John Wyeth Brother, Limited

Gerald Bradley

Terence J Ward

Alan C White

Albert Opalko

Richard J Yarwood

Janet C White

Geoffrey P Carr

(Endo)-N-[[[8-azabicyclo[3.2.1]octan-3-yl]amino]carbonyl]-2-(cyclopropylmet hyloxy)benzamide and pharmaceutically acceptable salts thereof possess 5-HT.sub.3 antagonistic activity and are useful in the treatment of neuro-psychiatric disorders (e.g. anxiety), gastro-intestinal disorders and migraine.

Treatment of anxiety and gastrointestinal disorders with azabicyclo

Aroyl ureas and carbamic acid derivatives of formula

Heterocyclic compounds useful as 5-HT.sub.3 antagonists

The invention concerns a new stable crystal form of anhydrous, crystalline 1,4-dihydro-2-(imidazol-1-ylmethyl)-6-methyl-4-(3-nitrophenyl)pyridine)-3, 5-dicarboxylic acid 3-ethyl 5-methyl diester hydrochloride, 'having a melting point greater than about 215.degree. C., an infra red spectrum (nujolmull) having sharp peaks at 3195 cm.sup.-1, 3100 cm.sup.-1, 2735 cm.sup.-1 and 2625 cm.sup.-1 and an x-ray powder diffraction pattern with specific peaks occurring at 2.theta.=12.3.degree. and 44.5.degree..'

Stable crystal form of

Morpholine derivatives of the formula ##STR1## and their acid addition salts, wherein n represents 1, 2 or 3, R.sup.3 is alkyl of 1 to 10 carbon atoms, R.sup.4 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cyclo (lower)alkylmethyl and OR.sup.5 is hydroxy, acyloxy or a protected hydroxy group possess analgesic and/or opiate antagonistic activity or are useful as intermediates for other compounds of formula I possessing such activity.

Analgesic method

Morpholine derivatives of the formula ##STR1## and their acid addition salts, wherein n represents 1, 2 or 3, R.sup.4 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cyclo(lower)alkylmethyl, R.sup.2 and R.sup.3 are each hydrogen or alkyl of 1 to 10 carbon atoms and OR.sup.5 is hydroxy, acyloxy or a protected hydroxy group possess analgesic and/or opiate antagonistic activity or are useful as intermediates for other compounds of formula I possessing such activity.

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Weybridge, United Kingdom

Gerald Bradley