- Oligomer modified diaromatic substituted compounds
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Disclosed are compounds comprising diaromatic substituted compound residues, namely the anti-viral (anti-HIV) drug delavirdine, covalently attached via a linkage to water-soluble, non-peptidic oligomers, specifically to poly(ethylene glycol) (PEG) oligome
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- FGFR2 MODULATORS
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A compound of Formula (I), or a pharmaceutically acceptable salt thereof, wherein:R3a, R2, R3b, R4b, L1, G and J are as defined in the specification, pharmaceutical compositionsthereof, and methods of use thereof.
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Page/Page column 45
(2012/05/20)
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- Strategy for 14C-labeling of a series of bis(heteroaryl) piperazines
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Four bis(heteroaryl)piperazines labeled with carbon-14 in the 2-position of imidazole moiety were prepared as part of a 4-step (or 5-step) sequence from 5-hydroxymethyl-2-mercapto-1-benzylimida-zole-[2-14C] as a key synthetic intermediate which
- Arjomandi, Omid Khalili,Saemian, Nader,Shirvani, Gholamhossein,Javaheri, Mohsen,Esmailli, Kameh
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scheme or table
p. 363 - 366
(2012/06/04)
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- PIPERAZINE AND PIPERIDINE MGLUR5 POTENTIATORS
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Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof, wherein A, B, D, Ar1, Ar2, R2, R3, R4, a, m and n are defined in the specification, methods for the use thereof, processes for making and pharmaceutical compositions containing the same.
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Page/Page column 38-39
(2008/12/07)
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- Synthesis and anti-HIV-1 activity of new delavirdine analogues carrying arylpyrrole moieties
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In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) values in the submicromolar range.
- Pinna,Loriga,Murineddu,Grella,Mura,Vargiu,Murgioni,La Colla
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p. 1406 - 1411
(2007/10/03)
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- Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors
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A variety of analogues of 1-[4-methoxy-3,5-dimethylbenzyl]-4-[3- (ethylamino)-2-pyridyl]piperazine hydrochloride (U-80493E) were synthesized and evaluated for their inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). Replacement of the substituted aryl moiety with various substituted indoles provided bis(heteroaryl)piperazines (BHAPs) that were 10-100-fold more potent than U-80493E. The pyridyl portion of the lead molecule was found to be very sensitive to modifications. Extensive preclinical evaluations of several of these compounds led to the selection of 1-[(5-methoxyindol-2-yl)carbonyl]-4-[3-(ethylamino)-2- pyridyl]piperazine methanesulfonate (U-87201E, atevirdine mesylate) for clinical evaluation.
- Romero,Morge,Biles,Berrios-Pena,May,Palmer,Johnson,Smith,Busso,Tan,Voorman,Reusser,Althaus,Downey,So,Resnick,Tarpley,Aristoff
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p. 999 - 1014
(2007/10/02)
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- Novel 21-Aminosteroids That Inhibit Iron-Dependent Lipid Peroxidation and Protect against Central Nervous System Trauma
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A novel class of 21-aminosteroids has been developed.Compounds within this series are potent inhibitors of iron-dependent lipid peroxidation in rat brain homogenates with IC50's as low as 3 μM.Furthermore, selected members enhance early neurolo
- Jacobsen, E. Jon,McCall, John M.,Ayer, Donald E.,VanDoornik, Fred J.,Palmer, John R.,et al.
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p. 1145 - 1151
(2007/10/02)
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