Beecham Group Plc

Novartis International Pharmaceutical, Ltd.

Abbott Laboratories Corporation

Beecham Plc

Michael R Harnden

Richard Lewis Jarvest

Paul G Wyatt

David M Duckworth

Stuart Bailey

Leslie J Jennings

Graham R Geen

Martin J Parratt

Nicholas David Wright

Halina T Serafinowska

Antiviral guanine derivatives

Antiviral phosphono-alken derivatives of purines

Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydrogen or hydroxy; and

Antiviral purine derivatives with improved gastrointestinal absorption

A compound of formula (I) ##STR1## or a salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, acyl or phosphate, provided that when one of R.sub.1 or R.sub.2 is phosphate, the other is hydrogen; or R.sub.1 and R.sub.2 are joined together to form a cyclic acetal group, a cyclic carbonate group or a cyclic phosphate group. Processes for preparing these compounds and their use in therapy is also described.

Purine derivatives

Compounds of formula (I), and pharmaceutically acceptable salts thereof ##STR1## wherein R.sub.1 is hydroxy, amino, chloro or OR.sub.7 wherein

Antiviral purine compounds

The present invention provides antiviral compounds of Formula (I): ##STR1## pharmaceutical compositions prepared therefrom, and methods of treatment of viral infections therewith.

A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 is hydroxy or amino;

Antiviral phosphonylalkoxy purines

Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydroxy or amino;

Antiviral purine derivatives

A compound of formula (I) ##STR1## or a salt or acyl derivative thereof, in which X represents chlorine, C.sub.1-6 alkoxy, phenoxy, phenyl C.sub.1-6 alkoxy, NH.sub.2, --OH or --SH, is useful in treating viral infections.

Guanine derivatives

Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydroxy, amino, chloro or OR.sub.7 wherein

Purine derivatives having antiviral activity

Compounds of formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydrogen or CH.sub.2 OH;

A crystalline monohydrate of the compound of formula (A) or a crystalline sodium salt monohydrate of the compound of formula (A): ##STR1## having antiviral activity, processes for their preparation and their use as pharmaceuticals.

Crystalline purine compounds

Thiazolinone analogues of indolmycin having anti-viral activity as well as a degree of antibacterial and antimycoplasmal activity in contrast to the known indolmycin which has only some antibacterial activity. Tautomers and a single enantiomer or mixture of enantiomers are included. Intermediates are described which are cyclized to produce the active antiviral substances. Suitable dosage forms and amounts are set forth and various routes of administration included including administration to the respiratory tract as by insufflation or inhalation.

Antiviral 2-amino-5-[1-(indol-3-yl)alkyl]-2-thiazolin-4-ones

A novel series of 2-amino-5-spiro substituted oxazolin-4-ones and intermediates for making said compounds. These compounds are prepared by first converting the appropriately substituted cycloketone to the corresponding cyclocyanohydrin; converting this compounds to the corresponding hydroxy acid; esterifying the hydroxy acid, and finally cyclizing the hydroester to form the 2-amino-5-spiro substituted oxazolin-4-one. These compounds exhibit central nervous system activity and are active as either stimulants or depressants, and some are useful as performance enhancers.

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Epsom, United Kingdom

Michael R Harnden