Hoffmann-la Roche Inc.

Roche Palo Alto LLC

Philip Stephen Jones

David Nigel Hurst

Martin John Parratt

Michael Richard Attwood

Brian William Dymock

Francis Xavier Wilson

Paul Brittain Kay

John Herbert Merrett

Tony Michael Raynham

Kevin Edward Burdon Parkes

Sally Redshaw

Michael John Broadhurst

Christopher H Hill

Daryl Simon Walter

Ian Reginald Kilford

Adrian Liam Gill

Robert Murray McKinnell

The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV infection.

Anti-HIV pyrazole derivatives

Disclosed are compounds of the general formulawhich are oxamide derivatives and inhibitors of the enzyme inosine monophosphate dehydrogenase (IMPDH).

Oxamide IMPDH inhibitors

Disclosed are novel pyrrole derivatives, a process for their manufacture, pharmaceutical compositions containing such compounds and the use of such compounds in the treatment of HIV mediated diseases.

Pyrrole derivatives

The invention is concerned with novel benzodiazepine derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are inhibitors of the human papillomavirus E1 helicase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HPV mediated diseases.

Inhibitors of HPV E1 helicase enzyme

The invention is concerned with novel pyrazole derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV mediated process.

The invention is concerned with novel imidazolone derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents against HIV infection.

Anti-HIV imidazolone derivatives

Antiviral medicaments

The invention relates to &agr;-ketoamides of the general formula

Alpha-ketoamide derivatives

The invention provides amino acid derivatives of the formula ##STR1## wherein E represents CHO or B(OH).sub.2 ;

Amino acid derivatives

Peptidyl inhibitors of viral proteases

Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, trifluoromethyl, nitro, cyano, lower alkyl, lower alkoxycarbonyl, lower alkylthio, lower alkylsulphonyl, lower alkanoyl, aroyl, carbamoyl, mono(lower alkyl)carbamoyl or di(lower alkyl)carbamoyl, R.sup.2 is hydrogen, lower alkyl or phenyl, R.sup.3 is hydrogen or lower alkyl, R.sup.4 and R.sup.5 each is hydrogen or R.sup.4 is hydroxy and R.sup.5 is hydrogen or R.sup.4 and R.sup.5 together are a carbon-carbon bond and R.sup.6 is an aryl or N-heteroaryl group carrying a hydroxy group in the 2-position or, in the case of a N-heteroaryl group, also a N-oxide group in the 2-position, and pharmaceutically acceptable acid addition salts of these compounds of formula I which are basic, possess pronounced potassium channel activating activity and can be used as medicaments, particularly in the control or prevention of hypertension, congestive heart failure, angina pectoris, peripheral and cerebral vascular disease and smooth muscle disorders.

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Welwyn Garden City, United Kingdom

Philip Stephen Jones