C07J71/00

TACCALONOLIDE MICROTUBULE STABILIZERS

This present disclosure relates to the fields of medicine and pharmaceuticals. In particular, the invention relates to the identification of epoxytaccalonolide microtubule stabilizers for use in inhibiting cell proliferation and disrupting normal cellular microtubule processes leading to cell death. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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.

Cyclopentanoperhydrophenanthrene framework compounds and preparation method therefor

The present invention pertains to the field of pharmaceutical chemistry, and relates to compounds having cyclopentanoperhydrophenanthrene skeletons and preparation methods therefore. The compounds have some physiological activity, and are useful as synthons/intermediates for further synthesizing some compounds having specific structures. These compounds and salts thereof are useful as lead compounds for synthesizing pharmaceuticals, pesticides and new materials. From this, further screen and preparation by chemical, biological and medical means offer new compounds that are more valuable and have important applications, achieving the object of inventing and creating new drugs.

Phosphate based linkers for intracellular delivery of drug conjugates

Phosphate-based linkers with tunable stability for intracellular delivery of drug conjugates are described. The phosphate-based linkers comprise a monophosphate, diphosphate, triphosphate, or tetraphosphate group (phosphate group) and a linker arm comprising a tuning element and optionally a spacer. A payload is covalently linked to the phosphate group at the distal end of the linker arm and the functional group at the proximal end of the linker arm is covalently linked to a cell-specific targeting ligand such as an antibody. These phosphate-based linkers have a differentiated and tunable stability in blood vs. an intracellular environment (e.g. lysosomal compartment).

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
20200024303 · 2020-01-23 ·

Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.

Process for preparation of corticosteroids

The present invention discloses a process for the preparation of pregnadiene derivatives having formula I, their stereoisomer and intermediate thereof. Formula I wherein each substituent is independently, R.sub.1 and R.sub.2 is hydrogen or C.sub.1-C.sub.8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl; R.sub.3 is hydrogen or wherein R.sub.5 represents C.sub.1-C.sub.8 straight, branched alkyl chain or cycloalkyl; R.sub.4 is hydrogen or halogen; R.sub.6 is hydrogen or halogen; ##STR00001##

STEROIDS AND PROTEIN-CONJUGATES THEREOF
20240101594 · 2024-03-28 ·

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

Method for producing biogas from waste liquid/residue after diosgenin extraction from <i>Dioscorea composita </i>by aluminum chloride

Disclosed is a method for producing biogas from a waste liquid/residue after diosgenin extraction by aluminum chloride. Specifically, in a fermentation vessel, an anaerobic sludge and a waste residue from diosgenin extraction by aluminum chloride are added at a volatile solids ratio of (1-3):(1-2), or a seeding sludge and a diosgenin waste liquid are added with an organic loading having a VS:COD ratio of (1-2):(1-2); and then the above components are fermented at 35-37 C. for 5-25 d such that biogas is produced. According to the method of the present invention, the maximum cumulative biogas production rates are 255.4 mL/g VS for waste residue and 326.9 mL/g COD for waste liquid, and throughout the fermentation period, ammoniacal nitrogen values are below 1500 mg/L and pH variation is within the normal range, and the COD removal rate for the fermentation broth is 91.11%.

PHENYL MALEIMIDE LINKER AGENTS

Compounds useful as linker-payload compounds are disclosed. The compounds have the following Structure (I):

##STR00001##

as a stereoisomer, enantiomer or tautomer thereof or a mixture thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, R.sup.4a, and R.sup.4b are as defined herein. Additional compounds, conjugates, methods of preparation, pharmaceutical compositions, and methods of treatment related to conjugates of compounds of Structure (I) and a targeting moiety, or binding fragment thereof, are also provided.

NOVEL SALTS AND POLYMORPHS OF SCY-078
20190359648 · 2019-11-28 · ·

SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078.