C14) arylamino, (C1-C8) alkyl, (C5-C14) -aryl , a heterocycle optionally substituted by oxo, (C5-C14) aryl (C1-C6) alkyl, amino- (C1-C6) -alkyl, (C1-C8) -alkylamino (C1-C6) -alkyl, di - ((C1-C8) alkyl) amino- (C1-C6) -alkyl, hydroxy (C1 -C6) alkyl, (C1-C6) alkyloxy (C1-C6) alkyl, (C1-C8) -alkyloxy optionally interrupted by one or more oxygen atoms, (C5-C14) aryl- (C1-C6) -alkyleneoxy, (C5-C14) -aryloxy, hydroxy- (C1-C6) alkyleneoxy, (C1-C6) -alkyloxy- (C1-C6) alkyleneoxy, amino- (C1-C6) -alkyleneoxy, (C1-C6) -alkylamino- (C1-C6) -alkyleneoxy, di ((C1-C8) -alkyl) amino- (C1-C6) alkyleneoxy, methylenedioxy, (C1-C6) -alkyloxycarbonyl, (C1-C6) -alkylcarbonyl, (C5-C14) aryl- (C1-C6) -alkylenecarbonyl, (C5-C14) -aryl-carbonyl, (C1-C6) -alkylaminocarbonyl, (C1-C6) alkanoylamino, (C1-C6) -alkyl-sulfonylamino, (C5-C14) - arylsulfonylamino, (C5-C14) -aryl- (C1-C6) -alkylene sulfonylamino, (C1-C6) -alkylamino-sulfonyl, (C5-C14) -aryl- (C1-C6) -alkylene-amino-sulfonyl, (C1-C6) - alkylsulfonyl, (C5-C14) -aryl- (C1-C8) alkylenesulfonyl or (C5-C14) -aryl-sulfonyl, said alkyl, aryl or heterocycle radicals being my smos not substituted or substituted by one or several groups mentioned above, - R11 represents hydrogen, (C1-C10) alkyl, (C6-C14) aryl or (C6-C14) aryl (C1-C6) alkyl, in all its stereoisomeric forms possible and their mixtures, as well as their physiologically acceptable addition salts and their prodrugs. - B represents a (C1-C4) alkylene-CH = CH- radical or a (C1-C4) alkylene-cyclopropylene radical, said cyclopropylene radicals or -CH = CH- being unsubstituted or substituted by a radical R2 and / or R3 , - R1 represents a hydrogen atom, a -SO3H group, a (C1-C6) alkyl radical unsubstituted or substituted by a radical as defined for R2, or represents a CH2 group that forms A carbon bond with A cyclic carbon, in order to obtain a 6-link cycle fused with phenyl,
机译:式(I)的化合物,其中:-X是氮原子或CH基,-Ar1表示未被取代或被一个或多个基团R2,R3或R4取代的碳环或杂环芳基,-A表示氢原子或-代表CH2基团,与R1形成环状碳碳键,以获得与苯基稠合的6键环,-Ar3代表未被取代或被一个或多个基团R8,R9或R10取代的碳环或杂环芳基-R2,R3,R4,R5,R6,R7,R8,R9或R10相同或不同,代表氟,氯,溴,氰基,单40双或三卤素(C1-C8)烷基,单双或三卤素(C1 -C8)-烷氧基,羟基,硝基,羧基,甲酰基,-SO3H,-OSO3H,(R11O)2P(O)-,(R11O)2P(O)-O-,氨基,(C1-C8)-烷基氨基,二((C1-C8)烷基)氨基,(C5-C14)芳基(C1-C6)烷基氨基或(C5-C14)芳基氨基,(C1-C8)烷基,(C5-C14)-芳基,任选被取代的杂环由氧代,(C5-C14)芳基(C1-C6)烷基,氨基-(C1-C6)-烷基, 8)-烷基氨基(C1-C6)-烷基,二-((C1-C8)烷基)氨基-(C1-C6)-烷基,羟基(C1-C6)烷基,(C1-C6)烷氧基(C1-C6 )烷基,(C1-C8)-烷氧基(可选地被一个或多个氧原子打断),(C5-C14)芳基-(C1-C6)-烷氧基,(C5-C14)-芳氧基,羟基-(C1-C6)烷氧基,(C1-C6)-烷氧基-(C1-C6)亚烷氧基,氨基-(C1-C6)-烷氧基,(C1-C6)-烷氨基-(C1-C6)-烷氧基,二((C1-C8)-烷基)氨基-(C1-C6)亚烷基氧基,亚甲基二氧基,(C1-C6)-烷氧基羰基,(C1-C6)-烷基羰基,(C5-C14)芳基-(C1-C6)-亚烷基羰基,(C5-C14)-芳基羰基,(C1-C6)-烷基氨基羰基,(C1-C6)烷酰基氨基,(C1-C6)-烷基磺酰基氨基,(C5-C14)-芳基磺酰基氨基,(C5-C14)-芳基-(C1-C6) -亚烷基磺酰基氨基,(C1-C6)-烷基氨基磺酰基,(C5-C14)-芳基-(C1-C6)-亚烷基-氨基磺酰基,(C1-C6)-烷基磺酰基,(C5-C14)-芳基- (C1-C8)亚烷基磺酰基或(C5-C14)-芳基磺酰基,所述烷基,芳基或杂环基是未被取代或取代的我的smos在上述一个或几个基团的d中,-R 11表示氢,可能的所有立体异构形式及其混合物的氢,(C 1 -C 10)烷基,(C 6 -C 14)芳基或(C 6 -C 14)芳基(C 1 -C 6)烷基。以及其生理上可接受的加成盐和前药。 -B代表(C1-C4)亚烷基-CH = CH-基团或(C1-C4)亚烷基-环丙烯基团,所述环丙烯基团或-CH = CH-未被取代或被基团R2和/或R3取代, -R 1表示氢原子,-SO 3 H基团,未被取代或被R 2所定义的基团取代的(C 1 -C 6)烷基,或表示与环碳形成A碳键的CH 2基。与苯基稠合的6键环

著录项

  • 公开/公告号ES2243725T3

    专利类型

  • 公开/公告日2005-12-01

    原文格式PDF

  • 申请/专利权人 AVENTIS PHARMA S.A.;

    申请/专利号ES20020730383T

  • 发明设计人 BABIN DIDIER;WESTON JOHN;

    申请日2002-05-02

  • 分类号C07D401/12;C07D233/60;A61K31/4725;A61K31/4164;A61P31/10;

  • 国家 ES

  • 入库时间 2022-08-21 21:36:05

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