C07F9/6503

Substituted bicyclic compounds

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): ##STR00001##
and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

BICYCLIC HETEROARYL DERIVATIVES AS ECTONUCLEOTIDE PYROPHOSPHATASE PHOSPHODIESTERASE 1 INHIBITORS
20250041319 · 2025-02-06 ·

The present disclosure provides certain bicyclic heteroaryl compounds that inhibit ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) enzymatic activity and are therefore useful for the treatment of diseases and conditions modulated at least in part by ENPP1. In some embodiments, the bicyclic heteroaryl compounds includes those of Formula (I):

##STR00001##

Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Neprilysin inhibitors
09670140 · 2017-06-06 · ·

In one aspect, the invention relates to compounds having the formula XII: ##STR00001##
where R.sup.a, R.sup.b, R.sup.2, R.sup.7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

Phosphine ligands for catalytic reactions

The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions.

QUINOLINE cGAS ANTAGONIST COMPOUNDS

The present disclosure provides compounds that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

PROCESS

The present disclosure generally relates to methods of synthesizing compounds useful as modulators of hepatitis B virus core protein assembly as well as novel synthetic intermediates. The methods disclosed may be used in the manufacture of compounds which may have allosteric effector properties against hepatitis B virus (HBV) core protein (Cp), a protein found as a dimer, a multimer, and as the protein shell of the HBV core. As one example, provided herein is a process for preparing compounds which may be useful for treating viral infections, such as hepatitis B.

FORMULATIONS COMPRISING N-SUBSTITUTED-DIOXOCYCLOBUTENYLAMINO-3-HYDROXY-PICOLINAMIDE COMPOUNDS AND USES THEREOF

The present disclosure relates to compositions comprising N-substituted-dioxocyclobutenylamino-3-hydroxy-picoliamide compounds or a pharmaceutically acceptable salt or hydrate thereof, methods of preparing said compositions, and uses thereof. The compositions may be useful in the treatment of conditions ameliorated by inhibition of CC chemokine receptor 6.

PHOSPHORUS COMPOUND AND USE THEREOF

The present invention relates to a phosphorus compound and the use thereof. Specifically, provided in the present invention is a compound of formula (I), or an optical isomer, racemate, solvate, pharmaceutically acceptable salt or deuterated compound thereof. The compound of the present invention has significant and excellent precision treatment effects on tumors that have low expression, no expression, low activity or no activity of mitochondrial permeability transition pores, low expression, no expression, low activity or no activity of peptidyl prolyl isomerase F, low expression or no expression of NNMT gene, high expression of DNA methylase, high expression of UHRFI, high methylation level at a nucleotide site in NNMT gene, and/or high methylation level of DNA at CpG site in NNMT gene region.

##STR00001##

Compounds for treating conditions related to oxidative stress
12459900 · 2025-11-04 ·

Disclosed herein are compounds for treating conditions related to oxidative stress/damage among other causes, with pharmaceutically accepted salts hydrate, solvate, optical isomer, or combination thereof, comprising lipophilic cation moieties linked to heterocyclics compounds of formula (I) and formula (8); ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may be selected from the group consisting of ##STR00002##
wherein X, Y, and Z are selected from the group consisting of H, methyl, ethyl, propyl, butyl, substituted or unsubstituted aryl, and heteroaryls; n is an integer selected from 0-18, and E is a phosphorous or nitrogen atom.

INHIBITORS OF MYC AND USES THEREOF
20260035360 · 2026-02-05 ·

Disclosed are substituted heterocyclic compounds and proteolysis-targeting chimeric molecules (PROTACs). The substituted heterocycles disclosed herein are shown to be useful in inhibiting c-MYC. The disclosed PROTACs are shown to induce degradation of c-MYC protein. The substituted heterocyclic compounds and proteolysis-targeting chimeric molecules (PROTACs) disclosed, herein may be utilized as therapeutics for treating cancer and cell proliferative disorders.