C07D417/04

Inhibitors of Beta-Hydroxylase for Treatment of Cancer
20180009798 · 2018-01-11 ·

The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

Inhibitors of Beta-Hydroxylase for Treatment of Cancer
20180009798 · 2018-01-11 ·

The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

HETEROCYCLE-SUBSTITUTED BICYCLIC AZOLE PESTICIDES

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof,

##STR00001##

wherein

Q is

##STR00002##

and A, R.sup.1, m, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Y.sup.1, Y.sup.2 and Y.sup.3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.

HETEROCYCLE-SUBSTITUTED BICYCLIC AZOLE PESTICIDES

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof,

##STR00001##

wherein

Q is

##STR00002##

and A, R.sup.1, m, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Y.sup.1, Y.sup.2 and Y.sup.3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.

Resorcinol Derivative As HSP90 Inhibitor

The present invention relates to a compound represented by formula (I) of a resorcinol derivative as an HSP90 inhibitor or pharmaceutically accepted salts thereof. The compound in the present invention has the activity of inhibiting heat shock protein HSP90. Therefore, the compound in the present invention is used to treat proliferative diseases such as cancer and neurodegenerative diseases. The present invention further provides the compounds and preparation methods for pharmaceutical compositions comprising the compounds, a method for treating diseases, and pharmaceutical compositions comprising the compounds.

##STR00001##

Resorcinol Derivative As HSP90 Inhibitor

The present invention relates to a compound represented by formula (I) of a resorcinol derivative as an HSP90 inhibitor or pharmaceutically accepted salts thereof. The compound in the present invention has the activity of inhibiting heat shock protein HSP90. Therefore, the compound in the present invention is used to treat proliferative diseases such as cancer and neurodegenerative diseases. The present invention further provides the compounds and preparation methods for pharmaceutical compositions comprising the compounds, a method for treating diseases, and pharmaceutical compositions comprising the compounds.

##STR00001##

Heteroaromatic compounds having activity against RSV

The invention concerns compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection. ##STR00001##

HIGH PENETRATION COMPOSITIONS AND THEIR APPLICATIONS
20230233516 · 2023-07-27 · ·

The invention provides compositions or pharmaceutical compositions of novel high penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. For example, HPCs of NSAIA have demonstrated indications such as treating hair loss and bold. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

HIGH PENETRATION COMPOSITIONS AND THEIR APPLICATIONS
20230233516 · 2023-07-27 · ·

The invention provides compositions or pharmaceutical compositions of novel high penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. For example, HPCs of NSAIA have demonstrated indications such as treating hair loss and bold. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

COMPOUNDS FOR MODULATING S1P1 ACTIVITY AND METHODS OF USING THE SAME

The present embodiments are directed, in part, to compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of S.sub.1P.sub.1 receptor and methods of using the same.