摘要:
1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate.
摘要:
This invention relates to an improved method for stereoselectively preparing 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I), which comprises the steps of reacting a 1-halo ribofuranose compound of formula (III) with a nucleobase of formula (IV) in a solvent to obtain a nucleoside of formula (II) with removing the silyl halide of formula (V) produced during the reaction; and deprotecting the nucleoside of formula (II) to obtain 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I).
摘要:
A method for preparing a 1-androstene derivative which comprises reacting a 2-iodo-androstane derivative with an oxidizing agent while maintaining the pH of the reaction mixture at a specific range gives the 1-androstene derivative with high purity and yield.
摘要:
A crystalline clopidogrel naphthalenesulfonate or a hydrate thereof, a method for preparing same, and a pharmaceutical composition containing same are provided.
摘要:
The mutual salt of raloxifene and bisphosphonic acid exhibits unexpectedly synergistic effects of two components to enhance bone mineral density (BMD), control blood-calcium density, and lower the serum cholesterol level.
摘要:
Disclosed is an IgG Fc fragment useful as a drug carrier. Also, the present invention discloses a recombinant vector expressing the IgG Fc fragment, a transformant transformed with the recombinant vector, and a method of preparing an IgG Fc fragment, comprising culturing the transformant. When conjugated to a certain drug, the IgG Fc fragment improves the in vivo duration of action of the drug and minimizes the in vivo activity reduction of the drug.
摘要:
Disclosed is a novel use of an immunoglobulin Fe fragment, and more particularly, a pharmaceutical composition comprising an immunoglobulin Fe fragment as a carrier. The pharmaceutical composition comprising an immunoglobulin Fe fragment as a carrier remarkably extends the serum half-life of a drug while maintaining the in vivo activity of the drug at relatively high levels. Also, when the drug is a polypeptide drug, the pharmaceutical composition has less risk of inducing immune responses compared to a fusion protein of the immunoglobulin Fe fragment and a target protein, and is thus useful for developing long-acting formulations of various polypeptide drugs.
摘要:
A PEG-polypeptide homodimer complex, which comprises a PEG linker and two molecules of a physiologically active polypeptide, wherein the two molecules of the physiologically active polypeptide are connected via the PEG linker, and each of the two molecules of the physiologically active polypeptide is modified with one molecule of PEG, is useful for the development of a polypeptide drug having a prolonged half-life in the blood.
摘要:
Ticlopidine and clopidogrel having high blood platelet aggregation inhibitory and anti-thrombotic activities are simply prepared by reacting a substituted thiophene derivative with a 2-chlorobenzylamine derivative.
摘要:
This invention provides a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, theremostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.