C07D261/20

ANTIOXIDANT INFLAMMATION MODULATORS: OLEANOLIC ACID DERIVATIVES WITH AMINO AND OTHER MODIFICATIONS AT C-17

This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula:

##STR00001##

wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Substituted benzofuran, benzopyrrole, benzothiophene, and structurally related complement inhibitors

Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity. ##STR00001##

Substituted benzofuran, benzopyrrole, benzothiophene, and structurally related complement inhibitors

Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity. ##STR00001##

INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Compounds of formula (I) wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b and R.sup.5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Compounds of formula (I) wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b and R.sup.5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

TRPM8 MODULATORS

Disclosed are TRPM8 modulators as defined by formula (I) for achieving a cooling effect on skin and mucousa.

BENZOTHIOPHENE DERIVATIVE REGULATOR, PREPARATION METHOD THEREFOR AND USE THEREOF
20230002364 · 2023-01-05 ·

A nitrogen-containing ring derivative regulator, a preparation method therefor and use thereof. In particular, the present invention relates to a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a G protein-coupled receptor regulator in the treatment or prevention of central nervous system diseases and/or mental diseases.

##STR00001##

Benzisoxazole compound

The present invention provides a compound, a salt thereof, or a prodrug thereof as a compound effective for preventing and/or treating fibrosis, the compound being represented by formula (1) ##STR00001##
(wherein A is an optionally substituted benzene ring; B is optionally substituted aryl or optionally substituted heteroaryl; X is an oxygen atom or a sulfur atom; Y is a nitrogen atom or a carbon atom; custom character of custom characterY is a single or double bond when Y is a carbon atom, or custom character of custom characterY is a single bond when Y is a nitrogen atom; each R.sup.1 independently represents lower alkyl, or two R.sup.1s may be bound to each other to form a spiro ring or a crosslinked structure, or two R.sup.1s may be bound to each other to form a saturated fused heterocycle together with nitrogen and carbon atoms constituting a ring containing Y; p is 0, 1, or 2; or (R.sup.1).sub.p is oxo).

Benzisoxazole compound

The present invention provides a compound, a salt thereof, or a prodrug thereof as a compound effective for preventing and/or treating fibrosis, the compound being represented by formula (1) ##STR00001##
(wherein A is an optionally substituted benzene ring; B is optionally substituted aryl or optionally substituted heteroaryl; X is an oxygen atom or a sulfur atom; Y is a nitrogen atom or a carbon atom; custom character of custom characterY is a single or double bond when Y is a carbon atom, or custom character of custom characterY is a single bond when Y is a nitrogen atom; each R.sup.1 independently represents lower alkyl, or two R.sup.1s may be bound to each other to form a spiro ring or a crosslinked structure, or two R.sup.1s may be bound to each other to form a saturated fused heterocycle together with nitrogen and carbon atoms constituting a ring containing Y; p is 0, 1, or 2; or (R.sup.1).sub.p is oxo).

COMPOUNDS FOR THE TREATMENT OF PARAMYXOVIRUS VIRAL INFECTIONS

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).