PROCEDURE FOR ATTACHING SUBSTANCES TO PARTICLES
    272.
    发明申请
    PROCEDURE FOR ATTACHING SUBSTANCES TO PARTICLES 审中-公开
    将物质连接到颗粒的程序

    公开(公告)号:WO1998008095A1

    公开(公告)日:1998-02-26

    申请号:PCT/US1997013742

    申请日:1997-08-05

    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 translation: 提供了将物质,特别是有机物质附着到一个或多个微粒上的方法。 该方法包括提供一定量的待附着到微粒上的物质以及一定量的微粒。 然后将有机物质引导通过第一导管(12,206),并将微粒通过第二导管(16,212)送出。 第一(12,206)和第二(16,212)管道在汇合点(26,214,305)处相遇,并且在那里物质和微粒混合,使得该物质附着并涂覆微粒 。 在优选实施例中,还提供了混合装置,例如用于将物质和微粒混合在一起的在线静态混合器(22,216,238,307,317,323,329)。 涂覆的微粒可以以免疫测定,核酸测定,细胞测定和治疗注射用途的所有方式使用。 本文中的微粒也可以用另一有机物质代替,以与第一有机物质共轭或附着。

    REAGENTS AND METHODS USEFUL FOR DETECTING DISEASES OF THE BREAST
    273.
    发明申请
    REAGENTS AND METHODS USEFUL FOR DETECTING DISEASES OF THE BREAST 审中-公开
    用于检测乳腺疾病的试剂和方法

    公开(公告)号:WO1998007857A1

    公开(公告)日:1998-02-26

    申请号:PCT/US1997014665

    申请日:1997-08-19

    CPC classification number: C07K14/47 C12Q1/6886 C12Q2600/136

    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 translation: 描述了称为BU101的蛋白质的子宫肌血清蛋白家族的新成员。 BU101由一组从乳腺组织转录的连续和部分重叠的RNA序列以及由此编码的多肽来定义。 还公开了表示BU101的最长连续序列的完全测序的克隆。 这些序列可用于检测,诊断,分期,监测,预后,预防或治疗或确定个体对乳腺疾病和状况(例如乳腺癌)的倾向。 还提供了特异性结合BU101编码的多肽或蛋白质的抗体,以及预防组织特异性BU101多肽的作用的激动剂或抑制剂,该分子可用于治疗乳腺疾病,肿瘤或转移瘤。

    AMINO-LIPOPEPTIDE ANTIFUNGAL AGENTS
    274.
    发明申请
    AMINO-LIPOPEPTIDE ANTIFUNGAL AGENTS 审中-公开
    氨基磷脂抗真菌药物

    公开(公告)号:WO1998006745A1

    公开(公告)日:1998-02-19

    申请号:PCT/US1997014053

    申请日:1997-08-11

    CPC classification number: C07K7/56 A61K38/00

    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。

    NON-SYMMETRICAL BIS-HETEROARYLMETHOXYPHENYLALKYL CARBOXYLATES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS
    275.
    发明申请
    NON-SYMMETRICAL BIS-HETEROARYLMETHOXYPHENYLALKYL CARBOXYLATES AS INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS 审中-公开
    作为紫苏酮生物合成酶的抑制剂的非对称双异吲哚氧基甲基羧酸酯

    公开(公告)号:WO1998004555A1

    公开(公告)日:1998-02-05

    申请号:PCT/US1997012138

    申请日:1997-07-14

    CPC classification number: C07D401/12 C07D215/14 C07D413/12 C07D417/12

    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 translation: 具有式(I)的化合物或其药学上可接受的盐,其中W和Y独立地选自(a)喹啉基; (b)被选自(b-1)卤素,(b-2)1至6个碳原子的烷基,(b-3)1-6个碳原子的卤代烷基取代的喹啉基和(b -4)1至6个碳原子的烷氧基; (c)苯并噻唑基; (d)被选自(d-1)卤素,(c-2)1-6个碳原子的烷基,(d-3)1-6个碳原子的卤代烷基取代的苯并噻唑基和(d -4)1至6个碳原子的烷氧基; (e)苯并恶唑基; (f)被选自(f-1)卤素,(c-2)1-6个碳原子的(f-2)烷基的取代基取代的苯并恶唑; (g)苯并咪唑基; (h)被选自(h-1)卤素,1至6个碳原子的(h-2)烷基的取代基取代的苯并咪唑基; (i)喹喔啉; (j)被选自(j-1)卤素,具有1至6个碳原子的(j-2)烷基)的取代基取代的喹喔啉基; (k)萘基; (I)被选自(I-1)卤素,(1-2)1-6个碳原子的烷基,(1-3)1-6个碳原子的烷氧基的取代基取代的萘基; 条件是W和Y不是同一个取代基; R 1和R 2独立地选自(a)氢,(b)1至6个碳原子的烷基,(c)1至6个碳原子的卤代烷基,(d)一个 至(6)个碳原子,(e)卤素; R 3选自(a)氢和(b)1至6个碳原子的烷基; X不存在或选自(a)1至6个碳原子的亚烷基,(b)1至6个碳原子的亚烯基和(c)1至6个碳原子的亚炔基; 并且M选自(a)药学上可接受的代谢可裂解基团,(b)-OR 4,其中R 4选自氢和1至6个碳原子的烷基( c)-NR 5 R 6其中R 5和R 6独立地选自氢,1至6个碳原子的烷基,羟基和1至6个碳原子的烷氧基。 这些化合物抑制白细胞三烯生物合成,并且可用于治疗过敏性和炎性疾病状态。

    6-O-SUBSTITUTED ERYTHROMYCIN COMPOUNDS AND METHOD FOR MAKING SAME
    278.
    发明申请
    6-O-SUBSTITUTED ERYTHROMYCIN COMPOUNDS AND METHOD FOR MAKING SAME 审中-公开
    6-O-取代的红霉素化合物及其制备方法

    公开(公告)号:WO1997042206A1

    公开(公告)日:1997-11-13

    申请号:PCT/US1997007702

    申请日:1997-05-06

    CPC classification number: C07H17/08 Y02P20/55

    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 translation: 具有式(II),(III),(IV),(V),(VI),(VII),(VIII)和(IX)的抗微生物化合物; 以及其药学上可接受的盐,酯和前药; 包含这些化合物的药物组合物; 通过施用这些化合物治疗细菌感染的方法; 和化合物的制备方法。

    CONTAINER CLOSURE SYSTEM
    279.
    发明申请
    CONTAINER CLOSURE SYSTEM 审中-公开
    集装箱封闭系统

    公开(公告)号:WO1997039720A1

    公开(公告)日:1997-10-30

    申请号:PCT/US1997005882

    申请日:1997-04-09

    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 translation: 用于输送流体的容器封闭系统。 该系统包括一个用于密封容器密封的结构。 封闭构件安装在止动件的上表面上。 封闭构件包括具有上表面和下表面的底座。 封闭构件还包括外壁和从底座的上表面延伸的内壁,内壁与外壁隔开。 底座通过内壁和外壁之间的针进入口限定。 内壁在其中限定一个室。 底座进一步限定了由内壁限定的邻近腔室的孔。 刺穿构件可移动地设置在由内壁限定的室内。 刺穿构件具有第一端部和第二端部,第一端部位于止动件的近侧。 穿刺尖端安装在第一端部上并被构造成刺穿塞子。 刺穿构件的第二端部构造成接合插入到由内壁限定的室中的路厄尔。 通过穿孔构件定义通道。

    9-OXIMESILYL ERYTHROMYCIN A DERIVATIVES
    280.
    发明申请
    9-OXIMESILYL ERYTHROMYCIN A DERIVATIVES 审中-公开
    9-氧西林红霉素衍生物

    公开(公告)号:WO1997036913A1

    公开(公告)日:1997-10-09

    申请号:PCT/US1997001955

    申请日:1997-02-06

    CPC classification number: C07H17/08

    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.

    Abstract translation: 提供了使用9-肟基红霉素A衍生物制备6-O-烷基红霉素A的方法。 还提供了用于制备6-O-烷基红霉素A的9-氧化肟基和6-O-烷基红霉素A衍生物。

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