194669-41-5Relevant articles and documents
20-HETE FORMATION INHIBITORS
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Paragraph 0257; 0258; 0271; 0272, (2020/08/23)
This disclosure provides novel heterocyclic compounds and methods for inhibiting the enzyme CYP4. Further disclosed methods include: a method of inhibiting the biosynthesis of 20-hydroxyeicosatetraenoic acid (20-HETE) in a subject in need thereof and a method of producing neuroprotection and decreased brain damage by preventing cerebral microvascular blood flow impairment and anti-oxidant mechanisms in a subject experiencing or having experienced an ischemic event.
Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators
Pinkerton, Anthony B.,Peddibhotla, Satyamaheshwar,Yamamoto, Fusayo,Slosky, Lauren M.,Bai, Yushi,Maloney, Patrick,Hershberger, Paul,Hedrick, Michael P.,Falter, Bekhi,Ardecky, Robert J.,Smith, Layton H.,Chung, Thomas D. Y.,Jackson, Michael R.,Caron, Marc G.,Barak, Lawrence S.
supporting information, p. 8357 - 8363 (2019/09/10)
Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous system where it acts as a neuromodulator. Neurotensin receptors have been implicated in a wide variety of CNS disorders, but despite extensive efforts to develop small molecule ligands there are few reports of such compounds. Herein we describe the optimization of a quinazoline based lead to give 18 (SBI-553), a potent and brain penetrant NTR1 allosteric modulator.
AROMATIC HETEROCYCLIC COMPOUNDS AND THEIR APPLICATION IN PHARMACEUTICALS
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Paragraph 00331, (2015/07/07)
Provided herein are novel aromatic heterocyclic compounds or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and their uses for treating Alzheimer's disease. Also provided herein are pharmaceutical compositions containing such compounds, and methods for using such compounds or pharmaceutical compositions thereof to treat Alzheimer's disease.
SMALL MOLECULE AGONISTS OF NEUROTENSIN RECEPTOR 1
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Paragraph 00406, (2014/07/08)
Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl- cyclopropane carboxamide derivatives as novel melatonin receptor ligands
Li, Guiying,Zhou, Hao,Jiang, Yu,Keim, Holger,Topiol, Sidney W.,Poda, Suresh B.,Ren, Yong,Chandrasena, Gamini,Doller, Darío
scheme or table, p. 1236 - 1242 (2011/04/16)
Two series of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives exhibiting diverse functionality at rat MT1 and MT2 receptors are reported. Compounds 11f and 18b (MT 1/MT2 agonist) have human microsomal intrinsic clearance comparable to ramelteon.
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARα/γ dual agonists
Kim, Eunkyung,Park, Chan Sun,Han, Taedong,Bae, Myung-Ho,Chong, Wonee,Lee, Choong Hyun,Shin, Young Ah,Ahn, Byung-Nak,Kim, Mi Kyung,Shin, Chang Yell,Son, Moon Ho,Kim, Jin Kwan,Moon, Ho Sang,Shim, Hyun Joo,Kim, Eun Jung,Kim, Soon Hoe,Lim, Joong In,Lee, Chun Ho
scheme or table, p. 4993 - 4996 (2009/05/26)
Aryl-tetrahydropyridine derivatives were prepared and their PPARα/γ dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARα/γ dual agonist with an EC50 of 1.73 and 0.64 μM in hPPARα and γ, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.
Tetrahydrobenzindole compounds
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, (2010/02/05)
A compound of formula (I) for use in the treatment or prevention of mental diseases A is N, CH, C having a double bond or CR5; each of B and Z is independently N, CH or CR1, with the proviso that A is N when B and/or Z is N; R1, R2, R3, R4and R5and n are as defined in the specification.