Amersham Pharmacia Biotech UK Limited

Nycomed Amersham Plc

Medical Research Council

Daniel M Brown

David Loakes

Alan L Hamilton

Clifford Leslie Smith

Adrian Christopher Simmonds

Shiv R Kumar

Mark McDougall

Satyam Nampalli

Fergal Hill

David Williams

Jan Balzarini

William Jonathan Cummins

Kei Moriyama

Patrick Finn

Ermanno Gherardi

Kazuo Negishi

Manuella Carla Zaccolo

Disclosed is a pharmaceutical composition comprising a ribonucleoside analogue in accordance with general formula I or II as herein defined, in admixture with a physiologically acceptable excipient diluent or carrier.

Inhibition of viruses

Nucleoside analogues or base analogues having structure (I), where X&equals;O or NH or S, Y&equals;N or CHR or CR , W&equals;N or NR or CHR or CR or S, n&equals;1 or 2; each R is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR where R is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.

Base analogues

Nucleoside analogues have structure (2) wherein Q is H or a sugar moiety or sugar analogue or a modified sugar or a nucleic backbone or backbone analogue, W is an alkylene or alkenylene chain of 0-5 carbon atoms, any of which may carry a substituent R , X is O or N or NR or CR , X&prime; is O or S or N, provided that when X&prime; is O or S, then X is C, Y is CH or N, R is NH or SMe or SO Me or NHNH , each of R and R is independently H or F or alkyl or alkenyl or aryl or acyl or a reporter moiety, R is independently H or alkyl or alkenyl or aryl or acyl or a reporter moiety, and R is H or &boxH;O or F or alkyl or aryl or a reporter moiety.

Tricyclic base analogues

Nucleoside analogues containing the degenerate base analogue P and derivatives thereof are provided with reporter moieties preferably comprising signal moieties. The nucleoside analogues are useful for labeling DNA or RNA or for incorporating in oligonucleotides.

Nucleoside analogues

Nucleoside analogues in which a group M replaces the natural base where M is (1) or (2) or (3), where each of X,, X,and X,are C or N, each of R,and R,is the same or different and each is H, NO,, CO, COR,, OR,, CN, O, CON(R,),, COOR,, SO,R,, SO,R,, SR,, NHCHO, (CH,),(R,),, halogen, or a reporter moiety, each of R,and R,is H or hydrocarbyl or a reporter moiety, and n is 0-4. The analogues are substrates for polymerase and terminal transferase enzymes.

Relating to mutagenesis of nucleic acids

Growing community of inventors

Cambridge, United Kingdom

Daniel M Brown