摘要:
The invention is directed to compounds of Formula (I) useful as delta and mu opioid receptor modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
摘要:
An electronic device includes an amplifier circuit coupled to a linearizer. The amplifier circuit may receive a first input signal including first and second frequencies and generate a first output signal including a delta frequency signal at a delta frequency, which is the difference between the first frequency and the second frequency. The linearizer includes a signal detector circuit, a current-mirror circuit, a low pass filter, a phase shifter, and a bias circuit. The signal detector circuit may generate a second output signal. The current-mirror circuit may adjust an amplitude of a signal. The low pass filter may eliminate a portion of the second output signal having frequencies greater than the delta frequency. The phase shifter may generate a feedback signal corresponding to the delta frequency signal. An amplitude and/or a phase of the feedback signal is different from an amplitude and/or a phase of the delta frequency signal.
摘要:
Disclosed are compounds, compositions and methods for treating various diseases and conditions, including pain. Such compounds are represented by Formula I as follows: wherein A, G, Y, R3, R4, and R5 are defined herein.
摘要:
A multiple antenna wireless system including a transmitter and a receiver comprises a reconfigurable large antenna array having a plurality of antennas. A plurality of RF chains in the transmitter is coupled to the reconfigurable large antenna array. A pilot assisted round robin channel estimation means tracks the fading channel; and an adaptive round robin transmit beamforming means beam forms the reconfigurable large antenna array. A method for multiple antenna wireless communication comprising the steps of tracking a plurality of fading channels in a reconfigurable large antenna array having a plurality of antennas using pilot assisted round robin channel estimation to selectively couple a plurality of RF chains in the transmitter to the reconfigurable large antenna array, and adaptively, round-robin transmit beamforming the reconfigurable large antenna array.
摘要:
Reference membrane components are either pre-labeled or labeled during assays for purposes of normalizing signals associated with binding or functional assays employing G-protein coupled receptor microarrays. A reference component may be included in a membrane in which the target GPCR is embedded or may be present in another membrane printed in conjunction with the target membrane on a microspot. Or, a GPCR microarray may be pre-labeled by incorporating a label on an exposed substrate in a defect in the printed microspot.
摘要:
In one embodiment, the present invention includes a method for constructing a data dependency graph (DDG) for a loop to be transformed, performing statement shifting to transform the loop into a first transformed loop according to at least one of first and second algorithms, performing unimodular and echelon transformations of a selected one of the first or second transformed loops, partitioning the selected transformed loop to obtain maximum outer level parallelism (MOLP), and partitioning the selected transformed loop into multiple sub-loops. Other embodiments are described and claimed.
摘要:
The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
摘要:
The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
摘要:
This invention describes a novel polysaccharide prodrug of 5-fluorouracil (5-FU) with enhanced target specificity for colorectal cancer treatment, and its preparation methods. The prodrug is synthesized by chemically linking anti-cancer drug 5-fluorouracil (5-FU) with a specially selected polysaccharide with molecular weight of 105˜107 Da containing galactose residues. Its distinctive characteristics are that it is a prodrug synthesized by chemically linking polysaccharides with 5-FU through different bridge links for the targeted treatment of colorectal cancer; that the polysaccharides in the chemical compound contain galactose residues; and that these polysaccharides are prepared from natural gums or plant materials. Due to these unique characteristics, as an oral preparation, the polysaccharide component of this novel prodrug can protect the active agent 5-FU from absorption (or metabolism) in the upper gastrointestinal tract and deliver a high concentration of the 5-FU to the colorectal area. Upon reaching the colorectal area, the 5-FU-galactose portion of the prodrug will bind to galectin-3, a-galactoside-binding protein implicated in tumor progression by interactions with its ligands, such as TF (Thomsen-Friedenreich, Galb3GalNAc), Tn (GalNAcaThr/Ser), and Sialy-Tn with galactose residues, which are highly expressed among colorectal cancer cells. Finally, the active 5-FU component will be released locally from the polysaccharide via enzymatic hydrolysis from the local bacterial flora, allowing it to actively kill the colorectal cancer cells. In summary, this novel target-specific prodrug can enhance the selectivity of 5-FU and increase its therapeutic effects in the treatment of colorectal cancer. In addition, with this enhanced target specificity, it is possible to maximize the 5-FU efficacy in cancer patients by having either less toxicity with the same or higher therapeutic dose, and/or administer a lower dosage (if so desired) to achieve the same therapeutic effects, but with much less toxicity. Multiple examples of various approaches to synthesize this novel prodrug are enclosed herein along with several animal model experiments to substantiate the claims as stated above.
摘要:
The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.