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    Substituted benzamide derivatives as glucokinase (GK) activators
    5.
    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。

    SHORT CHAIN PEPTIDOMIMETICS BASED ORALLY ACTIVE GLP 1 AGONIST AND GLUCAGON RECEPTOR ANTAGONIST
    6.
    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。

    SHORT-CHAIN PEPTIDES AS PARATHYROID HORMONE (PTH) RECEPTOR AGONIST
    7.
    发明申请
    SHORT-CHAIN PEPTIDES AS PARATHYROID HORMONE (PTH) RECEPTOR AGONIST 有权
    短链激酶（PTH）受体激动剂

    公开(公告)号：US20120108496A1

    公开(公告)日：2012-05-03

    申请号：US13259706

    申请日：2010-04-26

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

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

    IPC分类号： A61K38/10 ,  C07K7/08 ,  A61P19/10 ,  A61P31/00 ,  A61P19/02

    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之外，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

    Oxime derivatives
    9.
    发明授权
    Oxime derivatives 失效
    肟衍生物

    公开(公告)号：US08742117B2

    公开(公告)日：2014-06-03

    申请号：US13141757

    申请日：2009-12-22

    申请人： Harikishore Pingali ,  Mukul R. Jain ,  Pandurang Zaware

    发明人： Harikishore Pingali ,  Mukul R. Jain ,  Pandurang Zaware

    IPC分类号： C07D401/00 ,  A61K31/505

    CPC分类号： C07D413/14

    摘要： The present invention relates to novel oxime derivatives of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.

    摘要翻译： 本发明涉及通式（I）的新型肟衍生物，其互变异构形式，其立体异构体，其药学上可接受的盐，含有它们的药物组合物，其制备方法，这些化合物在医药中的用途以及涉及它们的中间体 制备。