C07J63/008

C4-modified oleanolic acid derivatives for inhibition of IL-17 and other uses

Disclosed herein are C4 modified oleanolic acid derivatives of the formula: Formula (X) or Formula (XII), 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. ##STR00001##

Natural and synthetic compounds for treating cancer and other diseases
11485755 · 2022-11-01 ·

This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, spleenic, kidney, lymphatic, pancreatic, stomach and thyroid cancers. This invention is an anti-adhesion therapy which uses the compound as a mediator or inhibitor of adhesion proteins and angiopoietins. It inhibits excess adhesion and inhibits cell attachment. It modulates angiogenesis. The compounds also use as mediator of cell adhesion receptor, cell circulating, cell moving and inflammatory diseases. The compounds are attached with angeloyl, acetyl, tigloyl, senecioyl, Crotonoyl, 3,3-Dimethylacryloyl, Cinnamoyl, Pentenoyl, Hexanoyl, benzoyl, Ethylbutyryl, benzoyl, dibenzoyl, alkanoyl, alkenoyl, benzoyl alkyl substituted alkanoyl, ethanoyl, propanoyl, propenoyl, butanoyl, butenoyl, pentanoyl, hexenoyl, heptanoyl, heptenoyl, octanoyl, octenoyl, nonanoyl, nonenoyl, decanoyl, decenoyl, propionyl, 2-propenoyl, 2-butenoyl, Isobutyryl, 2-methylpropanoyl, 2-ethylbutyryl, ethylbutanoyl, 2-ethylbutanoyl, butyryl, (E)-2,3-Dimethylacryloyl, (E)-2-Methylcrotonoyl, 3-cis-Methyl-methacryloyl, 3-Methyl-2-butenoyl, 3-Methylcrotonoyl, 4-Pentenoyl, (2E)-2-pentenoyl, Caproyl, 5-Hexenoyl, Capryloyl, Lauroyl, Dodecanoyl, Myristoyl, Tetradecanoyl, Oleoyl, O—C(2-18) Acyl.

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Provided herein is a compound of Formula (1-I): or a pharmaceutically acceptable salt thereof, wherein R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.6b, R.sup.11a, R.sup.11b, R.sup.16a, R.sup.16b, R.sup.19, R.sup.18, X, q, r, s, t, u, and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (1-I) and methods of using the compounds, e.g, in the treatment of CNS-related disorders.

##STR00001##

SAPONIN CONJUGATE AND VACCINE OR PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
20220323578 · 2022-10-13 ·

The present invention is directed to novel chemical compounds in which a lipophilic moiety such as a lipid, fatty acid, polyethylene glycol or terpene is covalently attached to a non-acylated or desacylated triterpene saponin via a carboxyl group present on the 3-O-glucuronic acid of the triterpene saponin. The attachment of a lipophile moiety to the 3-O-glucuronic acid of a saponin such as Quillaja desacylsaponin, lucyoside P, or saponin from Gypsophila, Saponaria and Acanthophyllum enhances their adjuvant effects on humoral and cell mediated immunity. Additionally, the attachment of a lipophile moiety to the 3-O-glucuronic acid residue of non- or des-acylsaponin yields a saponin analog that is easier to purify, less toxic, chemically more stable, and possesses equal or better adjuvant properties than the original saponin.

TRITERPENOID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR USE FOR TREATING A NUCLEAR RECEPTOR SUBFAMILY 4 GROUP A MEMBER 1-MEDIATED DISEASE

Disclosed herein are triterpenoid compounds, for example, a compound of Formula (I), and pharmaceutical compositions thereof. Also disclosed herein are methods of their use for treat.

##STR00001##

Triterpene saponin variants, methods of synthesis and use thereof

A number of triterpene saponin variants with different modifications on their central glycosyl ester linkage are described. Also described are methods of making and method of using such triterpene saponin variants.

Betulastatin compounds

The present disclosure relates to Betulastatin compounds, pharmaceutical compositions and kits comprising such compounds, and methods for using such compounds or pharmaceutical compositions.

APPLICATIONS OF AMIDE ANALOGS OF TRITERPENES IN CURES OF CANCER AND OTHER DISEASES
20230159436 · 2023-05-25 ·

This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, splenic, kidney, lymphatic, pancreatic, stomach, eye and thyroid cancers. The active compounds are amine, sulfonamides, amide, and urea analogs of triterpene.

SYNTHETIC TRITERPENOIDS WITH NITROGEN-BASED SUBSTITUENTS AT C-17 AND METHODS OF USE THEREOF

In some aspects, the present disclosure provides compounds of the formula: (I) and (II), wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used as antioxidant inflammation modulators. In some aspects, the present disclosure provides methods wherein the compounds and composition described herein are used for the treatment of diseases and disorders associated with inflammation and cancer.

##STR00001##

Triterpenoids with HIV maturation inhibitory activity

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: ##STR00001##
with X selected from C.sub.4-8 cycloalkyl, C.sub.4-8 cycloalkenyl, C.sub.4-9 spirocycloalkyl, C.sub.4-9 spirocycloalkenyl, C.sub.4-8 oxacycloalkyl, C.sub.4-8 dioxacycloalkyl, C.sub.6-8 oxacycloalkenyl, C.sub.6-8 dioxacycloalkenyl, C.sub.6 cyclodialkenyl, C.sub.6 oxacyclodialkenyl, C.sub.6-9 oxaspirocycloalkyl and C.sub.6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C.sub.1-6 alkyl-halo. These compounds are useful for the treatment of HIV and AIDS.