Abstract: Analogs and derivatives of omecamtiv mecarbil (OM), including an 18F-labeled analog, and methods of synthesis thereof. Cardiac myosin targeting vectors comprising a lipid anchoring/solubilizing moiety conjugated to a head made of OM or the OM analog or derivative. Liposomes comprising a cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of treating a cardiac condition or disease in a subject by administering to the subject the cardiac-treating cargo molecule and the cardiac myosin targeting vector. Methods of synthesizing an 18F-labeled analog of OM.

Abstract: The compound DMX-5804, IUPAC name 5-(4-(2-methoxyethoxy)phenyl)-7-phenyl-3,4a,7,7a-tetrahydro-4H-pyrrolo[2,3-d]pyrimidin-4-one, is a potent and selective inhibitor of mitogen-activated protein kinase kinase kinase kinase-4 (MAP4K4). The present disclosure describes a scalable and practical synthesis process for making DMX-5804. The process (1) doesn't rely on transition metals, (2) has reduced duration of reactions, (3) is streamlined with significantly improved yields using low cost raw materials, (4) includes no microwave-assisted reactions, (5) does not require column purification, and (6) generally results in crystalized products having over a 95% purity in each step. The present disclosure also describes DMX-5804 analogs and derivatives for use in inhibiting MAP4K4, and scalable and practical processes for making such DMX-5804 analogs.

Abstract: Benzylamino-oxoethyl benzamide compounds for use in treating diseases and conditions associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic ?-cell dysfunction and death, for example in the treatment of Type 1 and Type 2 diabetes. The compounds can also be used in treatments for chronic heart disease, neurodegenerative diseases, retinal degeneration, and other metabolic disorders associated with ER stress.

Abstract: Compounds and methods for treating insulin resistance, obesity, Type 2 diabetes, Nonalcoholic fatty liver disease (NAFLD), and peroxisome proliferator-activated receptor gamma (PPARy) serine 273 phosphorylation in subjects in need of such therapy.

Abstract: Hydroxybenzamide derivative compounds having ?-cell protective activity against ER stress, and methods of their use in treating diabetes and other conditions and diseases associated with ER stress. In one non-limiting embodiment, the derivative is 3-hydroxy-N-(4-(trifluoromethyl)benzyl)benzamide.

Abstract: Benzylamino-oxoethyl benzamide compounds for use in treating diseases and conditions associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic ?-cell dysfunction and death, for example in the treatment of Type 1 and Type 2 diabetes. The compounds can also be used in treatments for chronic heart disease, neurodegenerative diseases, retinal degeneration, and other metabolic disorders associated with ER stress.

Abstract: Benzylamino-oxoethyl benzamide compounds for use in treating diseases and conditions associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic ?-cell dysfunction and death, for example in the treatment of Type 1 and Type 2 diabetes. The compounds can also be used in treatments for chronic heart disease, neurodegenerative diseases, retinal degeneration, and other metabolic disorders associated with ER stress.