Patent classifications
A61K31/343
MITOCHONDRIAL PERMEABILITY TRANSITION PORE (mPTP)-OPENING INHIBITOR, NOVEL COMPOUND EXHIBITING mPTP-OPENING INHIBITORY ACTIVITY, AND USE THEREFOR
The present invention aims to provide a novel compound having a high mPTP-opening inhibitory activity and/or a useful therapeutic effect on various diseases. An aspect of the present invention relates to a mitochondrial permeability transition pore (mPTP)-opening inhibitor, a medicament or a pharmaceutical composition comprising a compound represented by formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are the same as defined in the specification and the claims, a stereoisomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, as an active ingredient. Another aspect of the present invention relates to a compound represented by formula (Ia), wherein R.sup.1a, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are the same as defined in the specification and the claims, a stereoisomer thereof, a prodrug thereof, or a salt thereof, or a solvate thereof.
MITOCHONDRIAL PERMEABILITY TRANSITION PORE (mPTP)-OPENING INHIBITOR, NOVEL COMPOUND EXHIBITING mPTP-OPENING INHIBITORY ACTIVITY, AND USE THEREFOR
The present invention aims to provide a novel compound having a high mPTP-opening inhibitory activity and/or a useful therapeutic effect on various diseases. An aspect of the present invention relates to a mitochondrial permeability transition pore (mPTP)-opening inhibitor, a medicament or a pharmaceutical composition comprising a compound represented by formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are the same as defined in the specification and the claims, a stereoisomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, as an active ingredient. Another aspect of the present invention relates to a compound represented by formula (Ia), wherein R.sup.1a, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are the same as defined in the specification and the claims, a stereoisomer thereof, a prodrug thereof, or a salt thereof, or a solvate thereof.
Therapeutic agents and methods
The invention provides glucocorticoid receptor antagonists for treatment of infection, neoplasia, and fatty liver disease.
Therapeutic agents and methods
The invention provides glucocorticoid receptor antagonists for treatment of infection, neoplasia, and fatty liver disease.
AUGMENTING ANTIGEN-NEGATIVE CELL DEATH IN ANTIGEN-TARGETED IMMUNOTHERAPIES
Combination therapies that include (i) an immune cell that expresses a chimeric antigen receptor (CAR) or similar molecule and (ii) a compound that preserves or potentiates the in vivo actions of tumor necrosis factor alpha (TNFα) against cancer cells are described. The combination therapies result in the killing of antigen-negative cells in the vicinity of immunotherapy targeted-antigen-positive cells reducing the survivability of escape variants and providing other benefits.
AUGMENTING ANTIGEN-NEGATIVE CELL DEATH IN ANTIGEN-TARGETED IMMUNOTHERAPIES
Combination therapies that include (i) an immune cell that expresses a chimeric antigen receptor (CAR) or similar molecule and (ii) a compound that preserves or potentiates the in vivo actions of tumor necrosis factor alpha (TNFα) against cancer cells are described. The combination therapies result in the killing of antigen-negative cells in the vicinity of immunotherapy targeted-antigen-positive cells reducing the survivability of escape variants and providing other benefits.
METHODS FOR TREATING OR PREVENTING CHRONIC KIDNEY DISEASE
Described herein are methods for treating or preventing chronic kidney disease, and other diseases, comprising the administration (3,5-dibromo-4-hydroxyphenyl)(2-(1-hydroxyethy)benzofuran-3-yl-4,5,6,7-d.sub.4)methanone, and solvates thereof.
METHODS FOR TREATING OR PREVENTING CHRONIC KIDNEY DISEASE
Described herein are methods for treating or preventing chronic kidney disease, and other diseases, comprising the administration (3,5-dibromo-4-hydroxyphenyl)(2-(1-hydroxyethy)benzofuran-3-yl-4,5,6,7-d.sub.4)methanone, and solvates thereof.
METHODS FOR TREATING OR PREVENTING CHRONIC KIDNEY DISEASE
Described herein are methods for treating or preventing chronic kidney disease, and other diseases, comprising the administration (3,5-dibromo-4-hydroxyphenyl)(2-(1-hydroxyethy)benzofuran-3-yl-4,5,6,7-d.sub.4)methanone, and solvates thereof.
Combinations of artemisinins, BCL-2 inhibitors, and kinase inhibitors for cancer treatment
Methods of treating cancer, such as leukemia, via administration of therapeutically effective amounts of artemisinins and one or more additional therapeutic agents are detailed herein. The artemisinins include artesunate, dihydroartemisinin, artemether, arteether, artelinate, ART-631, and ART-838. The one or more additional therapeutic agents include BCL-2 inhibitors such as ABT-199, ABT-263, and ABT-737; kinase inhibitors such as lestaurtinib, midostaurin, and sorafenib; and anti-neoplastic agents such as cytarabine, doxorubicin, etoposide, cyclophosphamide, triplotide, vinorelbine, cisplatin, and rituximab.