C07C279/04

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

The present invention 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, the imaging agent 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. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.

Compounds for inhibiting NS3 and compositions containing the inhibited protein

Imidazole-based compounds as hepatitis C virus (HCV) inhibitors. The compounds have an imidazole core that is disubstituted via amide links. Also described are a pharmaceutical composition incorporating the imidazole-based compound, a method of preparing these compounds, and a method for using the pharmaceutical composition in the treatment of HCV infection.

Clickable antimicrobial molecules and polymers
10709130 · 2020-07-14 · ·

In one aspect, the present disclosure relates to click-functional antimicrobial molecules (including small molecules or, in some cases, macromolecules) and the construction of antimicrobial polymers such as polyurethanes, polyesters, and polyacrylates, including through the use of such molecules. In some cases, the antimicrobial click-functional molecules are based on 1,2-benzisothiazolin-3-one (BIT), trimethylguanidine or tetramethylguanidine (TMG), polyhexamethylene guanidine (PHMG), fluorine-containing molecules, or a combination thereof. For example, 1,2-benzisothiazolin-3-one (BIT) functionalized with an alkyne (BIT-Al), trimethylguanidine or tetramethylguanidine (TMG) functioned with an alkyne (TMG-Al) or dual alkynes (TMG-dAl), and/or polyhexamethylene guanidine (PHMG) functionalized with an alkyne (PHMG-Al) are described herein. Clickable antimicrobial polymers can be used to form coatings or films.

Clickable antimicrobial molecules and polymers
10709130 · 2020-07-14 · ·

In one aspect, the present disclosure relates to click-functional antimicrobial molecules (including small molecules or, in some cases, macromolecules) and the construction of antimicrobial polymers such as polyurethanes, polyesters, and polyacrylates, including through the use of such molecules. In some cases, the antimicrobial click-functional molecules are based on 1,2-benzisothiazolin-3-one (BIT), trimethylguanidine or tetramethylguanidine (TMG), polyhexamethylene guanidine (PHMG), fluorine-containing molecules, or a combination thereof. For example, 1,2-benzisothiazolin-3-one (BIT) functionalized with an alkyne (BIT-Al), trimethylguanidine or tetramethylguanidine (TMG) functioned with an alkyne (TMG-Al) or dual alkynes (TMG-dAl), and/or polyhexamethylene guanidine (PHMG) functionalized with an alkyne (PHMG-Al) are described herein. Clickable antimicrobial polymers can be used to form coatings or films.

Photobase generator, compound, photoreactive composition, and reaction product

A photobase generator includes a compound including a first skeleton represented by the following formula (a), and a second skeleton including a nitrogen atom bonding to a bonding position of the first skeleton to form an amide group, wherein the compound generates a base, in which a hydrogen atom is bonding with the nitrogen atom of the second skeleton, by light irradiation, and the pKa of a conjugate acid of the base in water is 12 or more. In formula (a), G is a divalent aromatic group, and * represents the bonding position with the nitrogen atom. ##STR00001##

Photobase generator, compound, photoreactive composition, and reaction product

A photobase generator includes a compound including a first skeleton represented by the following formula (a), and a second skeleton including a nitrogen atom bonding to a bonding position of the first skeleton to form an amide group, wherein the compound generates a base, in which a hydrogen atom is bonding with the nitrogen atom of the second skeleton, by light irradiation, and the pKa of a conjugate acid of the base in water is 12 or more. In formula (a), G is a divalent aromatic group, and * represents the bonding position with the nitrogen atom. ##STR00001##

Tricyclic amino containing compounds for treatment or prevention of symptoms associated with endocrine dysfunction

The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.

Tricyclic Amino Containing Compounds for Treatment or Prevention of Symptoms Associated with Endocrine Dysfunction

The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.

NOVEL NAMPT ENZYME AGONIST AND PREPARATION AND USE THEREOF

The present invention provides a class of novel NAMPT enzyme agonist and preparation and use thereof, which has a structural formula as shown in formula I or formula II. The present invention screens the NAMPT agonist NAT from the chemical small molecule library, and the NAT exhibits a good cytoprotective effect and a good anti-neurodegeneration effect in animal models of neurodegeneration. We studied the binding of NAT to enzymes, and then carried out multiple rounds of structure optimization based on the chemical structure characteristics of NAT and its enzyme activity properties, and obtained a relatively defined structure-activity relationship. The present patent not only lays the foundation for developing innovative drugs for anti-aging and neurodegenerative diseases, but also theoretically provides a proof-of-concept that enhancing NAMPT enzyme activity plays an important role in neuroprotection.

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NOVEL NAMPT ENZYME AGONIST AND PREPARATION AND USE THEREOF

The present invention provides a class of novel NAMPT enzyme agonist and preparation and use thereof, which has a structural formula as shown in formula I or formula II. The present invention screens the NAMPT agonist NAT from the chemical small molecule library, and the NAT exhibits a good cytoprotective effect and a good anti-neurodegeneration effect in animal models of neurodegeneration. We studied the binding of NAT to enzymes, and then carried out multiple rounds of structure optimization based on the chemical structure characteristics of NAT and its enzyme activity properties, and obtained a relatively defined structure-activity relationship. The present patent not only lays the foundation for developing innovative drugs for anti-aging and neurodegenerative diseases, but also theoretically provides a proof-of-concept that enhancing NAMPT enzyme activity plays an important role in neuroprotection.

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