Medivir Ab

Nils-Gunnar Johansson

Xiao-Xiong Zhou

Per Engelhardt

Marita Hogberg

Bjorn G Lindborg

David Bernard Smith

Joseph Armstrong Martin

Ian Gilbert

Anna Winqvist

Gian Filippo Ruda

Corinne Nguyen

Alessandro Schipani

Ganasan Kasinathan

Dolores Gonzalez Pacanowska

Genaidy Kalyanov

M Robert Leanna

Michael Rasmussen

Genadiy Kalayanov

Genadiy Kalyanov

Björn Lindborg

4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydrofuran-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.

Antiviral nucleosides

Methods and novel intermediates for the preparation of and the treatment with acyclic nucleoside derivatives of the formula: 

Acyclic nucleoside derivatives

Deoxyuridine derivatives of the formula where

Dutpase inhibitors

4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.

Deoxyuridine derivatives of the formula (I) where Ris H or various substituents; D is &#x2014;NHCO&#x2014;, &#x2014;CONH&#x2014;, -0-, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;CH&#x2550;CH, &#x2014;C&#x2261;C&#x2014;, &#x2014;NR&#x2014;; Ris hydrogen or various substituents; Ris H, C-Calkyl, C-Calkanoyl; E is Si or C; R, Rand Rare independently selected from C-Calkyl, C-Calkenyl, C-Calkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;CHR&#x2014;, &#x2014;C(&#x2550;O)&#x2014;; J is &#x2014;CH&#x2014;, or when G is CHRmay also be &#x2014;O&#x2014; or &#x2014;NH&#x2014;; Ris H, F, &#x2014;CH, &#x2014;CHNH, &#x2014;CHOH; &#x2014;OHRis H, F, &#x2014;CH, &#x2014;CHNH, &#x2014;CHOH, &#x2014;CH(OH)CH, CH(NH)CH; or Rand Rtogether define an olefinic bond, or together form a &#x2014;CH-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria. 

DUTPase inhibitors

Deoxyuridine derivatives of Formula (I'); where A is O, S or CH; B is O, S or CHR; Ris H, or various substituents; Ris H, F; Ris H, F, OH, NH; or Rand Rtogether form a chemical bond; D is &#x2014;NHCO&#x2014;, &#x2014;CONH&#x2014;, &#x2014;O&#x2014;, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;CH&#x2550;CH, &#x2014;C&#x2261;C&#x2014;, &#x2014;NR&#x2014;; Ris hydrogen or various substituents; Ris H, C-Calkyl, C-Calkanoyl; E is Si or C; R, Rand Rare independently selected from C-Calkyl, C-Calkenyl, C-Calkynyl, or a stable monocyclic, bicyclic or tricyclic ring system have utility in the prophylaxis of treatment of parasitic diseases such as malaria. 

Dutpase Inhibitors

Compounds of the Formula I ##STR1## where one of R.sub.1 and R.sub.2 is --C(O)CH(CH(CH.sub.3).sub.2)NH.sub.2 or --C(O)CH(CH(CH.sub.3)CH.sub.2 CH.sub.3)NH.sub.2;

Growing community of inventors

Huddinge, Sweden

Nils-Gunnar Johansson