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13 条记录 (耗时 0.031 秒)

    Short-chain peptides as parathyroid hormone (PTH) receptor agonist
    1.
    发明授权
    Short-chain peptides as parathyroid hormone (PTH) receptor agonist 有权
    短链肽作为甲状旁腺激素（PTH）受体激动剂

    公开(公告)号：US08383581B2

    公开(公告)日：2013-02-26

    申请号：US13259706

    申请日：2010-04-26

    申请人： Rajesh Bahekar ,  Mukul R. Jain ,  Pankaj R. Patel

    发明人： Rajesh Bahekar ,  Mukul R. Jain ,  Pankaj R. Patel

    IPC分类号： A61K38/29

    CPC分类号： C07K14/635 ,  A61K38/00

    摘要： The present invention provides novel short-chain peptides, which primarily act as parathyroid hormone (PTH/PTH-1) receptor agonist. These short-chain peptides exhibit increased stability to proteolytic cleavage. Most of short-chain peptides were found to be stable in rat plasma up to 24 hours (in vitro), showed increased stability against GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes (in vitro). Due to increased metabolic stability, other than parenteral route of administration, some of the short-chain peptides can also be delivered by oral routes of administration, for the treatment/prevention of hypoparathyroidism and diseases characterized by bone mass reduction, such as osteoporosis, postmenopausal osteoporosis and for stimulating bone repair. A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z12-Z13-Z14-Z15-B

    摘要翻译： 本发明提供了主要作为甲状旁腺激素（PTH / PTH-1）受体激动剂的新型短链肽。 这些短链肽表现出增加的蛋白水解切割的稳定性。 发现大多数短链肽在大鼠血浆中稳定至多24小时（体外），显示出对GIT酶如胃蛋白酶和酸性胃pH以及针对肝微粒体（体外）的稳定性增加。 由于代谢稳定性增加，除了肠胃外给药途径外，一些短链肽也可以通过口服给药途径递送，用于治疗/预防甲状旁腺功能减退症和以骨量减少为特征的疾病，如骨质疏松症，绝经后 骨质疏松症和刺激骨修复。 A-Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8-Z9-Z10-Z11-Z12-Z13-Z14-Z15-B

    SHORT CHAIN PEPTIDOMIMETICS BASED ORALLY ACTIVE GLP 1 AGONIST AND GLUCAGON RECEPTOR ANTAGONIST
    2.
    发明申请
    SHORT CHAIN PEPTIDOMIMETICS BASED ORALLY ACTIVE GLP 1 AGONIST AND GLUCAGON RECEPTOR ANTAGONIST 审中-公开
    短链基团基于ORAGY活性GLP 1激动剂和GLUCAGON受体拮抗剂

    公开(公告)号：US20120264685A1

    公开(公告)日：2012-10-18

    申请号：US13502826

    申请日：2010-10-18

    申请人： Rajesh Bahekar ,  Mukul R. Jain ,  Pankaj R. Patel

    发明人： Rajesh Bahekar ,  Mukul R. Jain ,  Pankaj R. Patel

    IPC分类号： C07K7/08 ,  A61P17/02 ,  A61P3/10 ,  A61P3/00 ,  A61K38/10 ,  A61P3/06

    CPC分类号： C07K14/605 ,  A61K38/00

    摘要： The present invention provides novel short chain peptidomimetics, which act as GLP-1 receptors agonist and glucagon receptor antagonist. These dual acting peptidomimetics exhibit increased stability to proteolytic cleavage, especially against DPP-IV (Dipeptidyl peptidase-IV) enzyme, GIT enzymes such as pepsin and acidic stomach pH and also against liver microsomes (in vitro). Due to increased metabolic stability, other than parenteral route of administration, these short chain peptidomimetics can be delivered by oral routes of administration, for the treatment or prevention of diabetes and related metabolic disorders, such as obesity, hyperlipidemia and eating disorders.

    摘要翻译： 本发明提供新的短链肽模拟物，其作为GLP-1受体激动剂和胰高血糖素受体拮抗剂。 这些双重作用的肽模拟物表现出增加的蛋白水解切割的稳定性，特别是对DPP-IV（二肽基肽酶-IV）酶，GIT酶如胃蛋白酶和酸性胃pH以及针对肝微粒体（体外）的稳定性。 由于代谢稳定性增加，除了肠胃外给药途径之外，这些短链肽模拟物可以通过口服给药途径递送，用于治疗或预防糖尿病和相关的代谢紊乱，例如肥胖，高脂血症和进食障碍。

    Substituted benzamide derivatives as glucokinase (GK) activators
    3.
    发明授权
    Substituted benzamide derivatives as glucokinase (GK) activators 有权
    取代的苯甲酰胺衍生物作为葡萄糖激酶（GK）激活剂

    公开(公告)号：US08835469B2

    公开(公告)日：2014-09-16

    申请号：US13387885

    申请日：2010-07-22

    申请人： Rajendra Kharul ,  Mukul R. Jain ,  Pankaj R. Patel

    发明人： Rajendra Kharul ,  Mukul R. Jain ,  Pankaj R. Patel

    IPC分类号： C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61K31/428 ,  A61K31/496

    CPC分类号： C07D417/14 ,  C07D413/12 ,  C07D413/14

    摘要： The present invention relates to substituted benzamide derivatives of the Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.

    摘要翻译： 本发明涉及式I的取代苯甲酰胺衍生物及其药学上可接受的盐，药学上可接受的溶剂合物，对映异构体，非对映异构体，前药，代谢物和多晶型物，并且可用于治疗由葡萄糖激酶介导的疾病状态。 本文公开的化合物可用于降低血糖水平和用于增加用于治疗II型糖尿病的胰岛素分泌。 本发明还涉及制备本发明化合物的方法，含有这些化合物的药物组合物及其用途。

    Display apparatus for recording and/or playback device
    6.
    发明授权
    Display apparatus for recording and/or playback device 失效
    用于记录和/或播放装置的显示装置

    公开(公告)号：US4410923A

    公开(公告)日：1983-10-18

    申请号：US223718

    申请日：1981-01-09

    申请人： Pankaj R. Patel

    发明人： Pankaj R. Patel

    IPC分类号： G11B27/13 ,  G11B27/28 ,  G11B27/34 ,  G11B17/00 ,  G11B15/18 ,  G11B19/02 ,  G11B21/12

    CPC分类号： G11B27/13 ,  G11B27/28 ,  G11B27/34 ,  G11B2220/90

    摘要： Display apparatus is provided for a recording and/or playback device of the type having a movable record medium upon which cue signals may be recorded to indicate an end of "letter", an "instruction" or the like. A linear array of light indicating elements is selectively energized to provide a cursor indication of the present position of the record medium as it is moved relative to a reference position. Selected ones of these elements also are energized in response to the recording or playback of a cue signal to indicate the relative locations of the cue signals on the record medium. In one embodiment, a numerical display also is provided to indicate a time-related quantity of record medium which has been transported during a recording or playback operation. If the record medium is, for example, a magnetic tape transported from a supply reel to a take-up reel, motion pulses are generated as the tape is transported. Although the frequency of such motion pulses changes as the quantity of tape remaining on the supply reel changes, such pulses are counted in a "linearized" manner such that the numerical display is a linear representation of time that has been either consumed or that remains available for further use. In a preferred embodiment, prior to carrying out a transcribe operation, the recording medium is scanned to ascertain the presence of cue signals thereon; and appropriate ones of the light indicating elements are energized such that, at the completion of the scanning operation, the relative locations of the previously recorded cue signals are displayed. Preferably, during a transcribe operation, the numerical display indicates the quantity of time remaining between the cursor position and the immediately-following cue signal location.

    摘要翻译： 提供了一种用于具有可移动记录介质的类型的记录和/或重放装置的显示装置，在该可移动记录介质上可以记录提示信号以指示“信”的结尾，“指令”等。 选择性地激励光指示元件的线性阵列，以便在记录介质相对于参考位置移动时提供当前位置的光标指示。 响应于提示信号的记录或重放，这些元件中的选定的元件也被激励以指示记录介质上的提示信号的相对位置。 在一个实施例中，还提供数字显示器来指示在记录或重放操作期间已被传送的记录介质的时间相关量。 如果记录介质是例如从供带盘传送到卷取卷轴的磁带，则在传送带时产生运动脉冲。 虽然这样的运动脉冲的频率随着供应卷轴上剩下的带的数量而改变，但是这样的脉冲以“线性化”的方式被计数，使得数字显示是已经被消耗或保持可用的时间的线性表示 供进一步使用。 在优选实施例中，在执行转录操作之前，扫描记录介质以确定其上的提示信号的存在; 并且适当的指示元件被激励，使得在完成扫描操作时，显示先前记录的提示信号的相对位置。 优选地，在转录操作期间，数字显示指示在光标位置和紧跟着的提示信号位置之间剩余的时间量。