80912-60-3Relevant academic research and scientific papers
NOVEL 5 or 8-SUBSTITUTED IMIDAZO [1, 5-a] PYRIDINES AS SELECTIVE INHIBITORS OF INDOLEAMINE AND/OR TRYPTOPHANE 2, 3-DIOXYGENASES
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, (2018/04/20)
Disclosed herein are 5 or 8-substituted imidazo [1, 5-a] pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo [1, 5-a] pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8-substituted imidazo [1, 5-a] pyridines that can be useful for inhibiting indoleamine 2, 3-dioxygenase and/or tryptophane 2, 3-dioxygenase and for treating diseases or disorders mediated thereby.
Design and synthesis of novel small molecule CCR2 antagonists: Evaluation of 4-aminopiperidine derivatives
Vilums,Zweemer,Dekkers,Askar,De Vries,Saunders,Stamos,Brussee,Heitman,Ijzerman
supporting information, p. 5377 - 5380 (2015/01/09)
A novel N-(2-oxo-2-(piperidin-4-ylamino)ethyl)-3-(trifluoromethyl)benzamide series of human CCR2 chemokine receptor antagonists was identified. With a pharmacophore model based on known CCR2 antagonists a new core scaffold was designed, analogues of it synthesized and structure-affinity relationship studies derived yielding a new high affinity CCR2 antagonist N-(2-((1-(4-(3-methoxyphenyl)cyclohexyl)piperidin-4-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide.
Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists
Zhang, Xuqing,Hufnagel, Heather,Markotan, Thomas,Lanter, James,Cai, Chaozhong,Hou, Cuifen,Singer, Monica,Opas, Evan,McKenney, Sandra,Crysler, Carl,Johnson, Dana,Sui, Zhihua
supporting information; experimental part, p. 5577 - 5582 (2011/10/09)
A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.
GUANIDINE DERIVATIVES AND USE THEREOF AS NEUROPEPTIDE FF RECEPTOR ANTAGONISTS
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Page 49-52, (2010/02/08)
The invention relates to guanidine derivatives of formula (I) where: A = a chain of 3-c6 carbon atoms, one of which can be replaced by -N(R')- or -O- and R' = H or a substituent, where the ring skeleton only contains both double bonds of the thiazole component, the pharmaceutically-acceptable acid addition salts of basic compounds of formula (I), the pharmaceutically-acceptable salts of compounds of formula (I),, comprising acid groups, with bases, the pharmaceutically-acceptable esters of hydroxy or carboxyl group containing compounds of formula (I) and the solvates or hydrates thereof, which are partly known and partly novel and exhibit a neuropeptide FF receptor antagonist effect. The above are suitable for the treatment of pain and hyperalgesia, withdrawal symptoms in alcohol, psychotropic and nicotine dependencies, for improvement or cure of said dependencies, for regulation of insulin excretion, food intake, memory functions, blood pressure, electrolyte and energy management and for treatment of urinary incontinence. The above can be produced using generally used methods and processed to give medicaments.
Application of the β-azidonation reaction to the enantioselective synthesis of the lycorane amaryllidaceae alkaloids
Magnus,Bailey,Porter
, p. 13927 - 13936 (2007/10/03)
The prochiral ketone 5 was treated with the lithium salt of (+)-bis(α- methylbenzyl)amine, followed by triisopropylsilyl trifluoromethanesulfonate to give 10 (96%). β-Azidonation of 10 with (PhlO)(n)/TMSN3 rapidly produced 11 (95%) as a mixture
ANTIISCHEMIC PIPERAZINYL- AND PIPERIDINYL-CYCLOHEXANES
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, (2008/06/13)
Certain piperazinyl-and piperidinyl-substituted cyclohexanes have anti-ischemic properties.
1-(4-Aryl-cyclohexyl)piperidine derivatives, method of use thereof and pharmaceutical compositions thereof
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, (2008/06/13)
Novel 1-[1-(4-aryl-cyclohexyl)-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-ones and 1-aryl-8-(4-aryl-cyclohexyl)-1,3,8-triazaspiro[4,5]decan-4-ones which are useful as antiemetic-and neuroleptic agents.
