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    • 2. 发明授权
    • Ribonucleoside analogs with novel hydrogen bonding patterns
    • 具有新型氢键模式的核糖核苷类似物
    • US08389703B1
    • 2013-03-05
    • US13287169
    • 2011-11-02
    • Steven A. BennerHyo-Joong Kim
    • Steven A. BennerHyo-Joong Kim
    • C07H19/048C07H21/00C07H21/02
    • C07D405/04C12P19/34
    • This invention relates to nucleoside, nucleotide, and oligonucleotide analogs that incorporate non-standard nucleobase analogs, defined to be those that present a pattern of hydrogen bonds to a paired nucleobase analog in a complementary strand that is different from the pattern presented by adenine, guanine, cytosine, and thymine. The invention is specifically concerned with nucleotide analogs that present the donor-donor-acceptor, hydrogen bonding patterns on pyrimidine analogs, and especially those that are analogs of ribonucleotides, including protected ribonucleotides suitable for phosphoramidite-based synthesis of RNA. The heterocycles on these nucleoside analogs are aminopyridones that have electron withdrawing groups attached to the position analogous to the 5-position of the ring in standard pyrimidines, including nitro, cyano, and carboxylic acid derivatives.
    • 本发明涉及包含非标准核碱基类似物的核苷,核苷酸和寡核苷酸类似物,其被定义为与互补链中的配对核碱基类似物呈现氢键图案的不同于腺嘌呤,鸟嘌呤 ,胞嘧啶和胸腺嘧啶。 本发明特别涉及呈现供体 - 供体受体的核苷酸类似物,嘧啶类似物上的氢键型,特别是涉及核糖核苷酸类似物的核苷酸类似物,包括适合于基于亚磷酰胺的RNA合成的受保护的核糖核苷酸。 这些核苷类似物上的杂环是在标准嘧啶(包括硝基,氰基和羧酸衍生物)中具有连接到类似于环的5位的位置的吸电子基团的氨基吡啶酮。
    • 7. 发明申请
    • Cyclopentenol Nucleoside Compounds Intermediates for their Synthesis and Methods of Treating Viral Infections
    • 环戊烯醇核苷化合物的合成中间体和治疗病毒感染的方法
    • US20090270431A1
    • 2009-10-29
    • US12083571
    • 2006-10-19
    • David C.K. ChuJong Hyun ChoHyo-Joong Kim
    • David C.K. ChuJong Hyun ChoHyo-Joong Kim
    • A61K31/519C07D249/04A61K31/4192A61K31/437C07D471/04C07D487/04A61P31/12
    • C07D487/04C07H19/06C07H19/10C07H19/16C07H19/20
    • The present invention relates to compounds according to the structure (I), Where B is formula (Ia), formula (Ib) or formula (Ic); A is H, OR2 or halogen (F, Cl, Br, I, preferably F or Br, more preferably F); A′ is H, OR2 or halogen (F, Cl, Br, I, preferably F or Br, more preferably F); A″ is H or OR1, with the proviso that when A′ is OR, A is H; and when A is OR2, A′ is H; X is C—R3 or N; Y is C—R3 or N; preferably X or Y is N and X and Y are not both simultaneously N; R3 is H or C1-C3 alkyl; D is H or NHR2; E is absent or H; G is O or NHR2; J is N or C—R4; K is N or C—H; R4 is H, halogen (F, Cl, Br, I), CN, —C(═O)NH2, NH2, NO2, —C═C—H (cis or trans) or —C≡C—H; Ra is H or CH3; Each R1 is independently H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate, phosphodiester group; Each R2 is independently H, an acyl group, a C1-C20 alkyl or ether group; and Pharmaceutically acceptable salts, solvates or polymorphs thereof.
    • 本发明涉及根据结构(I)的化合物,其中B为式(Ia),式(Ib)或式(Ic); A是H,OR2或卤素(F,Cl,Br,I,优选F或Br,更优选F); A'是H,OR 2或卤素(F,Cl,Br,I,优选F或Br,更优选F); A“为H或OR 1,条件是当A'为OR时,A为H; 当A为OR2时,A'为H; X为C-R3或N; Y为C-R3或N; 优选X或Y为N,X和Y不同时为N; R3是H或C1-C3烷基; D是H或NHR 2; E不存在或H; G为O或NHR 2; J为N或C-R4; K为N或C-H; R4是H,卤素(F,Cl,Br,I),CN,-C(-O)NH2,NH2,NO2,-C-C-H(顺式或反式)或-C≡C-H; Ra为H或CH3; 每个R 1独立地是H,酰基,C 1 -C 20烷基或醚基,磷酸酯,二磷酸酯,三磷酸酯,磷酸二酯基团; 每个R 2独立地为H,酰基,C 1 -C 20烷基或醚基; 和其药学上可接受的盐,溶剂化物或多晶型物。