Abstract:
Antibacterial compounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds wherein A is =CR -; R is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R is selected from the group consisting of (a), (b), (c) and (d); R is halogen; R is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R is hydrogen, loweralkyl, halo(loweralkyl), or -NR R ; and R is halogen, loeralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl), as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
Abstract translation:具有式(I)的抗菌化合物及其药学上可接受的盐,酯和酰胺,其选择的优选实例包括其中A = CR 6 - 的那些化合物; R 1是3至8个碳原子的环烷基或取代的苯基; R 2选自(a),(b),(c)和(d); R 3是卤素; R 4是氢,低级烷基,药学上可接受的阳离子或前药酯基; R 5是氢,低级烷基,卤代(低级烷基)或-NR 13 R 14; 和R 6是卤素,低级烷基,卤代(低级烷基),羟基取代的低级烷基,低级烷氧基(低级烷基),低级烷氧基或氨基(低级烷基),以及含有这些化合物的药物组合物及其在治疗中的用途 的细菌感染。
Abstract:
This invention is directed to a method for obtaining a factor which potentiates the pesticidal activity of a Bacillus related pesticide, a chemical pesticide and/or a virus with pesticidal properties.
Abstract:
The present invention provides a method of detecting the amount of a target sequence which may be present in a test sample. The method uses an aggregate primer series, which comprises at least two primer sets, in an amplification reaction to detect the relative concentration of a target sequence which may be present in a test sample. The primer sets have different sensitivities and hybridize with sub-target sequences which are different regions of the target sequence. The method generally comprises cycling a test sample suspected of containing a target sequence, an aggregate primer series, and means necessary for performing an amplification reaction; and detecting any amplified sub-target sequences. Based on a qualitative detection of the amplified sub-target sequences generated by individual primer sets, the relative quantity of the target sequence can be determined.
Abstract:
A method for expressing a heterologous protein in a prokaryotic host cell, comprising the steps of: (a) providing a DNA vector having: (1) a control region operatively linked to a first genetic element encoding a carrier protein capable of expression in the host cell, and (2) a second genetic element encoding the heterologous protein, the second element being embedded within the first element such that the first and second elements are contiguous and in the same reading frame; (b) transforming the host cell with the DNA vector; and (c) expressing a fusion protein of the heterologous protein and the carrier protein, wherein the heterologous protein is joined at its N-terminus to a first domain of the carrier protein and at its C-terminus to a second domain of the carrier protein, and also a method for confirming intact expression of heterologous proteins, as well as fusion proteins, DNA constructs, plasmid vectors and transformed host cells relating to the above methods.
Abstract:
The present invention provides a compound of formula (I), (II), (III) or (IV), processes for the preparation of the compounds of the invention, intermediates useful in these processes, a pharmaceutical composition, and methods of using the compounds of the invention.
Abstract:
Compounds having the structure of general formula (I) or a pharmaceutically acceptable salt thereof have activity as inhibitors of cyclooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B4, C4, D4, and E4 and cyclooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optionally susbtituted carbocyclic aryl, (b) optionally substituted furyl, (c) optionally substituted benzo[b]furyl, (d) optionally substituted thienyl, (e) optionally substituted pyridyloxy, (f) optionally substituted pyridylalkyl, (g) optionally substituted benzo[b]thienyl, (h) optionally substituted pyridyl, (i) optionally substituted quinolyl, and (j) optionally substituted indolyl; X is selected from (a) optionally susbtituted alkyl, (b) optionally substituted alkenyl, and (c) optionally substituted alkynyl; R and R are independently selected from hydrogen, hydroxy, and alkyl; and Z is a residue of a non-steroidal anti-inflammatory drug of the general formula Z-COOH.
Abstract translation:具有通式(I)结构的化合物或其药学上可接受的盐具有作为环加氧酶和5-脂氧合酶抑制剂的活性,降低了白三烯B4,C4,D4和E4以及环氧合酶产物如前列腺素和血栓素的生物合成, 可用于治疗炎症和过敏性疾病状态。 化合物具有上述结构,其中A选自(a)任选取代的碳环芳基,(b)任选取代的呋喃基,(c)任选取代的苯并[b]呋喃基,(d)任选取代的噻吩基,(e) 吡啶基氧基,(f)任选取代的吡啶基烷基,(g)任选取代的苯并[b]噻吩基,(h)任选取代的吡啶基,(i)任选取代的喹啉基,和(j)任选取代的吲哚基; X选自(a)任选的取代的烷基,(b)任选取代的烯基,和(c)任选取代的炔基; R 1和R 2独立地选自氢,羟基和烷基; Z为通式Z-COOH的非甾体抗炎药物的残基。
Abstract:
The primary etiology of antibiotic-associated diarrhea (also known as pseudomembranous colitis) has been recognized as Clostridium difficile. It is believed that the indigenous microflora of a healthy individual suppresses the normally present C. difficile. However, when the indigenous microflora are disrupted (e.g., during antibiotic treatment) overgrowth of C. difficile may occur causing diarrhea and colitis. Treatment of C. difficile with antibiotics has proven effective, but many times relapse occurs; and dehydration due to diarrhea is an exacerbating problem. It has been suggested that normalization of the microflora will inhibit C. difficile relapse. Indigestible oligosaccharides have been shown to inhibit C. difficile infection. An oral rehydration solution containing such indigestible oligosaccharides also provides fluid and electrolyte replacement.
Abstract:
The present invention relates to calcium supplements and, in particular, to a solid supplement fortified with calcium glycerophosphate, vitamin D, vitamin C, vegetable oil and a gum selected from the group consisting of gum arabic, gum tragacanth and xanthan gum; to a beverage concentrate or additive (liquid or powder) containing calcium, vitamin D, a vegetable oil and a gum; and to a beverage made by reconstituting such beverage concentrates and additives to make a liquid nutritional product fortified with both calcium and vitamin D, and preferably having a low pH. Concentrates may be diluted with water or juices.
Abstract:
The present invention provides a method of producing a modified recombinant protein in a host cell using a single vector containing in tandem both the nucleotide sequence encoding an exogenous protein and an enzyme specific for modification of that protein. The invention also specifically provides a method of producing a recombinant phosphorylated human protein in a bacterial system using a single vector containing in tandem the nucleotide sequence encoding the human protein and a human kinase specific for phosphorylation of that protein.
Abstract:
Embodiments disclosed herein provide apparatus and methods for verifying a volume of fluid. According to one embodiment, an apparatus includes a receptacle for containing fluid, a first conductor operatively associated with the receptacle and a second conductor operatively associated with the receptacle offset from the first conductor. A source of a first electrical signal is electrically connected with the first conductor. A monitor is electrically connected with the second conductor for detecting a second electrical signal created in the second conductor. In another embodiment, a method includes positioning a receptacle adjacent a fluid dispense nozzle such that fluid dispensed from the nozzle enters the receptacle. A first electrical signal is applied to a first conductor operatively connected with the receptacle. A second electrical signal created in a second conductor operatively connected with the receptacle responsive to the first electrical signal is monitored.