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    Sustained release pyriproxifen compositions for parasite control
    62.
    发明授权
    Sustained release pyriproxifen compositions for parasite control 失效
    用于寄生虫控制的持续释放的艾曲瑞芬组合物

    公开(公告)号：US5632999A

    公开(公告)日：1997-05-27

    申请号：US108909

    申请日：1993-08-18

    申请人： Thomas A. Miller

    发明人： Thomas A. Miller

    IPC分类号： A01K13/00 ,  A01K27/00 ,  A01N37/52 ,  A01N43/40 ,  A01N47/12 ,  A01N53/02 ,  A61K9/00 ,  A01N25/34

    CPC分类号： A01N43/40

    摘要： The invention comprises a method of controlling fleas which includes continuously administering to the haircoat of a homeothermic animal an ovicidally effective amount of 2-(1-methyl-2-(4-phenoxyphenoxy)ethoxy)pyridine (pyriproxifen) from a sustained release matrix at a rate of 0.1 mcg/kg/day to 100 mcg/kg/day. The method may also include the use of additional ingredients such as insecticides, plasticizers, lubricants and antioxidants in a sustained release matrix.

    摘要翻译： 本发明包括一种控制跳蚤的方法，其包括向持续释放基质中的持续释放基质中持续施用有效量的2-（1-甲基-2-（4-苯氧基苯氧基）乙氧基）吡啶（吡氯西泮） 速率为0.1mcg / kg /天至100mcg / kg /天。 该方法还可以包括在持续释放基质中使用附加成分例如杀虫剂，增塑剂，润滑剂和抗氧化剂。

    Polymorphs of suberoylanilide hydroxamic acid
    65.
    发明授权
    Polymorphs of suberoylanilide hydroxamic acid 有权
    辛二酰苯胺异羟肟酸的多晶型物

    公开(公告)号：US08101663B2

    公开(公告)日：2012-01-24

    申请号：US12653073

    申请日：2009-12-07

    申请人： Thomas A. Miller ,  Victoria M. Richon

    发明人： Thomas A. Miller ,  Victoria M. Richon

    IPC分类号： A61K31/165 ,  C07C259/04

    CPC分类号： A61K31/19 ,  A61K9/0019 ,  A61K9/1652 ,  A61K9/4866 ,  A61K31/13 ,  A61K31/165 ,  A61K31/44 ,  A61K47/12 ,  A61K47/38 ,  C07B2200/13 ,  C07C259/06

    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. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.

    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。 本发明还提供了SAHA的新型I型多晶型物，其特征在于独特的X射线衍射图和差示扫描量热法谱，以及独特的晶体结构。

    Hydroxamic acid compounds and methods of use thereof
    66.
    发明授权
    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：US07799803B2

    公开(公告)日：2010-09-21

    申请号：US11710036

    申请日：2007-02-22

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

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

    IPC分类号： A61K31/04 ,  C07D215/38

    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

    Methods of inducing terminal differentiation
    67.
    发明申请
    Methods of inducing terminal differentiation 有权
    诱导终末分化的方法

    公开(公告)号：US20100210729A1

    公开(公告)日：2010-08-19

    申请号：US12799368

    申请日：2010-04-23

    申请人： Victoria M. Richon ,  Judy H. Chiao ,  William Kevin Kelly ,  Thomas A. Miller

    发明人： Victoria M. Richon ,  Judy H. Chiao ,  William Kevin Kelly ,  Thomas A. Miller

    IPC分类号： A61K31/195 ,  A61P35/00

    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。

    Polymorphs of suberoylanilide hydroxamic acid
    69.
    发明申请
    Polymorphs of suberoylanilide hydroxamic acid 有权
    辛二酰苯胺异羟肟酸的多晶型物

    公开(公告)号：US20090042992A1

    公开(公告)日：2009-02-12

    申请号：US12077396

    申请日：2008-03-18

    申请人： Thomas A. Miller ,  Victoria M. Richon

    发明人： Thomas A. Miller ,  Victoria M. Richon

    IPC分类号： A61K31/164 ,  A61P35/00

    CPC分类号： A61K31/19 ,  A61K9/0019 ,  A61K9/1652 ,  A61K9/4866 ,  A61K31/13 ,  A61K31/165 ,  A61K31/44 ,  A61K47/12 ,  A61K47/38 ,  C07B2200/13 ,  C07C259/06

    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. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.

    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。 本发明还提供了SAHA的新型I型多晶型物，其特征在于独特的X射线衍射图和差示扫描量热法谱，以及独特的晶体结构。

    Methods of treating cancer with HDAC inhibitors
    70.
    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：US20090012175A1

    公开(公告)日：2009-01-08

    申请号：US12217843

    申请日：2008-07-08

    申请人： Nicholas G. Bacopoulos ,  Judy H. Chiao ,  Thomas A. Miller ,  Carolyn M. Paradise ,  Victoria M. Richon

    发明人： Nicholas G. Bacopoulos ,  Judy H. Chiao ,  Thomas A. Miller ,  Carolyn M. Paradise ,  Victoria M. Richon

    IPC分类号： A61K31/192 ,  A61P35/00

    CPC分类号： A61K31/16 ,  A61K31/185

    摘要： The present invention provides methods of treating cancers, chemoprevention, 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来治疗癌症，化学预防，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。