C07C235/48

Branched Discrete PEG Constructs

Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through custom-character to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, custom-character, having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.

Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex

This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.

Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex

This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.

PPAR AGONISTS AND METHODS OF USE THEREOF

Provided herein are deuterated compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

SHIP1 MODULATORS AND METHODS RELATED THERETO

Compounds of formula (I):

##STR00001##

where R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and R.sup.7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

ORALLY AVAILABLE SEH/PDE4 DUAL INHIBITORS

Provided herein are novel bioavailable dual inhibitors capable of inhibiting both soluble epoxide hydrolase (sEH) and phosphodiesterase 4 (PDE4), and methods of using the same.

ORALLY AVAILABLE SEH/PDE4 DUAL INHIBITORS

Provided herein are novel bioavailable dual inhibitors capable of inhibiting both soluble epoxide hydrolase (sEH) and phosphodiesterase 4 (PDE4), and methods of using the same.

Phenyl derivatives as cannabinoid receptor 2 agonists

The invention relates to a compound of formula (I) ##STR00001##
wherein R.sup.1 to R.sup.3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Phenyl derivatives as cannabinoid receptor 2 agonists

The invention relates to a compound of formula (I) ##STR00001##
wherein R.sup.1 to R.sup.3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

P62-ZZ chemical inhibitor

A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.