摘要:
The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.
摘要:
Derivatives of drugs are provided, said derivatives comprising the H2S-releasing moiety 4-hydroxythiobenzamide that is either covalently linked to the drug or forms a salt with the drug. The compounds of the present invention exhibit enhanced activity or reduced side effects or both.
摘要:
The present invention relates to derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) having improved anti-inflammatory properties useful in the treatment of inflammation, pain and fever. More particularly, NSAIDs are derivatized with a hydrogen sulfide (H2S) releasing moiety to produce novel anti-inflammatory compounds having reduced side effects.
摘要:
Unique salts of trimebutine and N-monodesmethyl trimebutine, and their corresponding stereoisomers, having improved analgesic properties useful in the treatment of visceral pain are provided. The salts of the present invention are particularly useful in the treatment of conditions characterized by abdominal pain, such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS), diabetic gastroparesis, and dyspepsia.
摘要:
The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.
摘要:
Composite proppant particles each of which comprises a plurality of microbubbles and a resin binder are disclosed. Also disclosed are a method of using such composite proppant particles to prop fractures in wells formed in underground formations.
摘要:
A method and apparatus for refrigeration system control includes an evaporator pressure regulator and sensor in communication with one of a plurality of refrigeration circuits. The sensor is operable to measure a parameter of the refrigeration circuit. A controller is operable to adaptively control a suction pressure of the compressor rack based upon the measured parameter, whereby the controller controls a circuit temperature for one of the plurality of circuits. Further, the controller is operable to control the electronic evaporator pressure regulator to control the temperature in the one of a plurality of refrigeration circuits by determining a change in the parameter and updating a set point based upon the change of parameter.
摘要:
An electrical connector assembly is provided for mounting to a first side of a panel and through an opening in the panel. A connector housing is adapted for mounting through the opening in the panel and carries a plurality of terminals. A multi-function mounting/latch component includes at least one mounting boss for mounting the connector housing on a circuit board. The multi-function component includes at least one mounting aperture for receiving a mounting post of the connector housing for mounting the connector housing at the first side of the panel and through the opening in the panel. The multi-function component includes at least one latch arm projecting through the opening to a second side of the panel. A locking plate is engageable with the latch arm at the second side of the panel to hold the connector in assembly through the panel. The latch arm includes a latching aperture to facilitate latching the connector assembly to a complementary mating connector at the second side of the panel.
摘要:
Apparatus for presenting blind rivets (11) of the type comprising a shell (12) and a projecting stem (13), one at a time for pick-up by the nosepiece (28) of a rivet setting tool, includes gate means comprising a pair of guide members (24) for receiving a rivet (11) blown by air along a hose (39). The guide membes are urged by a spring (25) into their closed position, in which they arrest each rivet and position it in uniform orientation with its stem (13) projecting. Locating means (30) receives the nose piece (28) and guides it into the correct position and orientation for picking up the rivet by its projecting stem. A proximity detector (37) detects when the tool nose tip is correctly located, and actuates a pneumatically driven plunger (18) which pushes the guide members (24) apart to release the rivet into the tool nosepiece (28).
摘要:
The present invention relates to a method for producing novel 4-[1-oxoalkyl]-2,5-oxazolidinediones, (4-1 OOD), and their use in a stereoselective method of producing beta-lactam-containing compounds which include several biologically active compounds such as the well-known families of pencillin and cephalosporin antibiotics. The method of the present invention involves generally the reaction of the above-described 4-[1-oxoalkyl]-2,5-oxazolidinediones so produced with a thiol amine having a geometry amenable to forming the precursor of the desired beta-lactam-containing compound or, in one scheme, forming the beta-lactam-containing compound itelf directly. This is done either by direct reaction of the 4-1 ODD with a thiol amine (which by one pathway proceeds directly to the beta-lactam-containing compound) or by first converting the 4-1 OOD to its 2-[1-oxoalkyl]-2-amino acid form before its reaction with the thiol amine; and then forming the beta lactam by action of cyanogen). The beta-lactam-containing compounds can be further modified according to methods known in the art to produce specific derivatives as desired.