Patent classifications
A61K31/245
USE OF AR INHIBITOR AND/OR HIF-1 A A INHIBITOR IN PREPARATION OF MEDICAMENT
The present disclosure discloses use of a combination of an HIP-1α inhibitor and/or an AR inhibitor in inhibiting an .inflammatory cytokine storm,. treating or preventing viral pneumonia. The present disclosure finds that inhibitors HIF-1 a and AR prevent the transcription of inflammatory cytokine storm-related genes (IL6, MMP2, MMP13, ADAMTS4, ELN, VCAN. COL3A1 and VEGFA) in fibroblasts under low-oxygen environment by effectively inhibiting the interaction between HIF-1α and AR to reduce the expression quantity of the related genes, thereby influencing the activation of lung fibroblasts. Inhibition of activation of lung fibroblasts enables patients with acute respiratory distress syndrome (ARDS) due to severe respiratory tract infection to maintain the lung functions and improve clinical efficacy.
USE OF AR INHIBITOR AND/OR HIF-1 A A INHIBITOR IN PREPARATION OF MEDICAMENT
The present disclosure discloses use of a combination of an HIP-1α inhibitor and/or an AR inhibitor in inhibiting an .inflammatory cytokine storm,. treating or preventing viral pneumonia. The present disclosure finds that inhibitors HIF-1 a and AR prevent the transcription of inflammatory cytokine storm-related genes (IL6, MMP2, MMP13, ADAMTS4, ELN, VCAN. COL3A1 and VEGFA) in fibroblasts under low-oxygen environment by effectively inhibiting the interaction between HIF-1α and AR to reduce the expression quantity of the related genes, thereby influencing the activation of lung fibroblasts. Inhibition of activation of lung fibroblasts enables patients with acute respiratory distress syndrome (ARDS) due to severe respiratory tract infection to maintain the lung functions and improve clinical efficacy.
N-PHENYL-3-MERCAPTOPROPANAMIDE DERIVATIVES AS METALLO-BETA-LACTAMASE INHIBITORS FOR THE TREATMENT OF BACTERIAL INFECTIONS
The present invention related to novel inhibitors of metallo-β3-lactamases of formula (I)
##STR00001##
wherein R.sup.1 is an optionally substituted aryl group of an optionally substituted heteroaryl group, and the use thereof in the treatment of bacterial infections, especially in combination with β-lactam antibiotics.
N-PHENYL-3-MERCAPTOPROPANAMIDE DERIVATIVES AS METALLO-BETA-LACTAMASE INHIBITORS FOR THE TREATMENT OF BACTERIAL INFECTIONS
The present invention related to novel inhibitors of metallo-β3-lactamases of formula (I)
##STR00001##
wherein R.sup.1 is an optionally substituted aryl group of an optionally substituted heteroaryl group, and the use thereof in the treatment of bacterial infections, especially in combination with β-lactam antibiotics.
ARTICLE OF MANUFACTURE COMPRISING LOCAL ANESTHETIC, BUFFER, AND GLYCOSAMINOGLYCAN IN SYRINGE WITH IMPROVED STABILITY
An article of manufacture according to the present invention comprises a composition including a glycosaminoglycan, a local anesthetic, and a buffer packaged in a syringe or vial constructed from either glass or a plastic selected from the group consisting of cyclic olefin polymer, cyclic olefin copolymer, or high density non-nucleated polypropylene. The composition has unexpectedly improved stability on storage. The composition can be formulated for treatment of a urinary tract disease or condition, such as interstitial cystitis, also known as bladder pain syndrome or hypersensitive bladder syndrome.
ARTICLE OF MANUFACTURE COMPRISING LOCAL ANESTHETIC, BUFFER, AND GLYCOSAMINOGLYCAN IN SYRINGE WITH IMPROVED STABILITY
An article of manufacture according to the present invention comprises a composition including a glycosaminoglycan, a local anesthetic, and a buffer packaged in a syringe or vial constructed from either glass or a plastic selected from the group consisting of cyclic olefin polymer, cyclic olefin copolymer, or high density non-nucleated polypropylene. The composition has unexpectedly improved stability on storage. The composition can be formulated for treatment of a urinary tract disease or condition, such as interstitial cystitis, also known as bladder pain syndrome or hypersensitive bladder syndrome.
VIRAL INFECTION THERAPEUTIC
The present invention relates to an inhibitory agent of membrane fusion between a virus envelope and a cell membrane of a host cell for the virus, wherein the inhibitory agent comprises a serine protease inhibitor, and a therapeutic agent or a therapeutic composition, comprising the inhibitory agent. More specifically, the present invention relates to the inhibitory agent, wherein the serine protease inhibitor is one or more of a compound represented by the following general formula (I) or a salt thereof, or a solvate or hydrate thereof, and a therapeutic agent or a therapeutic composition, comprising the inhibitory agent:
##STR00001## wherein R.sub.1 represents a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group, a substituted or unsubstituted aromatic hydrocarbon group, or a substituted or unsubstituted aromatic heterocyclic group, each of which may optionally comprise a heteroatom.
VIRAL INFECTION THERAPEUTIC
The present invention relates to an inhibitory agent of membrane fusion between a virus envelope and a cell membrane of a host cell for the virus, wherein the inhibitory agent comprises a serine protease inhibitor, and a therapeutic agent or a therapeutic composition, comprising the inhibitory agent. More specifically, the present invention relates to the inhibitory agent, wherein the serine protease inhibitor is one or more of a compound represented by the following general formula (I) or a salt thereof, or a solvate or hydrate thereof, and a therapeutic agent or a therapeutic composition, comprising the inhibitory agent:
##STR00001## wherein R.sub.1 represents a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group, a substituted or unsubstituted aromatic hydrocarbon group, or a substituted or unsubstituted aromatic heterocyclic group, each of which may optionally comprise a heteroatom.
NON-TOXIC TOPICAL ANESTHETIC OPHTHALMIC COMPOSITIONS
Compositions and methods for prolonging the local anesthetic effect of site 1 sodium channel blockers and local anesthetics with minimal or reduced toxicity have been developed for ophthalmic use. It has been established that agents such as dexmedetomidine having alpha-2-adrenergic agonist and Hyperpolarization-activated cyclic nucleotide-gated channel antagonist activity can dramatically prolong the duration of nerve blockade when administered to the surface of, a compartment of or tissue adjacent to, the eye. A preferred active agent for prolonging the local anesthetic effect of site 1 sodium channel blockers or local anesthetics is Dexmedetomidine.
NON-TOXIC TOPICAL ANESTHETIC OPHTHALMIC COMPOSITIONS
Compositions and methods for prolonging the local anesthetic effect of site 1 sodium channel blockers and local anesthetics with minimal or reduced toxicity have been developed for ophthalmic use. It has been established that agents such as dexmedetomidine having alpha-2-adrenergic agonist and Hyperpolarization-activated cyclic nucleotide-gated channel antagonist activity can dramatically prolong the duration of nerve blockade when administered to the surface of, a compartment of or tissue adjacent to, the eye. A preferred active agent for prolonging the local anesthetic effect of site 1 sodium channel blockers or local anesthetics is Dexmedetomidine.