Ethanoic acid derivatives as dipeptidyl peptidase inhibitors
    2.
    发明申请
    Ethanoic acid derivatives as dipeptidyl peptidase inhibitors 审中-公开
    乙酸衍生物作为二肽基肽酶抑制剂

    公开(公告)号:US20070232573A1

    公开(公告)日:2007-10-04

    申请号:US11714634

    申请日:2007-03-06

    摘要: The present invention is directed to novel Ethanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, particularly in the treatment of type 2 diabetes and conditions that are associated with the same. In addition, the present invention provides pharmaceutical compositions useful in inhibiting DPP-IV enzyme, comprising a therapeutically effective amount of Ethanoic acid derivatives. Moreover, the present invention provides a method of inhibiting DPP-IV comprising administering to a mammal in need of such treatment a therapeutically effective amount of a single or a combination of Ethanoic acid derivatives of the invention. The invention further relates to the kits and other articles of manufacture for treating disease states associated with DPP-IV enzyme. The invention further relates to a method of identifying a compound that has dipeptidyl peptidase-IV enzyme inhibition activity, comprising following steps: 1. Define the residues of the active site of DPP-IV 2. Define the geometry and force field relationship of the residues identified above in (1) 3. Define the physical parameters of the active site identified in (1) 4. Validate the model based on mutational analysis and in-vitro inhibitor binding studies 5. Screen the library for scaffolds and small molecules that satisfy the model developed in (3) and validated in (4) above. 6. Dock each inhibitor identified in (5) above to the active site of DPP-IV defined in (1). 7. Minimize the energy of the inhibitor and DPP-IV complex using force fields used in (2) above. 8. Compare the energy of interaction of each inhibitor to that of known inhibitors. 9. Synthesize and validate in in-vitro assays

    摘要翻译: 本发明涉及作为二肽基肽酶-IV酶(“DPP-IV抑制剂”)的抑制剂的新型乙酸衍生物,其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病, 特别是在治疗2型糖尿病和与之相关的病症方面。 此外,本发明提供了可用于抑制DPP-IV酶的药物组合物,其包含治疗有效量的乙酸衍生物。 此外,本发明提供抑制DPP-IV的方法,包括向需要这种治疗的哺乳动物施用治疗有效量的本发明的乙酸衍生物的单一或组合。 本发明还涉及用于治疗与DPP-IV酶相关的疾病状态的试剂盒和其它制品。 本发明还涉及鉴定具有二肽基肽酶-IV酶抑制活性的化合物的方法,包括以下步骤:1.定义DPP-IV的活性位点的残基2.定义残基的几何形状和力场关系 (1)中确定的活性位点的物理参数定义(1)中确定的活性位点的物理参数4.基于突变分析和体外抑制剂结合研究验证模型5.筛选满足以下条件的支架和小分子的文库 (3)中开发并在上述(4)中验证的模型。 6.将上述(5)中鉴定的每种抑制剂停留在(1)中定义的DPP-IV的活性位点。 7.使用上述(2)中使用的力场,最小化抑制剂和DPP-IV复合物的能量。 8.比较每个抑制剂与已知抑制剂相互作用的能量。 9.在体外测定中合成和验证

    Heptanoic acid derivatives as dipeptidyl peptidase inhibitors
    3.
    发明申请
    Heptanoic acid derivatives as dipeptidyl peptidase inhibitors 审中-公开
    庚酸衍生物作为二肽基肽酶抑制剂

    公开(公告)号:US20080020971A1

    公开(公告)日:2008-01-24

    申请号:US11714404

    申请日:2007-03-06

    CPC分类号: C07C53/00

    摘要: The present invention is directed to novel heptanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, particularly in the treatment of type 2 diabetes and conditions that are associated with the same. In addition, the present invention provides pharmaceutical compositions useful in inhibiting DPP-IV enzyme, comprising a therapeutically effective amount of heptanoic acid derivatives. Moreover, the present invention provides a method of inhibiting DPP-IV comprising administering to a mammal in need of such treatment a therapeutically effective amount of a single or a combination of heptanoic acid derivatives of the invention. The invention further relates to the kits and other articles of manufacture for treating disease states associated with DPP-IV enzyme. The invention further relates to a method of identifying a compound that has dipeptidyl peptidase-IV enzyme inhibition activity, comprising following steps: 1. Define the residues of the active site of DPP-IV 2. Define the geometry and force field relationship of the residues identified above in (1) 3. Define the physical parameters of the active site identified in (I) 4. Validate the model based on mutational analysis and in-vitro inhibitor binding studies 5. Screen the library for scaffolds and small molecules that satisfy the model developed in (3) and validated in (4) above. 6. Dock each inhibitor identified in (5) above to the active site of DPP-IV defined in (I). 7. Minimize the energy of the inhibitor and DPP-IV complex using force fields used in (2) above. 8. Compare the energy of interaction of each inhibitor to that of known inhibitors. 9. Synthesize and validate in in-vitro assays

    摘要翻译: 本发明涉及作为二肽基肽酶-IV酶抑制剂的新型庚酸衍生物(“DPP-IV抑制剂”),其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病, 特别是在治疗2型糖尿病和与之相关的病症方面。 此外,本发明提供了可用于抑制DPP-IV酶的药物组合物,其包含治疗有效量的庚酸衍生物。 此外,本发明提供了抑制DPP-IV的方法,包括向需要这种治疗的哺乳动物施用治疗有效量的本发明的庚酸衍生物的单一或组合。 本发明还涉及用于治疗与DPP-IV酶相关的疾病状态的试剂盒和其它制品。 本发明还涉及鉴定具有二肽基肽酶-IV酶抑制活性的化合物的方法,包括以下步骤:1.定义DPP-IV的活性位点的残基2.定义残基的几何形状和力场关系 (1)中确定的活性位点的物理参数定义(I)中确定的活性位点的物理参数4.基于突变分析和体外抑制剂结合研究验证模型5.筛选满足以下条件的支架和小分子的文库 (3)中开发并在上述(4)中验证的模型。 6.将上述(5)中鉴定的每种抑制剂停留在(I)中定义的DPP-IV的活性位点。 7.使用上述(2)中使用的力场,最小化抑制剂和DPP-IV复合物的能量。 8.比较每个抑制剂与已知抑制剂相互作用的能量。 9.在体外测定中合成和验证

    Rice conferring resistance to environmental stress by targeting mnsod to the chloroplast
    4.
    发明申请
    Rice conferring resistance to environmental stress by targeting mnsod to the chloroplast 失效
    水稻通过将mnsod靶向叶绿体来赋予对环境胁迫的抵抗力

    公开(公告)号:US20070006349A1

    公开(公告)日:2007-01-04

    申请号:US10552887

    申请日:2002-12-09

    申请人: Villoo Patell

    发明人: Villoo Patell

    IPC分类号: A01H1/00 A01H5/00

    摘要: The present invention relates to the induction of the endogenous MnSOD expression in the Chloroplast which is ravages by reactive oxygen species ain one or more compartments of the plant cells and provides the means and wherewithal of cultivating crops in areas where it would not otherwise grow normally on account of environmental stress conditions inclusive of high and low temperatures, drought and ultra violet light, is resistant to herbicides thereby resulting in an increase in yield and also improved crop quality.

    摘要翻译: 本发明涉及在叶绿体中诱导内源性MnSOD表达,其中植物细胞的一个或多个区室受到活性氧的影响,并且提供了在其不能正常生长的区域中种植作物的方法和途径 考虑到包括高低温,干旱和紫外光在内的环境胁迫条件对除草剂具有抗性,从而导致产量增加,并且还提高了作物品质。

    Process for constructing dna based molecular marker for enabling selection of drought and diseases resistant germplasm screening
    5.
    发明申请
    Process for constructing dna based molecular marker for enabling selection of drought and diseases resistant germplasm screening 审中-公开
    构建基于dna的分子标记物的方法,用于选择干旱和抗病种质筛选

    公开(公告)号:US20050032050A1

    公开(公告)日:2005-02-10

    申请号:US10204849

    申请日:2001-02-26

    摘要: This invention relates to a process for constructing DNA-based molecular markers in plants comprising: identifying and selecting the gene sequences relating to stress from available database and literature; submitting the selected gene sequence for similarity search to obtain other sequences from the database similar to the selected gene sequence; subjecting the sequences obtained from similarity search to multiple alignment; removing redundant sequences if any, to get a data set of proteins involved in biotic and abiotic stress response; picking blocks or motifs from the data set of proteins on basis of statistical significance; subjecting the data set of proteins to Blockmaker to pick the same set of blocks or motifs; analysing the motifs for the functionality.

    摘要翻译: 本发明涉及一种在植物中构建基于DNA的分子标记物的方法,包括:鉴定和选择与可利用的数据库和文献中的压力有关的基因序列; 提交所选择的基因序列进行相似性检索,以从数据库中获得与选择的基因序列相似的其他序列; 对从相似性检索获得的序列进行多重比对; 去除冗余序列,如果有的话,得到参与生物和非生物胁迫反应的蛋白质的数据集; 基于统计学意义从蛋白质数据集中挑选块或基序; 将蛋白质的数据集传递给Blockmaker以选择相同的一组块或基序; 分析功能的图案。

    Construction of a Comparative Database and Identification of Virulence Factors Comparison of Polymorphic Regions in Clinical Isolates of Infectious Organisms
    6.
    发明申请
    Construction of a Comparative Database and Identification of Virulence Factors Comparison of Polymorphic Regions in Clinical Isolates of Infectious Organisms 审中-公开
    构建比较数据库和确定感染生物临床分离株中多态性区域的毒力因子比较

    公开(公告)号:US20080085284A1

    公开(公告)日:2008-04-10

    申请号:US11632108

    申请日:2007-04-09

    CPC分类号: C12Q1/689 C12Q2600/156

    摘要: The present invention is directed to novel nucleotide sequences to be used for diagnosis, identification of the strain, typing of the strain and giving orientation to its potential degree of virulence, infectivity and/or latency for all infectious diseases more particularly tuberculosis. The present invention also includes method for the identification and selection of polymorphisms associated with the virulence' and/or infectivity in infectious diseases more particularly in tuberculosis by a comparative genomic analysis of the sequences of different clinical isolates/strains of infectious organisms. The regions of polymorphisms, can also act as potential drug targets and vaccine targets. More particularly, the invention also relates to identifying virulence factors of M. tuberculosis strains and other infectious organisms to be included in a diagnostic DNA chip allowing identification of the strain, typing of the strain and finally giving orientation to its potential degree of virulence. Although the present invention has been illustrated with specific reference to the polymorphic region in the Mycobacterium tuberculosis, the said invention is not to be understood and construed as being limited to Tuberculosis but is applicable to all infectious diseases.

    摘要翻译: 本发明涉及新的核苷酸序列,用于诊断,鉴定菌株,分型和赋予其潜在的毒力程度,感染性和/或所有感染性疾病特别是结核病的潜伏期的方向。 本发明还包括通过对不同临床分离株/感染生物菌株的序列的比较基因组分析来鉴定和选择与感染性疾病相关的多态性和/或感染性疾病更特别地在结核病中的方法。 多态性区域也可以作为潜在的药物靶点和疫苗靶点。 更具体地说,本发明还涉及鉴定要包括在诊断DNA芯片中的结核分枝杆菌菌株和其他感染性生物体的毒力因子,其允许鉴定菌株,分型并最终赋予其潜在的毒力程度。 虽然已经具体参考结核分枝杆菌中的多态性区域来说明了本发明,但是本发明不被理解为并且被解释为限于结核病,而是适用于所有感染性疾病。

    Hexanoic acid derivatives as dipeptidyl peptidase inhibitors
    7.
    发明申请
    Hexanoic acid derivatives as dipeptidyl peptidase inhibitors 审中-公开
    己酸衍生物作为二肽基肽酶抑制剂

    公开(公告)号:US20080051452A1

    公开(公告)日:2008-02-28

    申请号:US11714584

    申请日:2007-03-06

    CPC分类号: C07C323/60

    摘要: The present invention is directed to novel hexanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, particularly in the treatment of type 2 diabetes and conditions that are associated with the same. In addition, the present invention provides pharmaceutical compositions useful in inhibiting DPP-IV enzyme, comprising a therapeutically effective amount of hexanoic acid derivatives. Moreover, the present invention provides a method of inhibiting DPP-IV comprising administering to a mammal in need of such treatment a therapeutically effective amount of a single or a combination of hexanoic acid derivatives of the invention. The invention further relates to the kits and other articles of manufacture for treating disease states associated with DPP-IV enzyme. The invention further relates to a method of identifying a compound that has dipeptidyl peptidase-IV enzyme inhibition activity, comprising following steps: 1. Define the residues of the active site of DPP-IV 2. Define the geometry and force field relationship of the residues identified above in (I) 3. Define the physical parameters of the active site identified in (1) 4. Validate the model based on mutational analysis and in-vitro inhibitor binding studies 5. Screen the library for scaffolds and small molecules that satisfy the model developed in (3) and validated in (4) above. 6. Dock each inhibitor identified in (5) above to the active site of DPP-IV defined in (1). 7. Minimize the energy of the inhibitor and DPP-IV complex using force fields used in (2) above. 8. Compare the energy of interaction of each inhibitor to that of known inhibitors. 9. Synthesize and validate in in-vitro assays

    摘要翻译: 本发明涉及作为二肽基肽酶-IV酶(“DPP-IV抑制剂”)的抑制剂的新型己酸衍生物,其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病, 特别是在治疗2型糖尿病和与之相关的病症方面。 此外,本发明提供了可用于抑制DPP-IV酶的药物组合物,其包含治疗有效量的己酸衍生物。 此外,本发明提供抑制DPP-IV的方法,包括向需要这种治疗的哺乳动物施用治疗有效量的本发明的己酸衍生物的单一或组合。 本发明还涉及用于治疗与DPP-IV酶相关的疾病状态的试剂盒和其它制品。 本发明还涉及鉴定具有二肽基肽酶-IV酶抑制活性的化合物的方法,包括以下步骤:1.定义DPP-IV的活性位点的残基2.定义残基的几何形状和力场关系 (1)中确定的活性位点的物理参数4.确定基于突变分析和体外抑制剂结合研究的模型5.筛选满足以下条件的支架和小分子的文库 (3)中开发并在上述(4)中验证的模型。 6.将上述(5)中鉴定的每种抑制剂停留在(1)中定义的DPP-IV的活性位点。 7.使用上述(2)中使用的力场,最小化抑制剂和DPP-IV复合物的能量。 8.比较每个抑制剂与已知抑制剂相互作用的能量。 9.在体外测定中合成和验证

    Nananoic acid derivatives as dipeptidyl peptidase inhibitors
    8.
    发明申请
    Nananoic acid derivatives as dipeptidyl peptidase inhibitors 审中-公开
    纳米酸衍生物作为二肽基肽酶抑制剂

    公开(公告)号:US20070270492A1

    公开(公告)日:2007-11-22

    申请号:US11714635

    申请日:2007-03-06

    摘要: The present invention is directed to novel nananoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, particularly in the treatment of type 2 diabetes and conditions that are associated with the same. In addition, the present invention provides pharmaceutical compositions useful in inhibiting DPP-IV enzyme, comprising a therapeutically effective amount of nananoic acid derivatives. Moreover, the present invention provides a method of inhibiting DPP-IV comprising administering to a mammal in need of such treatment a therapeutically effective amount of a single or a combination of nananoic acid derivatives of the invention. The invention further relates to the kits and other articles of manufacture for treating disease states associated with DPP-IV enzyme. The invention further relates to a method of identifying a compound that has dipeptidyl peptidase-IV enzyme inhibition activity, comprising following steps: 1. Define the residues of the active site of DPP-IV 2. Define the geometry and force field relationship of the residues identified above in (1) 3. Define the physical parameters of the active site identified in (1) 4. Validate the model based on mutational analysis and in-vitro inhibitor binding studies 5. Screen the library for scaffolds and small molecules that satisfy the model developed in (3) and validated in (4) above. 6. Dock each inhibitor identified in (5) above to the active site of DPP-IV defined in (1). 7. Minimize the energy of the inhibitor and DPP-IV complex using force fields used in (2) above. 8. Compare the energy of interaction of each inhibitor to that of known inhibitors. 9. Synthesize and validate in in-vitro assays

    摘要翻译: 本发明涉及作为二肽基肽酶-IV酶(“DPP-IV抑制剂”)的抑制剂的新型纳米酸衍生物,其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病, 特别是在治疗2型糖尿病和与之相关的病症方面。 此外,本发明提供了可用于抑制DPP-IV酶的药物组合物,其包含治疗有效量的纳米酸衍生物。 此外,本发明提供了抑制DPP-IV的方法,包括向需要这种治疗的哺乳动物施用治疗有效量的本发明的纳米酸衍生物的单一或组合。 本发明还涉及用于治疗与DPP-IV酶相关的疾病状态的试剂盒和其它制品。 本发明还涉及鉴定具有二肽基肽酶-IV酶抑制活性的化合物的方法,包括以下步骤:1.定义DPP-IV的活性位点的残基2.定义残基的几何形状和力场关系 (1)中确定的活性位点的物理参数定义(1)中确定的活性位点的物理参数4.基于突变分析和体外抑制剂结合研究验证模型5.筛选满足以下条件的支架和小分子的文库 (3)中开发并在上述(4)中验证的模型。 6.将上述(5)中鉴定的每种抑制剂停留在(1)中定义的DPP-IV的活性位点。 7.使用上述(2)中使用的力场,最小化抑制剂和DPP-IV复合物的能量。 8.比较每个抑制剂与已知抑制剂相互作用的能量。 9.在体外测定中合成和验证