C07J71/00

METHOD FOR THE SEPARATION OF THE ISOPRENIC CONSTITUENTS OF GUAYULE

Method for the separation of at least one isoprenic constituent from the resin of a plant of guayule and/or of the guayule type comprising the steps of: a) providing a defatted resin of guayule and/or of the guayule type; b) subjecting the defatted resin to partitioning of the liquid-liquid type with solvents that are immiscible in each other thus obtaining an apolar extract containing the isoprenic constituents guayulin A, guayulin B and argentatin B; and a polar extract containing the isoprene constituents argentatin A, argentatin C and argentatin D; and c) separating at least one isoprenic constituent from said polar extract and/or from the apolar extract thus obtained, wherein step c) comprises a step in which the polar extract is subjected to partitioning of the liquid-liquid type with solvents immiscible in each other and/or a step in which the apolar extract is subjected to partitioning of the solid-liquid type.

Method for preparing substituted 3,7-dihydroxy steroids
09994608 · 2018-06-12 · ·

The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S,10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17-ethynyl-androst-5-ene-3,7,17-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.

Method for preparing substituted 3,7-dihydroxy steroids
09994608 · 2018-06-12 · ·

The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S,10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17-ethynyl-androst-5-ene-3,7,17-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.

STEROIDS AND PROTEIN-CONJUGATES THEREOF
20180155389 · 2018-06-07 ·

Described herein protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.

PROGESTERONE ANTAGONISTS

Described herein are compounds which either act as pure antiprogestins or as antiprogestins with partial agonistic activity and methods of treating cancer using such compounds.

7-dehydrocholesterol derivatives and methods using same

The present invention provides, in certain aspects, novel 7-dehydrocholesterol (7DHC) derivatives that are useful in treating or preventing cancer, as well as in treating or preventing uncontrolled angiogenesis, in a subject. In certain embodiments of the present invention, the subject is a human. In other aspects, the present invention provides a method of preparing compounds of the invention, or a salt or solvate thereof.

Highly potent glucocorticoids

The present invention relates to novel glucocorticoid compounds. The invention also relates to methods of using these compounds, the synthesis of these compounds, and to compositions and formulations comprising the glucocorticoid compounds, and uses thereof.

CORTISTATIN ANALOGUES AND SYNTHESES AND USES THEREOF

Compounds of Formula (A), (B), (C), (D), (E), (A), (B), (C), (D), (E), (G1), and (G2) are useful as therapeutics for treating a wide variety of conditions in a host such as a human, e.g., including but not limited to, conditions associated with angiogenesis and/or which are mediated by CDK8 and/or CDK19 kinase activity. Also provided are methods of modulating the -catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGF/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using an effective amount of a compound of Formula (A), (B), (C), (D), (E), (A), (B), (C), (D), (E), (G1), or (G2).

C25 R AND S ISOMERS OF AMINOSTEROLS AND METHODS OF MAKING AND USING THE SAME

Compositions of C.sub.25 stereodefined aminosterols and methods of making the same and using the same in therapeutic applications.

Hydrophilic linkers for antibody drug conjugates
12134631 · 2024-11-05 · ·

Described herein protein drug conjugates and compositions thereof that are useful, for example, for the target-specific delivery of drugs to cells. By administering these compounds, compositions, and conjugates as described herein to specific target cells, side-effects due to non-specific binding phenomena, for example, to non-target cells are reduced. In certain embodiments, compounds, compositions, and conjugates are provided, which include hydrophilic residues in linker-payloads and protein conjugates thereof.