65784-33-0

Upstream product

• 67-56-1 methanol 
• 938-96-5 2-(4-Hydroxy-phenyl)-propionic acid 
• 100-06-1 1-(4-methoxyphenyl)ethanone 
• 99-93-4 4-Hydroxyacetophenone 
• 104-01-8 4-Methoxyphenylacetic acid 
• 942-54-1 2-(4-methoxyphenyl)propanoic acid 
• 10034-85-2 hydrogen iodide 
• 2628-16-2 p-acetoxystyrene 
• 201230-82-2 carbon monoxide 
• 39718-97-3 methyl 2-(4-aminophenyl)propanoate 
• 23786-14-3 4-methoxy-phenyl acetic acid methyl ester 
• 93453-79-3 1-(4-hydroxyphenyl)ethanol 
• 21850-61-3 2-(4-hydroxyphenyl)propanenitrile 
• 50415-73-1 methyl 2-(4-methoxyphenyl)propionate 

Downstream Products

• 91970-86-4 2-(4-ethoxy-phenyl)-propionic acid 
• 99834-87-4 2-[4-(5-Formyl-furan-2-yloxy)-phenyl]-propionic acid methyl ester 
• 77143-73-8 2-{4-[(4-Chloro-phenyl)-ethoxycarbonyl-methoxy]-phenyl}-propionic acid methyl ester 
• 99834-91-0 2-[4-(5-Acetyl-furan-2-yloxy)-phenyl]-propionic acid methyl ester 
• 82340-97-4 2-[4-(2-Nitro-phenoxy)-phenyl]-propionic acid methyl ester 
• 78430-78-1 2-[4-(2-Acetyl-phenoxy)-phenyl]-propionic acid methyl ester 
• 77143-74-9 2-{4-[(4-Bromo-phenyl)-ethoxycarbonyl-methoxy]-phenyl}-propionic acid methyl ester 
• 99834-92-1 2-[4-(5-Propionyl-furan-2-yloxy)-phenyl]-propionic acid methyl ester 
• 120608-36-8 methyl 2-<4-(2-acetyl-4-cyano)phenoxyphenyl>propionate 
• 77269-60-4 2-(4-Pentyloxy-phenyl)-propionic acid 
• 89618-33-7 methyl 2-(4-benzyloxyphenyl)propionate 
• 77143-80-7 2-[4-(Ethoxycarbonyl-phenyl-methoxy)-phenyl]-propionic acid methyl ester 
• 946073-01-4 methyl 2-{4-[(methylsulfonyl)oxy]phenyl}propanoate 
• 120569-05-3 methyl 2-<4-(4-cyano-2-hydroxymethyl)phenoxyphenyl>propionate 

Relevant academic research and scientific papers

DIHYDROPYRIMIDIN-2-ONE COMPOUNDS AND MEDICAL USE THEREOF

A compound of Formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is defined as in the specification.

A recyclable CO surrogate in regioselective alkoxycarbonylation of alkenes: Indirect use of carbon dioxide

Herein, we report a Pd-catalysed alkoxycarbonylation of alkenes based on the use of a recyclable CO2 reduction product, the crystalline and air-stable N-formylsaccharin, as a CO surrogate. The carbonylation proceeds under ambient conditions in an exceptionally complementary regioselective fashion yielding the desired branched products from styrene derivatives and valuable linear esters from alkyl-substituted alkenes.

Discovery of diarylhydantoins as new selective androgen receptor modulators

A novel selective androgen receptor modulator scaffold has been discovered through structural modifications of hydantoin antiandrogens. Several 4-(4-hydroxyphenyl)-N-arylhydantoins displayed partial agonism with nanomolar in vitro potency in transactivation experiments using androgen receptor (AR) transfected cells. In a standard castrated male rat model, several compounds showed good anabolic activity on levator ani muscle, dissociated from the androgenic activity on ventral prostate, after oral dosing at 30 mg/kg. (+)-4-[3,4-Dimethyl-2,5-dioxo-4-(4-hydroxyphenyl)imidazolidin-1-yl] -2-(trifluoromethyl)benzonitrile ((+)-11b) displayed anabolic potency with a strong dissociation between levator ani muscle and ventral prostate (A 50 = 0.5 mg/kg vs 70 mg/kg). The binding modes of two compounds, including (+)-11b, within the AR ligand-binding domain have been studied by cocrystallization experiments using a coactivator-like peptide. Both compounds bound to the same site, and the overall structures of the AR were very similar.

2-ARYL-PROPIONAMIDE DERIVATIVES USEFUL AS BRADYKININ RECEPTOR ANTAGONISTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

(R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B 1 pathway.

2-aryl-propionamide derivatives useful as bradykinin receptor antagonists and pharmaceutical compositions containing them

(R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B1 pathway.

Antileukotrienic phenethylamido derivatives of arylalkanoic acids in the treatment of ulcerative colitis

A series of arylalkanoic acid derivatives bearing methyl(phenethyl)amino groups were prepared and their inhibition of LTB4 biosynthesis was evaluated. Regression analysis showed the slightly different parabolic dependences of this activity on lipophilicity of α-methyl and α-unsubstituted alkanoic acid derivatives. The relationship derived for α-unsubstituted alkanoic acids was extended by previously prepared group of similar derivatives of arylacetic acids without any change of regression coefficients and statistical criteria. It was concluded that the most active compounds belong to 2-arylpropanoic acid derivatives with lipophilicity close to log Popt (=6.97). But generally, the structural changes in the acidic part of compounds under study did not yield the substantial improvement of LTB4 biosynthesis inhibition in comparison with the previously prepared series of derivatives IV. The anti-inflammatory effect of the compounds under study was evaluated in three animal models of inflammation and their possible utilization in the treatment of ulcerative colitis (UC) was followed. From 12 evaluated compounds, 4 compounds are more active in UC inhibition than the standard sulfasalazine but it can be stated that the change of connecting chain between aromatic ring and carboxyl did not bring about the important improvement of this activity in comparison with previous derivatives of arylacetic acids. Possible relation between LTB4 biosynthesis inhibition and ulcerative colitis is seriously broken by the compound 8a with carbonyl as the additional functional group on the connecting chain between carboxyl and aromatic ring.

Design of noncompetitive interleukin-8 inhibitors acting on CXCR1 and CXCR2

Chemokines CXCL8 and CXCL1 play a key role in the recruitment of neutrophils at the site of inflammation. CXCL8 binds two membrane receptors, CXCR1 and CXCR2, whereas CXCL1 is a selective agonist for CXCR2. In the past decade, the physiopathological role of CXCL8 and CXCL1 has been investigated. A novel class of small molecular weight allosteric CXCR1 inhibitors was identified, and reparixin, the first drug candidate, is currently under clinical investigation in the prevention of ischemia/reperfusion injury in organ transplantation. Reparixin binding mode to CXCR1 has been studied and used for a computer-assisted design program of dual allosteric CXCR1 and CXCR2 inhibitors. In this paper, the results of modeling-driven SAR studies for the identification of potent dual inhibitors are discussed, and three new compounds (56, 67, and 79) sharing a common triflate moiety have been selected as potential leads with optimized pharmacokinetic characteristics.

Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Synthesis and immunosuppressive activity of new artemisinin derivatives. 1. [12(β or α)-dihydroartemisininoxy]phen(ox)yl aliphatic acids and esters

A series of novel dihydroartemisinin derivatives were synthesized and evaluated on their immunosuppressive activity in the search for potential immunosuppressive agents with high efficacy and low toxicity. These compounds were assayed in their cytotoxicity of lymphocyte, inhibition activity on concanavalin A (ConA) induced T cell proliferation and lipopolysaccharide (LPS) induced B cell proliferation. Among them, 11b, 13b, 14d, 15b, 16, and 17 remarkably exhibited lower cytotoxicity and higher inhibition activity on the mitogen-induced T cell and B cell proliferation in comparison with artemisinin, artesunate, and artemether in vitro. More significantly, compound 11b displayed reduced cytotoxicity by over 100-fold compared with cyclosporin A (CsA) and comparable inhibition activity (SI = 848) on ConA-induced T cell proliferation to CsA (SI = 963) and more than 4000 times the inhibitory effect (SI = 28473) on LPS-induced B cell proliferation compared with CsA (SI = 7) in vitro. The in vivo experimental results showed that compound 16 could inhibit 2,4-dinitrofluorobenzene (DNFB)-induced delayed-type hypersensitivity (DTH) reaction and sheep red blood cell (SRBC) induced antibody production, respectively. The structure and activity relationships (SAR) of these compounds were also discussed.

Synthetic modification of the 2-oxypropionic acid moiety in 2-{4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy}propionic acid (XK469), and consequent antitumor effects. Part 4

The criteria for the activity of 2-{4-[(7-chloro-2-quinoxalinyl)oxy] phenoxy}propionic acid (XK469) and 2-{4-[(7-bromo-2-quinolinyl)oxy]phenoxy} propionic acid (SH80) against transplanted tumors in mice established in previous studies, require a (7-halo-2