Abstract:
Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Abstract:
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Abstract:
The present invention provides methods for improving the production of recombinant proteins through the use of pharmacological chaperones for the recombinant proteins. As exemplified by the present invention, the binding of a pharmacological chaperone to a recombinant protein expressed by a cell can stabilize the protein and increase export of the protein out of the cell's endoplasmic reticulum, and increase secretion of the protein by the cell.
Abstract:
Compositions having a texaphyrin-lipophilic molecule conjugate loaded into a biological vesicle and methods for imaging, diagnosis and treatment using the loaded vesicle are provided. For example, liposomes or red blood cells loaded with a paramagnetic texaphyrin-lipophilic molecule conjugate have utility as a blood pool contrast agent, facilitating the enhancement of normal tissues, magnetic resonance angiography, and marking areas of damaged endothelium by their egress through fenestrations or damaged portions of the blood vascular system. Liposomes or cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate can be photolysed, allowing for a photodynamic therapy effect at the site of lysis. Availability of red blood cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate provides a method for delivering a photodynamic therapeutic agent to a desired site with a high concentration of oxygen. By presenting the agent in this way, it is expected that a patient will experience less toxicity.
Abstract:
The invention concerns a method for the chemical modification of a surface based on the reaction of photolytically generated reactive intermediates derived from azido heterocycles with said surface.
Abstract:
Acid halides and anhydrides of acids of the formula ##STR1## with the substituent definitions given in the description are obtained by reacting the corresponding acids with organic or inorganic acid halides or acid anhydrides. The new compounds are intermediate products for the preparation of new reactive dyestuffs.
Abstract:
This invention relates to a process for the production of cyclohexanone oxime by reacting cyclohexanone with excess aqueous hydroxylamine in the presence of excess ammonia. More specifically, the invention relates to improving yields of the oxime while reducing undesirable by-product formation by use of two or more stages of reaction with correlated adjustment of reaction conditions in each stage. The invention also involves improved recovery of the unreacted hydroxylamine reactant for recycle in the process.
Abstract:
The present disclosure features citrate salts and pharmaceutical compositions useful for the treatment of BAF complex-related disorders. Also disclosed are methods for preparing compounds.