C07F9/65586

Polymeric tandem dyes with linker groups
11352502 · 2022-06-07 · ·

Compounds useful as fluorescent or colored dyes are disclosed. In some embodiments, the compounds have the following structure (I): ##STR00001##
or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1, L.sup.2, L.sup.3, L.sup.4, M.sup.1, M.sup.2, m, and n are as defined herein. Methods associated with preparation and use of such compounds is also provided.

HIGH-AFFINITY CU(I) LIGANDS AND METHODS OF USE THEREOF

Several dimethylphosphine sulfide- and phosphine-containing compounds have been discovered that chelate copper(I) with high affinity. In certain embodiments, the compounds can be used to quantify copper(I) in complex biological systems. In another embodiment, the compounds can be used for the treatment of copper(I)-related illnesses and conditions. In still other embodiments, the compounds are ratiometric probes.

PROGRAMMABLE POLYMERIC DRUGS

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L, L.sup.1, L.sup.2, M and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

##STR00001##

Cyclic phosphate substituted nucleoside derivatives for the treatment of liver diseases

The present invention relates to Compounds of Formula (I) or Formula (II): ##STR00001##
or a pharmaceutically acceptable salt, solvate or enantiomer thereof, wherein A, B, R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q and V are as defined herein. The present invention also relates to pharmaceutical compositions comprising a Compound of Formula (I) or Formula (II) and to their use in therapy.

SYNTHESIS OF BACKBONE MODIFIED MORPHOLINO OLIGONUCLEOTIDES AND CHIMERAS USING PHOSPHORAMIDITE CHEMISTRY
20220144867 · 2022-05-12 ·

Amine substituted morpholino oligonucleotides, other than the classical N,N-dimethylamino PMO analogue, and methods of efficiently synthesizing these oligonucleotides with high yield are provided. Morpholino oligonucleotides having thiophosphoramidate, phosphoramidate, and alkyl phosphoramidate linkers. Chimeras containing unmodified DNA/RNA and other analogs of DNA/RNA can be prepared. These oligonucleotides form duplexes with complementary DNA or RNA that are more stable than natural DNA or DNA/RNA complexes, are active with RNAse H1, and may be transfected into cells using standard lipid reagents. These analogues are therefore useful for numerous applications.

Prodrugs of prostate specific membrane antigen (PSMA) inhibitor

Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.

BISPHOSPHONATE-LINKED COMPOUNDS

The present invention concerns novel compounds useful in the treatment of cancer, particularly including compounds linking a bisphosphonate moiety with KBU2046, and pharmaceutically acceptable salts, co-crystals, polymorphs, solvates, hydrates, and enantiomers thereof, as well as methods for their production and pharmaceutical compositions comprising them.

CDK9 Inhibitors and Polymorphs Thereof For Use As Agents For Treatment of Cancer

A crystalline form and/or polymorph of a compound having the following structure (I), including tautomeric and zwitterionic forms thereof, are provided:

##STR00001##

Methods associated with preparation and use of the polymorphs, and pharmaceutical compositions comprising the same are also provided. Also provided are methods for preparing a compound having formula (I), or a salt, tautomer or zwitterionic form thereof.

Functionally-Modified Oligonucleotides And Subunits Thereof
20220127613 · 2022-04-28 ·

Functionally-modified oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.

STAT5 and STAT6 Degraders and Uses Thereof

Described herein are compounds of Formula I and pharmaceutically acceptable salts, solvates, or stereoisomers thereof, as well as their uses as STAT5 and/or STAT6 degraders.