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    Methods and compositions for degradation and/or inhibition of HER-family tyrosine kinases
    1.
    发明授权
    Methods and compositions for degradation and/or inhibition of HER-family tyrosine kinases 失效
    用于降解和/或抑制HER-家族酪氨酸激酶的方法和组合物

    公开(公告)号：US07271160B2

    公开(公告)日：2007-09-18

    申请号：US09960665

    申请日：2001-09-21

    申请人： Neal Rosen ,  Scott D. Kuduk ,  Samuel J. Danishefsky ,  Furzhong F. Zheng ,  Laura Sepp-Lorenzino ,  Ouatek Ouerfelli

    发明人： Neal Rosen ,  Scott D. Kuduk ,  Samuel J. Danishefsky ,  Furzhong F. Zheng ,  Laura Sepp-Lorenzino ,  Ouatek Ouerfelli

    IPC分类号： C07D403/02 ,  A61K31/395 ,  A61P35/00

    CPC分类号： C07D225/06 ,  A61K47/55

    摘要： Bifunctional molecules comprising two hsp-binding moieties which bind to hsp90 in the pocket to which ansamycin antibiotics bind connected via a linker are effective for inducing the degradation and/or inhibition of HER-family tyrosine kinases. For example, a compound of two geldanamycin moities joined by a four-carbon linker provides selective degradation of HER-family tyrosine kinases, without substantially affecting other kinases. These compounds can be used for treatment of HER-positive cancers with reduced toxicity, since these compounds potently kill cancer cells but affect fewer proteins than geldanamycin.

    摘要翻译： 包含两个hsp结合部分的双功能分子对于诱导HER​​-家族酪氨酸激酶的降解和/或抑制是有效的，所述hsp结合部分与口服中与安莎霉素抗生素通过接头连接的hsp90结合。 例如，通过四碳连接物连接的两个格尔德霉素系的化合物提供HER-家族酪氨酸激酶的选择性降解，而基本上不影响其它激酶。 这些化合物可用于治疗具有降低毒性的HER阳性癌症，因为这些化合物有效杀死癌细胞，但影响比格尔德霉素少的蛋白质。

    Methods and compositions for degradation and/or inhibition of HER-family tyrosine kinases
    2.
    发明授权
    Methods and compositions for degradation and/or inhibition of HER-family tyrosine kinases 有权
    用于降解和/或抑制HER-家族酪氨酸激酶的方法和组合物

    公开(公告)号：US07238682B1

    公开(公告)日：2007-07-03

    申请号：US09937192

    申请日：2000-04-07

    申请人： Neal Rosen ,  Scott D. Kuduk ,  Samuel J. Danishefsky ,  Furzhong F. Zheng ,  Laura Sepp-Lorenzino ,  Ouatek Ouerfelli

    发明人： Neal Rosen ,  Scott D. Kuduk ,  Samuel J. Danishefsky ,  Furzhong F. Zheng ,  Laura Sepp-Lorenzino ,  Ouatek Ouerfelli

    IPC分类号： C07D403/02 ,  A61K31/395 ,  A61P35/00

    CPC分类号： C07D403/12

    摘要： Bifunctional molecules comprising two hsp-binding moieties which bind to hsp90 in the pocket to which ansamycin antibiotics bind connected via a linker are effective for inducing the degradation and/or inhibition of HER-family tyrosine kinases. For example, a compound of two geldanamycin moities joined by a four-carbon linker provides selective degradation of HER-family tyrosine kinases, without substantially affecting other kinases. These compounds can be used for treatment of HER-positive cancers with reduced toxicity, since these compounds potently kill cancer cells but affect fewer proteins than geldanamycin.

    摘要翻译： 包含两个hsp结合部分的双功能分子对于诱导HER​​-家族酪氨酸激酶的降解和/或抑制是有效的，所述两个hsp结合部分与口服中与安莎霉素抗生素通过接头连接的hsp90结合。 例如，通过四碳连接物连接的两个格尔德霉素部分的化合物提供HER-家族酪氨酸激酶的选择性降解，而基本上不影响其它激酶。 这些化合物可用于治疗具有降低毒性的HER阳性癌症，因为这些化合物有效杀死癌细胞，但影响比格尔德霉素少的蛋白质。

    Methods and compositions for destruction of selected proteins
    4.
    发明授权
    Methods and compositions for destruction of selected proteins 失效
    用于破坏所选蛋白质的方法和组合物

    公开(公告)号：US06670348B1

    公开(公告)日：2003-12-30

    申请号：US09403434

    申请日：1999-10-20

    申请人： Neal Rosen ,  Samuel Danishefsky ,  Ouathek Ouerfelli ,  Scott D. Kuduk ,  Laura Sepp-Lorenzino

    发明人： Neal Rosen ,  Samuel Danishefsky ,  Ouathek Ouerfelli ,  Scott D. Kuduk ,  Laura Sepp-Lorenzino

    IPC分类号： A61K3131

    CPC分类号： C07D225/06 ,  A61K47/554 ,  C07J17/00 ,  C07J43/00

    摘要： Compounds having an ansamycin anitibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic leading to the degradation of proteins and death of the targeted cells. These compositions may have different specificity than the ansamycin alone, allowing for a more specific targeting of the therapy, and can be effective in instances where the ansamycin alone has no effect. Thus, these compounds provide an entirely new class of targeted chemotherapy agents with application, depending on the nature of the targeting moiety, to treatment of a variety of different forms of cancer. Such agents can further be used to promote selective degradation of proteins associated with the pathogenesis of others diseases, including antigens associated with autoimmune disorders and pathogenic proteins associated with Alzheimer's disease. Exemplary targeting moieties which may be employed in compounds of the invention include testosterone, estradiol, tamoxifen and wortmannin.

    摘要翻译： 具有安莎霉素无抗生素或与hsp90结合的其它部分的化合物偶联到特异性结合蛋白质，受体或标记的靶向部分可以提供安莎霉素抗生素的有效靶向递送，导致蛋白质的降解和靶细胞的死亡 。 这些组合物可以具有与单独的安莎霉素不同的特异性，允许治疗更具体的靶向，并且在单独使用安沙霉素没有作用的情况下可以是有效的。 因此，根据靶向部分的性质，这些化合物提供了一类全新的靶向化学疗法，可用于治疗多种不同形式的癌症。 此类试剂可进一步用于促进与其他疾病发病相关的蛋白质的选择性降解，所述疾病包括与自身免疫疾病相关的抗原和与阿尔茨海默病有关的病原性蛋白质。 可用于本发明化合物的示例性靶向部分包括睾酮，雌二醇，他莫昔芬和渥曼青霉素。

    SYSTEMIC DELIVERY OF MYOSTATIN SHORT INTERFERING NUCLEIC ACIDS (siNA) CONJUGATED TO A LIPOPHILIC MOIETY
    8.
    发明申请
    SYSTEMIC DELIVERY OF MYOSTATIN SHORT INTERFERING NUCLEIC ACIDS (siNA) CONJUGATED TO A LIPOPHILIC MOIETY 有权
    将肌松素干细胞干细胞（siNA）系统传递给一个亲水的小鼠

    公开(公告)号：US20160256570A1

    公开(公告)日：2016-09-08

    申请号：US15035950

    申请日：2014-11-10

    申请人： Laura SEPP-LORENZINO ,  Vasant JADHAV ,  Duncan BROWN ,  SIRNA THERAPEUTICS, INC.

    发明人： Marija Tadin-Strapps ,  Tayeba Khan ,  Walter Richard Strapps ,  Laura Sepp-Lorenzino ,  Vasant Jadhav ,  Duncan Brown

    IPC分类号： A61K48/00 ,  C12N15/113 ,  A61K47/48

    CPC分类号： A61K48/0058 ,  A61K31/713 ,  A61K47/543 ,  A61K47/554 ,  C12N15/1136 ,  C12N2310/14 ,  C12N2310/3515

    摘要： The present invention provides methods comprising the in vivo delivery of small nucleic acid molecules capable of mediating RNA interference and reducing the expression of myostatin, wherein the small nucleic acid molecules are introduced to a subject by systemic administration. Specifically, the invention relates to methods comprising the in vivo delivery of short interfering nucleic acid (siNA) molecules that target a myostatin gene expressed by a subject, wherein the siNA molecule is conjugated to a lipophilic moiety, such as cholesterol. The myostatin siNA conjugates that are delivered as per the methods disclosed are useful to modulate the in vivo expression of myostatin, increase muscle mass and/or enhance muscle performance. Use of the disclosed methods is further indicated for treating musculoskeletal diseases or disorders and/or diseases or disorders that result in conditions in which muscle is adversely affected.

    摘要翻译： 本发明提供了包括体内递送能够介导RNA干扰并降低肌生成抑制素表达的小核酸分子的方法，其中通过全身给药将小核酸分子引入受试者。 具体而言，本发明涉及包括体内递送针对受试者表达的肌生长抑制素基因的短干扰核酸（siNA）分子的方法，其中所述siNA分子与亲脂部分如胆固醇结合。 根据所公开的方法递送的肌生成抑制素siNA缀合物可用于调节肌生成抑制素的体内表达，增加肌肉质量和/或增强肌肉性能。 还公开了所公开的方法的使用用于治疗导致肌肉受到不利影响的病症的肌肉骨骼疾病或病症和/或疾病或病症。