Abstract:
A process for attaching a substance, especially an organic substance, onto one or more microparticles is provided. The process involves providing a quantity of a substance to be attached onto the microparticles, as well as a quantity of microparticles. The organic substance is then directed through a first conduit (12, 206) and the microparticles are sent through a second conduit (16, 212). The first (12, 206) and second (16, 212) conduits meet at a confluence point (26, 214, 305), and it is there that the substance and the microparticles mix such that the substance attaches to, and coats the microparticles. In a preferred embodiment, there is further provided mixing means such as an in-line static mixer (22, 216, 238, 307, 317, 323, 329) for mixing together the substance and the microparticles. The coated microparticles can be utilized in all manners of immunoassay, nucleic acid assay, cell assay and therapeutic injectable applications. The microparticles herein may also be replaced with another organic substance for conjugation or attachment to the first organic substance.
Abstract:
A novel member of the uteroglobin family of proteins, designated as BU101, is described. BU101 is defined by a set of contiguous and partially overlapping RNA sequences transcribed from breast tissue, and polypeptides encoded thereby. A fully sequenced clone representing the longest continuous sequence of BU101 is also disclosed. These sequences are useful for the detecting, diagnosing, staging, monitoring, prognosticating, preventing or treating, or determining the predisposition of an individual to diseases and conditions of the breast such as breast cancer. Also provided are antibodies which specifically bind to BU101-encoded polypeptide or protein, and agonists or inhibitors which prevent action of the tissue-specific BU101 polypeptide, which molecules are useful for the therapeutic treatment of breast diseases, tumors or metastases.
Abstract:
Disclosed are novel antifungal agents having formula (I) or a pharmaceutically acceptable acid, ester or prodrug thereof, wherein preferred compounds include those compounds wherein R1 is selected from the group consisting of -NH2; R2 is selected from the group consisting of hydrogen, fluoro, and hydroxyl; R3 is selected from the group consisting of -CH2(p-C6H4)3O(CH2)3CH3, -CH2(p-C6H4)O(CH2)6CH3, -COO(p-C6H4)O(CH2)6CH3, -CO(Piperazinyl)(p-C6H4)2OCH3, -CO(p-C6H4)O(CH2)6CH3, -CO(p-C6H4)(Piperazinyl)(p-C6H4)O(CH2)4CH3, -CO(p-C6H4)(Piperazinyl)(p-C6H4)O(CH2)6CH3, -CO(p-C6H4)(Piperazinyl)(p-C6H4)OCH3, and -CO(p-C6H4)(Piperazinyl)O(CH2)6CH3; et R4 is selected from the group consisting of -CH(OH)CH3, -CH2OH, -CH2CH3, -CH2CH2CH2NH2, -CH2(CH2)NH2, -CH2NH2, -CH2(CH2)2(NH)C=(NH)-NH2, -CH3, -CH2(Ph)OH, hydrogen, -CH2CH2COOH, and -CH2COOH. Also disclosed are pharmaceutical compositions containing such compounds and the use of the same in the treatment of fungal infections.
Abstract translation:公开了具有式(I)的新型抗真菌剂或其药学上可接受的酸,酯或前药,其中优选的化合物包括其中R 1选自-NH 2; R2选自氢,氟和羟基; R 3选自-CH 2(对-C 6 H 4)3 O(CH 2)3 CH 3,-CH 2(对-C 6 H 4)O(CH 2)6 CH 3,-COO(对-C 6 H 4)O(CH 2)6 CH 3,-CO( 哌嗪基)(对-C 6 H 4)2 OCH 3,-CO(p-C 6 H 4)O(CH 2)6 CH 3,-CO(p-C 6 H 4)(哌嗪基)(对-C 6 H 4)O(CH 2)4 CH 3,-CO(p-C 6 H 4) (哌嗪基)(p-C6H4)O(CH2)6CH3,-CO(对-C6H4)(哌嗪基)(对-C 6 H 4)OCH 3和-CO(对-C 6 H 4)(哌嗪基)O(CH 2) 其中R 4选自-CH(OH)CH 3,-CH 2 OH,-CH 2 CH 3,-CH 2 CH 2 CH 2 NH 2,-CH 2(CH 2)NH 2,-CH 2 NH 2,-CH 2(CH 2)2(NH)C =(NH) NH 2,-CH 3,-CH 2(Ph)OH,氢,-CH 2 CH 2 COOH和-CH 2 COOH。 还公开了含有这些化合物的药物组合物及其在治疗真菌感染中的用途。
Abstract:
Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein W and Y are independently selected from the group consisting of (a) quinolyl; (b) quinolyl substituted with a substituent selected from the group consisting of (b-1) halogen, (b-2) alkyl of one to six carbon atoms, (b-3) haloalkyl of one to six carbon atoms, and (b-4) alkoxy of one to six carbon atoms; (c) benzothiazolyl; (d) benzothiazolyl substituted with a substituent selected from the group consisting of (d-1) halogen, (d-2) alkyl of one to six carbon atoms, (d-3) haloalkyl of one to six carbon atoms, and (d-4) alkoxy of one to six carbon atoms; (e) benzoxazolyl; (f) benzoxazolyl substituted with a substituent selected from the group consisting of (f-1) halogen, (f-2) alkyl of one to six carbon atoms; (g) benzimidazolyl; (h) benzimidazolyl substituted with a substituent selected from the group consisting of (h-1) halogen, (h-2) alkyl of one to six carbon atoms; (i) quinoxalyl; (j) quinoxalyl substituted with a substituent selected from the group consisting of (j-1) halogen, (j-2) alkyl of one to six carbon atoms; (k) naphthyl; (l) naphthyl substituted with a substituent selected from the group consisting of (l-1) halogen, (1-2) alkyl of one to six carbon atoms, (1-3) alkoxy of one to six carbon atoms; with the proviso that W and Y are not simultaneously the same substituent; R and R are independently selected from the group consisting of (a) hydrogen, (b) alkyl of one to six carbon atoms, (c) haloalkyl of one to six carbon atoms, (d) alkoxy of one to six carbon atoms, and (e) halogen; R is selected from the group consisting of (a) hydrogen and (b) alkyl of one to six carbon atoms; X is absent or is selected from the group consisting of (a) alkylene of one to six carbon atoms, (b) alkenylene of one to six carbon atoms, and (c) alkynylene of one to six carbon atoms; and M is selected from the group consisting of (a) a pharmaceutically acceptable metabolically cleavable group, (b) -OR where R is selected from the group consisting of hydrogen and alkyl of one to six carbon atoms, (c) -NR R where R and R are independently selected from the group consisting of hydrogen, alkyl of one to six carbon atoms, hydroxy, and alkoxy of one to six carbon atoms. These compounds inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states.
Abstract:
A nutritional formulation containing an amount of diacetyltartaric acid esters of mono- and diglycerides effective to inhibit the infectious activity of pathogenic microorganisms is provided. A method of inhibiting the infectious activity of pathogenic microorganisms including the step of feeding the nutritional composition to a subject is also provided.
Abstract:
Antimicrobial compounds having formula (II), (III), (IV), (V), (VI), (VII), (VIII) and (IX); as well as the pharmaceutically acceptable salts, esters and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
Abstract:
A container closure system for delivering a fluid. The system includes a stopper constructed to seal fluidly a container. A closure member is mounted on an upper surface of the stopper. The closure member includes a base having an upper surface and a lower surface. The closure member further includes an outer wall and an inner wall extending from the upper surface of the base with the inner wall spaced from the outer wall. The base defines therethrough a needle access port between the inner and outer walls. The inner wall defines a chamber therein. The base further defines therethrough an aperture adjacent the chamber defined by the inner wall. A piercing member is movably disposed within the chamber defined by the inner wall. The piercing member has a first end portion and a second end portion, the first end portion being positioned proximally to the stopper. A piercing tip is mounted on the first end portion and is constructed to pierce the stopper. The second end portion of the piercing member is configured to engage a luer inserted into the chamber defined by the inner wall. A channel is defined through the piercing member.
Abstract:
A process of preparing 6-O-alkylerythromycin A using 9-oximesilyl erythromycin A derivatives is provided. 9-Oximesilyl- and 6-O-alkylerythromycin A derivatives used in the preparation of 6-O-alkylerythromycin A are also provided.