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
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Application No.: US11994633Application Date: 2006-07-05
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Publication No.: US07888367B2Publication Date: 2011-02-15
- Inventor: Xiao-Xiong Zhou , Christer Sahlberg
- Applicant: Xiao-Xiong Zhou , Christer 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](/abs-image/US/2011/02/15/US07888367B2/abs.jpg.150x150.jpg)
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.
Public/Granted literature
- US20080221140A1 1-[2',3' -Dideoxy-3' C-(Hydroxymethyl) - Beta-D-Erythro-Pentofuranosyl] Cytosine Derivatives as Hiv Public/Granted day:2008-09-11
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