478296-69-4

Upstream product

• 101623-69-2 (1-chloroethyl)-(4-nitrophenyl)carbonate 
• 100-02-7 4-nitro-phenol 

Downstream Products

• 1034191-21-3 1-(((4-nitrophenoxy)carbonyl)oxy)ethyl benzoate 
• 1034191-20-2 C₂₅H₂₇NO₉ 
• 1321458-86-9 1-((4-nitrophenoxy)carbonyloxy)ethyl 2-(2-(nitrooxy)ethoxy) acetate 
• 1321458-96-1 1-((4-nitrophenoxy)carbonyloxy)ethyl-2, 2-dimethyl-3-(nitrooxy)propanoate 
• 1224849-44-8 1-{[(4-nitrophenoxy)carbonyl]oxy)ethyl 3-methylbutanoate 
• 182747-71-3 α-butanoyloxyethyl para-nitrophenyl carbonate 

Relevant academic research and scientific papers

PRIMARY AMINE COMPOUND OR SECONDARY AMINE COMPOUND-ACIDIC POLYSACCHARIDE CONJUGATE AND PRODUCTION METHOD THEREFOR

Provided is a novel conjugate of a primary or secondary amine compound with an acidic polysaccharide, which is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof, where in Formula (I), D, R1, R2, A, a

Repeated dosing with NCX1404, a nitric oxide-donating pregabalin, re-establishes normal nociceptive responses in mice with streptozotocin-induced painful diabetic neuropathy

NCX1404 [(3S)-5-methyl-3-(((1-(4-(nitrooxy)butanoyloxy)ethoxy) carbonylamino) methyl)hexanoic acid] is a novel nitric oxide (NO)-donating pregabalin that is readily absorbed and processed in vivo to pregabalin and NO. We determined the antiallodynic response of NCX1404 after acute or after 7, 14, and 21 days of repeated daily oral dosing in mice with streptozotocin (STZ)-induced painful diabetic neuropathy (PDN). Pregabalin and its combination with the NO donor isosorbide mononitrate (ISMN) were used for comparison. The blood levels of pregabalin and nitrites, used as surrogate marker of NO release, after NCX1404 or pregabalin dosing were monitored in parallel experiments using liquid chromatography with tandem mass spectrometry (LC-MS/MS). NCX1404 and pregabalin resulted in similar pregabalin levels as it was their antiallodynic activity after acute dosing in STZ mice. However, NCX1404 resulted in disease-modifying properties when administered daily for 21 days, as indicated by the time- and dose-dependent reversal of STZ-induced mechanical allodynia (paw withdrawal threshold [PWT]Veh-21d = 1.3 v 0.15 g for vehicle; PWTNCX1404-21d = 1.4 ± 0.5 g, 2.9 ± 0.2 g? and 4.1 ± 0.2 g?, respectively for 19, 63, and 190 μmol/kg, oral gavage [PO] of NCX1404; ?P, 0.05 versus vehicle). This effect was not shared by pregabalin at equimolar doses (190 μmol/kg, PO, PWTPregab-21d = 1.4 ± 0.1 g?, ?P Veh-7d= 1.7 ± 0.16 g; PWTISMN-7d = 3.9 ± 0.34 g?; PWTPregab-7d = 1.3 ± 0.07 g; PWTISMN+pregab-7d = 3.8 ± 0.29 g?; ?P, 0.05) but not at later time points. The long-term effect of NCX1404 was independent of residual drug exposure and lasted for several days after the treatment was stopped. In summary, like pregabalin, NCX1404 is an effective antiallodynic agent. Differently from pregabalin, repeated dosing of NCX1404 re-established normal nociceptive responses in STZ-induced PDN in mice.

Macrocyclic prodrugs of a selective nonpeptidic direct thrombin inhibitor display high permeability, efficient bioconversion but low bioavailability

The only oral direct thrombin inhibitors that have reached the market, ximelagatran and dabigatran etexilat, are double prodrugs with low bioavailability in humans. We have evaluated an alternative strategy: the preparation of a nonpeptidic, polar direct

NITRIC OXIDE RELEASING COMPOUNDS FOR THE TREATMENT OF NEUROPHATIC PAIN

The present invention relates to nitric oxide releasing derivatives of serotonin norepinephrine reuptake inhibitors and their use for the treatment of pain, having the following general formula (I) or pharmaceutically acceptable salts thereof: wherein : A is selected from the formulas (1a) and (1b). The present invention also relates to pharmaceutical formulation comprising such derivatives, to a process for their preparation and to intermediates useful for their preparation.

NITRIC OXIDE RELEASING COMPOUNDS FOR THE TREATMENT OF NEUROPATHIC PAIN

The invention relates to nitrooxyderivatives of Gamma- aminobutyric acid analogs (GABA analogs) for treating neuropathic pain and in particular diabetic neuropathy. The invention also relates to pharmaceutical formulation comprising such derivatives, to a process for their preparation.

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to, the prevention and treatment of Alzheimer's disease.

Prodrugs of GABA analogs, compositions and uses thereof

The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.