166047-75-2

Upstream product

• 67-56-1 methanol 
• 132491-89-5 tris(cyanoethoxymethyl)aminomethane 
• 566168-32-9 [2-(2-cyano-ethoxy)-1,1-bis-(2-cyano-ethoxymethyl)-ethyl]-carbamic acid tert-butyl ester 

Downstream Products

• 200133-17-1 benzyl N-tris[2-{[({tris[[2-(methoxycarbonyl)ethoxy]methyl]methyl}amino)carbonyl]ethoxy}methyl]methylcarbamate 
• 220886-02-2 N-(N-benzyloxycarbonyl-glycinyl)-tris(carboxyethoxymethyl)aminomethane 
• 200133-20-6 di-tert-butyl 3,3'-((2-(((benzyloxy)carbonyl)amino)-2-((3-(tert-butoxy)-3-oxopropoxy)methyl)propane-1,3-diyl)bis(oxy))dipropionate 
• 200133-16-0 benzyl N-tris[(2-carboxyethyloxy)methyl]methylcarbamate 
• 175724-30-8 tris{[2-(tert-butoxycarbonyl)ethoxy]methyl}methylamine 
• 200133-15-9 N-(Benzyloxycarbonyl)-tris[((methoxycarbonyl)ethoxy)methyl]aminomethane 

Relevant academic research and scientific papers

A dendritic DPA annihilator—syntheses, photophysical properties and application for co-assembling enhanced triplet-triplet annihilation upconversion

A dendritic annihilator D-2 containing 18 peripherical methyl ester units was synthesized by attaching the branches on the phenyl unit of 9,10-diphenylanthracene (DPA). The absorption and emission spectra of D-2 are very similar to the unbranched DPA diacid 5 and the lower branched homolog D-1, while the fluorescence quantum yield increased with the degrees of the branching and was determined to be 86.9percent for D-2 in MeOH. D-2 was used as the annihilator for triplet-triplet annihilation upconversion with a Schiff-base Pt(II) complex serving as the sensitizer. It was found that D-2 showed very weak UC emission in MeOH with a UC quantum yield of only 1.4percent. Interestingly, the UC emission intensity increased significantly by adding different amounts of water in MeOH, the UC intensity was enhanced by more than 9 fold by adding 40percent water into MeOH, and the UC quantum yield was determined to be 10.2percent in MeOH with 40percent water. A mechanism for the enhancing of UC emission was proposed: When in MeOH, the large molecule size of the dendrimer limited the movability of the acceptor, and the shielding effect of the dendritic branches on the DPA core limited the intimate contacts among DPA cores or between DPA core and the sensitizer. When the water was added, D-2 aggregated to nanoparticles with internal hydrophobic cavities induced by the hydrophobic effect and π-π stacking of DPA core, the sensitizer Pt-1 was captured in the internal hydrophobic cavities, and thus, both the TTET and TTA processes were greatly accelerated which attributed to the enhanced TTA-UC.

High-loading resin beads for solid phase synthesis using triple branching symmetrical dendrimers

Resin beads with a loading of 200 nmol per bead have been prepared using a Generation 2.0 tris-based dendrimer to amplify resin loading sites.

Polyanion inhibitors of human immunodeficiency virus. Part IV. - Polymerized anionic surfactants : Influence of the density and distribution of anionic groups on the antiviral activity

The synthesis of a series of new polyanions, via γ-polymerization, of ω-unsaturated multi-charged anionic surfactants, has been realized. These polyanions were evaluated for their activity against HIV-1. All tested compounds proved active without presenting toxicity to the host cells (CEM-4 or MT-4).

TARGETED BIFUNCTIONAL DEGRADERS

The present invention provides, in one aspect, bifunctional compounds that can be used to promote or enhance degradation of certain circulating proteins. In another aspect, the present invention provides bifunctional compounds that can be used to promote or enhance degradation of certain autoantibodies. In certain embodiments, treatment or management of a disease and/or disorder requires degradation, removal, or reduction in concentration of the circulating protein or the autoantibody in the subject. Thus, in certain embodiments, administration of a compound of the invention to the subject removes or reduces the circulation concentration of the circulating protein or the autoantibody, thus treating, ameliorating, or preventing the disease and/or disorder. In certain embodiments, the circulating protein is TNF.

ENGINEERED ANTIBODIES AS MOLECULAR DEGRADERS THROUGH CELLULAR RECEPTORS

The present disclosure provides, in one aspect, bifunctional compounds that can be used to promote or enhance degradation of certain circulating proteins. In certain embodiments, the circulating protein mediates a disease and/or disorder in a subject, and treatment or management of the disease and/or disorder requires degradation, removal, or reduction in concentration of the circulating protein in the subject. Thus, in certain embodiments, administration of a compound of the disclosure to the subject removes or reduces the circulation concentration of the circulating protein, thus treating, ameliorating, or preventing the disease and/or disorder.

BI-FUNCTIONAL MOLECULES TO DEGRADE CIRCULATING PROTEINS

The present invention is directed to bi-functional compounds which find use as pharmaceutical agents in the treatment of disease states and/or conditions which are through.macrophage migration inhibitory factor (MIF) or immunoglubin G (IgG). The present invention is also directed to pharmaceutical compositions which comprise these bi- functional compounds as well as methods for treating disease states and/or conditions which are mediated through MIF/lgG or where MIF/lgG is a contributing factor to the development and perpetuation of diseases and/or conditions, especially including autoimmune diseases and cancer, among others. The purpose of the present invention is to provide a molecular strategy to lower plasma MIF/lgG level in patients with autoimmune diseases or certain types of cancers. The b.i -functional molecule construct is comprised of a MIF/IgQ-targeting motif, that is derived from small molecule MIF/lgG ligands, and an ASGPr- targeting motif that binds to hepatocyte asialoglycoprotein receptor { ASGPr). The compounds selectively bind MIF or IgG in plasma and subsequently engage the endo-lysosomal pathway of hepatocytes through ASGPr. As a consequence, MIF/igG is internalized and degraded by hepatocytes, thus resulting in potential attenuation of corresponding disease symptoms which are modulated through MIF/igG.

BIFUNCTIONAL SMALL MOLECULES TO TARGET THE SELECTIVE DEGRADATION OF CIRCULATING PROTEINS

The present invention is directed to bifunctional small molecules which contain a circulating protein binding moiety (CPBM) linked through a linker group to a cellular receptor binding moiety (CRBM) which is a membrane receptor of degrading cell such as a hepatocyte or other degrading cell. In embodiments, the (CRBM) is a moiety which binds to asialoglycoprotein receptor (an asialoglycoprotein receptor binding moiety, or ASGPRBM) of a hepatocyte. In additional embodiments, the (CRBM) is a moiety which binds to a receptor of other cells which can degrade proteins, such as a LRP1, LDLR, FcyRI, FcRN, Transferrin or Macrophage Scavenger receptor. Pharmaceutical compositions based upon these bifunctional small molecules represent an additional aspect of the present invention. These compounds and/or compositions may be used to treat disease states and conditions by removing circulating proteins through degradation in the hepatocytes or macrophages of a patient or subject in need of therapy. Methods of treating disease states and/or conditions in which circulating proteins are associated with the disease state and/or condition are also described herein.

Adaptable synthesis of C-glycosidic multivalent carbohydrates and succinamide-linked derivatization

A modular approach to the synthesis of trivalent C-glycosidic carbohydrates is described. The approach is illustrated employing carboxylate-terminated C-glycosidic d-mannose, d-glucose, and d-galactose derivatives with different length C1-linked spacer un

Facile synthesis of second-generation dendrons with an orthogonal functional group at the focal point

Facile synthesis of second-generation dendrons with an aldehyde, epoxy, or t-Boc group at the focal point and nine carboxylic acid groups at the periphery is reported. The scheme includes a coupling of the first-generation dendrons and a two-step, one-pot reaction that proceeds through a Boc deprotection and in situ conjugation at the focal point.