Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands
During a program directed at selective NK1 receptor antagonists, we serendipitously discovered an NK1 receptor ligand with additional affinity for the NK3 receptor. Recognising an opportunity for a drug discovery program aiming for dual NK1/NK3 receptor antagonists, we prepared a series of analogues from a novel, versatile building block. From this series emerged compounds with high and balanced affinities for the NK1 and the NK3 receptors. Typical representatives of this series were active in the gerbil foot tapping assay after oral administration.
Peters, Jens-Uwe,Hoffmann, Torsten,Schnider, Patrick,Stadler, Heinz,Koblet, Andreas,Alker, André,Poli, Sonia Maria,Ballard, Theresa M.,Spooren, Will,Steward, Lucinda,Sleight, Andrew J.
scheme or table
p. 3405 - 3408
(2010/07/16)
Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia
The present invention relates to a method of treating schizophrenia which comprises administering a therapeutically effective amount of a compound of formula I wherein R1, R2, and R3 are as defined in the specification or to pharmaceutically active acid-addition salts thereof.
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Page/Page column 14
(2010/02/15)
DUAL NK1/NK3 ANTAGONISTS FOR TREATING SCHIZOPHRENIA
The use of compounds of the general formula wherein the substituents are as described in claim 1 or pharmaceutically active acid-addition salts thereof for the preparation of medicaments for the treatment of schizophrenia.
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Page 135
(2008/06/13)
Substituted 4-phenyl-pyridine compounds with activity as antagonists of neurokinin 1 receptors
Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing.
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(2008/06/13)
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