152356-05-3Relevant academic research and scientific papers
Novel Potent Antagonists of Human Neuropeptide Y Y5 Receptors. Part 3: 7-Methoxy-1-hydroxy-1-substituted Tetraline Derivatives
Itani, Hiromichi,Ito, Harunobu,Sakata, Yoshihiko,Hatakeyama, Yoshifumi,Oohashi, Hiroko,Satoh, Yoshinari
, p. 799 - 802 (2002)
As a part of our continuing research on NPY-Y5 receptor antagonists in the series of novel 6-methoxybenzo[a]cycloheptene derivatives, we discovered a novel skeleton, 7-methoxy-1-hydroxytetraline 7 which had been used as an intermediate, to be more suitable for increasing potencies leading to compound 3 (FR230481). Additionally, we discovered that the naphthalenesulfonamide moiety which was thought to be an essential pharmacophore could be replaced by the 5-chlorobenzothiazolin-3-acetic acid moiety to lead to potent compound 4 (FR233118). The structure-activity relationships on compounds 3, 4 and their related derivatives are described. Unfortunately, although compounds 3 and 4 had very high affinities for Y5 receptors, their poor permeabilities to brain were shown by exo-vivo binding assays when orally administered.
Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: Substituted benzo[a]cycloheptene derivatives
Itani, Hiromichi,Ito, Harunobu,Sakata, Yoshihiko,Hatakeyama, Yoshifumi,Oohashi, Hiroko,Satoh, Yoshinari
, p. 757 - 761 (2007/10/03)
Novel benzo[a]cycloheptene derivatives were prepared for the purpose of searching new neuropeptide Y-Y5 (NPY-Y5) receptor antagonists. The structure-activity relationships are described and compound 2o (FR226928) showed the most potent affinity for Y5 receptor of all we prepared and was found to have higher potency and better selectivity for Y5 over Y1 receptor affinities when compared with the known lead compound 1.
Ethanolamine derivatives having sympathomimetic and anti-pollakiuria activities
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, (2008/06/13)
This invention relates to new ethanolamine derivatives having gut selective sympathomimetic and anti-pollakiuria activities and represented by the general formula [I]: STR1 wherein R1 is aryl or a heterocyclic group, each of which may be substituted with halogen, etc., R2 is hydrogen, halogen, nitro, hydroxy, lower alkyl optionally substituted with acyl, lower alkenyl optionally substituted with acyl, lower alkoxy optionally substituted with acyl, or amino optionally substituted with acyl(lower)alkyl, R3 is hydrogen, an N-protective group, or lower alkyl optionally substituted with lower alkylthio, n is an integer of 0 to 3, and a heavy solid line means a single bond or a double bond, provided that when n is 1, then 1) R1 is a condensed aromatic hydrocarbon group or a heterocyclic group, each of which may be substituted with halogen, etc., and the like, and pharmaceutically acceptable salts thereof to processes for the preparation thereof and to a pharmaceutical composition comprising the same.
