The present invention relates to compound of Formula I or a pharmaceutically acceptable salt thereof

##STR00001## wherein R.sup.1 is

##STR00002##

where the squiggly line indicates the point of attachment to the rest of the molecule; R.sup.2 is F or

##STR00003##

where the squiggly line indicates the point of attachment to the rest of the molecule; R.sup.3 is H or CH.sub.3; Z is O or is absent; and R.sup.4 is —OC.sub.1-3alkyl, C.sub.1-30alkyl, or —N(CH.sub.3).sub.2.

The present invention relates to fluorinated and alkylated bile acids.

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.

Substantially pure saponin extracts and orthogonal chromatographic methods for purification of saponin extracts are disclosed. The purified saponin extracts may include QS-21 and can have a purity of greater than 97%. The orthogonal chromatographic method uses reversed-phase (RP) chromatography followed by hydrophilic interaction liquid chromatography (HILIC) to generate substantially pure saponin extracts.

Described herein, inter alia, are compositions and methods for treating or preventing obesity and using the same.

The present disclosure relates to an ester derivative prodrug of inotodiol and use thereof. The prodrug not only has increased solubility with respect to an inorganic solvent and an organic solvent, but also has improved stability, and thus can be used in the treatment of various inflammatory diseases, including inflammatory diseases or allergic diseases.

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.

The invention relates to a saponin derivative based on a saponin comprising a triterpene aglycone and a first saccharide chain and/or a second saccharide chain, and comprising: an aglycone core structure comprising an aldehyde group which has been derivatised; and/or the first saccharide chain wherein the first saccharide chain comprises a carboxyl group, which has been derivatised; and/or the second saccharide chain wherein the second saccharide chain comprises at least one acetoxy group which has been derivatised. The invention also relates to a first pharmaceutical composition comprising the saponin derivative of the invention. In addition, the invention relates to a pharmaceutical combination comprising the first pharmaceutical composition of the invention and a second pharmaceutical composition comprising any one or more of an antibody-toxin conjugate, a receptor-ligand—toxin conjugate, an antibody-drug conjugate, a receptor-ligand—drug conjugate, an antibody-oligonucleotide conjugate or a receptor-ligand—oligonucleotide conjugate. The invention also relates to the first pharmaceutical composition or the pharmaceutical combination of the invention, for use as a medicament, or use in the treatment or prophylaxis of a cancer, an infectious disease, viral infection, hypercholesterolemia, primary hyperoxaluria, haemophilia A, haemophilia B, alpha-1 antitrypsin related liver disease, acute hepatic porphyria, transthyretin-mediated amyloidosis, or an auto-immune disease. Furthermore, the invention relates to an in vitro or ex vivo method for transferring a molecule from outside a cell to inside said cell, comprising contacting said cell with the molecule and with a saponin derivative of the invention.

The present disclosure relates to synthetic triterpenoids, methods for preparing such synthetic triterpenoids, and methods of using such synthetic triterpenoids to treat and/or prevent diseases or disorders such as cancers, particularly brain tumors, neuropsychiatric disorders, and neurodegenerative diseases.

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 and thyroid cancers. This invention provides compounds and compositions for up regulating levels of biomarker of Death Receptors including DR1, DR4 and DR5 or alike thereof, for the treatment of cancer and inhibition of cancer cell growth in a subject, and up regulating levels of biomarker of said Death Receptors in cells for the inhibition of cell growth. This invention is an anti-adhesion therapy which uses the compound as a mediator or inhibitor of adhesion proteins and angiopoietins, inhibiting excess adhesion and cell attachment. It modulates angiogenesis. The compounds are also used as mediators of cell adhesion receptor, cell circulating, cell moving and inflammatory diseases.