C07J63/00

C17-heteroaryl derivatives of oleanolic acid and methods of use thereof

Disclosed herein are novel C17-heteroaryl derivatives of oleanolic acid, including those of 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, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.

GLYCYRRHETINIC ACID DERIVATIVES FOR USE IN TREATING HYPERKALEMIA

The present invention provides a compound of formula (I) or a salt thereof: (Formula (I)) wherein X, L, V, R.sub.1; R.sub.2, R.sub.3 and R.sub.4, are as defined herein. The claimed compounds inhibit the enzyme 11-hydroxysteroid dehydrogenase type 2 (11-HSD2) and as a result are useful in the treatment of hyperkalemia by preventing cortisol from being oxidised to cortisone and thus allowing it to occupy the mineralocorticoid receptor, thus stimulating potassium excretion.

##STR00001##

STEROID COMPOUND, AND USE THEREOF AND PREPARATION METHOD THEREFOR
20220089637 · 2022-03-24 ·

The present invention relates to a steroid compound, a use thereof and a preparation method therefor. It is expected that such compound can effectively treat mental and neurological diseases, and has good active efficacy, pharmacokinetic (PK) performance, oral bioavailability, stability, safety, clearance rate, and/or metabolic performance and the like.

2,2-DIFLUOROPROPIONAMIDE DERIVATIVES OF BARDOXOLONE METHYL, POLYMORPHIC FORMS AND METHODS OF USE THEREOF
20220073559 · 2022-03-10 · ·

The present invention relates generally to the compound: N-((4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicen-4a-yl)-2,2-difluoropropanamide,
polymorphic forms thereof, methods for preparation and use thereof, pharmaceutical compositions thereof, and kits and articles of manufacture thereof.

Triterpene amine derivatives

The present invention concerns novel pharmaceutically active triterpene amine derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the triterpene amine compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C-28 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus-1 (HIV-1).

C-3 AND C-17 MODIFIED TRITERPENOIDS AS HIV-1 INHIBITORS

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I:

##STR00001##

These compounds are useful for the treatment of HIV and AIDS.

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.

Fluorinated and alkylated bile acids

The present invention relates to fluorinated and alkylated bile acids.

C-3 and C-17 modified triterpenoids as HIV-1 inhibitors

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: ##STR00001##
These compounds are useful for the treatment of HIV and AIDS.

TRITERPENE AMINE DERIVATIVES

The present invention concerns novel pharmaceutically active triterpene amine derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the triterpene amine compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C-28 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus-1 (HIV-1).