Glaxo Group Limited

Ian P Steeples

Gordon H Phillipps

Brian M Bain

Christopher Williamson

Franco Sartor

Stefania Beato

Raymond A Borella

The invention relates to anhydrous crystalline orvepitant maleate (Form 1), pharmaceutical formulations comprising the same, its use in therapy and processes for preparing the same, wherein orvepitant is as shown in formula (I). 

Anhydrous crystal form of ovrepitant maleate

Compounds of the general formula: ##STR1## wherein X represents a halogen atom or a trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group and Het represents an optionally substituted C-attached 5-7 membered aromatic heterocyclic ring which ring contains one or more heteroatoms selected from O, N and S and optionally carries a fused ring and where an acidic or basic group is present, the salts thereof have been found to possess excellent metaphase arresting ability and are of use in combating abnormal cell proliferation. Thus a knowledge of the cell division cycles of the normal and abnormal cells enables a cytotoxic drug to be administered while the abnormal cells are in a phase susceptible to attack and while the normal cells are in a non-susceptible phase. The compounds of the invention are prepared by alkylation, deprotection of a protected keto group, oxidation or electrophilic halogenation.

Substituted pyrimidin-2-ones, the salts thereof, pharmaceutical

Compounds of the formula ##STR1## wherein R.sup.1 represents a fluoro-, chloro- or bromo-methyl group or a 2'-fluoroethyl group, R.sup.2 represents a group COR.sup.6 where R.sup.6 is a C.sub.1-3 alkyl group or OR.sup.2 and R.sup.3 together form a 16.alpha.,17.alpha.-isopropylidenedioxy group; R.sup.3 represents a hydrogen atom, a methyl group (which may be in either the .alpha.- or .beta.-configuration) or a methylene group; R.sup.4 represents a hydrogen, chlorine or fluorine atom; R.sup.5 represents a hydrogen or fluorine atom and symbol    represents a single or double bond have good anti-inflammatory activity, particularly on topical applications. The compounds of formula I are prepared by esterification, halogenation, reduction, deprotection and reaction at a 9,11-double bond to form a 9.alpha.-halo-11.beta.-hydroxy grouping. Pharmaceutical compositions containing the compounds of formula I and methods for the use of the compounds are described and claimed.

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Ruislip Manor, United Kingdom

Ian P Steeples