C07H11/04

LIPID A MIMICS, METHODS OF PREPARATION, AND USES THEREOF

The invention provides lipid A mimics in which one or both of the sugar residues of a natural lipid A disaccharide backbone has been replaced with an aromatic group. These lipid A mimics may further differ from a natural lipid A molecule with respect to other structural characteristics, such as, a different number of phosphate groups present, changes in the number, structure and location of lipid chains and/or changes in the spacing and linkage of the sugar residues (or their aromatic replacements). The lipid A mimics may be lipid A agonists and as such may be useful as immunostimulatory agents in inducing or patenting an antibody and/or cell-mediated immune response, or may be lipid A antagonists and as such may be useful in treating or preventing a lipopolysaccharide (LPS)/lipid A-mediated disease or disorder. Also provided are methods for preparing the lipid A mimics.

LIPID A MIMICS, METHODS OF PREPARATION, AND USES THEREOF

The invention provides lipid A mimics in which one or both of the sugar residues of a natural lipid A disaccharide backbone has been replaced with an aromatic group. These lipid A mimics may further differ from a natural lipid A molecule with respect to other structural characteristics, such as, a different number of phosphate groups present, changes in the number, structure and location of lipid chains and/or changes in the spacing and linkage of the sugar residues (or their aromatic replacements). The lipid A mimics may be lipid A agonists and as such may be useful as immunostimulatory agents in inducing or patenting an antibody and/or cell-mediated immune response, or may be lipid A antagonists and as such may be useful in treating or preventing a lipopolysaccharide (LPS)/lipid A-mediated disease or disorder. Also provided are methods for preparing the lipid A mimics.

Phosphorylated heptose compounds: process for their preparation and use

Processes for the preparation of phosphorylated heptose compounds are provided. Embodiments of the invention relate to the chemical synthesis of heptopyranose phosphate compounds. Also, embodiments of the invention relate to the use of compounds according to the invention in modulating an immune response in a subject.

Camptothecin derivatives and preparation methods and applications thereof

The invention relates to novel camptothecin derivatives and their applications, tumor cell growth inhibitors, ternary complexes, and a method for improving the solubility of the camptothecin derivatives. The camptothecin derivatives are prepared by modifying the substance shown as Formula I with glycosylated triazole at position R.sup.3. In the structure shown as Formula I, R.sup.1 represents H, C.sub.1-10 alkyl, C.sub.1-10 alkyl-D or C.sub.1-10 haloalkyl; R.sup.2 represents H, CH.sub.2N(CH.sub.3).sub.2 or CH.sub.2N(CD.sub.3).sub.2; and R.sup.4 represents ##STR00001##
or H, wherein X represents N, O or S; and L represents polypeptide, C.sub.1-20 linear alkyl or derivatives thereof, C.sub.1-20 linear or branched acyl derivatives, C.sub.2-100 ethylene glycol or derivatives thereof. The camptothecin derivatives have high solubility, the anticancer drugs prepared from them have the advantages of wide anticancer spectrum and high safety, and have in vivo anticancer activity higher than irinotecan hydrochloride.

β-modified phosphoric acid compound precursor, β-modified phosphoric acid compound, reaction inhibitor and medicine containing the same, and method for inhibiting reaction

A β-modified phosphoric acid compound precursor that inhibits the progress of a phosphorylation reaction having a partial structure represented by ##STR00001##
where A.sub.1 represents —SR.sub.1, —S—S—R.sub.1, —SeR.sub.1, or —X, where X is a halogen selected from fluoro, chloro, bromo, and iodo; R.sub.1 represents hydrogen, an alkyl group having 1 to 20 carbon atoms, or the like; L.sub.1 represents hydrogen, an alkyl group having 1 to 20 carbon atoms, or the like; L.sub.2 represents an alkyl group having 1 to 20 carbon atoms, or the like; L.sub.1 and L.sub.2 may be linked to each other to form a 4 to 6-membered ring structure; L.sub.1 and L.sub.2 may each have a substituent; and the symbol * represents a bond to be bonded to a phosphate group by phosphorylation. Further, provided are a reaction inhibitor and a medicine, each of which includes the β-modified phosphoric acid compound precursor.

NICOTINAMIDE MONONUCLEOTIDE DERIVATIVES AND THEIR USES

The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival.

NICOTINAMIDE MONONUCLEOTIDE DERIVATIVES AND THEIR USES

The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival.

Nicotinamide mononucleotide derivatives and their uses

The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival.

Nicotinamide mononucleotide derivatives and their uses

The invention relates to compositions of nicotinamide mononucleotide derivatives and their methods of use. The invention also relates to methods of preparing nicotinamide mononucleotide derivatives. The invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinamide mononucleotide derivative. The invention relates to methods of using nicotinamide mononucleotide derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and improving cell and tissue survival.