Glaxo Group Limited

Glaxogrouplimited

Gordon G Weingarten

Stuart B Laing

Simon John Fawcett MacDonald

David C Humber

Anthony William James Cooper

Philip Alan Skone

Keith Biggadike

Diane Mary Coe

Ian B Campbell

Christine Edwards

Garry Fenton

James Michael Woolven

Graham George Adam Inglis

David House

Gianpaolo Bravi

Iain McFarlane McLay

Heather Anne Barnett

Haydn Terence Jones

Steven Philip Keeling

The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation, allergy and/or autoimmune conditions.

Non-steroidal glucocorticoid inhibitors and their use in treating inflammation, allergy and auto-immune conditions

The present invention provides compounds of formula (I): a process for their preparation, pharmaceutical compositions comprising the compounds and the preparation of said compositions, intermediates and use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation, allergy and/or skin disease.

Compounds

The present invention is directed to compounds of formula (I): whereinR represents a methyl or an ethyl groupX represents N, C&#x2014;H or C&#x2014;CHwhen X represents C&#x2014;H or C&#x2014;CH, Y represents Nwhen X represents N, Y represents C&#x2014;Hand physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.

Tetrahydro-naphthalene derivatives as glucocorticoid receptor modulators

The invention provides the compounds of formula (I) or a pharmaceutically acceptable salt thereof. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.

Pyrimidine derivative as selective COX-2 inhibitors

There are described compounds of formula (I) ##STR1## wherein R, R.sub.1 and R.sub.2 which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl group and R.sub.3 represents a C.sub.1-4 alkyl group with the proviso that, when both R.sub.1 and R.sub.2 represent hydrogen atoms, R.sub.3 represents other than a methyl group. These cefuroxime esters are valuable as providing orally administrable forms of the antibiotic cefuroxime. Methods of preparing cefuroxime esters, pharmaceutical compositions containing the esters and methods for their use in medicine are also described. Novel intermediates for use in the preparation of the cefuroxime esters are also described.

Cephalosporin antibiotics

A process for the preparation of a 3-carbamoyloxymethyl cephalosporin compound which comprises reacting a 3-hydroxymethyl cephalosporin with dihalophosphinyl isocyanate and converting the resulting 3-phosphonocarbamoyloxymethyl cephalosporin reaction product by hydrolysis to the desired compound. The isocyanates used in the process are readily available and easy to handle and thus the process avoids the use of hazardous and/or expensive reagents.

Process for preparing 3-carbamoyloxymethyl cephalosporins

A process for the preparation of cephalosporins having a phosphonocarbamoyloxymethyl group at the 3-position by reacting a cephalosporin having at the 3-position a group ##STR1## (wherein R.sup.4 and R.sup.5 are independently alkyl, aralkyl, alicyclic or aryl groups or together form a divalent group) with a compound of formula ##STR2## (wherein R.sup.6, R.sup.7 and R.sup.8 are independently alkyl, aralkyl, alicyclic or aryl groups or any two of R.sup.6, R.sup.7 and R.sup.8 together form a divalent group, and X is halogen) followed by hydrolysis. The 3-phosphonocarbamoyloxymethyl cephalosporin products of the process exhibit antibiotic activity, and if desired may be readily converted to 3-carbamoyloxymethyl cephalosporins which themselves show antibiotic activity.

Process for the preparation of cephalosporin compounds

A process for the preparation of a 3-carbamoyloxymethyl cephalosporin compound which comprises hydrolyzing a 3-phosphonocarbamoyloxymethyl cephalosporin compound. The hydrolysis is preferably effected at a pH in the range of pH3 to 4, for example using aqueous sodium hydrogen carbonate.

3-Phosphonocarbamoyloxymethyl cephalosporin compounds of formula ##STR1## (wherein R.sup.1 represents an acylamido group and R.sup.3 represents hydrogen, or a lower alkyl, alkylthio or alkoxy group) and non-toxic derivatives thereof. The compounds exhibit antibiotic activity.

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London, United Kingdom

Gordon G Weingarten