194669-45-9Relevant academic research and scientific papers
20-HETE FORMATION INHIBITORS
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Paragraph 0257-0262, (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.
PYRROLOTRIAZINES AS ALK INHIBITORS
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Page/Page column 29, (2014/12/12)
This application provides compounds of the general formula (I) and/or a salt thereof, where X, R1 and R2 are as defined herein. Compositions and therapeutic uses are also described.
GLYCOSIDASE INHIBITORS
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Page/Page column 67; 68, (2014/10/15)
Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
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
supporting information; experimental part, 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.
Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists
Pasternak, Alexander,Goble, Stephen D.,Vicario, Pasquale P.,Di Salvo, Jerry,Ayala, Julia M.,Struthers, Mary,DeMartino, Julie A.,Mills, Sander G.,Yang, Lihu
, p. 994 - 998 (2008/09/19)
This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had i
Synthesis of 4-substituted tetrahydropyridines by cross-coupling of enol phosphates
Larsen, Uffe S.,Martiny, Lars,Begtrup, Mikael
, p. 4261 - 4263 (2007/10/03)
Enol phosphates, synthesized from 4-piperidone, react by palladium catalyzed cross-coupling with arylboronic acids and by iron and palladium catalyzed cross-coupling with Grignard reagents to give 4-substituted tetrahydropyridines.
Design and synthesis of orally active inhibitors of TNF synthesis as anti-rheumatoid arthritis drugs
Chen, Jian Jeffrey,Dewdney, Nolan,Lin, Xiaohong,Martin, Robert L.,Walker, Keith A. M.,Huang, Jane,Chu, Frances,Eugui, Elsie,Mirkovich, Anna,Kim, Yong,Sarma, Keshab,Arzeno, Humberto,Van Wart, Harold E.
, p. 3951 - 3954 (2007/10/03)
A novel series of TNF inhibitors was identified based on the screening of existing MMP inhibitor libraries. Further SAR optimization led to the discovery of a novel lead compound. Its synthesis, efficacy in experimental animal models, and pharmacokinetic
SELECTIVE MELANIN CONCENTRATING HORMONE-1 (MCH1) RECEPTOR ANTAGONISTS AND USES THEREOF
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, (2008/06/13)
This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. This invention further provides a method of treating a feeding disorder in a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. In an embodiment of the invention, the feeding disorder is bulimia, bulimia nervosa or obesity.
