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17 条记录 (耗时 0.03 秒)

    Methods of using SAHA and Erlotinib for treating cancer
    1.
    发明申请
    Methods of using SAHA and Erlotinib for treating cancer 审中-公开
    使用SAHA和厄洛替尼治疗癌症的方法

    公开(公告)号：US20070197568A1

    公开(公告)日：2007-08-23

    申请号：US11592443

    申请日：2006-11-03

    申请人： Paul Bunn ,  Samir Witta ,  Victoria Richon ,  Stanley Frankel ,  Paul Deutsch ,  Sophia Randolph

    发明人： Paul Bunn ,  Samir Witta ,  Victoria Richon ,  Stanley Frankel ,  Paul Deutsch ,  Sophia Randolph

    IPC分类号： A61K31/517 ,  A61K31/19

    CPC分类号： A61K31/167 ,  A61K31/19 ,  A61K31/517 ,  A61K2300/00

    摘要： The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Erlotinib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.

    摘要翻译： 本发明涉及通过对有需要的受试者施用第一量的组蛋白脱乙酰酶（HDAC）抑制剂如辛二酰苯胺异羟肟酸（SAHA）或其药学上可接受的盐，治疗有需要的受试者的癌症的方法 或其水合物，以及第二量的一种或多种抗癌剂，包括厄洛替尼。 HDAC抑制剂和抗癌剂可以施用以包含治疗有效量。 在各个方面，HDAC抑制剂和抗癌剂的作用可以是相加的或协同的。

    Methods of inducing terminal differentiation
    4.
    发明申请
    Methods of inducing terminal differentiation 审中-公开
    诱导终末分化的方法

    公开(公告)号：US20080114069A1

    公开(公告)日：2008-05-15

    申请号：US11983469

    申请日：2007-11-09

    申请人： Victoria Richon ,  Judy Chiao ,  William Kelly ,  Thomas Miller

    发明人： Victoria Richon ,  Judy Chiao ,  William Kelly ,  Thomas Miller

    IPC分类号： A61K31/19

    CPC分类号： A61K9/4866 ,  A61K9/0019 ,  A61K9/1652 ,  A61K31/13 ,  A61K31/164 ,  A61K31/165 ,  A61K31/19 ,  A61K31/44 ,  A61K38/12 ,  A61K47/12 ,  A61K47/38

    摘要： The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

    摘要翻译： 本发明提供了通过施用包含有效的HDAC抑制剂的药物组合物选择性诱导肿瘤细胞的终末分化，细胞生长停滞和/或细胞凋亡和/或抑制组蛋白脱乙酰酶（HDAC）的方法。 本发明的药物组合物中活性化合物的口服生物利用度令人惊奇的高。 此外，药物组合物在长时间内意外地引起活性化合物的高，治疗有效的血液水平。 本发明进一步提供这些药物组合物的安全的每日给药方案，其易于遵循，并且其在体内导致治疗有效量的HDAC抑制剂。

    Methods of treating cancer with HDAC inhibitors
    6.
    发明申请
    Methods of treating cancer with HDAC inhibitors 审中-公开
    用HDAC抑制剂治疗癌症的方法

    公开(公告)号：US20060276547A1

    公开(公告)日：2006-12-07

    申请号：US11492478

    申请日：2006-07-24

    申请人： Nicholas Bacopoulos ,  Judy Chiao ,  Thomas Miller ,  Carolyn Paradise ,  Victoria Richon

    发明人： Nicholas Bacopoulos ,  Judy Chiao ,  Thomas Miller ,  Carolyn Paradise ,  Victoria Richon

    IPC分类号： A61K31/19 ,  A61K38/12

    CPC分类号： A61K31/19

    摘要： The present invention relates to methods of treating cancers, e.g., lymphoma. More specifically, the present invention relates to methods of treating diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

    摘要翻译： 本发明涉及治疗癌症例如淋巴瘤的方法。 更具体地，本发明涉及通过给药包含HDAC抑制剂例如辛二酰苯胺异羟肟酸（SAHA）的药物组合物来治疗弥漫性大B细胞淋巴瘤（DLBCL）的方法。 药物组合物的口服制剂具有有利的药代动力学特征，例如高生物利用度，并且令人惊讶地在长时间内引起活性化合物的高血药浓度。 本发明进一步提供这些药物组合物的安全的每日给药方案，其易于遵循，并且其在体内导致治疗有效量的HDAC抑制剂。

    Hydroxamic acid compounds and methods of use thereof
    7.
    发明申请
    Hydroxamic acid compounds and methods of use thereof 失效
    羟肟酸化合物及其使用方法

    公开(公告)号：US20070155785A1

    公开(公告)日：2007-07-05

    申请号：US11710036

    申请日：2007-02-22

    申请人： Ronald Breslow ,  Thomas Miller ,  Sandro Belvedere ,  Paul Marks ,  Victoria Richon ,  Richard Rifkind

    发明人： Ronald Breslow ,  Thomas Miller ,  Sandro Belvedere ,  Paul Marks ,  Victoria Richon ,  Richard Rifkind

    IPC分类号： A61K31/4709 ,  C07D401/02

    CPC分类号： C07D211/02 ,  C07D215/38 ,  C07D401/12

    摘要： The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

    摘要翻译： 本发明涉及一类具有至少两个含芳基基团的异羟肟酸衍生物，其中至少一个是喹啉基，异喹啉基或苄基部分，通过亚甲基链与异羟肟酸基团连接。 异羟肟酸化合物可用于治疗癌症，例如脑癌。 异羟肟酸化合物也可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。 因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。 本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如神经变性 疾病

    Crystal structure of a deacetylase and inhibitors thereof
    8.
    发明申请
    Crystal structure of a deacetylase and inhibitors thereof 审中-公开
    脱乙酰酶的晶体结构及其抑制剂

    公开(公告)号：US20070087427A1

    公开(公告)日：2007-04-19

    申请号：US11505214

    申请日：2006-08-16

    申请人： Nikola Pavletich ,  Michael Finnin ,  Jill Donigian ,  Victoria Richon ,  Richard Rifkind ,  Paul Marks ,  Ronald Breslow

    发明人： Nikola Pavletich ,  Michael Finnin ,  Jill Donigian ,  Victoria Richon ,  Richard Rifkind ,  Paul Marks ,  Ronald Breslow

    IPC分类号： C12N9/18 ,  G06F19/00

    CPC分类号： C12N9/16

    摘要： The present invention provides three-dimensional structural information from the hyperthermophilic bacterium Aquifex aeolicus which is a histone deacetylase-like protein (HDLP). HDLP shares 35.2% amino acid sequence identity with human histone deacetylase (HDAC1). The present invention further provides three-dimensional structural information of HDLP bound by inhibitor molecules. The three-dimensional structural information of the present invention is useful to design, isolate and screen deacetylase inhibitor compounds capable of inhibiting HDLP, HDAC family members and HDLP-related molecules. The invention also relates to nucleic acids encoding a mutant HDLP which facilitates the determination of the three-dimensional structure of HDLP in the presence of a zinc atom.

    摘要翻译： 本发明提供来自作为组蛋白脱乙酰酶样蛋白质（HDLP）的超嗜热菌Aquifex aeolicus的三维结构信息。 HDLP与人组蛋白脱乙酰酶（HDAC1）具有35.2％的氨基酸序列同一性。 本发明还提供了由抑制剂分子结合的HDLP的三维结构信息。 本发明的三维结构信息可用于设计，分离和筛选能够抑制HDLP，HDAC家族成员和HDLP相关分子的脱乙酰酶抑制剂化合物。 本发明还涉及编码突变型HDLP的核酸，其有助于在锌原子存在下测定HDLP的三维结构。