Patent classifications
C07H23/00
Ruthenium-based photolinkers and methods of use
The present invention provides ruthenium-based photolinker compounds, caged molecules comprising the ruthenium-based photolinker compounds, and methods of use. In certain aspects, the compositions disclosed herein comprise an active domain conjugated to a ruthenium-based photolinker, such that irradiation of the photolinker exposes the active domain.
METHOD OF PREPARING NUCLEASE-RESISTANT DNA-INORGANIC HYBRID NANOFLOWERS
The present invention relates to a method of preparing nucleic acid-inorganic hybrid nanoflowers, which comprises allowing a nucleic acid to react with a solution of a metal ion-containing compound at room temperature, thereby forming a complex between the metal ion and the nitrogen atom of an amide bond or amine group present in the nucleic acid. According to the present invention, organic-inorganic hybrid nanoflower structures may be synthesized using nucleic acid in a simple manner under an environmentally friendly condition without any toxic chemical substance. The produced organic-inorganic hybrid nanoflower structures show a high DNA encapsulation yield, have resistance against nuclease, and show significantly increased peroxidase activity. Thus, these nanoflower structures may be widely used as a gene therapy carrier and in biosensing technology.
METHOD OF PREPARING NUCLEASE-RESISTANT DNA-INORGANIC HYBRID NANOFLOWERS
The present invention relates to a method of preparing nucleic acid-inorganic hybrid nanoflowers, which comprises allowing a nucleic acid to react with a solution of a metal ion-containing compound at room temperature, thereby forming a complex between the metal ion and the nitrogen atom of an amide bond or amine group present in the nucleic acid. According to the present invention, organic-inorganic hybrid nanoflower structures may be synthesized using nucleic acid in a simple manner under an environmentally friendly condition without any toxic chemical substance. The produced organic-inorganic hybrid nanoflower structures show a high DNA encapsulation yield, have resistance against nuclease, and show significantly increased peroxidase activity. Thus, these nanoflower structures may be widely used as a gene therapy carrier and in biosensing technology.
SELECTIVE VALORIZATION OF BIOMASS SUGARS
Disclosed are methods of forming an epimer or a dehydrated isomer of a pyranose monosaccharide or a pyranose saccharide residue in an oligosaccharide or a glycoside.
4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF
The present invention is directed to 4′-substituted nucleoside derivatives of Formula I
##STR00001##
and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4′-substituted nucleoside derivatives of Formula I and derivatives thereof.
4'-SUBSTITUTED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS AND PREPARATIONS THEREOF
The present invention is directed to 4′-substituted nucleoside derivatives of Formula I
##STR00001##
and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4′-substituted nucleoside derivatives of Formula I and derivatives thereof.
PROCESS FOR PRODUCING 2'-O-FUCOSYLLACTOSE
The present invention relates to a method for preparing 2′-O-fucosyllactose, the intermediates obtainable by this method and the use of these intermediates. The preparation comprises the reaction of a protected fucose of the general formula (I) with a tri(C.sub.1-C.sub.6-alkyl)silyl iodide to give a protected 1-iodofucose followed by the reaction of the protected 1-iodofucose with a compound of the general formula (II), in the presence of at least one base and deprotecting the resulting coupling product to afford 2′-O-fucosyllactose.
##STR00001##
In this context, the variables are each defined as follows: R.sup.a and R.sup.b are the same or different and are —C(═O)—C.sub.1-C.sub.6-alkyl, or —C(═O)-phenyl, wherein said phenyl is unsubstituted or optionally has 1 to 5 substituents, or R.sup.a and R.sup.b together are a radical —(C═O)— or a substituted methylene radical —C(R.sup.dR.sup.e)—, R.sup.c is a radical R.sup.Si or is benzyl, wherein said benzyl is unsubstituted or optionally has 1, 2 or 3 substituents, R.sup.Si is a radical of the formula SiR.sup.fR.sup.gR.sup.h, where R.sup.f, R.sup.g and R.sup.h are the same or different and are C.sub.1-C.sub.8-alkyl for example, R.sup.1 is a radical —C(═O)—R.sup.11 or a radical SiR.sup.12R.sup.13R.sup.14 R.sup.2 are the same or different and are C.sub.1-C.sub.8-alkyl for example; R.sup.3 are the same or different and are for example C.sub.1-C.sub.8-alkyl or both radicals R.sup.3 together form a linear C.sub.1-C.sub.4-alkenyl, which is unsubstituted or has 1 to 6 methyl groups as substituents.
Transcriptome in vivo analysis (TIVA) and transcriptome in situ analysis (TISA)
Compositions and methods of capturing one or more nucleic acid molecules of a cell or subcellular compartment are described. In certain aspects, the compositions comprise a caged molecule comprising one or more photolinkers and an antisense oligonucleotide, which when uncaged hybridizes to a target nucleic acid molecule.
Transcriptome in vivo analysis (TIVA) and transcriptome in situ analysis (TISA)
Compositions and methods of capturing one or more nucleic acid molecules of a cell or subcellular compartment are described. In certain aspects, the compositions comprise a caged molecule comprising one or more photolinkers and an antisense oligonucleotide, which when uncaged hybridizes to a target nucleic acid molecule.
THERMALLY-CLEAVABLE PROTECTING AND LINKER GROUPS
The present invention relates to chemical linkers and protecting groups, compounds and compositions containing the chemical linkers or protecting groups, and intermediates and processes that can be used to prepare them. The chemical linkers and protecting groups are based on pyrrolidine and piperidine activating groups, which undergo intramolecular cyclisation upon heating with release of carbon dioxide, thereby releasing the organic compound from a substrate. In particular, those chemical linkers and protecting groups are useful in the solid phase synthesis of oligonucleotides according to the following representative schemes.