Back to results
US 7,115,634 B2Granted
4-aminopiperidine and their use as a medicine
AssigneeSociete de Conseils de Recherches et d'Applications Scientifiques
InventorsChristophe Thurieau, Jérôme Gonzalez, Christophe Moinet
Life of this patent
Estimating the term…
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.
Claims10
A compound of the formula
- in racemic, enantiomeric form or all combinations of these forms, wherein
- R1 is —(CH2)m-Y-Z11 or
- —(CH2)m-Z12,
- Z11 is (C1-C6)alkyl or optionally substituted aryl,
- Z12 is bis-phenyl optionally substituted aryl or -optionally substituted heteroaryl,
- R2 is selected from the group consisting of —C(Y)NHX1, —C(O)X2 and SO2X3;
- R3 is selected from the group consisting of hydrogen, an optionally substituted alkyl, alkenyl and alkynyl,
- X1 is selected from the group consisting of (C1-C15)alkyl, alkenyl, alkynyl, —(CH2)m-Y-Z21 and —(CH2)pZ22,
- Z21 is (C1-C6)alkyl
- Z22 is selected from the group consisting of cyclohexenyl, indanyl, bis-phenyl, (C3-C7)cycloalkyl and (C3-C7)heterocycloalkyl, aryl and heteroaryl optionally substituted
- X2 is selected from the group consisting of alkenyl optionally substituted by phenyl optionally substituted, alkynyl, —(CH2)m-W-(CH2)q-Z23 and —(CH2)p-U-Z24 wherein
- Z23 is (C1-C6)alkyl or aryl optionally substituted;
- Z24 is selected from the group consisting of cyclohexenyl, bis-phenyl, (C3-C7)cycloalkyl optionally substituted, (C3-C7)heterocycloalkyl, cyano, amino, mono and di-alkylamino, aryl and heteroaryl optionally substituted,
- X3 is selected from the group consisting of (C1-C10)alkyl, alkenyl optionally substituted by phenyl optionally substituted, —CF3, and
- —(CH2)pZ25,
- Z25 is aryl optionally substituted,
- Y is oxygen or sulfur,
- W is oxygen or sulfur or SO2;
- U is a covalent bond or oxygen;
- n is an integer from 0 to 4;
- m is an integer from 1 to 6;
- p is an integer from 0 to 6;
- q is an integer from 0 to 2,
- and their addition salts with pharmaceutically acceptable acids.
21 more elements
Dependencies are inferred from the claim text.