PKC modulating compounds of the formula ##STR1## Also disclosed are pharmaceutical compositions including these compounds which inhibit PKC activity, methods of using these compounds to inhibit PKC activity in mammals, and intermediates useful in preparing the PKC modulating compounds.
preparation of (S)-2-cyanopiperidine 4 provides a new access to 2-substituted piperidines. This synthesis is based on an enantioselective (R)-oxynitrilase-catalyzed reaction for the preparation of (R)-(+)-6-bromo-2-hydroxyhexanenitrile 1 and the subsequent cyclization of this compound to yield the piperidine ring. The utilization of 4 as the starting material for the synthesis of (S)-2-aminomethylpiperidine
A compound of the formula (I):
in which R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
, R
8
and R
9
are each as defined in the description, or a salt thereof.
The object compound of the present invention has pharmacological activities such as Tachykinin antagonism, and is useful for manufacture of a medicament for treating or preventing Tachykinin-mediated diseases.
(EN) PKC modulating compounds of formula (I). Also disclosed are pharmaceutical compositions including these compounds which inhibit PKC activity, methods of using these compounds to inhibit PKC activity in mammals, and intermediates useful in preparing the PKC modulating compounds.(FR) On décrit des composés modulant la protéine-kinase C (PKC) correspondant à la formule (I), ainsi que des compositions pharmaceutiques contenant lesdits composés qui inhibent l'activité de la PKC, des méthodes permettant d'utiliser ces composés pour inhiber l'activité de la PKC chez des mammifères, et des intermédiaires utiles pour la préparation de composés modulant la PKC.