摘要:
The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula 1 Wherein Z, X, R1, R2, R3, and R4 are as described in the specification.
摘要:
A method is disclosed for providing extended duration treatment or prevention of pain, inflammation and inflammation-related disorders in a subject in need of such extended duration treatment or prevention by administering to the subject a Cox-2 selective inhibitor having certain added substituent groups. Also disclosed is a method for extending the duration of the plasma half-life of diaryl-substituted Cox-2 selective inhibitors by substituting halogen, haloalkyl, haloalkoxy, alkyl, nitrile, cyano or alkoxy groups at certain positions on the diaryl-substituted rings of the inhibitor molecule. A novel composition comprising such extended duration Cox-2 selective inhibitors is also disclosed.
摘要:
This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.
摘要:
The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula 1 Wherein Z, X, R1, R 2, R3, and R4 are as described in the specification.
摘要:
A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R2 is selected from hydrido, alkyl, haloalkyl, alkoxycaronyl, cyano, cyanoalkyl, carboxyl, aminocaronyl, alkylaminocarbonyl, cycloalklaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, amioncarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R4 is optionally substituted at a substitutable position with one or more radicals selected from halo alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R2 and R3 are not both hydrido; further provided that R2 is not carboxyl or methyl when R3 is hydrido and when R4 is phenyl; further provided that R4 is not triazolyl when R2 is methyl; further provided that R4 is not arakenyl when R2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R4 is not phenyl when R2 is methyl and R3 is carboxyl; and further provided that R4 is not unsubstituted thienyl when R2 is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.
摘要:
A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, suitable for use in the treatment of a cyclooxygenase-2 mediated disease is provided. Also provided is a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutically-acceptable salt thereof, and a method for treatment of a cyclooxygenase-2 mediated disease by administering to a subject in need thereof a therapeutically-effective amount of the pharmaceutical composition.
摘要:
A device includes a radar system configured to be placed in a hiding mechanism, the radar system having one or more transmit antennas oriented within the hiding mechanism and configured to transmit one or more radar signals toward a barrier, one or more receive antennas oriented within the hiding mechanism and configured to receive reflection signals of the transmitted radar signal back through the barrier and back through the hiding mechanism, one or more transceivers coupled to the one or more transmit antennas and the one or more receive antennas, and an electronic processor to analyze the received reflection signals of the transmitted one or more radar signals, and determine, based on the analyzed received reflection signals, locations of the one or more individuals within a region at a side of the barrier.
摘要:
A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.
摘要:
A device includes a compressible conductive element including a first end and a second end, and an adjustment element coupled to the compressible conductive element, the adjustment element configured to adjust the compressible conductive element to a state of compression between an uncompressed mode and a compressed mode. The compressible conductive element is configured to couple to a source of electrical current at the first end and to radiate electromagnetic energy from the second end.