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    • 6. 发明授权
    • Substituted pyrrolo[2,3-d]pyrimidines as antifolates
    • 取代的吡咯并[2,3-d]嘧啶作为抗叶酸剂
    • US07951812B2
    • 2011-05-31
    • US12016528
    • 2008-01-18
    • Michael J. RobertsSimon Pedder
    • Michael J. RobertsSimon Pedder
    • C07D487/04A61K31/519A61P35/00A61P29/00A61P11/06A61P19/02
    • C07D487/04
    • The present invention is directed to antifolate compounds having the structure wherein: X is CHR9 or NR9; Y1, Y2, and Y3 independently are O or S; V1 and V2 independently are O, S, or NZ; Z is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, or alkaryl; R1 and R2 independently are H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, or alkaryl; R3 is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, hydroxyl, or halo; and R4, R5, R6, R7, R8, and R9 independently are H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, acyl, —C(O)-alkyl, —C(O)-alkenyl, or —C(O)—alkynyl; as well as pharmaceutically acceptable esters, amides, salts, solvates, and prodrugs thereof. The compounds are useful in pharmaceutical compositions and in methods of treating multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.
    • 本发明涉及具有以下结构的抗叶酸化合物:其中:X为CHR 9或NR 9; Y1,Y2和Y3独立地为O或S; V1和V2独立为O,S或NZ; Z是H,任选取代的烷基,任选取代的烯基,任选取代的炔基或烷芳基; R 1和R 2独立地为H,任选取代的烷基,任选取代的烯基,任选取代的炔基或烷芳基; R 3是H,任选取代的烷基,任选取代的烯基,任选取代的炔基,任选取代的烷氧基,羟基或卤素; R 4,R 5,R 6,R 7,R 8和R 9分别是H,任选取代的烷基,任选取代的烯基,任选取代的炔基,酰基,-C(O) - 烷基,-C(O) - 烯基或-C (O) - 炔基; 以及其药学上可接受的酯,酰胺,盐,溶剂合物和前药。 该化合物可用于药物组合物和治疗多种病症的方法,包括异常细胞增殖,炎性疾病,哮喘和关节炎。