Patent classifications
A61K31/409
PHARMACEUTICAL COMPOSITIONS WITH ANTIFLAVIVIRAL ACTIVITY
Provided is a method of inhibiting viral replication, including contacting one or more cells that has been infected or contacted with a flavivirus with an effective amount of niclosamide, temoporfin, nitazoxanide, tizoxanide, erythrosin B, methylene blue. Contacting one or more cells that have been infected with a flavivirus may include administering the compound to a mammal, a human, or other subject. The flavivirus may be Dengue virus serotype 1, Dengue virus serotype 2, Dengue virus serotype 3, Dengue virus serotype 4, yellow fever virus, West Nile virus, Zika virus, Japanese encephalitis virus, tick-born encephalitis virus, Powassan virus, St. Louis encephalitis virus, or other flavivirus.
Bilirubin derivative-based diagnostic and therapeutic ultrasound contrast agent
Provided is a bilirubin derivative-based ultrasound contrast agent for diagnosis and treatment. The fine particles including the bilirubin derivative are sensitive to reactive oxygen species (ROS), bind with hydrophobic drugs, and can effectively chelate metals such as iron oxide nanoparticles. Therefore, the fine particle of the present invention can be used as an ultrasound contrast agent for diagnosis, as a magnetic resonance imaging contrast agent, or as a carrier for hydrophobic drugs or platinum-based drugs.
Bilirubin derivative-based diagnostic and therapeutic ultrasound contrast agent
Provided is a bilirubin derivative-based ultrasound contrast agent for diagnosis and treatment. The fine particles including the bilirubin derivative are sensitive to reactive oxygen species (ROS), bind with hydrophobic drugs, and can effectively chelate metals such as iron oxide nanoparticles. Therefore, the fine particle of the present invention can be used as an ultrasound contrast agent for diagnosis, as a magnetic resonance imaging contrast agent, or as a carrier for hydrophobic drugs or platinum-based drugs.
Atropisomers of halogenated tetraphenylbacteriochlorins and chlorins and their use in photodynamic therapy
This invention relates to atroipsomers of reduced tetraphenylporphyrin derivatives with halogen atoms (F, Cl, Br) in the ortho positions of the phenyl groups, particularly halogenated tetraphenylchlorins and halogenated tetraphenylbacteriochlorins, which can be used in photodynamic therapy. According to the formulae of the invention, the ortho-phenyl substituents X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, X.sup.7 and X.sup.8 may be identical or different and represent halogen atoms or hydrogen atoms, provided that at least all of X.sup.2, X.sup.4, X.sup.6 and X.sup.8 are halogens, and the meta-phenyl substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently chosen from —OH, —OR or —SO.sub.2R″, where R″ are each independently chosen from —Cl, —OH, -aminoacid, —OR, —NHR, or —NR.sub.2, where R are alkyl of 1 to 12 carbon atoms or R.sub.2 represents cycloalkyl with 2 to 12 carbon atoms. The atropisomers of this invention have the majority of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 on the same side of the plane defined by the macrocycle. The invention also relates to an anticancer and/or antimicrobial and/or antiviral pharmaceutical composition where atropisomers α.sub.4 and α.sub.3β are the main active ingredients, such that the mixture of atropisomers α.sub.4 and α.sub.3β constitutes more than 70% of the atropisomers present in the active ingredient and/or the atropisomer α.sub.4 constitutes more than 20% of the atropisomers present in the pharmaceutical composition.
Atropisomers of halogenated tetraphenylbacteriochlorins and chlorins and their use in photodynamic therapy
This invention relates to atroipsomers of reduced tetraphenylporphyrin derivatives with halogen atoms (F, Cl, Br) in the ortho positions of the phenyl groups, particularly halogenated tetraphenylchlorins and halogenated tetraphenylbacteriochlorins, which can be used in photodynamic therapy. According to the formulae of the invention, the ortho-phenyl substituents X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, X.sup.7 and X.sup.8 may be identical or different and represent halogen atoms or hydrogen atoms, provided that at least all of X.sup.2, X.sup.4, X.sup.6 and X.sup.8 are halogens, and the meta-phenyl substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently chosen from —OH, —OR or —SO.sub.2R″, where R″ are each independently chosen from —Cl, —OH, -aminoacid, —OR, —NHR, or —NR.sub.2, where R are alkyl of 1 to 12 carbon atoms or R.sub.2 represents cycloalkyl with 2 to 12 carbon atoms. The atropisomers of this invention have the majority of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 on the same side of the plane defined by the macrocycle. The invention also relates to an anticancer and/or antimicrobial and/or antiviral pharmaceutical composition where atropisomers α.sub.4 and α.sub.3β are the main active ingredients, such that the mixture of atropisomers α.sub.4 and α.sub.3β constitutes more than 70% of the atropisomers present in the active ingredient and/or the atropisomer α.sub.4 constitutes more than 20% of the atropisomers present in the pharmaceutical composition.
Castration-resistant prostate cancer
This invention relates to inhibitors of UDP-glucose dehydrogenase, and more particularly to UDP-glucose dehydrogenase inhibitors that are useful in the treatment of prostate cancer. Methods of inhibiting UDP-glucose dehydrogenase and improving the efficacy of additional prostate cancer therapies are also provided.
Castration-resistant prostate cancer
This invention relates to inhibitors of UDP-glucose dehydrogenase, and more particularly to UDP-glucose dehydrogenase inhibitors that are useful in the treatment of prostate cancer. Methods of inhibiting UDP-glucose dehydrogenase and improving the efficacy of additional prostate cancer therapies are also provided.
COMPOSITIONS AND METHODS FOR TREATING HEMORRHAGIC STROKE
A pharmaceutical composition includes a ferrochelatase inhibitor and a pharmaceutically acceptable carrier. In another aspect, a method of treating a subject having, or at risk of having, a hemorrhagic stroke generally includes administering to the subject a pharmaceutical composition that includes a ferrochelatase inhibitor in an amount effective to ameliorate at least one symptom or clinical sign of hemorrhagic stroke.
COMPOSITIONS AND METHODS FOR TREATING HEMORRHAGIC STROKE
A pharmaceutical composition includes a ferrochelatase inhibitor and a pharmaceutically acceptable carrier. In another aspect, a method of treating a subject having, or at risk of having, a hemorrhagic stroke generally includes administering to the subject a pharmaceutical composition that includes a ferrochelatase inhibitor in an amount effective to ameliorate at least one symptom or clinical sign of hemorrhagic stroke.
COMPOSITIONS AND METHODS FOR TREATING HEMORRHAGIC STROKE
A pharmaceutical composition includes a ferrochelatase inhibitor and a pharmaceutically acceptable carrier. In another aspect, a method of treating a subject having, or at risk of having, a hemorrhagic stroke generally includes administering to the subject a pharmaceutical composition that includes a ferrochelatase inhibitor in an amount effective to ameliorate at least one symptom or clinical sign of hemorrhagic stroke.