14678-48-9Relevant academic research and scientific papers
HETEROARYL-1,2,4-TRIAZOLE AND HETEROARYL-TETRAZOLE COMPOUNDS FOR CONTROLLING ECTOPARASITES
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Page/Page column 47, (2017/12/14)
The present invention provides compounds of the formula : (I) wherein: X is O or S; Q1 and Q2 are independently CR5 or N, provided at least one of Q1 and Q2 is N; Y is a direct bond or CH2;
Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains
Taylor, Alexander M.,Vaswani, Rishi G.,Gehling, Victor S.,Hewitt, Michael C.,Leblanc, Yves,Audia, James E.,Bellon, Steve,Cummings, Richard T.,Co?té, Alexandre,Harmange, Jean-Christophe,Jayaram, Hari,Joshi, Shivangi,Lora, Jose M.,Mertz, Jennifer A.,Neiss, Adrianne,Pardo, Eneida,Nasveschuk, Christopher G.,Poy, Florence,Sandy, Peter,Setser, Jeremy W.,Sims, Robert J.,Tang, Yong,Albrecht, Brian K.
, p. 145 - 150 (2016/03/01)
Inhibition of the bromodomains of the BET family, of which BRD4 is a member, has been shown to decrease myc and interleukin (IL) 6 in vivo, markers that are of therapeutic relevance to cancer and inflammatory disease, respectively. Herein we report substituted benzo[b]isoxazolo[4,5-d]azepines and benzotriazolo[4,3-d][1,4]diazepines as fragment-derived novel inhibitors of the bromodomain of BRD4. Compounds from these series were potent and selective in cells, and subsequent optimization of microsomal stability yielded representatives that demonstrated dose- and time-dependent reduction of plasma IL-6 in mice.
MODULATORS OF HISTONE METHYLTRANSFERASE, AND METHODS OF USE THEREOF
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Page/Page column 156, (2012/06/30)
Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.
BROMODOMAIN INHIBITORS AND USES THEREOF
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, (2012/11/14)
The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Initial efforts toward the optimization of arylomycins for antibiotic activity
Roberts, Tucker C.,Schallenberger, Mark A.,Liu, Jian,Smith, Peter A.,Romesberg, Floyd E.
supporting information; experimental part, p. 4954 - 4963 (2011/10/04)
While most clinically used antibiotics were derived from natural products, the isolation of new broad-spectrum natural products has become increasingly rare and narrow-spectrum agents are typically deemed unsuitable for development because of intrinsic limitations of their scaffold or target. However, it is possible that the spectrum of a natural product antibiotic might be limited by specific resistance mechanisms in some bacteria, such as target mutations, and the spectra of such "latent" antibiotics might be reoptimized by derivatization, just as has been done with clinically deployed antibiotics. We recently showed that the spectrum of the arylomycin natural product antibiotics, which act via the novel mechanism of inhibiting type I signal peptidase, is broader than previously believed and that resistance in several key human pathogens is due to the presence of a specific Pro residue in the target peptidase that disrupts interactions with the lipopeptide tail of the antibiotic. To begin to test whether this natural resistance might be overcome by derivatization, we synthesized analogues with altered lipopeptide tails and identified several with an increased spectrum of activity against S. aureus. The data support the hypothesis that the arylomycins are latent antibiotics, suggest that their spectrum may be optimized by derivatization, and identify a promising scaffold upon which future optimization efforts might focus.
BICYCLIC ARYL SPHINGOSINE 1-PHOSPHATE ANALOGS
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, (2011/02/24)
Compounds that have agonist activity at one or more of the SlP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at SlP receptors.
OXAZOLE PYRIDINE DERIVATIVES USEFUL AS S1P1 RECEPTOR AGONISTS
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Page/Page column 142-143, (2010/09/18)
The present invention provides oxadiazole pyridine derivatives of Formula (I), their use as medicaments and their use for treating multiple sclerosis and other diseases
Efficient synthesis of β2-amino acid by homologation of α-amino acids involving the reformatsky reaction and Mannich-type imminium electrophile
Moumne, Roba,Lavielle, Solange,Karoyan, Philippe
, p. 3332 - 3334 (2007/10/03)
Development of new methods for the synthesis of β-amino acids is important as polymers of these compounds are promising peptidomimetic candidates in medicinal chemistry. We report here our findings on a new and highly efficient general strategy for the synthesis of β2-amino acids by homologation of α-amino acids, involving the Reformatsky reaction and Mannich-type imminium electrophile.
ALPHA-AMINOACYL BETA-AMINOACYL AMINODIOLS AS ANTI-HYPERTENSIVE AGENTS
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, (2008/06/13)
Compounds characterized generally as α-aminoacyl β-aminoactyl aminodiols are useful as renin inhibitors for the treatment of hypertension.
