72479-05-1Relevant articles and documents
Anti-inflammatory agents
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Page/Page column 127; 128, (2016/02/05)
Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation.
BICYCLIC AZA COMPOUNDS AS MUSCARINIC M1 RECEPTOR AGONISTS.
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, (2015/09/22)
This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1 , R2, R3 and R4 are as defined herein.
The fluorine-NHC gauche effect: A structural and computational study
Paul, Susann,Schweizer, W. Bernd,Rugg, Graham,Senn, Hans Martin,Gilmour, Ryan
supporting information, p. 5647 - 5659 (2013/07/11)
Herein, we report the synthesis and X-ray structural analysis of a collection of fluorinated metal N-heterocyclic carbenes (Ag, Au, Pd, Rh, Ir) and their precursor salts. The common structural feature of these species is a flanking fluoroethyl group, which is either freely rotating or embedded within a bicyclic framework. Solid state analysis confirmed a gauche conformational preference in all cases with the fluorine adopting a syn clinal arrangement (φ[NCCF]～60°) with respect to the triazolium nitrogen at the vicinal position of the NHC. A density functional theory analysis was employed to quantify these effects and evaluate the influence of electronic modulation of the carbenic carbon [(CN+); neutral carbene (C:); metal-bound carbene (CM)], on the relative gauche/anti preference, thus highlighting the potential of this conformational phenomenon as a useful molecular design strategy for controlling the topology of organometallic complexes.
TREATMENT OF DISEASES BY EPIGENETIC REGULATION
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Paragraph 0708, (2013/11/05)
The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.
TETRACYCLINE ANALOGS
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Page/Page column 162, (2012/03/09)
The present invention is directed to a compound represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.
82. Enantioselective reduction of electrophilic C=C bonds with sodium tetrahydroborate and 'semicorrin' cobalt catalysts
Misun, Marian,Pfaltz, Andreas
, p. 961 - 972 (2007/10/03)
'Semicorrin' cobalt complexes, prepared in situ from cobalt(II) chloride and the corresponding ligands, are efficient catalysts for the enantioselective reduction of electrophilic C=C bonds with NaBH4. The best selectivities (> 90% ee) are achieved with α,β-unsaturated carboxamides and carboxylates. Analogous α,β-unsaturated nitriles, sulfones, and phosphonates afford enantiomenc excesses of 50-70%. Interestingly, in the reduction of α,β-unsaturated sulfones, the highest enantioselectivities were obtained with unsymmetrical 'semicorrins', whereas in all other cases C2-symmetric 'semicorrins' proved to be superior.
Lactones, part 28: EPC-Synthesis, structure and pharmacology of 'lactonized' and 'lactamized' analogues of acetylcholine
Pieper,Trankle,Nieger,Mohr,Lehmann
, p. 15 - 21 (2007/10/02)
The enantiopure γ-aminomethyl-γ-butyrolactones (S)- and (R)-4a-d represent constrained analogues of acetylcholine, which were synthesized from D- or L-glutamic acid following two different routes. In addition, the corresponding lactames (S)- and (R)-10 were prepared by enantioselective synthesis. Only moderate activity was found at acetylcholine sites at the guinea pig atrium.
Man-designed bleomycin with altered sequence specificity in DNA cleavage
Otsuka,Masuda,Haupt,Ohno,Shiraki,Sugiura,Maeda
, p. 838 - 845 (2007/10/02)
The synthetic approach to the concerted antitumor mechanism of bleomycin is studied by introducing a dynamic change into the O2-activation moiety and DNA-binding site. A model PYML(6)-bleomycin previously reported, possessing an oxygen-activating methoxypyridine moiety and a DNA-binding bithiazole moiety, exhibits a nucleotide cleavage mode virtually identical with that of bleomycin. Herein reported is a newly designed bleomycin analogue, PYML(6)-(4R-APA)-distamycin, wherein the 4-methoxypyridine moiety and a DNA-binding distamycin component are connected through an (R)-4-aminopentanoic acid linker moiety. Synthesis of PYML(6)-(4R-APA)-distamycin is carried out by condensation of the hydroxyhistidine-pentatoic acid fragment with the methoxypyridien moiety, followed by introducing of the distamycin moiety. PYML(6)-(4R-APA)-distamycin cleaves a G4 phage DNA fragment (100 base pairs) at 1 μM concentration in the presence of Fe(II), oxygen, and dithiothreitol and induces dramatically altered adenine/thymine specificity. It is indicated that the specific recognition of base sequences for the cleavage is mainly controlled by the DNA affinity site and that the (R)-4-aminopentanoic acid linker seems to determine the proper arrangement of the iron-oxygen site and the distamycin moiety on DNA.
