AZOLE COMPOUNDS USED AS TUBERCULOSTATIC AND LEISHMANICIDE AGENTS
    1.
    发明申请
    AZOLE COMPOUNDS USED AS TUBERCULOSTATIC AND LEISHMANICIDE AGENTS 有权
    用作溶液和稀土助剂的AZOLE化合物

    公开(公告)号:US20110269803A1

    公开(公告)日:2011-11-03

    申请号:US12981315

    申请日:2010-12-29

    摘要: This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII. where: X is an atom of “C” or “N” where X is “N” the radicals do triazole ring are represented by: R1=COR2, CSR3, CN(R4)R5 or CF2R6; R2=H, NHNH2, alkyl, aryl substituted or not, OH, NR7R8 or OR9 R3=alkyl or aryl substituted or not R4=H, OH, alkyl or aryl substituted or not R5=R6=R7=R8=R9=R10=H, alkyl or aryl substituted or not where X is “C” the radicals do imidazolic ring are represented by: R1=COR2 R2=NHNH2, OH, OR3, or NR4R5 R3=alkyl or aryl substituted or not R4=R5=H, alkyl or aryl substituted or not R10=NHR6 or NR6R7 R6=R7=COR8 R8=aryl substituted or not while radical Rn can be located in any one or in more than one of the carbon atoms of the aromatic ring, and these radicals can be equal or different, represented by hydrogen, alkylic groups with 1 or more carbon atoms in a linear or branched chain alkenes or alkynes, hydroxyl, hydroxyalkyl or oxygenated functions in acyclic or cyclic systems forming an heterocyclic ring, free or substituted amines, thioalkyl, donators and/or removing groupings of electrons or halogens, thus “n” can vary from 1 to 5. This invention also refers to a pharmaceutical composition comprising, as active principle, at least one of the azole compounds represented by the general formula VIII, to the use of such compositions and to method of treatment or inhibition de tuberculosis and leishmaniasis.

    摘要翻译: 本发明涉及由通式VIII表示的化合物族中包括的新的1,2,3-三唑和咪唑化合物。 其中:X为“C”或“N”的原子,其中X为“N”,自由基为三唑环表示为:R1 = COR2,CSR3,CN(R4)R5或CF2R6; R 2 = H,NHNH 2,烷基,被取代或未取代的芳基,OH,NR 7 R 8或OR 9 R 3 =被取代或未取代的烷基或芳基R 4 = H,OH,烷基或芳基被取代或未被取代。R5 = R6 = R7 = R8 = R9 = H,烷基或芳基被取代或不取代,其中X为“C”的基团为咪唑环,其表示为:R1 = COR2 R2 = NHNH2,OH,OR3或NR4R5 R3 =烷基或芳基被取代或未取代R4 = R5 = 烷基或芳基被取代或未取代R 10 = NHR 6或NR 6 R 7 R 6 = R 7 = COR 8 R 8 =芳基被取代或未取代,而基团Rn可以位于芳环的任何一个或多于一个碳原子中,并且这些基团可以是 相同或不同的,由氢代表,直链或支链烯烃或炔烃中具有一个或多个碳原子的烷基,在形成杂环的无环或环状体系中的羟基,羟烷基或氧化官能团,游离或取代的胺,硫代烷基, 和/或去除电子或卤素的分组,因此“n”可以在1至5之间变化。本发明还涉及药物组合物 作为活性成分,本发明包含至少一种由通式VIII表示的唑类化合物,使用这种组合物以及治疗或抑制结核病和利什曼病的方法。

    PROCESS FOR ISOLATING PHYSALINS FROM PLANTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING PHYSALINS
    6.
    发明申请
    PROCESS FOR ISOLATING PHYSALINS FROM PLANTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING PHYSALINS 有权
    从植物中分离物质的方法和含有PHYSALINS的药物组合物

    公开(公告)号:US20050101519A1

    公开(公告)日:2005-05-12

    申请号:US10403003

    申请日:2003-04-01

    摘要: The present invention relates to a process for obtaining Physalis angulata extracts, particularly to isolate ergostane-type steroidal derivatives, such as physalins, which are useful in the treatment of infections caused by protozoans. The physalins of the invention have also prophylactic and therapeutic properties for treating auto-immune diseases in mammals. The isolation process to obtain physalins comprises the steps of: (a) grinding roots, leaves or stem-bark of Physalis ssp; (b) extracting the material obtained in step (a) with solvents selected from the group consisting of water and alcohols, such as methanol, ethanol, 1-propanol, 2-propanol, isobutanol; (c) evaporating the extract obtained in step (b) and washing the syrup material with a suitable solvent; (d) rapid filtering of the extract of step (c) and fractionating the components of the extract according to a polarity gradient of organic solvents; and (e) separating the steroidal components contained in the fractions by chromatography.

    摘要翻译: 本发明涉及一种用于获得肌ata提取物的方法,特别是用于分离麦角甾烷型甾体衍生物,例如生物素,其可用于治疗由原生动物引起的感染。 本发明的生理素还具有治疗哺乳动物自身免疫疾病的预防和治疗特性。 获得物质的分离过程包括以下步骤:(a)研磨Physalis ssp的根,叶或茎皮; (b)用选自水和醇的溶剂如甲醇,乙醇,1-丙醇,2-丙醇,异丁醇萃取步骤(a)得到的物质; (c)蒸发步骤(b)中获得的提取物并用合适的溶剂洗涤糖浆料; (d)快速过滤步骤(c)的提取物,并根据有机溶剂的极性梯度对提取物的组分进行分级; 和(e)通过色谱法分离所述级分中所含的甾体组分。

    Method for the Detection of Microorganisms by Fiber Optics
    7.
    发明申请
    Method for the Detection of Microorganisms by Fiber Optics 审中-公开
    光纤检测微生物的方法

    公开(公告)号:US20040076358A1

    公开(公告)日:2004-04-22

    申请号:US10721510

    申请日:2003-11-26

    IPC分类号: G02B006/00 G02B006/26

    摘要: The objective of the present invention is the detection/monitoring of microorganisms present in the air, water or foodstuffs through the use of a fiber optic biosensor with an evanescent-field. A first concretization of the present invention concerns a method for detection of contamination by specific microorganisms through the use of the evanescent-field of a sensitive fiber optic characterized by stages of: a) exposing the evanescent-field of the sensitive fiber optic using an appropriate technique based on physical and chemical properties; (b) permitting immediate contact of the exposed evanescent-field obtained in the stage (a) with the sample to be examined, with the aforementioned sample having a form adequate so as to obtain the generation of an optical signal in response to the presence of microorganisms in the sample; and, (c) demodulating the optical signal generated in stage (b) and using this value to quantify the microorganisms through an appropriate method. In a second concretization, the invention is directed to a composition for use in the detection of microorganisms characterized by comprising a selective culture medium for microorganisms needing to be detected and reactants capable of altering the properties of the medium to favor the interaction of the system fiber-microorganism interaction. In a third concretization the invention refers to a device for surveying microorganisms through the insertion of a sensitive fiber optic (11), with an adequately exposed evanescent-field, into a surface or volume of a biological culture medium (12) specific for the microorganism to be detected, comprising a demodulation system based on a fiber optic circuit and related components.

    摘要翻译: 本发明的目的是通过使用具有ev逝场的光纤生物传感器来检测/监测存在于空气,水或食品中的微生物。 本发明的第一具体化涉及通过使用敏感光纤的ev逝场来检测特定微生物的污染物的方法,其特征在于以下步骤:a)使用适当的方法暴露敏感光纤的消逝场 基于物理化学性质的技术; (b)允许将阶段(a)中获得的暴露的消逝场与被检样本立即接触,上述样本具有足够的形式,以便响应于存在的方式获得光信号的产生 样品中的微生物; (c)解调在阶段(b)中产生的光学信号,并使用该值通过适当的方法定量微生物。 在第二个具体实施方案中,本发明涉及用于检测微生物的组合物,其特征在于包括需要检测的微生物的选择性培养基和能够改变培养基的性质以有利于系统纤维相互作用的反应物 - 微生物相互作用。 在第三具体化中,本发明涉及一种用于通过将具有充分暴露的消逝场的敏感光纤(11)插入到微生物特异性的生物培养基(12)的表面或体积中来测量微生物的装置 包括基于光纤电路和相关部件的解调系统。

    COMPOUNDS DERIVED FROM ARTESUNATE, PREPARATION PROCESS, PHARMACEUTICAL COMPOSITION AND USE OF THE RESPECTIVE MEDICINE
    8.
    发明申请
    COMPOUNDS DERIVED FROM ARTESUNATE, PREPARATION PROCESS, PHARMACEUTICAL COMPOSITION AND USE OF THE RESPECTIVE MEDICINE 审中-公开
    从ARTESUNATE衍生的化合物,制备过程,药物组合物和使用相关药物

    公开(公告)号:US20120129887A1

    公开(公告)日:2012-05-24

    申请号:US13296155

    申请日:2011-11-14

    摘要: The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R1, R2, R3, R4, R5, and R6 in formula (II) are represented by: R1═H, CF3, CH3, OCH3, NH2, halogen; R2═H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3═H, m-OC6H4CF3, NH2; R4═H, CH3, OCH3, NH2, halogen; R5═H, CH3, CF3, NH2, halogen; R6═H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3)(CH2)3NH2; R7═(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3, (CH2)6, (CH2)8, (CH2)10, (CH2)12; R8═CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3. This invention also refers to a process of preparation of these compounds (formula I), and antiparasitic pharmaceutical compositions thereof.

    摘要翻译: 本发明涉及由通式(I)表示的新化合物,其中X由通式(II)表示,Y由通式(III)表示。 关系X至Y可以从1:1到1:7变化。 式(II)中的基团R 1,R 2,R 3,R 4,R 5和R 6表示为:R 1 = H,CF 3,CH 3,OCH 3,NH 2,卤素; (CH 2)2 N(C 2 H 5)(CH 2 CH 2 OH),CH(OH) R3 = H,m-OC6H4CF3,NH2; R4 = H,CH 3,OCH 3,NH 2,卤素; R5 = H,CH3,CF3,NH2,卤素; R6 = H,CF3,CH3,NH2,卤素,NH-R8-N-(C2H5)2,NHCH(CH3)(CH2)3NH2; (CH2)2,(CH2)3,CHCH3CH2,(CH2)4,(CH2)5,CHCH3(CH2)3,(CH2)6,(CH2)8,(CH2) R8 = CHCH3(CH2)3,CHCH3(CH2)CHCH3,(CH2)2,(CH2)3,(CH2)6,(CH2)3O(CH2) 本发明还涉及制备这些化合物(式I)的方法及其抗寄生虫药物组合物。

    Helminth-derived antigens having capacity of providing protection against parasites
    9.
    发明授权
    Helminth-derived antigens having capacity of providing protection against parasites 有权
    蠕虫衍生的抗原具有提供针对寄生虫的保护的能力

    公开(公告)号:US07534437B2

    公开(公告)日:2009-05-19

    申请号:US10544035

    申请日:2004-01-30

    摘要: The primary objective of the present invention is the development of new mutant forms of the Sm14 protein, for producing a greater production volume. The recombinant proteins here obtained were capable of providing protection against schistosome and fasciola infection. The level of protection of Sm14 recombinant proteins obtained in the present invention was similar to that reached in the parasite saline extract. The mutant proteins of the present invention have reached approximately 100% of renaturation after the heating at 80° C., different from wild forms of the Sm14 protein. Moreover, after storage for 2 months at 4° C., mutant proteins have shown smaller β-structure loss than wild forms that have shown formation with random structure, as demonstrated by the circular dichroism analysis, indicating the success of mutations.

    摘要翻译: 本发明的主要目的是开发新的突变形式的Sm14蛋白,用于产生更大的产量。 这里获得的重组蛋白能够提供针对血吸虫病和fasciola感染的保护。 在本发明中获得的Sm14重组蛋白的保护水平与寄生盐水提取物中达到的相似。 本发明的突变型蛋白质在80℃加热后与Sm14蛋白的野生型不同,达到约100%的复性。 此外,在4℃下保存2个月后,突变蛋白质显示比野生形式更小的β-结构损失,其显示出随机结构的形成,如通过圆二色性分析所证实的,表明突变的成功。