Amide compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
申请人:——
公开号:US20020103203A1
公开(公告)日:2002-08-01
Amide compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
PROCESS FOR THE ATTACHMENT OF A GALNAC MOIETY COMPRISING A (HETERO)ARYL GROUP TO A GLCNAC MOIETY, AND PRODUCT OBTAINED THEREBY
申请人:SynAffix B.V.
公开号:EP3097200A1
公开(公告)日:2016-11-30
[EN] PROCESS FOR THE ATTACHMENT OF A GALNAC MOIETY COMPRISING A (HETERO)ARYL GROUP TO A GLCNAC MOIETY, AND PRODUCT OBTAINED THEREBY<br/>[FR] PROCÉDÉ POUR LA FIXATION D'UNE FRACTION GALNAC COMPRENANT UN GROUPE (HÉTÉRO)ARYLE À UNE FRACTION GLCNAC, ET PRODUIT AINSI OBTENU
申请人:SYNAFFIX BV
公开号:WO2015112013A1
公开(公告)日:2015-07-30
The present invention relates to a process for attaching an N-acetylgalactosamine- (hetero)arylmoiety to an N-acetylglucosaminemoiety, the process comprising the step of contacting the N-acetylgalactosamine-(hetero)arylmoiety with the N- acetylglucosaminemoiety in the presence of a mutant galactosyltransferase, wherein the N-acetylglucosaminemoiety is according to Formula (1)the N- acetylgalactosamine-(hetero)arylmoiety is according to Formula (2): In a particularly preferred embodiment of the process according to the invention, the N-acetylgalactosamine-(hetero)arylmoiety comprises a 1,3-dipole functional group, and the N-acetylglucosaminemoiety is a terminal GlcNAc moiety of a glycoprotein glycan. The invention further relates to a productobtainable by the process according to the invention, in particular to glycoproteins. Also, the invention relates to several compounds comprising an N-acetylgalactosamine-(hetero)arylmoiety.
Tuning activation and self-immolative properties of the bioorthogonal alkene–azide click-and-release strategy
作者:Jessica M. Fairhall、Madoka Murayasu、Sumit Dadhwal、Sarah Hook、Allan B. Gamble
DOI:10.1039/d0ob00936a
日期:——
Combinations of aryl azides and trans-cyclooctenes have been studied in a bioorthogonal click-and-release strategy, with two reaction pairings rapidly releasing phenol at micromolar concentrations.