The present invention relates to an imidazoquinoline substituted phosphoric ester agonist, and a preparation therefor and an application thereof. Specifically, the compounds of the present invention have the structure shown in formula (I), wherein the definition of each group and substituent is as described in the description. Also disclosed in the present invention are a preparation method for the compound and use thereof as a TLR agonist.

##STR00001##

The present invention provides a new building block for peptide synthesis, which introduces a cleavage site that can be used to generate cleavable fragments subsequent to a peptide sequence.

This invention relates to antisense oligonucleotides comprising at least one N3′.fwdarw.P5′ phosphorodiamidate linkage (NPN) in the backbone as well as methods for using the same. The antisense oligonucleotides can effectively prevent or decrease protein expression.

A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by the formula (10) below:

##STR00001##

the method including removing the protecting group from the hydroxyl group in a compound represented by formula (7) below:

##STR00002##

(wherein P represents a protecting group, R.sup.3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms) to synthesize a compound represented by formula (8) below:

##STR00003##

(wherein R.sup.3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms).

Methods of making indole analogs using a rhodium-containing catalyst are described, along with methods of using the compounds to treat hyperglycemic, hyperlipidemic, or autoimmune disorders in mammals, and corresponding pharmaceutical compositions. Disclosed herein is a method of making indoles. The method comprises contacting a reactant of formula I wherein E is a protecting group, —SO2-Aryl, or —SO2-substituted-Aryl; and R and R2 are independently selected from the group consisting of hydrogen, halo, C1-C12-alkyl and aryl; with a rhodium(l)-containing catalyst.

An object of the present invention is to provide a novel compound useful for manufacturing salacinol, a method for manufacturing the compound, a method for manufacturing salacinol, methods for protecting and deprotecting a diol group, and a protective agent for a diol group. A compound represented by Formula (1) is a compound useful for manufacturing salacinol.

##STR00001##

(In the formula, each of R.sup.1a and R.sup.1b is a hydrogen atom or a hydroxy protective group; R.sup.2 is a hydroxy group or the like; and R.sup.3 is a hydroxy group or the like.)

The present disclosure is directed to intermediates and salts thereof useful for the preparation of spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1). Processes of preparing the intermediates, salts, and TPH inhibitors are also provided.

Provided are a method for efficiently manufacturing a nitrogen-containing compound, which is used for manufacturing a treatment agent for integrin-related diseases, or a salt thereof and a manufacturing intermediate of the compound or a salt thereof.

A method for manufacturing a novel nitrogen-containing compound or a salt thereof includes (1) a step of obtaining a compound represented by Formula [10] or a salt thereof through an amidation reaction; and (2) a step of deprotecting the compound represented by Formula [10] or a salt thereof.

##STR00001##

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.

A natural peptide comprising a cellular growth promoting fragment of a protein selected from SEQ ID NOs: 1 to 13, and a composition comprising a plurality of growth promoting peptides, is described. Also disclosed is the use of the peptides and compositions in prevention of ageing of human skin, treatment of diseases or conditions characterised by damaged epithelial cells or tissue such as colon cancer and peripheral inflammatory disorders, and wound treatment. Specific pea and rice protein derived peptides are described in SEQ ID NOs: 15 to 505, and 546 to 704.