The University of Birmingham

Mitsubishi Kasei Corporation

Beecham Group Plc

British Technology Group Limited

Stichting Rega Vzw

Rega Instituut Vzw

Richard T Walker

Erik D De Clercq

Albert S Jones

Hiromichi Tanaka

Masanori Baba

Tadashi Miyasaka

Masaru Ubasawa

Paul L Coe

Stewart A Noble

Gabriel A Verhelst

Philip J Barr

Compounds of formula I or a pharmaceutically acceptable salt thereof: ##STR1## in which formula R.sub.1 represents an aliphatic hydrocarbyl group; Ar represents a substituted or unsubstituted aromatic nucleus;

Antiviral compounds

1'-Deoxy-5-ethyl-4'-thio-.beta.-uridine as a compound including its physiologically functional derivatives, pharmaceutical compositions containing it and methods of treating herpes virus infections are described.

Antiviral pyrimidine nucleosides and methods for using same

The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I'] and having antiviral activity, particularly antiretroviral activity such as anti-HIV activity: ##STR1## and pharmaceutical compositions having antiviral activity and comprising the above-described derivative(s) as an active ingredient.

Pyrimidine derivatives and anti-viral agent containing the same as

Pyrimidine 4'-thionucleosides of the formula I ##STR1## wherein Y is hydroxy or amino, and X is chloro, bromo, iodo, trifluoromethyl, C.sub.2-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 haloalkenyl or C.sub.2-6 alkynyl and physiologically functional derivatives thereof. These compounds have utility as anti-vital agents.

Antiviral pyrimidine nucleosides

A pyrimidine nucleoside derivative and pharmaceutically acceptable salt thereof specified by the presence of ethyl group or isopropyl group at 5-position of the pyrimidine ring and the presence of a (substituted) phenylthio or a (substituted) benzyl group at 6-position of the pyrimidine ring is provided. The pyrimidine nucleoside derivative and pharmaceutically acceptable salt thereof show a markedly higher anti-retroviral activity than conventional analogous compounds and have a relatively low toxicity against the host cells, and therefore, are useful as an active ingredient of antiviral agent.

Pyrimidine nucleoside derivative and antiviral agent containing the

6-substituted acyclopyrimidine nucleoside derivatives and antiviral

The novel substance E-5-(2-bromovinyl)-2'-deoxyuridine and its corresponding iodovinyl derivative are gifted with specific antiviral activities towards herpes simplex virus. They may be synthesized by a condensation reaction followed by separation of anomers.

2'Deoxy-5-(2-halogenovinyl)-uridines, pharmaceutical compositions and

The compound of formula (I): ##STR1## wherein X is CFCl; and C.sub.1-6 alkanoyl esters and/or phosphate esters thereof, is active against herpes viruses.

Antiviral agents, their preparation and use

The invention relates to E-5-(2-halogenovinyl)-2'-deoxycytidines, e.g. E-5-(bromovinyl)-2'-deoxycytidine and E-5-(2-iodovinyl)-2'-deoxycytidine. These substances are endowed with specific antiviral activities towards herpes simplex virus and with an extremely low toxicity which makes them useful in antiviral medicines and for treatment of virus diseases in man and animal. They may be synthesized by introduction of an E-5-(2-halogenovinyl) sidechain into 2'-deoxycytidine, or by condensation of a trialkylsilyl derivative of E-5-(2-halogenovinyl)-cytosine with a hydroxyl-protected reactive derivative of 2'-deoxy-D-erythro-pentofuranose.

Growing community of inventors

Birmingham, United Kingdom

Richard T Walker