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1. 发明申请

WO2012037411A9 ESTROGEN RECEPTOR MODULATORS AND USES THEREOF 审中-公开
公开(公告)号：WO2012037411A9
公开(公告)日：2012-03-22
申请号：PCT/US2011/051845
申请日：2011-09-15
申请人： ARAGON PHARMACEUTICALS, INC. , SMITH, Nicholas, D. , KAHRAMAN, Mehmet , GOVEK, Steven, P. , NAGASAWA, Johnny, Y. , LAI, Andiliy, G. , JULIEN, Jackaline, D. , HERBERT, Mark R. , BONNEFOUS, Celine , DOUGLAS, Karensa L.
发明人： SMITH, Nicholas, D. , KAHRAMAN, Mehmet , GOVEK, Steven, P. , NAGASAWA, Johnny, Y. , LAI, Andiliy, G. , JULIEN, Jackaline, D. , HERBERT, Mark R. , BONNEFOUS, Celine , DOUGLAS, Karensa L.
IPC分类号： C07D231/56 , C07D249/18 , C07D409/06 , C07D401/06 , A61K31/416 , A61K31/4192 , A61P35/00
摘要： Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

2. 发明申请

WO2012037410A9 ESTROGEN RECEPTOR MODULATORS AND USES THEREOF 审中-公开
公开(公告)号：WO2012037410A9
公开(公告)日：2012-03-22
申请号：PCT/US2011/051843
申请日：2011-09-15
申请人： ARAGON PHARMACEUTICALS, INC. , SMITH, Nicholas, D. , KAHRAMAN, Mehmet , GOVEK, Steven, P. , NAGASAWA, Johnny, Y. , LAI, Andiliy, G. , BONNEFOUS, Celine , JULIEN, Jackaline D.
发明人： SMITH, Nicholas, D. , KAHRAMAN, Mehmet , GOVEK, Steven, P. , NAGASAWA, Johnny, Y. , LAI, Andiliy, G. , BONNEFOUS, Celine , JULIEN, Jackaline D.
IPC分类号： C07D231/56 , A61K31/416 , A61P35/00
摘要： Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

3. 发明申请

WO2011156518A2 ESTROGEN RECEPTOR MODULATORS AND USES THEREOF 审中-公开
标题翻译：雌激素受体调节剂及其用途
公开(公告)号：WO2011156518A2
公开(公告)日：2011-12-15
申请号：PCT/US2011/039669
申请日：2011-06-08
申请人： ARAGON PHARMACEUTICALS, INC. , KAHRAMAN, Mehmet , GOVEK, Steven, P. , NAGASAWA, Johnny, Y. , SMITH, Nicholas, D.
发明人： KAHRAMAN, Mehmet , GOVEK, Steven, P. , NAGASAWA, Johnny, Y. , SMITH, Nicholas, D.
IPC分类号： C07D405/12 , C07D405/10 , C07D311/04 , A61K31/453 , A61K31/352 , A61P35/00 , A61P25/28
CPC分类号： A61K31/352 , A61K31/4025 , A61K31/403 , A61K31/4178 , A61K31/439 , A61K31/453 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D311/60 , C07D405/12 , C07D407/14 , C07D471/08 , C07D487/08
摘要： Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
摘要翻译：本文描述的是雌激素受体调节剂的化合物。还描述了包括本文所述化合物的药物组合物和药物，以及使用这种雌激素受体调节剂单独使用并与其它化合物联合用于治疗介导或依赖于雌激素受体的疾病或病症的方法。

4. 发明申请

WO2010048149A2 HETEROCYCLIC MODULATORS OF GPR119 FOR TREATMENT OF DISEASE 审中-公开
标题翻译： GPR119的杂环调节剂治疗疾病
公开(公告)号：WO2010048149A2
公开(公告)日：2010-04-29
申请号：PCT/US2009/061281
申请日：2009-10-20
申请人： KALYPSYS, INC. , SMITH, Nicholas, D. , BONNEFOUS, Celine , KAHRAMAN, Mehmet , NOBLE, Stewart, A. , PAYNE, Joseph, E. , GOVEK, Steven, P.
发明人： SMITH, Nicholas, D. , BONNEFOUS, Celine , KAHRAMAN, Mehmet , NOBLE, Stewart, A. , PAYNE, Joseph, E. , GOVEK, Steven, P.
IPC分类号： A61K31/506 , A61P9/00
CPC分类号： A61K31/506 , A61K45/06 , A61K2300/00
摘要： Disclosed herein are compounds and methods which may be useful as inhibitors of GPR 119 for the treatment or prevention of diseases including cardiovascular and metabolic diseases.
摘要翻译：本文公开了可用作GPR 119抑制剂用于治疗或预防包括心血管和代谢疾病的疾病的化合物和方法。

5. 发明申请

WO2011159769A2 INDANE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF 审中-公开
标题翻译： INDANE ESTROGEN受体调节剂及其用途
公开(公告)号：WO2011159769A2
公开(公告)日：2011-12-22
申请号：PCT/US2011/040466
申请日：2011-06-15
申请人： ARAGON PHARMACEUTICALS, INC. , GOVEK, Steven, P. , SMITH, Nicholas, D.
发明人： GOVEK, Steven, P. , SMITH, Nicholas, D.
IPC分类号： C07D207/04 , C07D207/08 , A61K31/40 , A61P35/00
CPC分类号： C07D295/096 , A61K9/0014 , A61K9/0019 , A61K9/0095 , A61K9/2054 , A61K9/2095 , A61K9/4866 , A61K47/10 , A61K47/14 , A61K47/38 , C07D207/06 , C07D207/08 , C07D295/088
摘要： Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
摘要翻译：本文描述的是雌激素受体调节剂的化合物。还描述了包括本文所述化合物的药物组合物和药物，以及使用这种雌激素受体调节剂单独使用并与其它化合物联合用于治疗介导或依赖于雌激素受体的疾病或病症的方法。

6. 发明申请

WO2010088518A2 HETEROCYCLIC MODULATORS OF GPR119 FOR TREATMENT OF DISEASE 审中-公开
标题翻译： GPR119用于治疗疾病的杂环调节剂
公开(公告)号：WO2010088518A2
公开(公告)日：2010-08-05
申请号：PCT/US2010/022588
申请日：2010-01-29
申请人： KALYPSYS, INC. , KAHRAMAN, Mehmet , SMITH, Nicholas, D. , BONNEFOUS, Celine , NOBLE, Stewart, A. , PAYNE, Joseph, E.
发明人： KAHRAMAN, Mehmet , SMITH, Nicholas, D. , BONNEFOUS, Celine , NOBLE, Stewart, A. , PAYNE, Joseph, E.
IPC分类号： C07D487/14 , C07D487/04 , C07D403/14 , A61P3/00 , A61P3/10
CPC分类号： C07D487/04
摘要： Disclosed herein are compounds and methods which may be useful as inhibitors of GPRl 19 for the treatment or prevention of diseases including cardiovascular and metabolic diseases.
摘要翻译：本文公开了可用作GPR111抑制剂用于治疗或预防包括心血管和代谢疾病在内的疾病的化合物和方法。

7. 发明申请

WO2011103202A2 ANDROGEN RECEPTOR MODULATORS AND USES THEREOF 审中-公开
标题翻译：雄激素受体调节剂及其用途
公开(公告)号：WO2011103202A2
公开(公告)日：2011-08-25
申请号：PCT/US2011/025106
申请日：2011-02-16
申请人： ARAGON PHARMACEUTICALS, INC. , SMITH, Nicholas, D. , BONNEFOUS, Celine , JULIEN, Jackaline, D.
发明人： SMITH, Nicholas, D. , BONNEFOUS, Celine , JULIEN, Jackaline, D.
IPC分类号： C07D401/04 , C07D487/04 , A61K31/4439 , A61K31/5025 , A61P5/26 , A61P5/28
CPC分类号： C07D401/04 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/5025 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/635 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors.
摘要翻译：本文描述的是雄激素受体调节剂的化合物。还描述了包括本文所述化合物的药物组合物和药物，以及使用这些雄激素受体调节剂单独和与其它化合物组合用于治疗介导或依赖于雄激素受体的疾病或病症的方法。

8. 发明申请

WO2013090829A1 ESTROGEN RECEPTOR MODULATORS AND USES THEREOF 审中-公开
标题翻译：雌激素受体调节剂及其用途
公开(公告)号：WO2013090829A1
公开(公告)日：2013-06-20
申请号：PCT/US2012/069926
申请日：2012-12-14
申请人： ARAGON PHARMACEUTICALS, INC.
发明人： SMITH, Nicholas, D. , GOVEK, Steven, P. , KAHRAMAN, Mehmet , JULIEN, Jackaline, D. , NAGASAWA, Johnny, Y. , LAI, Andiliy, G.
IPC分类号： C07D405/12 , C07D405/14 , A61K31/4025 , A61P35/00
CPC分类号： C07D405/12 , C07D311/58 , C07D311/70 , C07D405/14 , C07D413/12
摘要： Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
摘要翻译：这里描述的是雌激素受体调节剂的化合物。还描述了包含本文所述化合物的药物组合物和药物，以及单独使用这些雌激素受体调节剂并与其它化合物组合使用以治疗介导或依赖于雌激素受体的疾病或病症的方法。 >

9. 发明申请

WO2013184681A1 CRYSTALLINE FORMS OF AN ANDROGEN RECEPTOR MODULATOR 审中-公开
标题翻译：雄性受体调节剂的结晶形式
公开(公告)号：WO2013184681A1
公开(公告)日：2013-12-12
申请号：PCT/US2013/044116
申请日：2013-06-04
申请人： ARAGON PHARMACEUTICALS, INC. , SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人： SMITH, Nicholas, D. , HERBERT, Mark, R. , OUERFELLI, Ouathek , DILHAS, Anna
IPC分类号： C07D401/04 , A61K31/4439 , A61K31/4184 , A61P35/00
CPC分类号： C07D401/04
摘要： Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
摘要翻译：本文描述的是雄激素受体调节剂4- [7-（6-氰基-5-三氟甲基吡啶-3-基）-8-氧代-6-硫代-5,7-二氮杂螺[3.4]辛-5-醇的无定形和结晶形式基] -2-氟-N-甲基苯甲酰胺。还描述了适用于包括雄激素受体调节剂的哺乳动物的药物组合物，以及使用雄激素受体调节剂单独和与其它化合物组合用于治疗与雄激素受体活性相关的疾病或病症的方法。

10. 发明申请

WO2014018926A8 METHODS AND COMPOSITIONS FOR DETERMINING RESISTANCE TO ANDROGEN RECEPTOR THERAPY 审中-公开
标题翻译：确定对雄激素受体治疗抵抗的方法和组合物
公开(公告)号：WO2014018926A8
公开(公告)日：2014-01-30
申请号：PCT/US2013/052395
申请日：2013-07-26
申请人： ARAGON PHARMACEUTICALS, INC.
发明人： JOSEPH, James, David , HAGER, Jeffrey , SENSINTAFFAR, John, Lee , LU, Nhin , QIAN, Jing , SMITH, Nicholas, D.
IPC分类号： C12Q1/68 , A61K31/00 , C07K14/72 , C07K16/28
摘要： Described herein are modified androgen receptor polypeptides that are resistant to inhibition by an androgen receptor inhibitor. Described herein are compositions, combinations, and kits containing the modified androgen receptor polypeptides and methods of using the modified androgen receptor polypeptides. Also described herein are methods of using the modified androgen receptor polypeptides as screening agents for the identification and design of third-generation androgen receptor modulators. Also described herein are third-generation androgen receptor modulators that inhibit the activity of the modified androgen receptor polypeptides. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions, including cancers, such as castration resistant prostate cancers, that are mediated or dependent upon androgen receptors.
摘要翻译：本文描述了对雄激素受体抑制剂的抑制具有抗性的修饰的雄激素受体多肽。本文描述了含有修饰的雄激素受体多肽的组合物，组合物和试剂盒以及使用该修饰的雄激素受体多肽的方法。本文还描述了使用修饰的雄激素受体多肽作为用于鉴定和设计第三代雄激素受体调节剂的筛选剂的方法。本文还描述了抑制修饰的雄激素受体多肽的活性的第三代雄激素受体调节剂。还描述了包含本文所述化合物的药物组合物和药物，以及单独或与其他化合物组合使用此类雄激素受体调节剂用于治疗疾病或病症（包括癌症例如去势抵抗性前列腺癌）的方法，是介导的或依赖于雄激素受体。

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