436864-52-7

Upstream product

• 2150-45-0 methyl 2,6-dihydroxybenzoate 
• 75178-87-9 (4-hydroxybutyl)carbamic acid tert-butyl ester 
• 303-07-1 2,6-Dihydroxybenzoic acid 
• 75178-90-4 N-(tert-butyloxycarbonyl)-5-aminopentanol 
• 1972-28-7 diethylazodicarboxylate 

Downstream Products

• 952339-49-0 2-benzyloxy-6-(4-tert-butoxycarbonylamino-butoxy)-benzoic acid methyl ester 
• 623563-64-4 2-(4-aminobutoxy)-6-benzyloxybenzoic acid methyl ester 
• 436864-60-7 methyl 2-[(5-{[2-(acetylamino)-3-(4-{2-[(benzhydryloxy)carbonyl][(benzyloxy)(oxo)acetyl]anilino}-3-ethylphenyl)propanoyl]amino}pentyl)oxy]-6-hydroxybenzoate 
• 436864-58-3 methyl 2-{4-[(N-[(allyloxy)carbonyl]-4-{{2-[(benzhydryloxy)carbonyl]phenyl}[tert-butoxy(oxo)acetyl]amino}-L-phenylalanyl)amino]butoxy}-6-hydroxybenzoate 
• 1205538-23-3 methyl 2-{4-[(N-acetyl-4-[(carboxycarbonyl)(2-carboxyphenyl)amino]-3-ethylphenylalanyl)amino]butoxy}-6-hydroxybenzoate 
• 918657-87-1 2-{4-[2-acetylamino-3-(4-carboxymethoxy-3-hydroxy-phenyl)-propionylamino]-butoxy}-6-hydroxy-benzoic acid methyl ester 
• 474917-81-2 2-{4-[2-tert-butoxycarbonylamino-3-(4-nitro-phenyl)-propionylamino]-butoxy}-6-hydroxy-benzoic acid methyl ester 
• 474917-82-3 methyl 2-(4-{[4-amino-N-(tert-butoxycarbonyl)-L-phenylalanyl]amino}butoxy)-6-hydroxybenzoate 
• 436864-53-8 methyl 2-(4-aminobutoxy)-6-hydroxybenzoate 

Relevant academic research and scientific papers

Convergent Protein Phosphatase Inhibitor Design for PTP1B and TCPTP: Exchangeable Vanadium Coordination Complexes on Graphene Quantum Dots

Development of potent and specific inhibitors of protein tyrosine phosphatase 1B (PTP1B) with desired drug-like properties is still a challenge. Based on the crystal structures of PTP1B transition state analog consisting of a vanadate peptide, a novel approach is proposed to design PTP1B inhibitors, in which the tyrosyl vanadate ester of a PTP1B peptide mimic (PL1) is stably integrated on the membrane permeable graphene quantum dots (GQDs). The vanadate complexes (GQD-PL1-VV) prepared exhibit high potency (Ki?= 6?± 1?× 10?9 m) and selectivity (selectivity index SI >200?for PTP1B versus the T-cell protein tyrosine phosphatase, TCPTP) in solution and in HepG2 cells. Oral administration of GQD-PL1-VV in db/db model mice shows selective PTP1B inhibition in liver and fat tissues and exhibits improved anti-diabetic activity compared to bis(maltolato)oxovanadium(IV). Moreover, exchange of PL1 to a TCPTP-specific ligand (PL2) results in potent TCPTP inhibition (Ki?= 59?± 12?× 10?9 m) as expected with SI ≈23 versus PTP1B. Overall, the present results provide a paradigm shift and a general design of phosphatase inhibitors consisting of GQDs, a complexing targeting ligand and vanadium (V) for selective regulation of PTP1B both in vitro and vivo.

1-ORTHOFLUOROPHENYL SUBSTITUTED 1, 2 , 5-THIAZOLIDINEDIONE DERIVATIVES AS PTP-AS INHIBITORS

Compounds of the formula (I) are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

Selective protein tyrosine phosphatatase inhibitors

Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.

Selective protein tyrosine phosphatase 1B inhibitors: Targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands

Protein tyrosine phosphatase (PTPase) 1B (PTP1B) has been implicated as a key negative regulator of both insulin and leptin signaling cascades. We identified several salicylic acid-based ligands for the second phosphotyrosine binding site of PTP1B using a NMR-based screening. Structure-based linking with a catalytic site-directed oxalylarylaminobenzoic acid-based pharmacophore led to the identification of a novel series of potent PTP1B inhibitors exhibiting 6-fold selectivity over the highly homologous T-cell PTPase (TCPTP) and high selectivity over other phosphatases.

Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B

Monoacid-based PTP1B inhibitors with improved physiochemical properties have been investigated. A (2-hydroxy-phenoxy) acetic acid-based phosphotyrosyl mimetic has been linked with an optimized second arylphosphate binding site ligand to produce compound 20 with low micromolar potency against PTP1B, good selectivity over TCPTP (20-fold) and high cell permeability in the Caco-2 system.

Selective protein tyrosine phosphatatase inhibitors

Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.