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    • 74. 发明申请
    • ORGANO-PHOSPHORUS COMPOUNDS AND THEIR UTILIZATION
    • 磷光体有机物及其用途
    • WO00037477A1
    • 2000-06-29
    • PCT/EP1999/010274
    • 1999-12-22
    • A61K31/675A01N57/24A61P31/00A61P31/04A61P31/12C07F9/553C07F9/572C07F9/58C07F9/59C07F9/62C07F9/6561A61P33/00
    • C07F9/62C07F9/5537C07F9/5722C07F9/592C07F9/65616
    • The invention relates to organo-phosphorus compounds of formula (I), wherein A is selected from the group consisting of a (C1-9) alkylene radical, -C-O-C- and -C-N-C- or A corresponds to formula (II), wherein one or more carbon atoms selected from the group consisting of C3, C4, C5 and their substituents can also be absent and at least one of the substituents of B1 to B10 is a C3-8-cycloalkyl-(C0-9)-alkyl group in which R1 is selected from the group consisting of five and six membered heterocycles having at least one nitrogen atom in the ring or polycyclic carbon atoms containing one of said heterocycles, wherein at least one of said nitrogen atoms belongs to a hydroxamic acid group or a hydroxamic acid ester group. The invention also relates to the utilization of the above-mentioned compounds in the therapeutic and prophylactic treatment of infections in human beings and animals caused by virus, bacteria, fungi and parasites and as fungicides, bactericides and herbicides in plants.
    • 其中选自(C 1-9)亚烷基的基团,和-COC-选择-CNC- A中的通式(I)的有机磷化合物,或其中A是式(II),其特征在于,一个 或多个选自C3,C4,C5,与他们的取代基一起也可以省略选择的碳原子数,和B1中的至少一个取代基的至B10呈现C 3-8 - 环烷基 - (C0-9) - 烷基,其中R1 由具有该组中的环或含有这些杂环中的至少一个的多环烃的至少一个氮原子,包括5-和6-元杂环,选自其中这些氮原子的异羟肟酸基团中的至少一个或Hydroxamsäureestergruppe所属以及其使用的 治疗性和预防性治疗人类和动物中引起的感染病毒,细菌,真菌和寄生虫,和杀真菌剂,杀菌剂和除草剂 植物。
    • 75. 发明申请
    • FIVE-MEMBERED HETEROARYL COMPOUNDS
    • 五分共振化合物
    • WO00001688A1
    • 2000-01-13
    • PCT/JP1999/003549
    • 1999-07-01
    • C07F9/572C07D401/04A61K31/44A61K31/445A61K31/505C07D401/14C07D403/04C07D403/14C07D413/04C07F9/6558
    • C07F9/5722
    • [Problem] Provision of compounds exhibiting an excellent inhibitory activity against the production of inflammatory cytokines. [Means for solution] Compounds represented by general formula (I); or pharmacologically acceptable salts, esters or other derivatives thereof, wherein A is a five-membered heteroaryl ring; Ar and Ar are each optionally substituted aryl or the like; Q is optionally substituted arylene or the like; R is H, optionally substituted arkyl or the like; R is H, optionally substituted alkyl or the like; and R is -WR , -S(O)mWR , -N(WR )R , -PO(OR )(OR ) or the like (wherein m is 0 to 2; W is alkylene or the like; R is azido, C(=NOR )R or the like; R , R and R are each H, alkyl or the like; and R and R are each H, alkyl or the like).
    • [问题]提供对产生炎性细胞因子具有优异抑制活性的化合物。 [溶解方法]通式(I)表示的化合物; 或其药理学上可接受的盐,酯或其它衍生物,其中A是五元杂芳基环; Ar 1和Ar 2各自为任选取代的芳基等; Q是任选取代的亚芳基等; R 1是H,任选取代的烷基等; R 2是H,任选取代的烷基等; 和R 3是-WR 4,-S(O)m W R 4,-N(WR 4)R 5,-PO(OR 6)(OR 7) )等(其中m为0〜2; W为亚烷基等; R 4为叠氮基,C(= NOR 8)R 9等; R 5,R 8 >和R 9各自为H,烷基等; R 6和R 7各自为H,烷基等。