Invention Grant
US07888367B2 1-[2′,3′ -dideoxy-3′ C-(hydroxymethyl)—beta-D-erythro-pentofuranosyl] cytosine derivatives as HIV 失效
1- [2',3'-二脱氧-3'C-(羟甲基)-β-D-赤 - 戊呋喃糖基]胞嘧啶衍生物作为HIV

  • Patent Title: 1-[2′,3′ -dideoxy-3′ C-(hydroxymethyl)—beta-D-erythro-pentofuranosyl] cytosine derivatives as HIV
  • Patent Title (中): 1- [2',3'-二脱氧-3'C-(羟甲基)-β-D-赤 - 戊呋喃糖基]胞嘧啶衍生物作为HIV
  • Application No.: US11994633
    Application Date: 2006-07-05
  • Publication No.: US07888367B2
    Publication Date: 2011-02-15
  • Inventor: Xiao-Xiong ZhouChrister Sahlberg
  • Applicant: Xiao-Xiong ZhouChrister Sahlberg
  • Applicant Address: SE Huddinge
  • Assignee: Medivir AB
  • Current Assignee: Medivir AB
  • Current Assignee Address: SE Huddinge
  • Agency: Birch, Stewart, Kolasch and Birch, LLP
  • Priority: GB0513835.9 20050707
  • International Application: PCT/EP2006/063919 WO 20060705
  • International Announcement: WO2007/006707 WO 20070118
  • Main IPC: C07D493/04
  • IPC: C07D493/04 A61K31/513
1-[2′,3′ -dideoxy-3′ C-(hydroxymethyl)—beta-D-erythro-pentofuranosyl] cytosine derivatives as HIV
Abstract:
Compounds of the formula (I) wherein: R1 is independently H1—OR3, —NHR4; C1-C4 alkyl; or, when n is 2, adjacent R1 together define an olefinic bond; R2 is H; or when the gem R1 is C1-C4 alkyl, that R2 may also be C1-C4 alkyl; or when the gem R1 is —OR3, that R2 may also be —C(═O)OH or a pharmaceutically acceptable ester thereof; R3 is independently H, or a pharmaceutically acceptable ester thereof; R4 is independently H or a pharmaceutically acceptable amide thereof; R5 and R6 are H or an amine prodrug moiety n is 1, 2 or 3; and pharmaceutically acceptable salts thereof; have utility in the treatment or prophylaxis of HIV, especially reverse transcriptase mutants which allow an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.
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