29419-14-5Relevant articles and documents
Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H- benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes
Stjernlof,Ennis,Hansson,Hoffman,Ghazal,Sundell,Smith,Svensson,Carlsson,Wikstrom
, p. 2202 - 2216 (1995)
A series of 1-, 3-, and 4-substituted analogs to the potent 5-HT(1A) agonist 8-(dipropylamino)6,7,8,9-tetrahydro-3H-benz[e]indole-1-carbaldehyde (5) were prepared and tested in vitro at 5-HT(1A), 5-HT(1Dα), 5-HT(1Dβ), D2, and D3 rece
Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: Discovery of PF-3084014
Brodney, Michael A.,Auperin, David D.,Becker, Stacey L.,Bronk, Brian S.,Brown, Tracy M.,Coffman, Karen J.,Finley, James E.,Hicks, Carol D.,Karmilowicz, Michael J.,Lanz, Thomas A.,Liston, Dane,Liu, Xingrong,Martin, Barbara-Anne,Nelson, Robert B.,Nolan, Charles E.,Oborski, Christine E.,Parker, Christine P.,Richter, Karl E.G.,Pozdnyakov, Nikolay,Sahagan, Barbara G.,Schachter, Joel B.,Sokolowski, Sharon A.,Tate, Barbara,Wood, Douglas E.,Wood, Kathleen M.,Van Deusen, Jeffrey W.,Zhang, Lei
scheme or table, p. 2637 - 2640 (2011/06/20)
A novel series of tetralin containing amino imidazoles, derived from modification of the corresponding phenyl acetic acid derivatives is described. Replacement of the amide led to identification of a potent series of tetralin-amino imidazoles with robust central efficacy. The reduction of brain Aβ in guinea pigs in the absence of changes in B-cells suggested a potential therapeutic index with respect to APP processing compared with biomarkers of notch related toxicity. Optimization of the FTOC to plasma concentrations at the brain Aβ EC50 lead to the identification of compound 14f (PF-3084014) which was selected for clinical development.
Heteroaryl β-tetralin ureas as novel antagonists of human TRPV1
Jetter, Michele C.,Youngman, Mark A.,McNally, James J.,McDonnell, Mark E.,Zhang, Sui-Po,Dubin, Adrienne E.,Nasser, Nadia,Codd, Ellen E.,Flores, Christopher M.,Dax, Scott L.
, p. 6160 - 6163 (2008/03/18)
We report on a series of α-substituted-β-tetralin-derived and related phenethyl-based isoquinolinyl and hydroxynaphthyl ureas as potent antagonists of the human TRPV1 receptor. The synthesis and Structure-activity relationships (SAR) of the series are described.
N-SUBSTITUTED AMINOTETRALINS AS LIGANDS FOR THE NEUROPEPTIDE Y Y5 RECEPTOR USEFUL IN THE TREATMENT OF OBESITY AND OTHER DISORDERS
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Page 33-34; 36, (2010/02/07)
beta -Aminotetralin derivatives of the formula: which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a beta -aminotetralin derivative as the active ingredient are described. The beta -aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.
The synthesis of novel cis-α-substituted-β-aminotetralins
Youngman, Mark A.,Willard, Nicole M.,Dax, Scott L.,McNally, James J.
, p. 2215 - 2227 (2007/10/03)
Teteralones were converted, in 1 to 3 steps, to α-substituted tetralones. Subsequent reductive amination with ammonium acetate/sodium cyanoborohydride gave the corresponding α-substituted-β-aminotetralins, on a multigram scale, with minimal chromatography for the entire transformation.
Novel guanidinobenzamides
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, (2008/06/13)
Compounds of formula IA and IB are new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical form
COMPOUND HAVING TETRAHYDRONAPHTHALENE SKELETON AND LIQUID CRYSTAL COMPOSITION CONTAINING THE SAME
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Page 67, (2010/01/31)
A tetrahydronaphthalene derivative represented by the general formula (I) and a liquid crystal composition containing the same. A compound represented by the general formula (I) shows superior liquid crystallinity and co-solubility with conventional liquid crystal compounds and compositions. Furthermore, addition of such a compound enables the threshold voltage to be significantly reduced with almost no deleterious effect on the responsiveness. In addition, a compound of the present invention can also be easily produced industrially, is colorless, and is chemically stable. Consequently, liquid crystal compositions containing such a compound are extremely useful as liquid crystals, and are particularly suitable for liquid crystal displays requiring a wide operating temperature range, low voltage driving and a high response speed.
N-substituted aminotetralins as ligands for the neuropeptide Y Y5 receptor useful in the treatment of obesity and other disorders
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, (2008/06/13)
β-Aminotetralin derivatives of the formula: STR1 which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a β-aminotetralin derivative as the active ingredient are described. The β-aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.
Bicyclic amine derivatives and their use as anti-psychotic agents
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, (2008/06/13)
This invention relates to compounds of formula (I) STR1 which are useful as modulators of D3 receptors, in particular as antipsychotic agents.
Antihyperglycemic Activity of Novel Naphthalenyl 3H-1,2,3,5-Oxathiadiazole 2-Oxides
Ellingboe, John W.,Lombardo, Louis J.,Alessi, Thomas R.,Nguyen, Thomas T.,Guzzo, Frieda,et al.
, p. 2485 - 2493 (2007/10/02)
A series of naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides was prepared and tested for antihyperglycemic activity in the db/db mouse, a model for type 2 (non-insulin dependent) diabetes mellitus.Substitution at the 1-,5-, or 8-positions of the naphthalene ring with a halogen was found to be beneficial to antihyperglycemic activity. 4--3H-1,2,3,5-oxathiadiazole 2-oxide (45), one of the most potent compounds in this series, was selected for further pharmacological evaluation.