Patent classifications
C07F9/65616
PROCESSES FOR THE PREPARATION OF AMORPHOUS TENOFOVIR ALAFENAMIDE HEMIFUMARATE AND A PREMIX THEREOF
An amorphous form of tenofovir alafenamide hemifumarate and process for the preparation of the same. A premix of amorphous tenofovir alafenamide hemifumarate with pharmaceutically acceptable excipients and process for the preparation of the same are also disclosed.
NOVEL 3' END CAPS, 5' END CAPS AND COMBINATIONS THEREOF FOR THERAPEUTIC RNA
The disclosure relates to nucleic acids that contain modifications at the 5′-end, 3′-end or 5′-end and 3′-ends, and compounds that can be used to make the modified nucleic acids are disclosed. The modified nucleic acids have improved expression, lower immunogenicity and improved stability compared to unmodified nucleic acids.
Oligonucleotides for treating expanded repeat diseases
The invention provides for a method for selectively reducing the expression of a mutant mRNA and/or protein having an expanded nucleotide repeat relative to a wild-type mRNA, comprising contacting a cell with an antisense oligonucleotide of sufficient length and complementarity to the expanded nucleotide repeat. More particularly it relates to selectively reducing the expression of mutant Huntington protein associated with Huntington's disease. The antisense oligonucleotide comprising either a nucleotide or a repeated three nucleotide sequence as defined in the claims.
Bridged-cyclo-ProTides as prodrugs of therapeutic nucleosides and nucleotides
Provided herein are bridged cyclic phosphates and phosphoramidates (bc-ProTides) of nucleosides, which is a compound, its stereoisomers, isotope-enriched analogs, pharmaceutically acceptable salts, hydrates, solvates, or crystalline or polymorphic forms thereof, with the following structure: ##STR00001##
These compounds can be used for the treatment of viral infections and/or neoplastic diseases in mammals. By optimizing combinations of Y.sub.2, Y.sub.3, R.sup.0, and M, the cleavability of these compounds as prodrugs can be attuned for different tissue targeting with various functional combinations. Also disclosed are processes and methods for preparation of these compounds.
Reversible chemoenzymatic labeling of native and fusion carrier protein motifs
Provided herein, inter alia, are methods and compositions for removing a phosphopantethiene analog moiety from an ACP-phosphopantetheine conjugate thereby providing Apo-ACP proteins.
METHODS FOR THE MONO-AMIDATION OF PHOSPHATES AND PHOSPHONATES
Provided is a method for the preparation of mono-amidated phosphates or phosphonates as well as mono-amidated phosphates and phosphonates prepared by such method.
METHODS FOR THE PREPARATION OF RIBOSIDES
- Steven Donald Axt ,
- Pavel Robertovich Badalov ,
- Katrien Brak ,
- Silvio Campagna ,
- Andrei Chtchemelinine ,
- Edward Doerffler ,
- Morin Mae Frick ,
- Detian Gao ,
- Lars V. Heumann ,
- Brittanie Hoang ,
- Willard Lew ,
- Robert Ronald MILBURN ,
- Sean Timothy Neville ,
- Bruce Ross ,
- Erik Rueden ,
- Robert William Scott ,
- Dustin Siegel ,
- Andrew C. Stevens ,
- Clarissa Tadeus ,
- Tiago Vieira ,
- Andrew W. Waltman ,
- Xianghong Wang ,
- Mark Charles Whitcomb ,
- Lydia Wolfe ,
- Chia-Yun Yu
Provided are methods of preparing compounds and pharmaceutical compositions for treating Filoviridae virus infections The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
ADENOSINE RECEPTOR ANTAGONISTS AND USES THEREOF
Disclosed herein are compounds, compositions, formulations, and methods for modulating the A.sub.2B adenosine receptor.
Functionally-modified oligonucleotides and subunits thereof
Functionally-modified oligonucleotide analogs 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.
Modulators of 5′-nucleotidase, ecto and the use thereof
Compounds that modulate the conversion of AMP to adenosine by 5′-nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5′-nucleotidase, ecto is also provided.