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394 条记录 (耗时 0.028 秒)

    Preparation of purines
    42.
    发明申请
    Preparation of purines 失效

    公开(公告)号：US20050101570A1

    公开(公告)日：2005-05-12

    申请号：US11011352

    申请日：2004-12-14

    申请人： John Mansfield Dales

    发明人： John Mansfield Dales

    IPC分类号： C07D473/40 ,  C07D473/00 ,  C07D473/32 ,  A61K31/675 ,  A61K31/522 ,  C07D473/14

    CPC分类号： C07D473/00

    摘要： A process for the preparation of a compound of formula (A) wherein: X is hydrogen or hydroxy, chloro, C1-6 alkoxy or pheny C1-6 alkoxy; and Ra and Rb are hydrogen, or acyl or phosphate derivatives thereof, which process comprises: (i) the preparation of a compound of formula (I) wherein R1 is C1-6 alkyl, or phenyl C1-6 alkyl in which the phenyl group is optionally substituted; R2 is hydrogen, hydroxy, chlorine, C1-6 alkoxy, phenyl C1-6 alkoxy or amino; and R3 is halogen, C1-6 alkylthio, C1-6 alkylsulphonyl, azido, an amino group or a protected amino group, which preparation comprises the reaction of a compound of formula (II) wherein R2 and R3 are as defined for formula (I) with a compound of formula (V) wherein L is a leaving group and R1 is as defined for formula (I), to give a compound of formula (VI), and thereafter converting the intermediate compound of formula (VI) to a compound of formula (I) via decarboxylation, and as necessary or desired, interconverting variables R1, R2 and R3 to further values of R1, R2 and R3; (ii) the conversion of the resulting compound of formula (I) to a compound of formula (A) by converting variable R3, when other than amino, to amino, reducing the ester groups CO2R1 to CH2OH and optionally forming acyl or phosphate derivates thereof, and as necessary or desired converting variable R2 in the compound of formula (I) to variable X in the compound of formula (A); characterized in that R2 is chloro in formula (I).

    Antiviral compounds
    43.
    发明申请
    Antiviral compounds 失效
    抗病毒化合物

    公开(公告)号：US20040002475A1

    公开(公告)日：2004-01-01

    申请号：US10183878

    申请日：2002-06-25

    发明人： Gholam Hossein Hakimelahi

    IPC分类号： A61K031/7076 ,  A61K031/675 ,  A61K031/522 ,  C07H019/04 ,  C07D473/18 ,  C07D473/32

    CPC分类号： C07H19/04

    摘要： This invention relates to purine compounds of formula (I): 1 R1 is NH2 or OH; R2 is H or NH2; R3 is H or alkyl; each of m and n, independently, is 1, 2, 3, or 4; X is O, S, or NH; and Y is H, halogen, ORa, P(O)(ORa)2, or P(O)(ORa)(ORb), in which Ra is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, and Rb is 2 wherein A is adenine, guanine, cytosine, uracil, or thymine; Rc is H or OH; Rd is H or alkyl; Re is H, alkyl, or 5-ethylidene-(3,4-dialkoxyl)-furan-2-one; provided that if R1 is NH2, R2 is H; and if R1 is OH, R2 is NH2.

    摘要翻译： 本发明涉及式（I）的嘌呤化合物：R1是NH2或OH; R2是H或NH2; R3是H或烷基; m和n各自独立地是1,2,3或4; X是O，S或NH; 并且Y是H，卤素，OR a，P（O）（OR a）2或P（O）（OR a）（OR b）） 烷基，芳基，杂芳基，环基，杂环基和R b是其中A是腺嘌呤，鸟嘌呤，胞嘧啶，尿嘧啶或胸腺嘧啶; R c是H或OH; R d是H或烷基; R e是H，烷基或5-亚乙基 - （3,4-二烷氧基） - 呋喃-2-酮; 条件是如果R1是NH2，R2是H; 并且如果R 1是OH，则R 2是NH 2。