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    • 3. 发明授权
    • Pyrimidine derivatives for labeled binding partners
    • 用于标记结合配偶体的嘧啶衍生物
    • US5763588A
    • 1998-06-09
    • US481719
    • 1995-06-07
    • Mark D. MatteucciRobert J. Jones
    • Mark D. MatteucciRobert J. Jones
    • C12N15/09A61K31/565A61K31/70A61K31/7042A61K31/7052C07D239/46C07D239/47C07D239/52C07D239/54C07D405/04C07D487/04C07D487/14C07D491/14C07D498/04C07D498/14C07F7/22C07F9/09C07H19/00C07H19/04C07H19/06C07H19/22C07H21/00C07H21/02C12P19/34C12Q1/68C07D239/70
    • C07D239/47C07D239/54C07D405/04C07D487/04C07F7/2212C07H19/06C07H19/073C07H21/00C12Q1/6816C12Q1/686Y02P20/55
    • Compounds having particular interest as labels and various novel uses in diagnostics and therapeutics are provided which have structure (1) ##STR1## wherein R.sup.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 NCH.sub.2 R.sup.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.sup.6 or .dbd.O; R.sup.6 is independently H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, NO.sub.2, N(R.sup.3).sub.2, C.tbd.N or halo, or an R.sup.6 is taken together with an adjacent R.sup.6 to complete a ring containing 5 or 6 ring atoms;, R.sup.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.sup.1 is ##STR2## in which D.sup.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.sup.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.
    • 提供具有特别感兴趣的化合物作为标记物和诊断和治疗中的各种新用途,其具有结构(1) r H; a和b为0或1,条件是a和b的总数为0或1; A是N或C; X是S,O,-C(O) - ,NH或NCH 2 R 6; Y是-C(O) - ; Z与A一起形成包含5或6个环原子的芳基或杂芳基环结构,其中杂芳基环包含单个O环杂原子,单个N环杂原子,单个S环杂原子,单个O和单个N 由碳原子分隔的环状杂原子,由碳原子分隔的单个S和单个N环杂原子,由碳原子分隔的2个N个杂原子或至少两个被碳原子分隔的3个N个环杂原子, 并且其中所述芳基或杂芳基环碳原子未被取代,除了H或至少1个非桥环碳原子被R6或= O取代; R6独立地为H,C1-C6烷基,C2-C6烯基,C2-C6炔基,NO2,N(R3)2,C 3BONDN或卤素,或R6与相邻的R6一起形成含有5 或6个环原子; R 3为保护基或H; 和其互变异构体,溶剂合物和盐类; 并且条件是当a为0时,b为1,R1为羟基,单,二或三磷酸封端,或仅含有碱基A,G,T和C的寡脱氧核糖核苷酸; D3为H或OH; 那么Z不是未取代的苯基。 还提供了用于制备和使用结构(1)化合物的新型中间体和方法。