Imperial Chemical Industries Limited

National Research Development Corporation

Geraint Jones

David S Thomson

Peter W Caulkett

Michael G Collis

Simon M Poucher

John Preston

Rodney B Hargreaves

Roger James

John R Evans

Murdoch A Eakin

Jean C Arnould

Michael J Cooper

Clive G Knight

John L Gordon

John T Dingle

John S Lowe

Compounds of the formula I: ##STR1## wherein: X is O, S or NH; n is O or an integer of from 1 to 3; R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl; R.sup.2 is CH.sub.2 R.sup.3, NHR.sup.4, SO.sub.2 NR.sup.5 YNR.sup.6 R.sup.7 or R.sup.8, in which R.sup.3 is hydroxy, (1-4C)alkoxy or (1-4C)alkylsulphonyl; R.sup.4 is (1-4C)alkylsulphonyl, (1-4C)haloalkylsulphonyl, formyl, carbamoyl or 2,6-dichloro-4-(2-(1,1-dimethylethyl)amino-1-hydroxyethyl)phenyl; R.sup.5 is hydrogen or (1-4C)alkyl; Y is CO or (1-6C)alkylene; R.sup.6 and R.sup.7 are independently (1-4C)alkyl, or R.sup.6 is hydrogen and R.sup.7 is (1-4C)alkyl, (1-4C)haloalkyl, phenyl(1-4C)alkyl or, when Y is (1-6C)alkylene, is (1-4C)alkylaminocarbonyl or (5-6C)cycloalkylaminocarbonyl; and R.sup.8 is a sugar residue of formula II in which R.sup.9 represents hydrogen, methyl or hydroxymethyl and m is 2 or 3; A is N or CT in which T is hydrogen or (1-4C)alkyl; or a pharmaceutically acceptable salt thereof, processes for their manufacture and pharmaceutical compounds containing them. The compounds are useful as adenosine antagonists.

2-furyl-triazalo [1,5-a]-[1,3,5]triazines and pyrazolo

A compound of the formula I ##STR1## wherein: R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl;

Azole derivatives

The invention concerns novel, pharmaceutically useful compounds of formula I in which Q is a 5-membered heteroaryl optionally bearing 1 or 2 substituents independently selected from (1-4C)alkyl and halogeno;

[1,2,4]-Triazolo[1,5-a]and pyrazolo[2,3-a][1,3,5]triazine derivatives

A compound of the formula I ##STR1## wherein: A.sup.1 and A.sup.2 are each independently N or CT in which T is hydrogen or (1-4C)alkyl;

Heterocyclic compounds

2-(2-Hydroxy-3-phenoxypropylamino)ethylphenoxyacetamide compounds are disclosed as useful in the treatment of obesity and related conditions. Processes for their preparation are described, as are novel intermediates and pharmaceutical compositions containing them.

Chemical compounds

The invention concerns novel glyceride esters of anti-bacterial halogenated phenols having the formula I in which Ra and Rb are independently (3-20C)alkyl or (3-20C)alkenyl; Rc and Rd are independently chloro or bromo; Re is hydrogen, chloro or bromo; and A is (1-6C)alkylene optionally bearing one or two (1-4C)alkyl substituents. The esters are of use in the prophylaxis and/or therapy of acne vulgaris. Pharmaceutical compositions for topical administration and processes for the manufacture of the esters are also provided.

Halogenophenyl glyceride esters for use in the prophylaxis and/or

The invention concerns di- and tri-esters derived from alkanoic, (cycloalkyl)alkanoic, benzoic or phenylalkanoic acids with N-(acylaminoalkyl)-dihydroxyphenylethanolamines, and pharmaceutically acceptable salts thereof; processes for their preparation and manufacture; and pharmaceutical compositions thereof. The esters are useful for the topical treatment of an area of inflammation affecting the skin of a warm-blooded animal. Representative esters of the invention are 1-[3,4-bis(pivaloyloxy)phenyl]-2-[2-(2-phenylacetamido)ethylamino]-ethanol , 1-[3,4-bis(pivaloyloxy)phenyl]-2-[1,1-dimethyl-2-(2-phenoxyacetamido)ethy lamino]-ethanol, and the hydrochlorides and hydrobromides thereof.

Esters

Pharmaceutical liposome compositions containing an anti-inflammatory steroid derivative bearing a lipophilic substituent, for example cortisol 21-hexadecanoate. Method of treatment of inflammation at a site involving an enclosed cavity, for example the treatment of rheumatic disease, comprising injecting a said pharmaceutical liposome composition into said cavity. Specified new steroid derivatives, for example fluocinolone acetamide 21-hexadecanoate.

Pharmaceutical compositions

The invention concerns di- and tri-esters derived from alkanoic, (cycloalkyl)alkanoic, benzoic or phenylalkanoic acids with N-(acylaminoalkyl)-dihydroxyphenylethanolamines, and pharmaceutically acceptable salts thereof; processes for their preparation and manufacture; and pharmaceutical compositions thereof. The esters are useful for the topical treatment of an area of inflammation affecting the skin of a warm-blooded animal. Representative esters of the invention are 1-[3,4-bis(pivaloyloxy)phenyl]-2-[2-(2-phenylacetamido)ethylamino]-ethanol , 1-[3,4-bis(pivaloyloxy)phenyl]-2-[1,1-dimethyl-2-(2-phenoxyacetamido)-eth ylamino]-ethanol, and the hydrochlorides and hydrobromides thereof.

The invention concerns compounds of the formula:- R.sup.1.CH(OH).CH.sub.2 NH.CR.sup.2 R.sup.3.A.sup.1. NH.CO.CHR.sup.4.A.sup.2.NR.sup.5. Q I wherein R.sup.1 is 3,4-bis[(3-8C)alkanoyloxy]-phenyl, 3,5- bis [(3-8C)alkanoyloxy]phenyl, 3-[(3-8C)alkanoyloxy]methyl-4-[(3-8C)alkanoyloxy]phenyl, 4-[(3-8C)alkanoyloxy]phenyl, 2-chlorophenyl or 3,5-dichloro-4-aminophenyl; R.sup.2 and R.sup.3 are independently hydrogen or (1-4C) alkyl; A.sup.1 is (1-4C) alklylene; A.sup.2 is a direct bond or (1-4C) alkylene; R.sup.4 is hydrogen, (1-6C)alkyl, phenyl-(1-4C)alkyl or halogenophenyl-(1-4 C)alkyl; and R.sup.5 is (1-6C)alkyl; or R.sup.4 and R.sup.5 together form (2-5C) alkylene; and Q is (3-12C) alkanoyl, [(3-6C)alkoxy]carbonyl, phenylacetyl, phenoxyacetyl, benzoyl or benzyloxycarbonyl, the phenyl rings of which may optionally bear a substitutent selected from halogeno, (1-4C)alkyl, (1-4C)alkoxy and trifuloromethyl; and the pharmaceutically acceptable acid-addition salts thereof; processes for their manufacture; and pharmaceutical compositions thereof. The compounds of formula I are topical anti-inflammatory agents. A representative compound is 1-[3,4-bis (pivaloyloxy)phenyl]-2-{2-[(N-phenylacetyl-proyly)amino]-1,1-dimethyl-ethy lamino}ethanol.

1-Phenyl-2-aminoethanol derivatives

The invention concerns new topical anti-inflammatory 1-phenyl-2-aminoethanol derivatives of the general formula:

Pharmaceutical compositions, containing a 4,4'-dihydroxy-3,3'-triphenylmethanedicarboxylic acid (or an oxidized derivative) as active ingredient, are described and are prepared conventionally in a form suitable for topical administration e.g. ointment. The compositions are useful for the treatment of inflammatory diseases and inflammatory conditions of the skin. Many of the active ingredients are novel compounds. A representative novel active ingredient is 4'-cyano-4,4'-dihydroxy-5,5'-dimethyl-3,3'-triphenylmethanedicarboxylic acid.

Triaryl or diarylpyridyl methanes

Pharmaceutical compositions, containing a 4,4'-dihydroxy-3,3'-triphenylmethanedicarboxylic acid (or an oxidized derivative) as active ingredient, are described and are prepared conventionally in a form suitable for topical administration, e.g., ointment. The compositions are useful for the treatment of inflammatory diseases and inflammatory conditions of the skin. Many of the active ingredients are novel compounds. A representative novel active ingredient is 4'-cyano-4,4'-dihydroxy-5,5'-dimethyl-3,3'-triphenylmethanedicarboxylic acid.

Pharmaceutical compositions and method of use

Optionally substituted 4-oxo-1,4-dihydrocinnolin-3-ylpropionic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and a method of treatment using them. A representative compound is ethyl 6-ethyl-1-methyl-4-oxo-1,4-dihydrocinnolin-3-ylpropionate. Compounds active as inhibitors of effects following the combination of reagin-like antibodies and their antigens.

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Macclesfield, United Kingdom

Geraint Jones