C07C205/43

PHOTO-CLEAVABLE PRIMER COMPOSITIONS AND METHODS OF USE

In one embodiment, the present application discloses a photo-cleavable surface binding compound of the Formula I and Formula II:

##STR00001##

wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound.

Small Molecules That Covalently Modify Transthyretin
20170190660 · 2017-07-06 ·

A family of covalent kinetic stabilizer compounds that selectively and covalently react with the prominent plasma protein transthyretin in preference to more than 4000 other human plasma proteins is disclosed. A contemplated compound corresponds in structure to Formula I, below, where the various substituents are defined within, and

##STR00001##

reacts chemoselectively with one or two of four Lys-15 -amino groups within the transthyretin tetramer. The crystal structure confirms the binding orientation of the compound substructure and the conjugating amide bond. A covalent transthyretin kinetic stabilizer exhibits superior amyloid inhibition potency, compared to a non-covalent counterpart, and inhibits cytotoxicity associated with amyloidogenesis.

Small Molecules That Covalently Modify Transthyretin
20170190660 · 2017-07-06 ·

A family of covalent kinetic stabilizer compounds that selectively and covalently react with the prominent plasma protein transthyretin in preference to more than 4000 other human plasma proteins is disclosed. A contemplated compound corresponds in structure to Formula I, below, where the various substituents are defined within, and

##STR00001##

reacts chemoselectively with one or two of four Lys-15 -amino groups within the transthyretin tetramer. The crystal structure confirms the binding orientation of the compound substructure and the conjugating amide bond. A covalent transthyretin kinetic stabilizer exhibits superior amyloid inhibition potency, compared to a non-covalent counterpart, and inhibits cytotoxicity associated with amyloidogenesis.

Industrial process for making an Ivacaftor and its intermediates

The present invention relates to an improved process for the preparation of Ivacaftor intermediates. The present invention is also provides industrial applicable, commercially and eco-friendly viable process for the preparation of Ivacaftor.

Industrial process for making an Ivacaftor and its intermediates

The present invention relates to an improved process for the preparation of Ivacaftor intermediates. The present invention is also provides industrial applicable, commercially and eco-friendly viable process for the preparation of Ivacaftor.

PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

The invention provides a process for the preparation of a compound of Formula 1,

##STR00001##

comprising coupling a carboxylic acid of Formula 2

##STR00002##

with an aniline of Formula 3

##STR00003##

in the presence of a coupling agent.

Industrial Process for Making an Ivacaftor and its Intermediates

The present invention relates to an improved process for the preparation of Ivacaftor intermediates. The present invention is also provides industrial applicable, commercially and eco-friendly viable process for the preparation of Ivacaftor

Industrial Process for Making an Ivacaftor and its Intermediates

The present invention relates to an improved process for the preparation of Ivacaftor intermediates. The present invention is also provides industrial applicable, commercially and eco-friendly viable process for the preparation of Ivacaftor

Trialkyne Linking Agents and Methods of Use

Described are improved linking agents that are useful for facilitating the attachment of targeting groups, pharmacokinetic (PK) enhancers or modifiers, or other delivery agents to oligonucleotides. The described linking agents may exhibit improved reaction yields, stability, and biological activity, particularly when used in connection with oligonucleotide-based compounds, such as RNA interference (RNAi) agents.

Xanthine oxidase inhibitors and methods of use

Small molecule xanthine oxidase inhibitors are provided, as well as compositions, methods for their use for treating disorders, mediated at least in part, by xanthine oxidase.