67137-56-8

Upstream product

• 19432-68-9 methyl 2-thiopheneacetate 
• 3141-27-3 2,5-dibromothiophen 
• 96-32-2 bromoacetic acid methyl ester 
• 1918-77-0 Thiophene-2-acetic acid 

Downstream Products

• 928846-98-4 [5-(2-amino-phenyl)-thiophen-2-yl]-acetic acid methyl ester 
• 934176-74-6 [5-(3-nitro-phenyl)-thiophen-2-yl]-acetic acid methyl ester 
• 934176-66-6 [5-(4-nitro-phenyl)-thiophen-2-yl]-acetic acid methyl ester 
• 934176-75-7 [5-(3-amino-phenyl)-thiophen-2-yl]-acetic acid methyl ester 
• 934176-67-7 [5-(4-amino-phenyl)-thiophen-2-yl]-acetic acid methyl ester 
• 934176-26-8 (5-{2-[2-(3,4,5-trimethoxy-phenyl)-acetylamino]-phenyl}-thiophen-2-yl)-acetic acid methyl ester 
• 934176-43-9 (5-{2-[2-(2,3,4-trimethoxy-phenyl)-acetylamino]-phenyl}-thiophen-2-yl)-acetic acid methyl ester 
• 934176-27-9 (5-{2-[2-(3,4,5-trimethoxy-phenyl)-acetylamino]-phenyl}-thiophen-2-yl)-acetic acid 
• 934176-52-0 (5-{2-[3-(3,4,5-trimethoxy-phenyl)-acryloylamino]-phenyl}-thiophen-2-yl)-acetic acid methyl ester 
• 864518-32-1 (5-{2-[2-(2,3,4-trimethoxy-phenyl)-acetylamino]-phenyl}-thiophen-2-yl)-acetic acid 
• 934176-56-4 (5-{2-[3-(2,3,4-trimethoxy-phenyl)-acryloylamino]-phenyl}-thiophen-2-yl)-acetic acid methyl ester 
• 934176-57-5 (5-{2-[3-(2,3,4-trimethoxy-phenyl)-acryloylamino]-phenyl}-thiophen-2-yl)-acetic acid 
• 934176-51-9 (5-{2-[3-(2,3,4-trimethoxy-phenyl)-propionylamino]-phenyl}-thiophen-2-yl)-acetic acid 
• 934176-29-1 (5-{2-[3-(3,4,5-trimethoxy-phenyl)-propionylamino]-phenyl}-thiophen-2-yl)-acetic acid methyl ester 

Relevant academic research and scientific papers

METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

Composite taken as URAT 1 inhibitor

The invention provides a series of composite with a formula (I), wherein n is selected from 1, 2 or 3, X is selected from O or S, Q is selected from C or N, and R is selected from H, halogen or -C1-6.The composite can be used as the URAT 1 inhibitor and can be used for treating hyperuricemia and gout.

NOVEL COMPOUNDS AND THEIR USE IN THERAPY

The present invention relates to novel chemical compounds formula (I) (C)n-B-(A)m-B-(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five-and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (-CO-), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.

NOVEL THIOPHENE COMPOUNDS AND METHOD FOR IN VIVO IMAGING

The present invention relates to novel labelled compounds of formula (I) (C)n-B-(A)m-B-(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group ( -CO- ), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1, for use in imaging amyloid deposits and aggregated protein in living patients. The invention further relates to imaging methods using labelled or unlabelled compounds of formual I and the use of unlabelled compounds in such methods.

SELF-ASSEMBLING PEPTIDES BEARING ORGANIC ELECTRONIC FUNCTIONALITY AND APPLICATIONS EMPLOYING THE SAME

The aqueous self-assembly of oligopeptide-flanked π-conjugated molecules into discrete one-dimensional nanostructures is described. Unique to these molecules is the fact that the π-conjugated unit has been directly embedded within the peptide backbone by way of a synthetic amino acid with π-functionality that is compatible with standard Fmoc-based peptide synthesis or by way of a diacid or other bis(electrophile) that can covalently cross-link peptide chains presented on a synthesis support. The peptide-based molecular designs enforce intimate π-π communication within the aggregates after charge-screening and self-assembly, making these nanostructures attractive for optical or electronic applications in biological environments. In other embodiments, a convenient method to incorporate π-electron units into peptides that assemble into amyloid-like supramolecular polymers is disclosed. Self-assembly manipulates these “electronic peptides” into delocalized sub-10 nm one dimensional (1-D) nanostructures under completely aqueous conditions.

Novel Hydroxylated Aromatic Compounds

Pharmaceutical compositions comprising at least one compound of the formula (I) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning —X— is e.g. and Y being e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.

One-dimensional optoelectronic nanostructures derived from the aqueous self-assembly of π-conjugated oligopeptides

The aqueous self-assembly of oligopeptide-flanked π-conjugated molecules into discrete one-dimensional nanostructures is described. Unique to these molecules is the fact that the π-conjugated unit has been directly embedded within the peptide backbone by way of a synthetic amino acid with π-functionality that is compatible with standard Fmoc-based peptide synthesis. The peptide-based molecular design enforces intimate π-π communication within the aggregate after charge-screening and self-assembly, making these nanostructures attractive for optical or electronic applications in biological environments. The synthesis and assembly are reported along with spectroscopic and morphological characterization of the new nanomaterials. Copyright

Rational design of novel, potent small molecule pan-selectin antagonists

This report describes the first results of a rational hit-finding strategy to design novel small molecule antiinflammatory drugs targeting selectins, a family of three cellular adhesion molecules. Based on recent progress in understanding of molecular interaction between selectins and their natural ligands as well as progress in clinical development of synthetic antagonists like 1 (bimosiamose, TBC1269), this study was initiated to discover small molecule selectin antagonists with improved pharmacological properties. Considering 1 as template structure, a ligand-based approach followed by focused chemical synthesis has been applied to yield novel synthetic small molecules (MWr 500) with a trihydroxybenzene motif, bearing neither peptidic nor glycosidic components, with nanomolar in vitro activity. Biological evaluation involves two kinds of in vitro assays, a static molecular binding assay, and a dynamic HL-60 cell attachment assay. As compared to controls, the novel compounds showed improved biological in vitro activity both under static and dynamic conditions.

NOVEL PHLOROGLUCINOL DERIVATIVES HAVING SELECTIN LIGAND ACTIVITY

Pharmaceutical compositions comprising at least one compound of the formula (I) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning -X- is e.g. and Y being e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.