21395-93-7Relevant academic research and scientific papers
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.
NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE
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, (2013/03/26)
Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.
An optimised synthetic approach to a chiral derivatising agent and the utilisation of a dimerisation reaction in the synthesis of a novel C2-symmetric diphosphine ligand
Williams, Glynn D.,Wade, Charles E.,Clarkson, Guy J.,Wills, Martin
, p. 664 - 670 (2007/10/03)
We report an optimised synthetic approach to the chiral derivatising agent (5R)-methyl-1-(chloromethyl)-2-pyrrolidinone. In addition, the observation of an unwanted dimerisation product is turned to our advantage by providing a method for the synthesis of a new class of C2-symmetric chiral diphosphine.
Copper(I) mediated cross-coupling of amino acid derived organozinc reagents with acid chlorides
Hjelmgaard, Thomas,Tanner, David
, p. 1796 - 1805 (2008/02/05)
This paper describes the development of a straightforward experimental protocol for copper-mediated cross-coupling of amino acid derived β-amido-alkylzinc iodides 1 and 3 with a range of acid chlorides. The present method uses CuCN·2LiCl as the copper source and for organozinc reagent 1 the methodology appears to be limited to reaction with more stable acid chlorides, providing the desired products in moderate yields. When applied to organozinc reagent 3, however, the protocol is more general and provides the products in good yields in all but one of the cases tested. The Royal Society of Chemistry 2006.
5(R)-Methyl-1-(chloromethyl)-2-pyrrolidinone: A New Reagent for the Determination of Enantiomeric Composition of Alcohols
Smith, Michael B.,Dembofsky, Bruce T.,Son, Young Chan
, p. 1719 - 1725 (2007/10/02)
We have prepared a new chiral nonracemic reagent (5(R)-methyl-1-(chloromethyl)-2-pyrrolidinone) in enantiopure form that reacts with alcohols containing a stereogenic center to produce diastereomeric N-(alkoxymethyl)-2-pyrrolidinone derivatives.These derivatives exhibit large and easily observed diastereotopic signals in the proton NMR that allow direct determination of diastereomeric ratio (percent dr) for the product.
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.
