The present invention is directed to use of kifunensine for increasing sialylation of a glycosylated polypeptide, wherein a cell that produces the glycosylated polypeptide is contacted with kifunensine. Also provided are related methods for increasing sialylation of a glycosylated polypeptide and producing a glycosylated polypeptide, as well as glycosylated polypeptides and pharmaceutical compositions comprising the same, and their use in medicine.

The present invention is directed to use of kifunensine for increasing sialylation of a glycosylated polypeptide, wherein a cell that produces the glycosylated polypeptide is contacted with kifunensine. Also provided are related methods for increasing sialylation of a glycosylated polypeptide and producing a glycosylated polypeptide, as well as glycosylated polypeptides and pharmaceutical compositions comprising the same, and their use in medicine.

The present invention relates to tetrahydrobenzo-isoquinoline sulfonamide derivatives of formula (1), processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses, non-allergic mast cell responses or certain autoimmune responses), and in particular disorders caused by the interaction of IgE with the FcεRI receptor.

##STR00001##

This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.

The present invention relates to compounds of Formula (Ia) or pharmaceutically acceptable salts, hydrates, solvates, clathrates, polymorphs, stereoisomers thereof. It further discloses a pharmaceutical composition comprising compounds of Formula (Ia) and the use of compounds of Formula (Ib), in particular for the use in the treatment of diseases or disorders wherein disrupting Rad51-BRCA2 interaction is beneficial.

##STR00001##

The present invention relates to compounds of Formula (Ia) or pharmaceutically acceptable salts, hydrates, solvates, clathrates, polymorphs, stereoisomers thereof. It further discloses a pharmaceutical composition comprising compounds of Formula (Ia) and the use of compounds of Formula (Ib), in particular for the use in the treatment of diseases or disorders wherein disrupting Rad51-BRCA2 interaction is beneficial.

##STR00001##

The compound represented by formula (I), and racemates, stereoisomers, tautomers, isotopic markers, nitrogen oxides, solvates, polymorphs, metabolites, esters, pharmaceutically acceptable salts, or prodrugs thereof have ROCK inhibitory activity. The compound represented by formula (1) has good safety, good metabolic stability, and a low risk of potential hepatotoxicity. Further, the compound represented by formula (I) has a simple preparation method and is easy to purify, and therefore has good application prospects.

##STR00001##

The compound represented by formula (I), and racemates, stereoisomers, tautomers, isotopic markers, nitrogen oxides, solvates, polymorphs, metabolites, esters, pharmaceutically acceptable salts, or prodrugs thereof have ROCK inhibitory activity. The compound represented by formula (1) has good safety, good metabolic stability, and a low risk of potential hepatotoxicity. Further, the compound represented by formula (I) has a simple preparation method and is easy to purify, and therefore has good application prospects.

##STR00001##

Provided are methods for treating neuropathic pain by administering to a subject in need thereof a compound comprising phenyl-indole scaffold, wherein the compound has a modulatory effect on cannabinoid type 1 receptor (CB.sub.1R). Pharmaceutical compositions containing compounds comprising phenyl-indole scaffolds and pharmaceutically acceptable carriers are also provided, along with methods of using the same.

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##STR00002##

Provided herein are indole compounds that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease