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|Title:||Derivatives of 4-aminopiperidine and their use as a medicament|
|Abstract:||A subject of the present application is new derivatives of 4-aminopiperidines of formula ##STR00001## in which R.sub.1, R.sub.2 and R.sub.3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.|
|Inventor(s):||Thurieau; Christophe (Paris, FR), Gonzalez; Jerome (Annemasse, JP), Moinet; Christophe (Montreal, CA)|
|Assignee:||Ipsen Pharma S.A.S. (Boulogne-Billancourt, FR)|
1. Compounds of the general formula: ##STR01211## in racemic, enantiomeric form or all combinations of these forms, in which: R.sub.1 represents a
--(CH.sub.2).sub.m--Z.sub.12 radical in which Z.sub.12 represents optionally substituted aryl; R.sub.2 represents a radical of formula --C(Y)NHX.sub.1, wherein X.sub.1 represents a (CH.sub.2).sub.pZ.sub.22 radical in which Z.sub.22 represents aryl
optionally substituted; R.sub.3 represents an optionally substituted alkyl; Y represents an oxygen atom; m is an integer from 1 to 6; and p is an integer from 0 to 6; or their addition salts with pharmaceutically acceptable mineral or organic acids.
2. The compound of claim 1, wherein the aryl represented by Z.sub.12 is substituted with one or more fluoro, chloro, bromo, iodo, alkyl, alkoxy, alkylthio, --CF.sub.3, --OCF.sub.3, phenyl, phenoxy or aminosulphonyl.
3. The compound of claim 1, wherein the aryl represented by Z.sub.22 is substituted with one or more fluoro, chloro, bromo, iodo, alkyl, alkenyl, alkoxy, alkylthio, CF.sub.3, OCF.sub.3, nitro, cyano, azido, aminosulphonyl, piperidinosulphonyl, mono- or di-alkylamino, --C(O)--O-alkyl, --C(O)-alkyl, optionally substituted phenyl, phenoxy, phenylthio or benzyloxy.
4. The compound of claim 1, wherein the aryl represented by Z.sub.12 is substituted with one or more fluoro, chloro, bromo, iodo, alkyl or alkoxy.
5. The compound of claim 1, wherein the aryl represented by Z.sub.22 is substituted with one or more fluoro, chloro, bromo, iodo, alkyl, alkoxy, alkylthio, CF.sub.3, OCF.sub.3, nitro, cyano, azido, piperidinosulphonyl, --C(O)--O-alkyl, --C(O)-alkyl or phenyl.
6. The compound of claim 1, wherein R.sub.3 is unsubstituted alkyl.
7. The compound of claim 1, wherein R.sub.3 is methyl.
8. The compound of claim 1, wherein Z.sub.12 and Z.sub.22 are optionally substituted phenyl or naphthyl.
9. The compound of claim 1, wherein m and p are simultaneously 1.
10. A pharmaceutical composition comprising a compound of claim 1 or an addition salt thereof with a pharmaceutically acceptable mineral or organic acid.
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