Patent classifications
C07F9/2429
METHODS AND COMPOSITIONS FOR SYNTHESIS OF TWO-PHOTON CLEAVABLE PHOSPHORAMIDITE MOLECULES FOR OLIGONUCLEOTIDE CONJUGATION
The syntheses of two phosphoramidite building blocks based on BNSF and BNSMB structures are disclosed. Furthermore, some common molecular intermediates have been designed and linked to the central biphenyl core of the two molecules, resulting in a versatile and cost-effective design. These compounds can be effectively introduced to DNA oligonucleotides via the well-established standard cyanoethylphosphoramidite chemistry on the nucleic acid synthesizer. Fragmentation of these BNSF- and BNSMB-functionalized DNA strands is achieved by both one-photon and two-photon photolysis of photoliable bonds of [2-(2-nitrophenyl)propoxy]carbonyl groups on BNSF and BNSMB molecules respectively, resulting in two short pieces of single-stranded DNAs. The versatile design and facile synthesis of these two-photon photocleavage phosphoramidite molecules are beneficial to synthetic chemists and photochemists for the development of new caged compounds which enables to introduce into oligonucleotides as light-triggered carriers via solid-phase synthesis for a wide range of applications in materials science, polymer, chemistry, biology and DNA nanoecthnology.
HIGH PENETRATION PRODRUG COMPOSITIONS OF MUSTARDS AND MUSTARD-RELATED COMPOUNDS
The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of mustards and mustard-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
Antimicrobial Compounds and Methods of Use
Organophosphorus or organosulfur compounds and methods of using the compounds as cleaning agents, particle dispersants, or surfactants, or to remove, disperse or inhibit the growth of a biofilm, or inhibit the growth of, or kill a fungus or bacteria are provided.
High penetration prodrug compositions of mustards and mustard-related compounds
The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of mustards and mustard-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
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.
Photocleavable linker molecules with diarylsulphide backbone for transient bioconjugate synthesis
The present description refers to photocleavable compounds which can be used as a photocleavable linker in order to link two biomolecules, such as oligonucleotides and peptides. The present description further refers to a method for the synthesis of said photocleavable compounds. ##STR00001##
Methods for treating Filoviridae virus infections
Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV: ##STR00001##
The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
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 comprising a compound Formula VIII for treating Filoviridae virus infections. In one aspect, the compound of Formula VIII is formed from a reaction mixture comprising the compound of Formula IX, the compound of Formula X, a coupling agent such as magnesium chloride and a non-nucleophilic base such as diisopropylethylamine. The compound of Formula IX can be formed from a compound of Formula V and a cyanating agent. The compound of Formula V can be synthesized from a reaction mixture comprising a deprotonating agent such as phenylmagnesium chloride; a silylating agent such as chlorotrimethylsilane; a coupling agent such as isopropylmagnesium chloride, an additive such as LaCl.sub.3-2LiCl, LaCl.sub.3, CeCl.sub.3, NdCl.sub.3, or YCl.sub.3; a compound of Formula VI; and 7-iodopyrrolo[2,1-f][1,2,4]triazin-4-amine. The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
Antimicrobial compounds and methods of use
Organophosphorus or organosulfur compounds and methods of using the compounds as cleaning agents, particle dispersants, or surfactants, or to remove, disperse or inhibit the growth of a biofilm, or inhibit the growth of, or kill a fungus or bacteria are provided.
AKR1C3 INHIBITOR AND MEDICAL USE
Described are compounds that act as AKR1C3 inhibitors or pharmaceutically acceptable salts or solvates or isotopically substituted compounds thereof and methods thereof.