US 7,888,510 B2 · 2-′4(phenylamino)-piperidin-1-yl!-n-phenyl-acetamine derivatives and related compounds as neuropeptide Y5 (NPY5) ligands for the treatment of obesity

Abstract

It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man. Said object was achieved by providing 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1.

Claims6

Dependent claims

A 1,4-disubstituted piperidine compounds of general formula (I), wherein

R1, R2, R3, R4 are each independently selected from the group consisting of H, F, Cl, Br, OH, CH3, and OCH3,
B represents a —CH2—OH or —(C═O)—O—CH3 group,
R11 is selected from the group consisting of unsubstituted phenyl, phenyl that is optionally at least mono-substituted with one or more substituents independently selected from the group consisting of cyclohexyl, phenyl, phenoxy, benzoyl, —C(═O)—C1-2-alkyl, —C(H)(OH)(phenyl) and —C(H)(OH)(CH3),
a group of formula (A)
wherein
n is 1 or 2,
X represents CH,
Y represents CH—OH or C(═O),
a group of formula (B),
a group of formula (C),
and a group of formula (E),
wherein
RE represents H, a branched or unbranched C1-4-alkyl radical or a branched or unbranched C1-4-alkoxy radical,
Z represents CH2, O, S, CH—OH, C(═O) or N—RF where RF represents H or a branched or unbranched C1-4-alkyl-radical,
optionally in form of one of its stereoisomers, its racemate or in form of a mixture of at least two of its stereoisomers, or a salt.

12 more elements

Dependencies are inferred from the claim text.

2-′4(phenylamino)-piperidin-1-yl!-n-phenyl-acetamine derivatives and related compounds as neuropeptide Y5 (NPY5) ligands for the treatment of obesity

Life of this patent

2-′4(phenylamino)-piperidin-1-yl!-n-phenyl-acetamine derivatives and related compounds as neuropeptide Y5 (NPY5) ligands for the treatment of obesity

Life of this patent

Abstract

Claims6