C07D207/08

NOVEL ANNULATION CATALYSTS VIA DIRECT C-H BOND AMINATION

Disclosed are compounds, methods, reagents, systems, and kits for the preparation and utilization of monomeric or polymeric metal-based compounds. These metal-based compounds are organometallic catalysts composed of substituted dipyrrin ligands bound to transition metals. C—H bond functionalization catalysis can be performed with the disclosed organometallic catalysts to yield C—N bonds to generate substituted bicyclic, spiro, and fused nitrogen-containing heterocycles, all common motifs in various pharmaceutical and bioactive molecules.

ORTHO-PHTHALALDEHYDE CONTAINING LINKERS AND USE FOR PREPARATION OF ANTIBODY-DRUG CONJUGATE
20220017462 · 2022-01-20 ·

Provided herein are novel ortho-Phthalaldehyde (OPA) containing linkers (OPA-L) and the use of OPA-L for the preparation of Antibody-drug conjugate (ADC) via the formation of Phthalimidine through the reaction of primary amine on antibody (e.g., residue of Lysine) and ortho-Phthalaldehyde. The advantage of this OPA-L is high reactivity and can be applied in different types of antibodies to form stably-linked conjugates. The use of OPA-L for the preparation of ADC is advantageous for mild and wide condition of conjugation, for instance, low percentage of organic solvent required, wide range of pH and temperature can be used.

Synthesis of 1:1:1 co-crystal of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(β-D-glucopyranos-1-yl)-benzene, L-proline and water

The invention relates to a process for the manufacture of the crystalline compound according to formula (I) comprising the steps (a) deacetylating the final intermediate (FI), (b) forming the crystalline compound according to formula (I) by reacting the deacetylated final intermediate of step (a) with L-proline and water and isolating the final reaction product; processes of manufacturing intermediates thereof; process intermediates and their uses in the processes according to the present invention.

SPECIFIC CONJUGATION LINKERS, SPECIFIC IMMUNOCONJUGATES THEREOF, METHODS OF MAKING AND USES SUCH CONJUGATES THEREOF

The present invention relates to novel linkers containing a 2,3-disubstituted succinic group, or 2-monosubstituted, or 2,3-disubstituted fumaric or maleic (trans (E)- or cis (Z)-butenedioic), or acetylenedicarboxyl group for conjugation of a cytotoxic agent, and/or one or more different functional molecules per linker to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule specifically. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

Chemotherapeutic oxazolone derivatives and pharmaceutical compositions thereof

Cytotoxic compounds containing a phenyl core, amide link(s), an imidazolinone or a propenamide moiety. Also described are pharmaceutical compositions incorporating the cytotoxic compounds and methods for treating cancer. These compounds are cytotoxic against breast, prostate, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.

METHODS FOR SEPARATION AND RECOVERY OF RARE EARTH ELEMENTS FROM AQUEOUS SOLUTIONS USING DIGLYCOLAMIDE DERIVATIVES

A method for extracting rare earth elements from aqueous solution, comprising: (i) acidifying an aqueous solution containing said rare earth elements with an inorganic acid to result in an acidified aqueous solution containing said rare earth elements and containing the inorganic acid in a concentration of 1-12 M, wherein said rare earth elements are selected from lanthanides, actinides, or combination thereof, and (ii) contacting the acidified aqueous solution with an aqueous-insoluble hydrophobic solution comprising a rare earth extractant compound dissolved in an aqueous-insoluble hydrophobic solvent to result in extraction of one or more of the rare earth elements into the aqueous-insoluble hydrophobic solution by binding of the rare earth extractant compound to the one or more rare earth elements, wherein the rare earth extractant compound has the following structure:

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provided that at least one of the conditions (a)-(d) applies.

Farnesoid X receptor agonists and uses thereof

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

Farnesoid X receptor agonists and uses thereof

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

Compositions for treating neurodegenerative diseases

The present disclosure relates to novel compounds, and pharmaceutical compositions thereof, useful for treating for treating neurodegenerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed. Representative members of these compounds include: ##STR00001##

Compositions for treating neurodegenerative diseases

The present disclosure relates to novel compounds, and pharmaceutical compositions thereof, useful for treating for treating neurodegenerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed. Representative members of these compounds include: ##STR00001##