192650-25-2

Upstream product

• 1363334-41-1 C₁₇H₂₁NO₆ 
• 16642-79-8 3-(4-nitrophenyl)propionic acid 
• 107324-93-6 3-(p-nitrophenyl)propanoyl chloride 
• 123-54-6 acetylacetone 
• 100-11-8 1-bromomethyl-4-nitro-benzene 

Downstream Products

• 782475-33-6 C₁₆H₂₁NO₆ 
• 192650-26-3 4-[4-(3,5-dioxo-hexyl)-phenylcarbamoyl]-butyric acid 
• 220689-91-8 C₁₂H₁₅NO₂ 
• 1363334-43-3 C₂₆H₄₂N₃O₆⁽¹⁺⁾*Cl^(1-) 
• 1363334-40-0 C₂₂H₃₄N₃O₄⁽¹⁺⁾*Cl^(1-) 
• 1363334-42-2 C₂₁H₂₉NO₇ 
• 905569-07-5 C₁₄H₁₇NO₅ 
• 929088-03-9 3-[4-(2-{2-[2-(2-{2-[4-(3,5-dioxo-hexyl)-phenylcarbamoyl]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-ethoxy)-phenyl]-N-[2'-(isoxazol-5-ylsulfamoyl)-4-oxazol-2-yl-biphenyl-2-ylmethyl]-N-methyl-propionamide 
• 929088-02-8 N-[4-(3,5-dioxo-hexyl)-phenyl]-3-{2-[2-(2-{2-[4-({[2'-(isoxazol-5-ylsulfamoyl)-4-oxazol-2-yl-biphenyl-2-ylmethyl]-methyl-carbamoyl}-methyl)-phenoxy]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-propionamide 
• 929087-93-4 N-(2'-(isoxazol-5-ylsulfamoyl)-4-{2-[2-(2-{2-[2-(4-{2-[2-(2-methyl-[1,3]dioxolan-2-ylmethyl)-[1,3]dioxolan-2-yl]-ethyl}-phenylcarbamoyl)-ethoxy]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-biphenyl-2-ylmethyl)-3,3,N-trimethyl-butyramide 
• 929087-89-8 3-(2-{2-[2-({[2'-(isoxazol-5-ylsulfamoyl)-4-oxazol-2-yl-biphenyl-2-ylmethyl]-methyl-carbamoyl}-methoxy)-ethoxy]-ethoxy}-ethoxy)-N-(4-{2-[2-(2-methyl-[1,3]dioxolan-2-ylmethyl)-[1,3]dioxolan-2-yl]-ethyl}-phenyl)-propionamide 
• 929087-81-0 N-[4-(2-{2-[2-(2-{2-[4-(3,5-dioxo-hexyl)-phenylcarbamoyl]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-ethoxy)-2'-(isoxazol-5-ylsulfamoyl)-biphenyl-2-ylmethyl]-3,3,N-trimethyl-butyramide 
• 929087-92-3 3-{2-[2-(2-{2-[2-formyl-2'-(isoxazol-5-ylsulfamoyl)-biphenyl-4-yloxy]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-N-(4-{2-[2-(2-methyl-[1,3]dioxolan-2-ylmethyl)-[1,3]dioxolan-2-yl]-ethyl}-phenyl)-propionamide 
• 929087-80-9 N-[4-(3,5-dioxo-hexyl)-phenyl]-3-(2-{2-[2-({[2'-(isoxazol-5-ylsulfamoyl)-4-oxazol-2-yl-biphenyl-2-ylmethyl]-methyl-carbamoyl}-methoxy)-ethoxy]-ethoxy}-ethoxy)-propionamide 

Relevant academic research and scientific papers

Synthesis of a novel analytical reagent for the determination of active sites for conjugation on a catalytic aldolase monoclonal antibody

An optimized and scalable synthesis of a novel analytical reagent for the determination of the number of active sites available for conjugation on a catalytic aldolase monoclonal antibody (mAb) is described. The original conditions suffered from lack of reproducibility, incomplete reactions, and required several chromatographies and lyophilizations that afforded material of low purity. A redesigned route and optimized protocols have been developed that eliminate the use of toxic and unsafe reagents such as HMPA and HATU. In addition, the number of chromatographies has been reduced to only one and time-consuming and energy-intensive lyophilizations are no longer required. The overall yield has been considerably improved from the original 4% to 20% after telescoping the last two steps of the synthesis and this new approach allowed for the preparation of material with higher chemical purity (≥99% vs the initial 90%) to meet specifications.

GLUCAGON-LIKE PROTEIN-1 RECEPTOR (GLP-1R) AGONIST COMPOUNDS

The present invention provides GA targeting compounds which comprise GA targeting agent-linker conjugates linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to prevent or treat diabetes or diabetes-related conditions.

ANTI-ANGIOGENIC COMPOUNDS

The present invention provides AA targeting compounds which comprise AA targeting agent-linker conjugates which are linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to treat disorders connected to abnormal angiogenesis.

Chemically programmed antibodies: Endothelin receptor targeting CovX-Bodies

Aryl sulfonamide-based endothelin antagonists were synthesized and covalently linked to the reactive lysine of the m38C2 antibody to create a series of CovX-Bodies. These chemically programmed antibodies behaved as potent endothelin receptor antagonists in vitro and had antitumor efficacy in a prostate cancer xenograft model which, on a molar basis, far exceeded the activity of the parent small molecule.

Anti-angiogenic compounds

The present invention provides AA targeting compounds which comprise AA targeting agent-linker conjugates which are linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to treat disorders connected to abnormal angiogenesis.

Artificial aldolases from peptide dendrimer combinatorial libraries

Peptide dendrimers were investigated as synthetic models for aldolase enzymes. Combinatorial libraries were prepared with aldolase active residues such as lysine and proline placed at the dendrimer core or near the surface. On-bead selection for aldolase activity was carried out using the dye-labelled 1,3-diketone 1a, suitable for covalent trapping of enamine-reactive side-chains, and the fluorogenic enolization probe 6. Aldolase dendrimers catalyzed the aldol reaction of acetone, dihydroxyacetone and cyclohexanone with nitrobenzaldehyde. Much like enzymes, the dendrimers exhibited strong aldolase activity in aqueous medium, but were also active in organic solvent. Dendrimer-catalyzed aldol reactions reached complete conversion in 3 h at 25 °C with 1 mol% catalyst and gave aldol products with up to 65% ee. A positive dendritic effect in catalysis was observed with both lysine and proline based aldolase dendrimer catalysts. The Royal Society of Chemistry 2006.