Patent classifications
A61K31/426
Pharmaceutical Formulations for Managing Uric Acid Content in Human Body
The present invention relates to pharmaceutical formulations to treat gout by managing uric acid content in human body by control of making of uric acid in the body and/or removing uric acid from the body. Further, such formulations for treatment of gout are fast available for pharmacological action. Pharmaceutical formulation of the present invention is orally disintegrating solid pharmaceutical dosage form of febuxostat for treating hyperuricemia.
Applications of novel thiazole derivative in treating inflammatory bowel diseases
The present invention relates to applications of a novel thiazole derivative in treating ulcerative colitis and in the preparation of drugs for treating ulcerative colitis. The present invention specifically relates to applications of a compound represented by formula I and a pharmaceutical composition containing the compound represented by formula I, in treating ulcerative colitis and in the preparation of drugs for treating ulcerative colitis: ##STR00001##
Applications of novel thiazole derivative in treating inflammatory bowel diseases
The present invention relates to applications of a novel thiazole derivative in treating ulcerative colitis and in the preparation of drugs for treating ulcerative colitis. The present invention specifically relates to applications of a compound represented by formula I and a pharmaceutical composition containing the compound represented by formula I, in treating ulcerative colitis and in the preparation of drugs for treating ulcerative colitis: ##STR00001##
Compositions and methods for delaying the incidence of labor
The invention provides compositions and methods for delaying the onset of delivery in a pregnant subject, such as a pregnant human subject, that is undergoing or at risk of undergoing preterm labor at a gestational age of from about 24 weeks to about 34 weeks. Using the compositions and methods described herein, such subjects may be administered nifedipine in combination with a prostaglandin F2α (PGF2α) antagonist. Exemplary PGF2α receptor antagonists that may be used for the treatment or prevention of preterm labor as described herein include 1,3-thiazolidine-2-carboxamide compounds, such as (3S)-3-({[(2S)-3-(biphenyl-4-ylsulfonyl)-1,3-thiazolidin-2-yl]carbonyl}-amino)-3-(4-fluorophenyl)propyl L-valinate or a pharmaceutically acceptable salt thereof (e.g., (3S)-3-({[(2S)-3-(biphenyl-4-ylsulfonyl)-1,3-thiazolidin-2-yl]carbonyl}-amino)-3-(4-fluorophenyl)propyl L-valinate hydrochloride. Using the compositions and methods described herein, a subject may be dosed with a PGF2α receptor antagonist and a reduced amount or frequency of nifedipine relative to the amount or frequency of nifedipine that would otherwise be used if the nifedipine were given in the absence of the PGF2α receptor antagonist.
Compositions and methods for delaying the incidence of labor
The invention provides compositions and methods for delaying the onset of delivery in a pregnant subject, such as a pregnant human subject, that is undergoing or at risk of undergoing preterm labor at a gestational age of from about 24 weeks to about 34 weeks. Using the compositions and methods described herein, such subjects may be administered nifedipine in combination with a prostaglandin F2α (PGF2α) antagonist. Exemplary PGF2α receptor antagonists that may be used for the treatment or prevention of preterm labor as described herein include 1,3-thiazolidine-2-carboxamide compounds, such as (3S)-3-({[(2S)-3-(biphenyl-4-ylsulfonyl)-1,3-thiazolidin-2-yl]carbonyl}-amino)-3-(4-fluorophenyl)propyl L-valinate or a pharmaceutically acceptable salt thereof (e.g., (3S)-3-({[(2S)-3-(biphenyl-4-ylsulfonyl)-1,3-thiazolidin-2-yl]carbonyl}-amino)-3-(4-fluorophenyl)propyl L-valinate hydrochloride. Using the compositions and methods described herein, a subject may be dosed with a PGF2α receptor antagonist and a reduced amount or frequency of nifedipine relative to the amount or frequency of nifedipine that would otherwise be used if the nifedipine were given in the absence of the PGF2α receptor antagonist.
COMBINATION THERAPY HAVING ANTIOXYDANT PROPERTIES
The present invention relates to novel uses of nitazoxanide, or analogues thereof.
COMBINATION THERAPY HAVING ANTIOXYDANT PROPERTIES
The present invention relates to novel uses of nitazoxanide, or analogues thereof.
COMBINATION THERAPY HAVING ANTIOXYDANT PROPERTIES
The present invention relates to novel uses of nitazoxanide, or analogues thereof.
HYDROGEN PEROXIDE-RESPONSIVE KEAP1-NRF2 PPI INHIBITOR PRODRUG, AND PREPARATION METHOD THEREFOR
The present application relates to a hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug, and a preparation method therefor. The hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug pro2 has a chemical structure as shown below. By modifying a key carboxyl pharmacophore in a Keap1-Nrf2 inhibitor with a H.sub.2O.sub.2-responsive thiazolidinone moiety, a novel ROS-responsive antioxidant prodrug pro2 is synthesized. The H.sub.2O.sub.2 activated prodrug pro2 can simultaneously achieve targeted activation of Nrf2 and enhancement of therapeutic efficacy in the body. The prodrug is based on the concept of ROS activation-ROS clearance therapy, is the first example of a H.sub.2O.sub.2-responsive prodrug suitable for oral administration, and is expected to be used clinically by virtue of the characteristics of druggability and high targeting ability.
HYDROGEN PEROXIDE-RESPONSIVE KEAP1-NRF2 PPI INHIBITOR PRODRUG, AND PREPARATION METHOD THEREFOR
The present application relates to a hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug, and a preparation method therefor. The hydrogen peroxide-responsive Keap1-Nrf2 PPI inhibitor prodrug pro2 has a chemical structure as shown below. By modifying a key carboxyl pharmacophore in a Keap1-Nrf2 inhibitor with a H.sub.2O.sub.2-responsive thiazolidinone moiety, a novel ROS-responsive antioxidant prodrug pro2 is synthesized. The H.sub.2O.sub.2 activated prodrug pro2 can simultaneously achieve targeted activation of Nrf2 and enhancement of therapeutic efficacy in the body. The prodrug is based on the concept of ROS activation-ROS clearance therapy, is the first example of a H.sub.2O.sub.2-responsive prodrug suitable for oral administration, and is expected to be used clinically by virtue of the characteristics of druggability and high targeting ability.