Patent classifications
C07H23/00
COMPOUNDS COMPRISING CLEAVABLE LINKER AND USES THEREOF
Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a SO.sub.2 functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.
Polymyxin-based pharmaceutical composition for treating infectious diseases
Field of application: The invention relates to medicine and pharmacy and allows to obtain new pharmaceutical compositions based on polymyxin for the treatment of severe infectious diseases, but not possessing nephrotoxic properties in therapeutic doses. Technical result: New combined dosage forms based on the antibiotic polymyxin with low nephrotoxicity and high activity.
Polymyxin-based pharmaceutical composition for treating infectious diseases
Field of application: The invention relates to medicine and pharmacy and allows to obtain new pharmaceutical compositions based on polymyxin for the treatment of severe infectious diseases, but not possessing nephrotoxic properties in therapeutic doses. Technical result: New combined dosage forms based on the antibiotic polymyxin with low nephrotoxicity and high activity.
Stereoselective synthesis and process for the manufacturing of 2′-deoxynucleosides
Methods for stereoselective synthesis and manufacturing of 2′-deoxynucleosides, such as 2′-ribonucleosides, are disclosed. In some embodiments, the 2′-deoxynucleoside is a β-anomer of a 2′-deoxynucleoside having a 3′ α hydroxyl, 4′ β hydroxymethyl configuration. Nonlimiting examples of compounds prepared by the disclosed methods include 4′-thio-2′-deoxycytidine (T-dCyd) and 5-aza-4′-thio-2′-deoxycytidine (5-aza-T-dCyd; aza-T-dCyd; aza-T-dC).
Stereoselective synthesis and process for the manufacturing of 2′-deoxynucleosides
Methods for stereoselective synthesis and manufacturing of 2′-deoxynucleosides, such as 2′-ribonucleosides, are disclosed. In some embodiments, the 2′-deoxynucleoside is a β-anomer of a 2′-deoxynucleoside having a 3′ α hydroxyl, 4′ β hydroxymethyl configuration. Nonlimiting examples of compounds prepared by the disclosed methods include 4′-thio-2′-deoxycytidine (T-dCyd) and 5-aza-4′-thio-2′-deoxycytidine (5-aza-T-dCyd; aza-T-dCyd; aza-T-dC).
Methods and compositions for administration of iron
The present invention generally relates to treatment of iron-related conditions with iron carbohydrate complexes. One aspect of the invention is a method of treatment of iron-related conditions with a single unit dosage of at least about 0.6 grams of elemental iron via an iron carbohydrate complex. The method generally employs iron carbohydrate complexes with nearly neutral pH, physiological osmolarity, and stable and non-immunogenic carbohydrate components so as to rapidly administer high single unit doses of iron intravenously to patients in need thereof.
Methods and compositions for administration of iron
The present invention generally relates to treatment of iron-related conditions with iron carbohydrate complexes. One aspect of the invention is a method of treatment of iron-related conditions with a single unit dosage of at least about 0.6 grams of elemental iron via an iron carbohydrate complex. The method generally employs iron carbohydrate complexes with nearly neutral pH, physiological osmolarity, and stable and non-immunogenic carbohydrate components so as to rapidly administer high single unit doses of iron intravenously to patients in need thereof.
PHARMACEUTICAL COMPOSITION COMPRISING NOVEL AZOLOPYRIMIDINE HETEROCYCLIC COMPOUND AS ACTIVE INGREDIENT
The present invention relates to a pharmaceutical composition for the prophylaxis or treatment of cancer comprising a novel azolopyrimidine heterocyclic compound as an active ingredient, and the pharmaceutical composition for the prophylaxis or treatment of cancer of the present invention can be used as a small molecular immunotherapy anticancer agent which modulates an adenosine pathway by comprising the azolopyrimidine heterocyclic compound.
FLUORESCENT GTP ANALOGUES AND USE
The invention relates to compounds of formula:
##STR00001##
in which X, Y, L and Ln.sup.3+ are as defined in the description.
Method of preparing ferric carboxymaltose
Provided is a method of preparing ferric carboxymaltose with weight average molecular weight between 100,000 and 400,000. The method includes reacting an oxidized maltodextrin solid with an iron (III) salt solution in acidic and basic conditions in sequence to afford ferric carboxymaltose, wherein the oxidized maltodextrin solid has a dextrose equivalent of less than 4. The ferric carboxymaltose prepared by the method can withstand high-temperature sterilization with high stability and facilitate storage.