C07J63/008

METHODS OF CARBON-CARBON BOND FRAGMENTATION
20220169580 · 2022-06-02 ·

The present disclosure relates to methods of carbon-carbon bond fragmentation.

GLYCYRRHETINIC ACID DERIVATIVES FOR TREATING HYPERKALEMIA

The present invention provides a compound of formula (I) or a salt thereof:

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wherein X, L, V, R.sub.1, R.sub.2, R.sub.3 and R.sub.4, are as defined herein.

SAPONIN PURIFICATION

Saponin extracts containing at least 93% QS-21 main peak and 0.25-3% 2018 component by UV absorbance at 214 nm, methods for making said extracts, their use as vaccine adjuvants and related aspects.

METHODS AND COMPOSITIONS FOR IRREVERSIBLE ENZVME INHIBITION
20220160879 · 2022-05-26 ·

The present invention relates to compounds, methods, and compositions for irreversibly inhibiting protein targets, including Keap1 and/or LONP1 protease. In certain aspects, the present invention relates to conjugates and/or cross-linked conjugates comprising a protein or a protein complex and a bifunctional triterpenoid, such as 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-2-yl)-1H-imidazole (“CDDO-2P-Im”), 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-3-yl)-1H-imidazole (“CDDO-3P-Im”), or derivatives thereof.

METHOD FOR PRODUCING A COMPOSITION COMPRISING A 3-O-p-COUMAROYL ESTER OF TORMENTIC ACID FROM A PLANT CELL CULTURE, APPLICATIONS THEREOF AS ANTIPARASITIC AGENT FOR THE TREATMENT OF TRYPANOSOMIASIS

The present invention relates to a method for the production of a (poly)hydroxylated pentacyclic triterpene composition including a 3-O-p-coumaroyl ester of tormentic acid from a plant suspension cell culture, to a pharmaceutical composition comprising at least 3-O-p-coumaroyl ester of tormentic acid for a use in the prevention and/or the treatment of trypanosomiasis, optionally in admixture with other (poly)hydroxylated pentacyclic triterpenes, and to 3-O-p-coumaroyl ester of tormentic acid for its use as an antiparasitic agent for the prevention and/or the treatment of trypanosomiasis, optionally in admixture with other (poly)hydroxylated pentacyclic triterpenes.

SAPONIN-BASED VACCINE ADJUVANTS
20220152196 · 2022-05-19 ·

A number of MS- and natural-saponin-based vaccine adjuvant candidates have been prepared. The MS derivatives were prepared by incorporating a terminal-functionalized side chain into the C3 glucuronic acid unit of the natural saponins MS I and II through amide formation reaction; and the QS analogs were prepared via multi-step organic synthesis. These unnatural saponins showed significantly different immunostimulant activity profiles, suggesting that the structure of side chain, triterpenoid core, and oligosaccharide domain together orchestrate each saponin's characteristic potentiation of immune responses.

NOVEL TRITERPENONE DERIVATIVES AS HIV INHIBITORS

The present invention relates to novel triterpenone derivatives of formula (I); and pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined herein. The invention also relates to novel triterpenone derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.

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COMPOUNDS FOR TREATING CNS DISORDERS

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Provided herein in part is a compound of Formula (I): or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of using the compounds, e.g, in the treatment of CNS- related disorders.

METHODS AND COMPOSITIONS FOR INHIBITING THE NLRP3 INFLAMMASOME AND/OR LON PROTEASE
20220133748 · 2022-05-05 ·

The present invention relates to methods, compositions, and combinations for inhibiting the NLRP3 inflammasome and/or LON protease as well as methods, compositions, and combinations for treating cancer, particularly blood cancer or brain cancer. In certain aspects, the compositions and combinations include a synthetic triterpenoid, such as 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-2-yl)-1H-imidazole (“CDDO-2P-Im”) and 1-[2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl]-4(-pyridin-3-yl)-1H-imidazole (“CDDO-3P-Im”).

C4-MODIFIED OLEANOLIC ACID DERIVATIVES FOR INHIBITION OF IL-17 AND OTHER USES

Disclosed herein are C4 modified oleanolic acid derivatives of the formula:

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as well as analogs thereof, wherein the variables are defined herein. In addition, disclosed herein are pharmaceutical compositions of these derivatives or analogs, methods for their manufacture, and methods for their use, including for the prevention and treatment of diseases or disorders associated with overproduction of IL-17.