Burroughs Wellcome Co.

Glaxo Wellcome Inc.

University College Cardiff Consultants Limited

Other

Alan T Hudson

Victoria S Latter

Winston E Gutteridge

Anthony W Randall

Sadie Vile

David Drysdale Miller

Mary Pudney

Laddawan Chunchatprasert

Patrick Vivian Shannon

Paul Barraclough

Ann Louise Walker

George Stuart Cockerill

Stephen Barry Guntrip

Kathryn Jane Smith

Karl Witold Franzmann

William H Richards

Martin John Page

Pierre P Debont

Stephen Carl McKeown

Substituted heteroaromatic compounds of formula (A) wherein X is N or CH; in which (a) represents a fused 5, 6 or 7-membered heterocyclic ring and R,is a group ZR,wherein Z is joined to R,through a (CH,)p group in which p is 0, 1, or 2 and Z represents a group V(CH,), V(CF,), (CH,)V, (CF,)V, V(CRR&prime;), V(CHR) or V where R and R&prime; are each C,alkyl and in which V is a hydrocarbyl group containing 0, 1 or 2 carbon atoms, carbonyl, dicarbonyl, CH(OH), CH(CN), sulphonamide, amide, O, S(O),or NR,where R,is hydrogen or R,is C,alkyl; and R,is an optionally substituted C,cycloalkyl or an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety; or R,is a group ZR,in which Z is NR,, and NR,and R,together form an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety, are protein tyrosine kinase inhibitors. The compounds are described, as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of psoriasis, fibrosis, atherosclerosis, restenosis, auto-immune disease, allergy, asthma, transplantation rejection, inflammation, thrombosis, nervous system diseases, and cancer.

Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors

The present invention relates to heterocyclic compounds which have been found to have anti-tumour activity. More specifically, the invention concerns pyrrolo[2,3-b]carbazoles and 1H-[1] benzothieno [2,3-f] indoles, methods for their preparation, pharmaceutical formulations containing them and their use as anti-tumour agents. The compounds have low toxicity against normal cell lines whilst exhibiting anti-tumour cell activity.

Antitumor tetracyclic compounds

The present invention relates to the use of 2-�4-(4-chlorophenyl)cyclohexyl!-3-hydroxy-1,4-naphthoquinone or a physiologically acceptable salt or other physiologically funtional derivative thereof for the manufacture of a medicament for the treatment and/or prophylaxis of toxoplasmosis in animals, to pharmaceutical compositions for the treatment and/or prophylaxis of toxoplasmosis, comprising said compound as active ingredient and to a method of treating or preventing toxoplasmosis in an animal which comprises administering to said animal an effective amount of said compound.

Medicaments for the treatment of toxoplasmosis

Pyrrolo�3,2-b-!-carbazoles and 1H�1!benzothieno �2,3-f! indoles having

The present invention relates to pharmaceutical compositions for the treatment and/or prophylaxis of protozoal infections caused by Kinetoplastida, Apicomplexa, Anaerobic protozoa and Microsporidia comprising 2-�4-(4-chlorophenyl)cyclohexyl!-3-hydroxy-1,4-naphthoquinone or a physiologically acceptable salt or other functional derivative thereof as active ingredient and to a method of treating or preventing said protozoal infections in an animal which comprises administering to said animal an effective amount of said compound.

Antiprotozoal medicaments

Heterocyclic compounds

Use of 2-(4-(4-chlorophenyl)cyclohexyl)-3-hydroxy-1,4-Naphthoquinone for

Method of treatng protozoal infections caused by microsporidia

The present invention relates to pharmaceutical compositions for the treatment and/or prophylaxis of protozoal infections caused by Kinetoplastida, Apicomplexa, Anaerobic protozoa and Mircosporidia comprising 2-[4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone or a physiologically acceptable salt or other functional derivative thereof as active ingredient and to a method of treating or preventing siad protozoal infections in an animal which comprises administering to said animal an effective amount of siad compound.

Method for treating animals infected with Babesia spp.

A method for treating or preventing a Pneumocystis carinii infection in a mammal by administering a certain naphthoquinone compound or physiologically acceptable salts thereof.

Medicaments

Novel antiprotozoal naphthoquinones having the general formula ##STR1## (wherein either R.sup.1 is hydrogen and R.sup.2 is selected from C.sub.1-6 alkoxy, aralkoxy, C.sub.1-6 alkyl-C.sub.1-6 alkoxy, phenyl substituted by one or two groups selected from halogen and C.sub.1-6 alkyl, halogen and perhalo-C.sub.1-6 alkyl; or R.sup.1 and R.sup.2 are both C.sub.1-6 alkyl or phenyl; and n is 0 or 1) and salt thereof. The compounds of formula (I) are useful for the treatment or prophylaxis of protozoal diseases including malaria, theileriosis and coccidiosis. Various processes for preparing compounds of formula (I) are described.

Naphthoquinone derivatives

Novel combinations of an antiprotozoal naphthoquinone and a 4-pyridinol or an alkanoic ester thereof wherein the antiprotozoal activity of the combination is potentiated with respect to the corresponding activity of the components of the combination. The combinations are especially useful for the treatment or porphylaxis of malaria.

Antiprotozoal agents

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Beckenham, United Kingdom

Alan T Hudson