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Details for Patent: 5,132,459

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Details for Patent: 5,132,459

Title: Propenylamines, processes for their production, pharmaceutical compositions containing them and their use as pharmaceuticals
Abstract:Compounds of formula I ##STR1## wherein R.sub.1 represents a group of formula ##STR2##
Inventor(s): Stuetz; Anton (Maria Enzersdorf, AT)
Assignee: Sandoz Ltd. (Basel, CH)
Filing Date:Jul 21, 1989
Application Number:07/384,237
Claims:1. A compound in trans configuration of the formula: ##STR85## wherein R.sub.1 is a radical of formula IIa, ##STR86## R.sub.2, R.sub.3, R.sub.5, and R.sub.8 are each hydrogen, R.sub.4 is methyl, and

R.sub.6 is a radical of formula IIIa

where R.sub.11 is alkyl of 2 to 6 carbon atoms or a chemotherapeutically acceptable acid addition salt thereof.

2. A compound as claimed in claim 1 the form of its hydrochloride.

3. A chemotherapeutical composition comprising an effective amount of a compound as claimed in claim 1 or a chemotherapeutically acceptable acid addition salt thereof in admixture with a chemotherapeutically acceptable diluent or carrier.

4. A method of treating diseases or infections caused by mycetes which comprises administering to a subject in need of treatment an effective amount of a compound as claimed in claim 1 or a chemotherapeutically acceptable acid addition salt thereof.

5. A compound according to claim 1 selected from the group in which R.sub.1 is 1-naphthyl, R.sub.2 is H, R.sub.3 is H, R.sub.4 is CH.sub.3 and R.sub.5, R.sub.6 and the configuration are ##STR87## i) H, --C.tbd.C--(CH.sub.2).sub.2 --CH.sub.3, and trans; j) H, --C.tbd.C--(CH.sub.2).sub.4 --CH.sub.3, and trans;

k) H, --C.tbd.C--(CH.sub.2).sub.5 --CH.sub.3, and trans;

or a chemotherapeutically acceptable acid addition salt thereof.

6. The compound according to claim 1 in which R.sub.1 is 1-naphthyl, R.sub.2 is H, R.sub.3 is CH.sub.3, R.sub.5 is H, R.sub.6 is ##STR88## and the configuration is trans, or a chemotherapeutically acceptable acid addition salt thereof.

7. A compound according to claim 1 in which R.sub.11 is alkyl of 3 to 5 carbon atoms.

8. A compound according to claim 1 in which R.sub.11 is alkyl of 5 or 6 carbon atoms.
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