New Optically Pure Compounds for Improved Therapeutic Efficiency
    1.
    发明申请
    New Optically Pure Compounds for Improved Therapeutic Efficiency 有权
    用于提高治疗效果的新型光学纯化合物

    公开(公告)号:US20110201559A1

    公开(公告)日:2011-08-18

    申请号:US12993427

    申请日:2008-05-22

    摘要: The present invention relates to new optically pure compounds displaying an improved anticancer activity compared to previously known complex mixtures of stereoisomers thereof. Such compounds are of formula (I): wherein each X independently represents any amino acid; n is 0 or 1; m is an integer between 0 and 3; k is an integer of at least 3; Psi is a reduced bond of formula replacing the peptide amide bond between Lys and Pro; and wherein Lys residues in pseudopeptide units of said compound of formula (I) are either all in L configuration or all in D configuration. A method for preparing such compounds, and therapeutic uses thereof are also provided. The synthetic method involves the selective reduction of the peptide bond between Lys and Pro in a dipeptide intermediate with borane. The therapeutic uses are against cancer, inflammation and for wound healing.

    摘要翻译: 本发明涉及与先前已知的其立体异构体的复合混合物相比显示改善的抗癌活性的新的光学纯化合物。 这样的化合物具有式(I):其中每个X独立地表示任何氨基酸; n为0或1; m是0和3之间的整数; k是至少3的整数; Psi是取代Lys和Pro之间的肽酰胺键的式的还原键; 并且其中所述式(I)化合物的假肽单元中的Lys残基全部为L构型或全部为D构型。 还提供了制备这些化合物的方法及其治疗用途。 合成方法包括用二硼化物中间体与硼烷选择性还原Lys和Pro之间的肽键。 治疗用途是针对癌症,炎症和伤口愈合。

    Optically pure compounds for improved therapeutic efficiency
    2.
    发明授权
    Optically pure compounds for improved therapeutic efficiency 有权
    光学纯化合物,提高治疗效率

    公开(公告)号:US09243030B2

    公开(公告)日:2016-01-26

    申请号:US12993427

    申请日:2008-05-22

    摘要: The present invention relates to new optically pure compounds displaying an improved anticancer activity compared to previously known complex mixtures of stereoisomers thereof. Such compounds are of formula (I): wherein each X independently represents any amino acid; n is 0 or 1; m is an integer between 0 and 3; k is an integer of at least 3; Psi is a reduced bond of formula replacing the peptide amide bond between Lys and Pro; and wherein Lys residues in pseudopeptide units of said compound of formula (I) are either all in L configuration or all in D configuration. A method for preparing such compounds, and therapeutic uses thereof are also provided. The synthetic method involves the selective reduction of the peptide bond between Lys and Pro in a dipeptide intermediate with borane. The therapeutic uses are against cancer, inflammation and for wound healing.

    摘要翻译: 本发明涉及与先前已知的其立体异构体的复合混合物相比显示改善的抗癌活性的新的光学纯化合物。 这样的化合物具有式(I):其中每个X独立地表示任何氨基酸; n为0或1; m是0和3之间的整数; k是至少3的整数; Psi是取代Lys和Pro之间的肽酰胺键的式的还原键; 并且其中所述式(I)化合物的假肽单元中的Lys残基全部为L构型或全部为D构型。 还提供了制备这些化合物的方法及其治疗用途。 合成方法包括用二硼化物中间体与硼烷选择性还原Lys和Pro之间的肽键。 治疗用途是针对癌症,炎症和伤口愈合。

    New hybrid oligomers, their preparation process and pharmaceutical compositions containing them
    5.
    发明申请
    New hybrid oligomers, their preparation process and pharmaceutical compositions containing them 有权
    新的杂化低聚物,其制备方法和含有它们的药物组合物

    公开(公告)号:US20060211625A1

    公开(公告)日:2006-09-21

    申请号:US11378050

    申请日:2006-03-17

    IPC分类号: A61K38/10 C07K7/08

    摘要: The present invention relates to compositions and methods for producing therapeutic oligomeric compounds. In one aspect the invention relates to methods for administering the oligomeric compounds for the treatment and prevention of disease, for example, a fungal infection, bacterial infection, or cancer, in a mammal. In particular, the invention relates to medicaments comprising various novel oligomeric compounds and pharmaceutically acceptable salts thereof. The compounds of the invention may optionally be administered with at least one of a pharmaceutically acceptable excipient, pharmacologically active agent or a combination thereof.

    摘要翻译: 本发明涉及用于制备治疗性低聚化合物的组合物和方法。 一方面,本发明涉及用于治疗和预防哺乳动物疾病例如真菌感染,细菌感染或癌症的寡聚化合物的施用方法。 特别地,本发明涉及包含各种新型寡聚化合物及其药学上可接受的盐的药物。 本发明的化合物可以任选地与药学上可接受的赋形剂,药理学活性剂或其组合中的至少一种给药。

    Hybrid oligomers, their preparation process and pharmaceutical compositions containing them
    6.
    发明授权
    Hybrid oligomers, their preparation process and pharmaceutical compositions containing them 有权
    杂交寡聚体,其制备方法和含有它们的药物组合物

    公开(公告)号:US07691807B2

    公开(公告)日:2010-04-06

    申请号:US11378050

    申请日:2006-03-17

    IPC分类号: A61K38/00

    摘要: The present invention relates to compositions and methods for producing therapeutic oligomeric compounds. In one aspect the invention relates to methods for administering the oligomeric compounds for the treatment and prevention of disease, for example, a fungal infection, bacterial infection, or cancer, in a mammal. In particular, the invention relates to medicaments comprising various novel oligomeric compounds and pharmaceutically acceptable salts thereof. The compounds of the invention may optionally be administered with at least one of a pharmaceutically acceptable excipient, pharmacologically active agent or a combination thereof.

    摘要翻译: 本发明涉及用于制备治疗性低聚化合物的组合物和方法。 一方面,本发明涉及用于治疗和预防哺乳动物疾病例如真菌感染,细菌感染或癌症的寡聚化合物的施用方法。 特别地,本发明涉及包含各种新型寡聚化合物及其药学上可接受的盐的药物。 本发明的化合物可以任选地与药学上可接受的赋形剂,药理学活性剂或其组合中的至少一种给药。

    HYBRID OLIGOMERS, THEIR PREPARATION PROCESS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    9.
    发明申请
    HYBRID OLIGOMERS, THEIR PREPARATION PROCESS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权
    混合低聚物,其制备方法和含有它们的药物组合物

    公开(公告)号:US20100298206A1

    公开(公告)日:2010-11-25

    申请号:US12708217

    申请日:2010-02-18

    摘要: The present invention relates to compositions and methods for producing therapeutic oligomeric compounds. In one aspect the invention relates to methods for administering the oligomeric compounds for the treatment and prevention of disease, for example, a fungal infection, bacterial infection, or cancer, in a mammal. In particular, the invention relates to medicaments comprising various novel oligomeric compounds and pharmaceutically acceptable salts thereof. The compounds of the invention may optionally be administered with at least one of a pharmaceutically acceptable excipient, pharmacologically active agent or a combination thereof.

    摘要翻译: 本发明涉及用于制备治疗性低聚化合物的组合物和方法。 一方面,本发明涉及用于治疗和预防哺乳动物疾病例如真菌感染,细菌感染或癌症的寡聚化合物的施用方法。 特别地,本发明涉及包含各种新型寡聚化合物及其药学上可接受的盐的药物。 本发明的化合物可以任选地与药学上可接受的赋形剂,药理学活性剂或其组合中的至少一种给药。