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    • 3. 发明申请
    • PENEM DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    • 派宁衍生物,其制剂和含有它们的药物组合物
    • WO1994006803A1
    • 1994-03-31
    • PCT/EP1993002493
    • 1993-09-15
    • A. MENARINI INDUSTRIE FARMACEUTICHE RIUNITE ...ISTITUTO LUSOFARMACO D'ITALIA S.P.A.ALTAMURA, MariaARCAMONE, Federico, MariaPERROTTA, EnzoPESTELLINI, VittorioSBRACI, PieroCASCIO, Giuseppe
    • A. MENARINI INDUSTRIE FARMACEUTICHE RIUNITE ...ISTITUTO LUSOFARMACO D'ITALIA S.P.A.
    • C07D499/88
    • C07D499/88
    • Described are penems derivatives of general formula (I) wherein R1 is chosen in the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, C3-C7 cycloalkyl, optionally protected C1-C6 hydroxyalkyle; R2 is chosen in the group consisting of carboxyl group free or esterified with a group easily activated "in vivo", carboxylate anion; R3 is chosen in the group consisting of H, C1-C4 alkyl optionally substituted; R4 is chosen in the group consisting of: H, C1-C6 alkyl optionally substituted, C1-C6 hydroxyalkyl optionally substituted, C1-C6 mercaptoalkyl optionally substituted, C1-C6 aminoalkyl optionally substituted, C1-C6 alkyl substituted by a quaternary ammonium group, C1-C6 carboxyalkyl optionally substituted, cycloalkyl, aryl, arylalkyl, heterocyclyl-alkyl optionally substituted, saturated or unsaturated heterocycle wherein the heteroatoms in the heterocyclic ring can be N, O, S, or R3 and R4 linked together form a heterocyclic ring having 3-7 atoms, optionally substituted, saturated or unsaturated which can contain other heteroatoms as O, N, S. R5 and R6 independently from one another are chosen in the group consisting of: H, C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 mercaptoalkyl, C1-C6 aminoalkyl, alkenyl, cycloalkyl, aryl, arylalkyl, alkylaryl, heterocyclyl-alkyl, C1-C6 alkyl carboxyamide wherein the alkyl group can be linear or branched (all these groups optionally substituted), or R5 and R6 taken together form an heterocyclic ring having 3-7 atoms optionally substituted, n is chosen in the group consisting of: 1, 2, 3; and their pharmaceutically acceptable salts.
    • 描述的是通式(I)的青蒿衍生物,其中R 1选自H,C 1 -C 6烷基,C 1 -C 6烷氧基,C 3 -C 7环烷基,任选保护的C 1 -C 6羟基烯烃; R2选自无羧基或酯基化,易于活化的“体内”,羧酸根阴离子; R3选自H,任选取代的C 1 -C 4烷基; R4选自:任选取代的H,任选取代的C 1 -C 6烷基,任选取代的C 1 -C 6羟基烷基,任选取代的C 1 -C 6巯基烷基,任选取代的C 1 -C 6氨基烷基,被季铵基团取代的C 1 -C 6烷基, C 1 -C 6羧基烷基任选取代的,环烷基,芳基,芳基烷基,杂环基 - 烷基任选取代的饱和或不饱和杂环,其中杂环中的杂原子可以是N,O,S或R 3和R 4连接在一起形成具有3 -7个原子,任选取代的,饱和或不饱和的,其可以含有其它杂原子作为O,N,S。R5和R6彼此独立地选自:H,C1-C6烷基,C1-C6羟基烷基,C1 -C 6巯基烷基,C 1 -C 6氨基烷基,烯基,环烷基,芳基,芳基烷基,烷基芳基,杂环基 - 烷基,C 1 -C 6烷基羧酰胺,其中烷基可以是直链或支链(所有这些基团任选取代) d R6一起形成任选取代的具有3-7个原子的杂环,n选自:1,2,3; 及其药学上可接受的盐。