62773-65-3

Upstream product

• 64-17-5 ethanol 
• 89-57-6 5-Aminosalicylic Acid 
• 7664-93-9 sulfuric acid 
• 42348-40-3 ethyl 5-nitrosalicylate 

Downstream Products

• 80074-19-7 5-(2-chloro-acetylamino)-2-hydroxy-benzoic acid ethyl ester 
• 1062213-99-3 4'-bromo-N-(4'-hydroxy-3'-(hydroxymethyl)-biphenyl-4-yl)-sulfonamide 
• 1062213-61-9 ethyl 5-(4'-bromobiphenyl-4-ylsulfonamido)-2-hydroxybenzoate 
• 15722-48-2 olsalazine 
• 80074-63-1 5-[(N,N-diethyl-glycyl)-amino]-2-hydroxy-benzoic acid ethyl ester 
• 337520-13-5 4-(1-t-butoxycarbonylpiperidin-4-yloxy)-3-ethoxycarbonylaniline 

Relevant academic research and scientific papers

Photocatalytic Selective Reduction by TiO2 of 5-Nitrosalicylic Acid Ethyl Ester: A Mild Route to Mesalazine

Abstract: Photoexcited TiO2 dispersed in a de-aerated acetonitrile/2-propanol (CH3CN/2-PrOH) reaction mixture catalyzes the quick and selective reduction of 5-nitrosalicylic acid methyl ester to the corresponding aniline, an immediat

Novel analogs of sulfasalazine as system xc ? antiporter inhibitors: Insights from the molecular modeling studies

System xc ? (Sxc ?), a cystine-glutamate antiporter, is established as an interesting target for the treatment of several pathologies including epileptic seizures, glioma, neurodegenerative diseases, and multiple sclerosis. Erastin, sorafenib, and sulfasalazine (SSZ) are a few of the established inhibitors of Sxc ?. However, its pharmacological inhibition with novel and potent agents is still very much required due to potential issues, for example, potency, bioavailability, and blood–brain barrier (BBB) permeability, with the current lead molecules such as SSZ. Therefore, in this study, we report the synthesis and structure–activity relationships (SAR) of SSZ derivatives along with molecular docking and dynamics simulations using the developed homology model of xCT chain of Sxc ? antiporter. The generated homology model attempted to address the limitations of previously reported comparative protein models, thereby increasing the confidence in the computational modeling studies. The main objective of the present study was to derive a suitable lead structure from SSZ eliminating its potential issues for the treatment of glioblastoma multiforme (GBM), a deadly and malignant grade IV astrocytoma. The designed compounds with favorable Sxc ? inhibitory activity following in vitro Sxc ? inhibition studies, showed moderately potent cytotoxicity in patient-derived human glioblastoma cells, thereby generating potential interest in these compounds. The xCT-ligand model can be further optimized in search of potent lead molecules for novel drug discovery and development studies.

Mesalazine derivatives

Provided herein are compounds that are prodrugs for mesalazine. Generally, the compounds described herein correspond to a mesalazine molecule wherein the amino group is replaced by a novel protecting group. For example, in the compounds of Formula I descr

4-substituted pyridine-2-formamide compound, preparation method thereof and application

The invention discloses a 4-substituted pyridine-2-formamide compound, a preparation method thereof and an application. The 4-substituted pyridine-2-formamide compound has a structure as shown in a formula I, and the chemical name of the compound is 4-{4-[3-(4-chlorine-3-trifluoromethyl-phenyl)-ureide]-3-carboxyl phenoxy}-N-picoline-2-carboxylic methylamine. According to the preparation method of the 4-substituted pyridine-2-formamide compound, 4-chlorine-2-picolinic acid serves as an initial raw material, and the compound in the formula I is prepared by acylating chlorination, amination, substitution reaction and condensation reaction. The 4-substituted pyridine-2-formamide compound retains a Sorafenib efficacy structure, 5-aminosalicylic acid or aminosalicylic acid ester achieving a positive pharmacological function in the metabolic process replaces p-aminophenol with large toxic and side effects, efficacy can be improved, and the toxic and side effects are reduced.

BIPHENYL-4-YL-SULFONIC ACID ARYLAMIDES AND THEIR USE AS THERAPEUTIC AGENTS

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl sulfonamides and related compounds (collectively referred to herein as "BPSAAA compounds"), as described herein, and including, for example, biphenyl-4-sulfonic acid (hydroxyalkyl-phenyl)-amides and related compounds. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment and/or prevention, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of, inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activation in rheumatoid arthritis, osteoporosis, cancer associated bone disease, Paget's disease and the like.

Condensed 4-aminopyridines with antirheumatic activity

Compounds of formula I STR1 and pharmaceutically acceptable salts thereof in which one of A or B represents N and the other represents N or C--R3 ; R1 represents hydrogen, halo, alkyl, hydroxy, carboxyalkenyl, alkoxycarbonylalkenyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, halogenated alkyl, carboxy, alkoxycarbonyl, alkanoylamino or carbamoylalkenyl; R2 represents hydrogen, alkyl, halo, alkoxy, hydroxy, alkanoyloxy, or phenoxy; R3 represents hydrogen or alkyl; R4 represents hydrogen, halo, alkoxycarbonyl, cyano, benzyloxycarbonyl, alkanoyl, benzoyl, alkyl, carboxy, alkylthio or carbamoyl; R5 represents hydrogen or alkyl; R9 represents hydrogen or alkyl; R10 represents phenyl, pyridyl or pyrimidinyl substituted by OR6 and optionally further substituted wherein R6 represents hydrogen, alkyl, alkoxycarbonyl or carbamoyl, alicyclic hydrocarbon, phenyl, cycloalkylalkyl, arylalkyl or pyridyl; or when R10 represents phenyl, OR6 represents a monosaccharide group or a disaccharide group; which are antirheumatic agents. Compositions containing these compounds and processes to prepare them are also disclosed.

Benzoic acid derivatives and use thereof

A pharmaceutical composition for use in the treatment of psoriasis comprises 4-aminosalicylic acid (4-ASA) or 5-aminosalicylic acid (5-ASA) or a functional derivative thereof, said pharmaceutical composition being in a form suitable for topical administration. Furthermore, 4- or 5-ASA or a functional derivative thereof are used for the manufacture of pharmaceutical compositions for treating psoriasis, atopic dermatitis, allergic dermatitis, contact dermatitis, seborrhoic dermatitis, or acne diseases. The derivatives have the formulae: STR1 where W is COOX, wherein X is H, Li, Na, K, Mg0.5, Ca0.5, Zn0.5, Al0.33, Fe(II)0.5, Fe(III)0.33, NH4, NH3 R1, NH2 R12, NHR13, NR14, or R1, where R1 is substituted or unsubstituted C1-6 -alkyl, aryl-C1-4 -alkyl, or heteroaryl-C1-4 -alkyl; or COX, where X is NR1 R1', where R1' has the same meaning as R1 defined above and R1 and R1' may be identical or different; Y is H or R1 CO, where R1 is defined as above; Z1 and Z2, which may be identical or non-identical are H, R1 or R1 CO, where R1 is defined as above, or Z1 and Z2 represent R2, where R2 is substituted or unsubstituted C1-6 -alkylidene or aryl-C1-6 -alkylidene, or heteroaryl-C1-6 -alkylidene, or Z1, Z2 together with the nitrogen atom to which they are attached may represent a 3 to 7 membered saturated or unsaturated heterocyclic ring, or may represent a group of the formula --N=N--R3 where R3 is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.