A61K31/4439

PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CHRONIC MYELOID LEUKEMIA AND METHOD USING THE SAME
20180008579 · 2018-01-11 · ·

Provided are a pharmaceutical composition for preventing or treating chronic myeloid leukemia and a method of preventing or treating chronic myeloid leukemia using the same, thereby being effectively applied to the prevention or treatment of chronic myeloid leukemia.

PROLONGED ANTI-DIABETIC EFFECT OF FIBROBLAST GROWTH FACTOR 1 (FGF1)

Disclosed are compositions and methods for inducing sustained diabetes remission by single administration of FGF1 to the brain. The composition and methods described herein result in basal glucose clearance by using a dosage of FGF1 that is lower than that needed for systemic efficacy and is devoid of the risk of hypoglycemia and changes in body weight, food intake, hepatic glucose production, insulin secretion or insulin sensitivity.

PROLONGED ANTI-DIABETIC EFFECT OF FIBROBLAST GROWTH FACTOR 1 (FGF1)

Disclosed are compositions and methods for inducing sustained diabetes remission by single administration of FGF1 to the brain. The composition and methods described herein result in basal glucose clearance by using a dosage of FGF1 that is lower than that needed for systemic efficacy and is devoid of the risk of hypoglycemia and changes in body weight, food intake, hepatic glucose production, insulin secretion or insulin sensitivity.

PROLONGED ANTI-DIABETIC EFFECT OF FIBROBLAST GROWTH FACTOR 1 (FGF1)

Disclosed are compositions and methods for inducing sustained diabetes remission by single administration of FGF1 to the brain. The composition and methods described herein result in basal glucose clearance by using a dosage of FGF1 that is lower than that needed for systemic efficacy and is devoid of the risk of hypoglycemia and changes in body weight, food intake, hepatic glucose production, insulin secretion or insulin sensitivity.

Modulators of alpha-synuclein proteolysis and associated methods of use

The present disclosure relates to bifunctional compounds, which find utility as modulators of α-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon. Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Modulators of alpha-synuclein proteolysis and associated methods of use

The present disclosure relates to bifunctional compounds, which find utility as modulators of α-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon. Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Phenylpyrrolidinone formyl peptide 2 receptor agonists

The disclosure relates to compounds of Formulae (I)-(IX), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases. ##STR00001##

Phenylpyrrolidinone formyl peptide 2 receptor agonists

The disclosure relates to compounds of Formulae (I)-(IX), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases. ##STR00001##

THIOHYDANTOIN ANDROGEN RECEPTOR ANTAGONISTS FOR THE TREATMENT OF CANCER
20180008587 · 2018-01-11 ·

Disclosed are compounds, compositions and methods for treating and/or ameliorating diseases, syndromes, disorders, or conditions associated with AR mutant receptors linked to castration-resistant prostate cancer, in a subject, including a mammal and/or human, in need thereof, who has demonstrated resistance to a first or second generation AR antagonist, comprising, consisting of, and/or consisting essentially of, administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula (I)

##STR00001##

wherein R.sub.1, G, R.sub.10, and R.sub.11 are defined herein.

THIOHYDANTOIN ANDROGEN RECEPTOR ANTAGONISTS FOR THE TREATMENT OF CANCER
20180008587 · 2018-01-11 ·

Disclosed are compounds, compositions and methods for treating and/or ameliorating diseases, syndromes, disorders, or conditions associated with AR mutant receptors linked to castration-resistant prostate cancer, in a subject, including a mammal and/or human, in need thereof, who has demonstrated resistance to a first or second generation AR antagonist, comprising, consisting of, and/or consisting essentially of, administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula (I)

##STR00001##

wherein R.sub.1, G, R.sub.10, and R.sub.11 are defined herein.