39062-64-1

Upstream product

• 56961-30-9 2-chloro-5-hydroxybenzoic acid 
• 100-44-7 benzyl chloride 
• 2516-96-3 2-chloro-5-nitrobenzoic acid 
• 100-39-0 benzyl bromide 
• 876299-64-8 5-benzyloxy-2-chlorobenzoic acid benzyl ester 
• 89-54-3 2-chloro-5-aminobenzoic acid 
• 39062-63-0 2-chloro-5-hydroxybenzoic acid ethyl ester 

Downstream Products

• 82578-53-8 5-Benzyloxy-N-(4-benzyloxy-3-trifluormethylphenyl)anthranilsaeure 
• 39062-65-2 5-phenylmethoxy-2-[(3-trifluoromethylphenyl)amino]benzoic acid 
• 39062-67-4 2-[[3-(trifluoromethyl)phenyl]amino]-5-hydroxybenzoic acid 
• 76874-95-8 5,4'-Dihydroxyflufenaminsaeure 
• 82578-49-2 methyl 5-phenylmethoxy-2-[(3-trifluoromethylphenyl)amino]benzoate 
• 82578-50-5 5-Benzyloxy-2-(3-trifluoromethyl-phenylamino)-benzoic acid 2-(2-hydroxy-ethoxy)-ethyl ester 
• 76874-96-9 5-hydroxy-etofenamate 
• 101284-52-0 2-(carboxymethylamino)-5-(benzyloxy)benzoic acid 

Relevant academic research and scientific papers

Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule

Indirubins have been identified as potent ATP-competitive protein kinase inhibitors. Structural modifications in the 5-and 3′-position have been extensively investigated, but the impact of substituents in 5′-position is not equally well-studied. Here, we report the synthesis of new indirubin 3′-and 5′-derivatives in the search of water-soluble indirubins by introducing basic centers. Antiproliferative activity of all compounds in tumor cells was evaluated along with kinase inhibition of selected compounds. The results show the 3′-position to tolerate large substituents without compromising activity, whereas bulk and rigid substituents in 5′-position appear unfavorable. Screening molecular targets of water-soluble 3′-oxime ethers revealed 6ha as preferential inhibitor of insulin-like growth factor 1 receptor (IGF-1R) in a panel of 22 protein kinases and in cells. Consistently, 6ha inhibited tumor cell growth in the NCI 60 cell line panel and induced apoptosis. The results indicate that the 5′-position provides limited space for chemical modifications and identify 6ha as a potent water-soluble indirubin-based IGF-1R inhibitor.

N-Phenylbenzamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore

Persistent opening of the mitochondrial permeability transition pore (PTP), an inner membrane channel, leads to mitochondrial dysfunction and renders the PTP a therapeutic target for a host of life-threatening diseases. Herein, we report our effort toward identifying small-molecule inhibitors of this target through structure-activity relationship optimization studies, which led to the identification of several potent analogues around the N-phenylbenzamide compound series identified by high-throughput screening. In particular, compound 4 (3-(benzyloxy)-5-chloro-N-(4-(piperidin-1-ylmethyl)phenyl)benzamide) displayed noteworthy inhibitory activity in the mitochondrial swelling assay (EC50=280 nm), poor-to-very-good physicochemical as well as in vitro pharmacokinetic properties, and conferred very high calcium retention capacity to mitochondria. From the data, we believe compound 4 in this series represents a promising lead for the development of PTP inhibitors of pharmacological relevance.

SMALL MOLECULE INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION PORE (mtPTP)

The present technology relates to compounds of any one of Formula I, II, IIa, III, IV, and/or V as described herein and their tautomers and/or pharmaceutically acceptable salts, compositions, and methods of uses thereof.

Substituted benzamides with activity towards EP4 receptors

The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.

SUBSTITUTED BENZAMIDES WITH ACTIVITY TOWARDS EP4 RECEPTORS

The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.

NOVEL PYRAZOLONE-DERIVATIVES AND THEIR USE AS PD4 INHIBITORS

The compounds of formula (1) wherein R1 represents a phenyl derivative of formulae (a), (b) or (c) R10 is 1-3C-alkyl and R11 is 1-3C-alkyl, or R10 and R11 together with the carbon atom, to which they are bonded, form a spiro-linked 3-, 4-, 5- or 6-membered hydrocarbon ring, A is C(O) or S(O)2, and R12 is phenyl, naphthalenyl, pyridinyl, quinolinyl, isoquinolinyl, quinoxalinyl, 1,6-naphthyridinyl, 1,8-naphthyridinyl, indolyl, phenyl substituted by R13, R14, R15 and R16, pyridinyl substituted by R17 and R18, naphthalenyl substituted by R19 and R20, quinolinyl substituted by R21 or indolyl substituted by R22, are novel effective inhibitors of the type 4 phosphodiesterase.

BENZAMIDE DERIVATIVES AS EP4 RECEPTOR AGONISTS

A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1, R2, R3, R4, R5, m, n and X are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.

Synthesis and properties of nuclear hydroxylated derivatives of flufenamic acid and etofenamate

Synthesis of six nuclear hydroxylated derivatives of flufenamic acid and etofenamate (5-OH-, 4'-OH and 5,4'-(OH2) on a preparative scale is described. All compounds show low toxicity, by only weak anti-inflammatory activity in the rat paw kaolin edema test as compared to 2-(2-hydroxyethoxy)ethyl-N-(α,α,α-trifluoro-m-tolyl)-anthranilate (etofenamate, active substance of Rheumon Gel).