Patent classifications
A61K31/4365
Treatment or prevention of cardiovascular events via the administration of a colchicine derivative
A method for the treatment or prevention of a cardiovascular event in a subject with atherosclerotic vascular disease comprising the step of: b) administering a therapeutically effective amount of a compound of formula (I), a known colchicine derivative and/or a salt thereof ##STR00001##
wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-6 cycloalkyl, halogen, C.sub.1-4 haloalkyl, nitro, amino, C.sub.2-4 acylamino, C.sub.1-4 alkyl or dialkylamino, hydroxyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, a group of the formula —SO.sub.2N(R.sup.x).sub.2 or SO.sub.2R.sup.x where R.sup.x is C.sub.1-4 alkyl, C.sub.1-4 acyloxy, or optionally substituted phenyl, optionally substituted phenoxy; R.sub.7 and R.sub.8 independently represent hydrogen, C.sub.1-4 alkyl or C.sub.1-4 acyl; and R.sub.5′, R.sub.5″, R.sub.6′ and R.sub.6″ independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-6 cycloalkyl, halogen, C.sub.1-4 haloalkyl, nitro, amino, C.sub.2-4 acylamino, hydroxyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio a group of the formula —SO.sub.2N(R.sup.x).sub.2 or SO.sub.2R.sup.x where R.sup.x is C.sub.1-4 alkyl, C.sub.1-4 acyloxy, or optionally substituted phenyl.
Methods for treating cognitive deficits in a subject having schizophrenia, bipolar disorder, or psychiatric depression, and exhibiting cognitive deficits by administering an antagonist of the Na+-K+-2Cl-cation-chloride cotransporter isoform 1 (NKCC1)
Disclosed are methods for treating a psychiatric disease or disorder and/or symptoms thereof in a subject in need thereof, the method comprising administering to the subject an effective amount of an antagonist of the Na+-K+-2Cl— cation-chloride cotransporter isoform 1 (NKCC1) for treating the psychiatric disorder and/or the symptoms thereof in the subject. The methods further may include administering to the subject a dopamine D1 agonist and/or a GABA.sub.A agonist, optionally at a subeffective dose, where co-administering the antagonist of NKCC1 improves the efficacy of the dopamine D1 agonist and/or the GABA.sub.A agonist, optionally at the subeffective dose, for treating the psychiatric disease or disorder and/or symptoms thereof.
Methods for treating cognitive deficits in a subject having schizophrenia, bipolar disorder, or psychiatric depression, and exhibiting cognitive deficits by administering an antagonist of the Na+-K+-2Cl-cation-chloride cotransporter isoform 1 (NKCC1)
Disclosed are methods for treating a psychiatric disease or disorder and/or symptoms thereof in a subject in need thereof, the method comprising administering to the subject an effective amount of an antagonist of the Na+-K+-2Cl— cation-chloride cotransporter isoform 1 (NKCC1) for treating the psychiatric disorder and/or the symptoms thereof in the subject. The methods further may include administering to the subject a dopamine D1 agonist and/or a GABA.sub.A agonist, optionally at a subeffective dose, where co-administering the antagonist of NKCC1 improves the efficacy of the dopamine D1 agonist and/or the GABA.sub.A agonist, optionally at the subeffective dose, for treating the psychiatric disease or disorder and/or symptoms thereof.
INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR TREATING CORONARY DISORDERS
A method of treating preventing, minimizing, and/or reversing congestive heart failure, cardiomyopathy, and/or reduction of cardiac ejection fraction in a subject in need thereof includes administering to the subject a therapeutically effective amount of a 15-PGDH inhibitor.
INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR TREATING CORONARY DISORDERS
A method of treating preventing, minimizing, and/or reversing congestive heart failure, cardiomyopathy, and/or reduction of cardiac ejection fraction in a subject in need thereof includes administering to the subject a therapeutically effective amount of a 15-PGDH inhibitor.
INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR TREATING CORONARY DISORDERS
A method of treating preventing, minimizing, and/or reversing congestive heart failure, cardiomyopathy, and/or reduction of cardiac ejection fraction in a subject in need thereof includes administering to the subject a therapeutically effective amount of a 15-PGDH inhibitor.
Anti-androgens for the treatment of non-metastatic castration-resistant prostate cancer
Described herein are methods of treating non-metastatic castrate-resistant prostate cancer using an approved drug product comprising apalutamide, enzalutamide or darolutamide. Also described here are drug products containing apalutamide enzalutamide or darolutamide, and methods of selling or offering for sale an anti-androgen drug product.
Anti-androgens for the treatment of non-metastatic castration-resistant prostate cancer
Described herein are methods of treating non-metastatic castrate-resistant prostate cancer using an approved drug product comprising apalutamide, enzalutamide or darolutamide. Also described here are drug products containing apalutamide enzalutamide or darolutamide, and methods of selling or offering for sale an anti-androgen drug product.
Anti-androgens for the treatment of non-metastatic castration-resistant prostate cancer
Described herein are methods of treating non-metastatic castrate-resistant prostate cancer using an approved drug product comprising apalutamide, enzalutamide or darolutamide. Also described here are drug products containing apalutamide enzalutamide or darolutamide, and methods of selling or offering for sale an anti-androgen drug product.
COMPOUNDS THAT INTERACT WITH THE RAS SUPERFAMILY FOR THE TREATMENT OF CANCERS, INFLAMMATORY DISEASES, RASOPATHIES, AND FIBROTIC DISEASE
Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.