C07C235/64

Histone acetyltransferase activators and uses thereof

The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

Antimicrobial compound and use thereof

The present invention relates to: coralmycin A and B, which are novel compounds exhibiting antimicrobial activity, an isomer thereof, a derivative thereof or a pharmaceutically acceptable salt thereof; a microorganism of the genus Corallococcus producing the same; and an antimicrobial use thereof. The coralmycin A and B have very strong antimicrobial activity against antibiotic-resistant bacteria such as MRSA, QRSA, VRE, VISA, etc.; Acinetobacter baumannii, which is a multidrug-resistant microorganism; and also against gram-positive microorganisms and gram-negative microorganisms. Therefore, the present invention can be very useful for prevention, treatment and alleviation of various microbial infections, and thus can be widely applied to the medical supply, quasi-drug, food, and feed industries.

Antimicrobial compound and use thereof

The present invention relates to: coralmycin A and B, which are novel compounds exhibiting antimicrobial activity, an isomer thereof, a derivative thereof or a pharmaceutically acceptable salt thereof; a microorganism of the genus Corallococcus producing the same; and an antimicrobial use thereof. The coralmycin A and B have very strong antimicrobial activity against antibiotic-resistant bacteria such as MRSA, QRSA, VRE, VISA, etc.; Acinetobacter baumannii, which is a multidrug-resistant microorganism; and also against gram-positive microorganisms and gram-negative microorganisms. Therefore, the present invention can be very useful for prevention, treatment and alleviation of various microbial infections, and thus can be widely applied to the medical supply, quasi-drug, food, and feed industries.

DP antagonist

An object of the present invention is to provide a DP receptor antagonist. A compound represented by general formula (I): ##STR00001## (wherein all symbols are as shown in the specification) and a pharmaceutically acceptable salt thereof have DP receptor antagonistic activity and are also highly safe, and thus are useful as active ingredients of pharmaceuticals for DP receptor-mediated diseases. In addition, the compound represented by the general formula (I) and the pharmaceutically acceptable salt thereof also have good transferability to the central nervous system, and thus are particularly useful as a preventive and/or therapeutic agent for diseases associated with DP receptors present in the central nervous system among DP receptor-mediated diseases, that is, sleep-wake disorders.

DP antagonist

An object of the present invention is to provide a DP receptor antagonist. A compound represented by general formula (I): ##STR00001## (wherein all symbols are as shown in the specification) and a pharmaceutically acceptable salt thereof have DP receptor antagonistic activity and are also highly safe, and thus are useful as active ingredients of pharmaceuticals for DP receptor-mediated diseases. In addition, the compound represented by the general formula (I) and the pharmaceutically acceptable salt thereof also have good transferability to the central nervous system, and thus are particularly useful as a preventive and/or therapeutic agent for diseases associated with DP receptors present in the central nervous system among DP receptor-mediated diseases, that is, sleep-wake disorders.

HISTONE ACETYLTRANSFERASE MODULATORS AND COMPOSITIONS AND USES THEREOF

Compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.

HISTONE ACETYLTRANSFERASE (HAT) REGULATORS AND USES THEREOF

The invention provides for compounds that are HAT activators or inhibitors. The invention further provides a method for treating neurodegenerative diseases, cancer and other malignant conditions, or to increase memory in a subject not suffering from a neurodegenerative disease by administering HAT activators or inhibitors to a subject in need thereof. The method further comprises co-administration of HD AC inhibitors with HAT activators or HD AC activators with HAT inhibitors.

Compounds and methods for inhibiting viral replication and methods of treating and preventing flaviviral infections

The present disclosure relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof. The present disclosure further relates to methods of inhibiting viral replication including contacting one or more cells that have been infected with a virus with an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein the virus comprises a flavivirus. Also disclosed is a method of treating and/or preventing a flavivirus infection and/or a condition resulting from a flavivirus infection including administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof under conditions effective to treat and/or prevent a flavivirus infection and/or a condition resulting from a flavivirus infection.

COMPOUNDS AND METHODS FOR INHIBITING VIRAL REPLICATION AND METHODS OF TREATING AND PREVENTING FLAVIVIRAL INFECTIONS
20220024884 · 2022-01-27 ·

The present disclosure relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof. The present disclosure further relates to methods of inhibiting viral replication including contacting one or more cells that have been infected with a virus with an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein the virus comprises a flavivirus. Also disclosed is a method of treating and/or preventing a flavivirus infection and/or a condition resulting from a flavivirus infection including administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof under conditions effective to treat and/or prevent a flavivirus infection and/or a condition resulting from a flavivirus infection.

Selective androgen receptor degrader (SARD) ligands and methods of use thereof

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including cyclic and heterocyclic anilide rings and their synthetic precursors, and mono-, di-, or multi-substituted N-heterocyclic rings, R-isomers, non-hydroxylated and/or non-chiral propanamides in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.