摘要:
This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
摘要:
Various applications are presented of a vector field method of computing one or more eigenvalues and eigenvectors of a symmetric matrix. The vector field method computes an eigenvector by computing a discrete approximation to the integral curve of a special tangent vector field on the unit sphere. The optimization problems embedded in each iteration of the vector field algorithms admit closed-form solutions making the vector field approach relatively efficient. Among the several vector fields discussed is a family of vector fields called the recursive vector fields. Numerical results are presented that suggest that in some embodiments the recursive vector field method yields implementations that are faster than those based on the QR method. Further, the vector field method preserves, and hence can fully exploit the sparseness on the given matrix to speed up computation even further. Preprocessing that contracts the spectral radius of the given matrix further accelerates the systems.
摘要:
In the exploration for petroleum or natural gas, drilling targets are identified by locating local maxima of horizontal gradient in the top-of-geopressure surface of a region of exploration. The probability of finding hydrocarbon deposits is significantly improved where the drilling targets are local maxima of the horizontal gradient in the top-of-geopressure surface which coincide with local maxima of subsurface heat flow in the region of exploration, particularly where the local maxima in the horizontal gradient of the top-of-geopressured surface is concentrated across major fault offsets and are parallel to the predominant strike directions of the faults. The top-of-geopressure surface may be remotely sensed by performing complex trace analysis on reflection seismic traces gathered for the region of exploration to derive corresponding reflection strength attribute traces. The corresponding reflection strength traces are first smoothed and then subject to further complex trace analysis to derive the envelope amplitudes of the smoothed reflection strength traces, which are referred to as second reflection strength traces. The second reflection strength traces are then analyzed to locate an uppermost distinct subsurface boundary between high and low amplitude components thereof. Such a distinct boundary is then identified as the top-of-geopressure surface for the region of exploration.
摘要:
Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.
摘要:
A truck for pulling a semi-trailer includes an operator cab positioned on a frame and a fifth wheel mounted on the frame for receiving an underside of the semi-trailer. The trailer when attached to the truck defines a gap between a forward most portion of the semi-trailer and rearward most portion of the operator cab. A fairing can be located on the frame, aft of the operator cab and forward of at least a portion of the fifth wheel. The fairing can block at least a portion of the air flow attempting to enter the gap from below the frame.
摘要:
This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell Or the inhibition of the conversion of cortisone to Cortisol in a cell.
摘要:
Disclosed is a compound represented by Formula (I): or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (I) or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof and methods of inhibiting 11β-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Values for the variables in Formula (I) are defined herein.
摘要:
The invention relates to compositions containing compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R, R1, R2, R3, and n are defined in the detailed description and claims. In addition, the present invention relates to novel formulations containing compounds of formula I for improved delivery of nucleic acids such as siRNA to the cytoplasm of target cells. In particular embodiments these formulations comprise compounds of formula I, phospholipids, cholesterol, and pegylated lipids. The present invention also relates to methods of manufacturing and using such compounds and compositions.
摘要:
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.