6-o-substituted ketolide having antibacterial activity
    11.
    发明专利
    6-o-substituted ketolide having antibacterial activity 审中-公开
    具有抗生素活性的6-O-取代的硬脂酸乙酯

    公开(公告)号:JP2013047243A

    公开(公告)日:2013-03-07

    申请号:JP2012228250

    申请日:2012-10-15

    CPC classification number: C07H17/08 Y02P20/55

    Abstract: PROBLEM TO BE SOLVED: To provide new semi-synthesized macrolides having antibacterial activity, a pharmaceutical composition including these compounds, and a medical treatment method of remedy.SOLUTION: There is provided a 6-O-substituted erythromycin ketolide derivative expressed by formula (IV-A), where in formula, Rc is hydrogen or a hydroxy-protective group; R is a substituted methyl group; A, B, D and E are each selected from hydrogen, a 1-6C alkyl which may be substituted by a substituent, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, hydroxy, 1-6C alkoxy, and halogen of Br, Cl, F or I, or the like, under conditions that at least two of A, B, D and E are both hydrogen.

    Abstract translation: 要解决的问题:提供具有抗菌活性的新的半合成大环内酯类,包括这些化合物的药物组合物和补救药物治疗方法。 解决方案:提供由式(IV-A)表示的6-O-取代的红霉素酮内酯衍生物,其中在式中,Rc是氢或羟基保护基; R是取代的甲基; A,B,D和E各自选自氢,可被取代基取代的1-6C烷基,芳基,取代的芳基,杂芳基,取代的杂芳基,杂环烷基,羟基,1-6C烷氧基和Br的卤素, Cl,F或I等,在A,B,D和E中的至少两个都是氢的条件下。 版权所有(C)2013,JPO&INPIT

    POLYMORPHIC AND OTHER CRYSTALLINE FORM OF cis-FTC
    12.
    发明专利
    POLYMORPHIC AND OTHER CRYSTALLINE FORM OF cis-FTC 审中-公开
    顺式FTC的多晶和其他晶体形式

    公开(公告)号:JP2013040192A

    公开(公告)日:2013-02-28

    申请号:JP2012229555

    申请日:2012-10-17

    CPC classification number: C07D411/04

    Abstract: PROBLEM TO BE SOLVED: To provide new polymorphic and other crystalline forms of FTC, to provide a new method for preparing and isolating polymorphic and other crystalline forms of FTC and to provide a use of FTC polymorphic body, FTC of other phases and treatment purpose.SOLUTION: A solid phase of (-)-cis-FTC, which can be distinguished from form (I) (-)-cis-FTC by means of X-ray power diffraction pattern, thermal properties and methods of manufacture and is designated herein as amorphous (-)-FTC and (form II (-)-cis-FTC) and (form III (-)-cis FTC), is provided. Likewise, hydrated crystalline form of (±)-cis-FTC (that is, cis-FTC of racemic body) which can be distinguished from other forms of FTC by means of X-ray power diffraction pattern, thermal properties and methods of manufacture, and a dehydrated form of the hydrate are provided. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. These forms are particularly desirably used for treating HIV or hepatitis B.

    Abstract translation: 要解决的问题:提供新的多晶型和其他结晶形式的FTC,以提供制备和分离FTC的多晶型和其他结晶形式的新方法,并提供使用FTC多态体,其他阶段的FTC, 治疗目的。 解决方案:( - ) - 顺式 - FTC的固相,其可以通过X射线功率衍射图,热性质和制造方法与形式(I)( - ) - 顺式 - FTC区分开来 在本文中被指定为无定形( - ) - FTC和(形式II( - ) - 顺式 - FTC)和(形式III( - ) - 顺式FTC)。 同样地,通过X射线功率衍射图,热性质和制造方法可以与其他形式的FTC区分(±) - 顺式 - FTC(即外消旋体的顺式-FTC)的水合晶形, 并提供水合物的脱水形式。 这些FTC形式可用于制造其他形式的FTC或药物组合物。 这些形式特别适合用于治疗艾滋病毒或乙型肝炎。版权所有:(C)2013,JPO&INPIT

    Process for preparing formulation of lipid-regulating drug
    13.
    发明专利
    Process for preparing formulation of lipid-regulating drug 审中-公开
    制备脂质调节药物的方法

    公开(公告)号:JP2012149078A

    公开(公告)日:2012-08-09

    申请号:JP2012063143

    申请日:2012-03-21

    CPC classification number: A61K31/216 A61K9/1623 A61K9/1635 A61K9/1652

    Abstract: PROBLEM TO BE SOLVED: To provide small particles of lipid-regulating drugs, more preferably fenofibrate, having comparable dissolution and absorption characteristics to the particles of such drugs prepared by the prior art techniques without the need of micronizing the lipid-regulating drug or utilizing surfactants.SOLUTION: A process for preparing a formulation of a lipid-regulating drug comprises dissolving the lipid-regulating drug such as fenofibrate in a solvent free of surfactant, premixing an excipient such as lactose, starch, polyvinyl pyrrolidone, and magnesium stearate, wet granulating the drug solution/excipient mixture, drying the mixture and forming a final dosage form.

    Abstract translation: 要解决的问题:提供小颗粒的脂质调节药物,更优选非诺贝特,其具有与通过现有技术制备的这些药物的颗粒相当的溶解和吸收特性,而不需要使脂质调节药物微粉化 或利用表面活性剂。 解决方案:制备脂质调节药物的制剂的方法包括将脂质调节药物如非诺贝特溶于不含表面活性剂的溶剂中,预先混合赋形剂如乳糖,淀粉,聚乙烯吡咯烷酮和硬脂酸镁, 湿法造粒药物溶液/赋形剂混合物,干燥混合物并形成最终剂型。 版权所有(C)2012,JPO&INPIT

    Antigen construct useful in detection and identification of antibody to hiv
    14.
    发明专利
    Antigen construct useful in detection and identification of antibody to hiv 有权
    抗原结构可用于检测和鉴定抗艾滋病毒

    公开(公告)号:JP2012105649A

    公开(公告)日:2012-06-07

    申请号:JP2011272432

    申请日:2011-12-13

    Abstract: PROBLEM TO BE SOLVED: To provide a new antigen construct useful as a reagent in immunoassay for detection and identification of antibodies to human immunodeficiency virus type 1 (HIV-1) group M, HIV-1 group O and human immunodeficiency virus type 2 (HIV-2), polynucleotides useful for the preparation of antigens, DNA clone, expression vectors, and transformed host cells.SOLUTION: There are provided isolated HIV-1 group O env polypeptides obtained from the HIV-1 isolate HAM112, as well as (a) antigen constructs comprising fusions of one or more of each of HIV-1 group O env polypeptides and HIV-1 group M env polypeptide and (b) additional antigen constructs containing additional group O sequences.

    Abstract translation: 待解决的问题:提供一种新的抗原构建体,用作免疫测定中用于检测和鉴定1型人类免疫缺陷病毒(HIV-1)组M,HIV-1组O和人类免疫缺陷病毒类型的抗体的试剂 2(HIV-2),可用于制备抗原的多核苷酸,DNA克隆,表达载体和转化的宿主细胞。 提供了从HIV-1分离株HAM112获得的分离的HIV-1组O env多肽的分离株,以及(a)包含HIV-1基因O型多肽中的一种或多种的融合物的抗原构建体, HIV-1组M env多肽和(b)另外的含有另外的O组的抗原构建体。 版权所有(C)2012,JPO&INPIT

    Noninvasive measurement instrument
    16.
    发明专利
    Noninvasive measurement instrument 有权
    非测量仪器

    公开(公告)号:JP2012045429A

    公开(公告)日:2012-03-08

    申请号:JP2011267232

    申请日:2011-12-06

    Abstract: PROBLEM TO BE SOLVED: To improve calibration accuracy to seasonal and psychological variation of tissue property.SOLUTION: A noninvasive measurement instrument has a measurement probe 1 supposed to get into touch with a trial subject, a light source 6 and a photodetector 7 to be connected to the measurement probe, and a computer section 5 for controlling the light source and photodetector to optically and noninvasively measure information relating to glucose in the trial subject and predict the value of glucose by a calibration model from an output of the photodetector. The computer section updates the calibration model by executing regression estimation based on the acquired data by noninvasive measurement on a different day and the corresponding reference measurement value and predicts glucose density from the acquired data by noninvasive measurement by using the updated calibration model.

    Abstract translation: 要解决的问题:提高校准精度对组织属性的季节和心理变化。 解决方案:无创测量仪器具有测试探头1,该测量探针1应与试验对象接触,要连接到测量探针的光源6和光电检测器7以及用于控制光源的计算机部分5 光电检测器光学和非侵入性地测量与试验对象中的葡萄糖相关的信息,并且通过来自光电检测器的输出的校准模型预测葡萄糖的值。 计算机部分通过基于所获取的数据通过不同日期的无创测量和相应的参考测量值执行回归估计来更新校准模型,并且通过使用更新的校准模型通过非侵入式测量从所获取的数据中预测葡萄糖浓度。 版权所有(C)2012,JPO&INPIT

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