Patent classifications
C07H11/00
Process for the preparation of sucrose octasulfate octakistriethylammonium salt (TASOS) powder and uses thereof
The present invention refers to a process for preparing sucrose octasulfate octakistriethylammonium salt (TASOS) powder, comprising the steps of combining a TASOS solution with a polar organic solvent(s) and triethylamine, thereby obtaining a TASOS solution, the polar organic solvent(s), and triethylamine; concentrating said TASOS solution; combining it with 2-methyltetrahydrofuran and/or tetrahydrofuran and triethylamine, thereby obtaining a mixture; and stirring said mixture until a white TASOS powder is obtained.
The present invention also refers to a sucrose octasulfate octakistriethylammonium salt (TASOS) powder having a purity of at least 96%, the use of the sucrose octasulfate octakistriethylammonium salt (TASOS) powder for preparing a pharmaceutical composition, and the use of tetrahydrofuran or 2-methyltetrahydrofuran as antisolvent for the preparation of TASOS powder.
Finally, the present invention refers to a pharmaceutical composition prepared by using the sucrose octasulfate octakistriethylammonium salt (TASOS) powder of the present invention, and to the pharmaceutical composition for use in treating cancer.
SULFATED POLYSACCHARIDE COMPOUND AND THE PREPARATION AND USE THEREOF
The present invention relates to a sulfated polysaccharide compound and the preparation and use thereof, and in particular to a narrow distribution low molecular weight, highly sulfated pentosan (in this instance a xylan) referred to as glucuronoxylan sulfate (GXS). The invention has been developed primarily for use in the treatment of various clinical conditions. However, it will be appreciated that the invention is not restricted this particular field of use.
Preparation of new intermediate of heparin pentasaccharide and preparation method thereof
The present invention relates to a process of a chemically synthetic drug, and in particular, to a new intermediate of a heparin pentasaccharide and a preparation method thereof. The process has high reaction efficiency, and an easy reaction operation. The reaction intermediate is easy to be purified, and is appropriate for an industrialization production.
Preparation of new intermediate of heparin pentasaccharide and preparation method thereof
The present invention relates to a process of a chemically synthetic drug, and in particular, to a new intermediate of a heparin pentasaccharide and a preparation method thereof. The process has high reaction efficiency, and an easy reaction operation. The reaction intermediate is easy to be purified, and is appropriate for an industrialization production.
Methods for the synthesis of functionalized nucleic acids
The present application, among other things, provides technologies, e.g., reagents, methods, etc. for preparing oligonucleotides comprising phosphorothiotriesters linkages, e.g., oligonucleotides having the structure of IIIa, IIIb or IIIc. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ia or Ib with a silylating reagent to provide a silyloxyphosphonate, and reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa or IIb to provide an oligonucleotide of structure IIIa or IIIb. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ic with a silylating reagent to provide a silyloxyphosphonate, reacting the silyloxyphosphonate with a bis(thiosulfonate) reagent of structure IVc to provide a phosphorothiotriester comprising a thiosulfonate group of structure Vc, and then reacting the phosphorothiotriester comprising a thiosulfonate group of structure Vc with a nucleophile of structure VIc to provide an oligonucleotide of structure IIIc.
Sucrose octasulfates of magnesium, preparation method thereof and pharmaceutical cosmetic uses of same
The invention relates to a sucrose octasulfate of magnesium, having general formula I, the preparation method thereof and the use of same in the pharmaceutical and/or cosmetic field, wherein 0n4, n is an integer and Y represents OH, Cl, Br, I, NO.sub.3, C.sub.6H.sub.5O.sub.7, CH.sub.3CO.sub.2, CF.sub.3CO.sub.2 or OCH.sub.3.
Sucrose octasulfates of magnesium, preparation method thereof and pharmaceutical cosmetic uses of same
The invention relates to a sucrose octasulfate of magnesium, having general formula I, the preparation method thereof and the use of same in the pharmaceutical and/or cosmetic field, wherein 0n4, n is an integer and Y represents OH, Cl, Br, I, NO.sub.3, C.sub.6H.sub.5O.sub.7, CH.sub.3CO.sub.2, CF.sub.3CO.sub.2 or OCH.sub.3.
Synthetic pentasaccharides having short half-life and high activity
The invention concerns a pentasaccharide compound of formula (I) ##STR00001## and the salts thereof. The invention also concerns a pharmaceutical composition comprising the synthetic pentasaccharide compound of formula (I) and its salts. The invention further concerns these compounds for use as a medicament, and in particular intended to treat blood clotting disorders, to prevent ischaemia reperfusion injury associated with solid organ transplantation, or to reduce the risk of blood clotting in an extracorporeal blood circuit during cardiac surgery, extracorporeal membrane oxygenation, or during circulatory assistance such as artificial heart.
Synthetic pentasaccharides having short half-life and high activity
The invention concerns a pentasaccharide compound of formula (I) ##STR00001## and the salts thereof. The invention also concerns a pharmaceutical composition comprising the synthetic pentasaccharide compound of formula (I) and its salts. The invention further concerns these compounds for use as a medicament, and in particular intended to treat blood clotting disorders, to prevent ischaemia reperfusion injury associated with solid organ transplantation, or to reduce the risk of blood clotting in an extracorporeal blood circuit during cardiac surgery, extracorporeal membrane oxygenation, or during circulatory assistance such as artificial heart.
SULFATED GLYCOSAMINOGLYCAN COMPOUNDS, METHODS, AND USES THEREOF
Provided herein include sulfated glycosaminoglycans including sulfated disaccharides, tetrasaccharides, and oligosaccharides and methods of synthesizing heparan sulfate disaccharide, tetrasaccharide, oligosaccharide library in solution-phase. Provided herein also includes a method of treating neurological diseases or disorders with sulfated glycosaminoglycans such as 4-O-sulfated chondroitin sulfate polysaccharides.