Claims for Patent: 8,110,574

Summary for Patent: 8,110,574

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 in which R1, R2 and R3 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):	Christophe Thurieau, Jérôme Gonzalez, Christophe Moinet
Assignee:	Ipsen Pharma SAS
Application Number:	US12/946,504
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,110,574
Patent Claims:	1. Compounds of the general formula: in racemic, enantiomeric form or all combinations of these forms, in which: R1 represents a —(CH2)m—Z12 radical in which Z12 represents optionally substituted aryl; R2 represents a radical of formula —C(Y)NHX1, wherein X1 represents a (CH2)pZ22 radical in which Z22 represents aryl optionally substituted; R3 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 Z12 is substituted with one or more fluoro, chloro, bromo, iodo, alkyl, alkoxy, alkylthio, —CF3, —OCF3, phenyl, phenoxy or aminosulphonyl. 3. The compound of claim 1, wherein the aryl represented by Z22 is substituted with one or more fluoro, chloro, bromo, iodo, alkyl, alkenyl, alkoxy, alkylthio, CF3, OCF3, 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 Z12 is substituted with one or more fluoro, chloro, bromo, iodo, alkyl or alkoxy. 5. The compound of claim 1, wherein the aryl represented by Z22 is substituted with one or more fluoro, chloro, bromo, iodo, alkyl, alkoxy, alkylthio, CF3, OCF3, nitro, cyano, azido, piperidinosulphonyl, —C(O)—O-alkyl, —C(O)-alkyl or phenyl. 6. The compound of claim 1, wherein R3 is unsubstituted alkyl. 7. The compound of claim 1, wherein R3 is methyl. 8. The compound of claim 1, wherein Z12 and Z22 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.