50534-24-2Relevant academic research and scientific papers
IDO INHIBITORS
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Paragraph 1973, (2016/10/27)
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
1-Amido-1-phenyl-3-piperidinylbutanes - CCR5 antagonists for the treatment of HIV. Part 1
Barber, Christopher G.,Blakemore, David C.,Chiva, Jean-Yves,Eastwood, Rachel L.,Middleton, Donald S.,Paradowski, Kerry A.
scheme or table, p. 1075 - 1079 (2009/08/07)
The development of a new class of CCR5 antagonist replacing the tropane core of maraviroc by piperidine with a branched N-substituent is described. Compound 15h shows good whole cell antiviral activity together with microsomal stability and only weak activity at the hERG ion channel.
CHEMICAL COMPOUNDS I
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Page/Page column 36, (2010/02/15)
Compounds of formula (I) compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides
Cumming, John G.,Cooper, Anne E.,Grime, Ken,Logan, Chris J.,McLaughlin, Sharon,Oldfield, John,Shaw, John S.,Tucker, Howard,Winter, Jon,Whittaker, David
, p. 5012 - 5015 (2007/10/03)
SAR and DMPK studies led to the identification of substituted N-alkyl-N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-2-phenylacetamides as potent and orally bioavailable ligands for the human CCR5 chemokine receptor.
CHEMICAL COMPOUNDS
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Page/Page column 26, (2010/02/12)
Compounds of formula (I): [Chemical formula should be inserted here. Please see paper copy] compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
Anilide derivative, production and use thereof
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, (2008/06/13)
This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.
Alkyl substituted piperadinyl and piperazinyl anti-AIDS compounds
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, (2008/06/13)
Anti-AIDS compounds of formula (I) STR1 wherein R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification and R8 is alkyl of substituted alkyl.
Targeting delavirdine/atevirdine resistant HIV-1: Identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors
Romero, Donna L.,Olmsted, Robert A.,Poel, Toni Jo,Morge, Raymond A.,Biles, Carolyn,Keiser, Barbara J.,Kopta, Laurice A.,Friis, Jan M.,Hosley, John D.,Stefanski, Kevin J.,Wishka, Donn G.,Evans, David B.,Morris, Joel,Stehle, Randy G.,Sharma, Satish K.,Yagi, Yoshihiko,Voorman, Richard L.,Adams, Wade J.,Tarpley, W. Gary,Thomas, Richard C.
, p. 3769 - 3789 (2007/10/03)
A novel class of bis(heteroaryl)piperazine (BHAP) analogs which possesses the ability to inhibit NNRTI (non-nucleoside reverse transcriptase inhibitor) resistant recombinant HIV-1 reverse transcriptase (RT) and NNRTI resistant variants of HIV-1 has been identified via targeted screening. Further investigation of the structure-activity relationships of close congeners of these novel (alkylamino)piperidine BHAPs (AAP-BHAPs) led to the synthesis of several compounds possessing the desired phenotype (e.g., activity against recombinant RTs carrying the Y181C and P236L substitutions). Further structural modifications were required to inhibit metabolism and modulate solubility in order to obtain compounds with the desired biological profile as well as appropriate pharmaceutical properties. The AAP-BHAPs with the most suitable characteristics were compounds 7, 15, and 36.
