Patent classifications
C07C305/24
Process for the preparation of a sulfated derivative of 3,5-diiodo-o-[3-iodophenyl]-l-tyrosine
The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chlorosulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.
Process for the preparation of a sulfated derivative of 3,5-diiodo-o-[3-iodophenyl]-l-tyrosine
The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chlorosulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.
Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
##STR00001##
Metabolites of N-(4-{[6,7-Bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
##STR00001##
SYNERGISTIC CANNABINOID ESTERS, THEIR SALTS AND USES THEREOF
Cannabinoid esters and their soluble salts with synergistic or additive therapeutic counterparts and stable formulations thereof, as well as their edible, beverage and medicinal applications. The synergistic or additive cannabinoid esters may be used as drugs or prodrugs for treating various conditions related to the modulation or biased modulation of cannabinoid receptors, including but not limited to, pain and inflammation, arthritis, cancer, glaucoma, neurodegenerative disorders, multiple sclerosis, renal fibrosis, fibrotic disorder, mental health disorders, addiction, motor function disorders and gastrointestinal and metabolic disorders.
Metabolites of N-{4-([6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
The invention relates to metabolites of cabozantinib (I) as well as uses thereof. ##STR00001##
Metabolites of N-{4-([6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
The invention relates to metabolites of cabozantinib (I) as well as uses thereof. ##STR00001##
METABOLITES OF N-(4-{[6,7-BIS(METHYLOXY)QUINOLIN-4-YL]OXY}PHENYL)-N'-(4-FLUOROPHENYL)CYCLOPROPANE-1,1-DICARBOXAMIDE
The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
##STR00001##
METABOLITES OF N-(4-{[6,7-BIS(METHYLOXY)QUINOLIN-4-YL]OXY}PHENYL)-N'-(4-FLUOROPHENYL)CYCLOPROPANE-1,1-DICARBOXAMIDE
The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
##STR00001##
Compositions and methods for sulfation of carbohydrates and peptides via electron-deficient aryl sulfate diesters
In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.