C07F9/6503

IMMUNOMODULATOR

Disclosed is a compound capable of inhibiting interleukin 17A (IL-17A), which is represented by formula (I). An application of the compound or a stereoisomer thereof in the preparation of drugs for inhibiting IL-17A is also provided.

##STR00001##

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
20220362266 · 2022-11-17 ·

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

##STR00001##

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.

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.

THERAPEUTIC COMPOUNDS FOR HIV VIRUS INFECTION

The present disclosure relates generally to certain compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions provided herein may be used for the treatment or prevention of a Retroviridae infection, including an HIV infection.

NOVEL BISPHOSPHONIC ACID DERIVATIVE AND APPLICATION FOR SAME

The novel bisphosphonic acid ester derivatives represented by the following formula (1):


Y—Cy—(NH).sub.m—(CH.sub.2).sub.n—C(X)(PO(OR.sup.1)(OR.sup.2)).sub.2   (1)

wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.

NOVEL BISPHOSPHONIC ACID DERIVATIVE AND APPLICATION FOR SAME

The novel bisphosphonic acid ester derivatives represented by the following formula (1):


Y—Cy—(NH).sub.m—(CH.sub.2).sub.n—C(X)(PO(OR.sup.1)(OR.sup.2)).sub.2   (1)

wherein each symbol is as defined in the DESCRIPTION, which has an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom, and the acid moiety is esterified with a POM group, an n-butanoyloxymethyl (BuOM) group and the like, exhibit a superior direct or indirect cytotoxicity effect on tumor cells and virus infected cells.

GDF-8 Inhibitors

Described are GCF-8 inhibitors of the formula (I),

##STR00001##

and pharmaceutically acceptable salts thereof, wherein n, R.sup.1, R.sup.2, R.sup.5, R.sup.6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.

Antibacterial 2H-indazole derivatives

The invention relates to antibacterial compounds of formula I ##STR00001##
wherein R.sup.1 is H or halogen; R.sup.2 is alkynyloxy or the group M; R.sup.3 is H or halogen; M is one of the groups ##STR00002##
wherein A is a bond, CH.sub.2CH.sub.2, CH═CH or C≡C and R.sup.1A, R.sup.2A, R.sup.3A, R.sup.1B and R.sup.1C are as defined in claim 1;
and salts thereof.