发明名称 PYRIMIDINE DERIVATIVES FOR LABELED BINDING PARTNERS
摘要 Compounds having particular interest as labels and various novel uses in diagnostics and therapeutics are provided which have structure (1), wherein R<1> is a binding partner, a linker or H; a and b are 0 or 1, provided that the total of a and b is 0 or 1; A is N or C; X is S, O, -C(O)-, NH or NCH2R<6>; Y is -C(O)-; Z is taken together with A to form an aryl or heteroaryl ring structure comprising 5 or 6 ring atoms wherein the heteroaryl ring comprises a single O ring heteroatom, a single N ring heteroatom, a single S ring heteroatom, a single O and a single N ring heteroatom separated by a carbon atom, a single S and a single N ring heteroatom separated by a carbon atom, 2 N ring heteroatoms separated by a carbon atom, or 3 N ring heteroatoms at least two of which are separated by a carbon atom, and wherein the aryl or heteroaryl ring carbon atoms are unsubstituted with other than H or at least 1 nonbridging ring carbon atom is substituted with R<6> or =O; R<6> is independently H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, NO2, N(R<3>)2, CN or halo, or an R<6> is taken together with an adjacent R<6> to complete a ring containing 5 or 6 ring atoms; R<3> is a protecting group or H; and tautomers, solvates and salts thereof; and provided that where a is 0, b is 1, and R<1> is ( alpha ) in which D<2> is independently hydroxyl, blocked hydroxyl, mono-, di- or triphosphate, or an oligodeoxyribonucleotide otherwise containing only the bases A, G, T and C; and D<3> is H or OH; then Z is not unsubstituted phenyl. Also provided are novel intermediates and methods for the preparation and use of the structure (1) compounds.
申请公布号 WO9507918(A2) 申请公布日期 1995.03.23
申请号 WO1994US10536 申请日期 1994.09.16
申请人 GILEAD SCIENCES, INC. 发明人 MATTEUCCI, MARK, D.;JONES, ROBERT, J.;LIN, KUEI-YING
分类号 C12N15/09;A61K31/565;A61K31/70;A61K31/7042;A61K31/7052;C07D239/46;C07D239/47;C07D239/52;C07D239/54;C07D405/04;C07D487/04;C07D487/14;C07D491/14;C07D498/04;C07D498/14;C07F7/22;C07F9/09;C07H19/00;C07H19/04;C07H19/06;C07H19/22;C07H21/00;C07H21/02;C12P19/34;C12Q1/68 主分类号 C12N15/09
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