C07D237/04

Use of sanglifehrin macrocyclic analogues as anticancer compounds

The present invention relates to sanglifehrin macrocyclic analogues according to Formula (I), ##STR00001##
particularly for use in treatment of cancer, especially liver cancer.

Dihydropyridazine-based antioxidants and uses thereof

Dihydropyridazines compounds having antioxidant properties and uses thereof are described herein. These compounds can function as antioxidants that prevent oxidation of materials, including polymers, and as free radical inhibitors to stabilize reactive chemicals, such as monomers against free radical reactions. The dihydropyridazines can be added as small molecule additives or they can be incorporated into molecules bearing dienophilic CC double bonds through a Carboni Lindsey reaction, which can reduce environmental and health exposure to antioxidants in plastics and allow for a greater quantity of the antioxidants to be used.

Dihydropyridazine-based antioxidants and uses thereof

Dihydropyridazines compounds having antioxidant properties and uses thereof are described herein. These compounds can function as antioxidants that prevent oxidation of materials, including polymers, and as free radical inhibitors to stabilize reactive chemicals, such as monomers against free radical reactions. The dihydropyridazines can be added as small molecule additives or they can be incorporated into molecules bearing dienophilic CC double bonds through a Carboni Lindsey reaction, which can reduce environmental and health exposure to antioxidants in plastics and allow for a greater quantity of the antioxidants to be used.

Pharmaceutical Compositions for Subcutaneous Administration of Levosimendan

A composition containing levosimendan, one or more solubilizing and/or stabilizing agents, and one or more additional pharmaceutically acceptable additives. The one or more solubilizing and/or stabilizing agents may be a cyclodextrin or a cyclodextrin derivative. The cyclodextrin derivative may be a derivative of an alpha-cyclodextrin, or beta-cyclodextrin, or a gamma-cyclodextrin. The cyclodextrin derivative may contain a butyl ether spacer group, an alkyl ether space group, or both. The one or more additional pharmaceutically acceptable additives may be a non-citrate buffer. The composition may be used in a method of treating a health condition, such as heart failure, pulmonary hypertension, chronic kidney disease, amyotrophic lateral sclerosis, stroke, in advance of a planned cardiac surgery, or other health conditions for which a minimally invasive or repeated administration of levosimendan may be beneficial. The composition may be administered subcutaneously.

DIHYDROPYRIDAZINE ANTIOXIDANT SUNSCREENS

Herein polymers and particles which comprise a plurality of dihydropyridazine or hydropyridazine functional groups are described. Methods for their formation and specific monomers which may be used in their formation are also described. The polymers and particles are UV absorbing, hydrogen-donor antioxidant materials which signal a depletion of antioxidant ability by a decrease in visible fluorescence. These polymers and particles may be used as UV protectants for a variety of materials and substrates and may even be used in a topically applied formulation for human skin.

6-PHENYL-4,5-DIHYDROPYRIDAZIN-3(2H)-ONE DERIVATIVES AS PDE3A AND PDE3B INHIBITORS FOR TREATING CANCER

The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I): The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I):

##STR00001##

6-PHENYL-4,5-DIHYDROPYRIDAZIN-3(2H)-ONE DERIVATIVES AS PDE3A AND PDE3B INHIBITORS FOR TREATING CANCER

The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I): The present invention provides 6-phenyl-4,5-dihydropyridazin-3(2H)-one derivatives of formula (I):

##STR00001##

COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS

The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS

The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

COMPOUNDS THAT PARTICIPATE IN COOPERATIVE BINDING AND USES THEREOF
20200199102 · 2020-06-25 ·

The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for example through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein (e.g., a eukaryotic target protein such as a mammalian target protein or a fungal target protein or a prokaryotic target protein such as a bacterial target protein). These compounds bind endogenous intracellular presenter proteins, such as the FKBPs or cyclophilins, and the resulting binary complexes selectively bind and modulate the activity of intracellular target proteins. Formation of a tripartite complex among the presenter protein, the compound, and the target protein is driven by both protein-compound and protein-protein interactions, and both are required for modulation of the targeted protein's activity.