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    • 53. 发明申请
    • Compound
    • 复合
    • US20060074060A1
    • 2006-04-06
    • US11234868
    • 2005-09-23
    • Nigel VickerHarshani LawrenceGillian AllanChristian BubertDelphine Sophie FischerAlan PurohitMichael ReedBarry Victor Potter
    • Nigel VickerHarshani LawrenceGillian AllanChristian BubertDelphine Sophie FischerAlan PurohitMichael ReedBarry Victor Potter
    • A61K31/58C07J71/00
    • C07J71/00C07J41/00
    • There is provided a compound of Formula (I) wherein (I) R2 is selected from (i) an alkyloxyalkyl group (ii) a nitrile group, and wherein R2 is capable of forming a hydrogen bond (iii) alkylaryl group, wherein the aryl group is substituted by other than a C1-10 group (iv) alkenylaryl group wherein the aryl group is substituted (v) alkylheteroaryl group, wherein when heteroaryl group comprises only C and N in the ring, the aryl group is substituted by other than a methyl group (vi) alkenylheteroaryl group, (vii) ═N—O-alkyl or ═N—O—H group (viii) branched alkenyl (ix) alkyl-alcohol group (x) amide or alkylamide wherein (a) the alkyl of the alkylamide is —CH2— or —Ch2Ch2—, (b) the amide is di-substituted and/or (c) the amide is substituted with at least one of alkyl heterocycle group, alkenyl heterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) —CHO so that R1 together with R3 provide the enol tautomer (a); OR R2 together with R3 form (xii) a pyrazole wherein (a) R4 is ═N—O-alkyl or ═N—O—H group, (b) the pyrazole is substituted with one of alkyl-OH group, alkyl ester group, alkyloxyalkyl group, branched alkyl group, and an amide and/or (c) the 2 position is substituted with a group selected from —OH and —O-hydrocarbyl (xiii) a heteroaryl ring to provide a compound of the formula (b); (II) R2 is selected from groups capable of forming a hydrogen bond, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group and a sulphonamide group; and (III) R3 is selected from —OH, ═O, or a C(═O)—mimetic.
    • 提供式(I)化合物,其中(I)R 2选自(ⅰ)烷氧基烷基(ⅱ)腈基,其中R2能够形成氢键(ⅲ)烷基芳基,其中芳基 基团被取代的芳基(ⅴ)烷基杂芳基以外的C 1-10基团(ⅳ)链烯基芳基取代,其中当杂芳基仅在环中仅包含C和N时,芳基被除了 甲基(vi)烯基杂芳基,(vii)-NO-烷基或-NOH基(viii)支链烯基(ix)烷基 - 醇基(x)酰胺或烷基酰胺,其中(a)烷基酰胺的烷基是-CH2- 或-C 2 -C 12 - ,(b)酰胺是二取代的和/或(c)酰胺被烷基杂环基,烯基杂环基,烷基杂芳基,烯基杂芳基,杂芳基,烷基胺基,烷氧基烷基中的至少一个 基团,烷基芳基,直链或支链烷基,(xi)-CHO,使得R1起始 与R3提供烯醇互变异构体(a); OR 2与R 3一起形成(xii)吡唑,其中(a)R4是-NO-烷基或-NOH基,(b)吡唑被烷基-OH基,烷基酯基,烷氧基烷基,支链烷基 基团和酰胺和/或(c)2位被选自-OH和-O-烃基(xiii)杂芳基环的基团取代,以提供式(b)的化合物; (II)R2选自能够形成氢键的基团,氨基磺酸酯基,膦酸酯基,硫代膦酸酯基,磺酸酯基和磺酰胺基; 和(III)R 3选自-OH,-O或C(-O) - 模仿物。