Glaxo Group Limited

Barry A Coomber

Gordon H Phillipps

David C Humber

George B Ewan

Alan Naylor

Russell Michael Hagan

Keith Thomas Bunce

Mark Ladlow

Andrew Richard Whittington

Andrew B McElroy

David B Ewan

Anthony J Pateman

The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. ##STR1## wherein R represents the ring A ##STR2## or 2-pyridinyl or 2-pyridinyl-N-oxide; R.sup.1 is selected from halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, and S(O).sub.n C.sub.1-4 alkyl groups;

Medical use for tachykinin antagonists

##STR1## wherein R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group; R.sup.2 is a hydrogen atom, a C.sub.1-6 alkoxy group or a C.sub.2-5 alkanoyloxy group;

11.alpha.-Amino-androstanes

Compounds of the formula ##STR1## wherein R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group;

11.alpha.-amino-androstanes

Compounds of the formula ##STR1## wherein R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group, and R.sup.2 is a C.sub.1-6 alkyl group or a C.sub.3-6 cycloalkyl group and the D-homo analogues thereof having the group --CO.sub.2 R.sup.2 (wherein R.sup.2 is as defined above) at the 17.alpha..beta.-position, and acid addition salts thereof have activity as antidysthythmic agents and may be applicable for the treatment of dysrthymias in humans or animals. The compounds may be provided in the form of compositions in admixture with pharmaceutical carriers and excipients and may be prepared by a variety of processes known for producing steroids of this type. The invention also provides intermediates for the preparation of the compounds of formula (I) wherein R.sup.2 and/or R.sup.1 are replaced with hydrogen atoms, and processes for the preparation of such intermediates.

11.alpha.-Amino-3.beta.-hydroxy-androstanes

Compounds of formula ##STR1## wherein: R.sup.1 is a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group;

Compounds of formula ##STR1## (wherein): R.sup.1 is a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.3-7 cycloalkyl group; and

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Pinner, United Kingdom

Barry A Coomber