C07D215/42

2-quinolone derived inhibitors of BCL6

The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: Formula I wherein X.sub.1, X.sub.2, X.sub.3, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated. ##STR00001##

CARBAMATE COMPOUNDS AND METHODS OF MAKING AND USING SAME

This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.

CARBAMATE COMPOUNDS AND METHODS OF MAKING AND USING SAME

This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.

NITROXOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
20230295094 · 2023-09-21 ·

The present invention discloses a nitroxoline derivative, a preparation method therefor, and use thereof. Specifically, the present discloses a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing same, and use thereof in treating infectious diseases or cancers. The compound of the present invention has excellent anti-tumor activity and antibacterial activity, and can be developed into a drug for treating tumors and infectious diseases. The definition of each group in general formula (I) is the same as that in the description.

##STR00001##

NITROXOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
20230295094 · 2023-09-21 ·

The present invention discloses a nitroxoline derivative, a preparation method therefor, and use thereof. Specifically, the present discloses a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing same, and use thereof in treating infectious diseases or cancers. The compound of the present invention has excellent anti-tumor activity and antibacterial activity, and can be developed into a drug for treating tumors and infectious diseases. The definition of each group in general formula (I) is the same as that in the description.

##STR00001##

Anti-infective and anti-inflammatory compounds

Lysosomally accumulated substances that release a nitroxy group, or a short chain fatty acid or a product of anaerobic metabolism or a thiol or a sulfide often from an ester or similar labile linkage have anti-inflammatory, anti-cancer and anti-bacterial activity. They are useful in treating infectious, inflammatory and malignant disease.

Anti-infective and anti-inflammatory compounds

Lysosomally accumulated substances that release a nitroxy group, or a short chain fatty acid or a product of anaerobic metabolism or a thiol or a sulfide often from an ester or similar labile linkage have anti-inflammatory, anti-cancer and anti-bacterial activity. They are useful in treating infectious, inflammatory and malignant disease.

SMALL MOLECULE INHIBITORS OF ACETYL COENZYME A SYNTHETASE SHORT CHAIN 2 (ACSS2)

The present invention relates to compounds of formula (I). The compounds may be used to modulate the acetyl coenzyme A synthetase short chain.sub.2 (ACSS.sub.2) protein and may thereby treat, ameliorate or prevent a disease selected from cancer, bacterial infection, viral infection, parasitic infection, fungal infection, neurodegenerative disease, neurological disorder, cerebrovascular disease, cardiovascular disease, non-alcoholic fatty liver disease and obesity. Alternatively, or additionally, the compounds may be used to promote healthy ageing. (I)

##STR00001##

PAPD5 INHIBITORS AND METHODS OF USE THEREOF

The present application provides compounds that are PAPD5 inhibitors and are useful in treating a variety of conditions such as cancer, telomere diseases, and aging-related and other degenerative disorders.

PAPD5 INHIBITORS AND METHODS OF USE THEREOF

The present application provides compounds that are PAPD5 inhibitors and are useful in treating a variety of conditions such as cancer, telomere diseases, and aging-related and other degenerative disorders.