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1. 发明申请

WO2016100652A3 PROCESS FOR THE PREPARATION OF A DIARYLTHIOHYDANTOIN COMPOUND 审中-公开
标题翻译：制备二芳基羟基烟酰胺化合物的方法
公开(公告)号：WO2016100652A3
公开(公告)日：2016-08-25
申请号：PCT/US2015066356
申请日：2015-12-17
申请人： ARAGON PHARMACEUTICALS INC
发明人： HAIM CYRIL BEN , HORVATH ANDRAS , WEERTS JOHAN ERWIN EDMOND
IPC分类号： C07D213/84 , C07D213/61 , C07D401/04
CPC分类号： C07D401/04 , C07D213/61 , C07D213/84
摘要： Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.
摘要翻译：公开了用于制备目前正在研究用于治疗前列腺癌的化合物（X）的方法和中间体。

2. 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。

3. 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。

4. 发明申请

WO2020144649A1 PHARMACEUTICAL COMPOSITION COMPRISING ENZALUTAMIDE DISPERSED IN APPLE SAUCE 审中-公开
公开(公告)号：WO2020144649A1
公开(公告)日：2020-07-16
申请号：PCT/IB2020/050196
申请日：2020-01-10
申请人： ARAGON PHARMACEUTICALS, INC.
发明人： CHIEN, Dr. Caly
IPC分类号： A61K31/4439 , A61K45/06 , A61P35/00 , A23L2/00 , A61K31/4166
摘要： Disclosed herein are pharmaceutical compositions and methods of treating prostate cancer including castrate resistant prostate cancer, metastatic castration resistant prostate cancer and nonmetastatic castration resistant prostate cancer with an approved drug product containing an antiandrogen selected from the group consisting of enzalutamide, apalutamide and darolutamide.

5. 发明申请

WO2020144646A1 APALUTAMIDE DISPERSED IN APPLESAUCE FOR TREATING PROSTATE CANCER 审中-公开
公开(公告)号：WO2020144646A1
公开(公告)日：2020-07-16
申请号：PCT/IB2020/050192
申请日：2020-01-10
申请人： ARAGON PHARMACEUTICALS, INC.
发明人： CHIEN, Dr. Caly
IPC分类号： A61K31/4155 , A61K45/06 , A61P35/00 , A23L2/00
摘要： Disclosed herein are pharmaceutical compositions and methods of treating prostate cancer including castrate resistant prostate cancer, metastatic castration resistant prostate cancer and nonmetastatic castration resistant prostate cancer with an approved drug product containing an antiandrogen selected from the group consisting of enzalutamide, apalutamide and darolutamide.

6. 发明申请

WO2017209939A1 ANTICANCER COMPOSITIONS 审中-公开
标题翻译：抗癌组合物
公开(公告)号：WO2017209939A1
公开(公告)日：2017-12-07
申请号：PCT/US2017/032815
申请日：2017-05-16
申请人： ARAGON PHARMACEUTICALS, INC.
发明人： BERTELS, Johny , MENSCH, Jurgen
IPC分类号： A61K31/58 , A61K31/4439 , A61K9/14 , A61K9/16 , A61K9/20 , A61P35/00 , A61K31/573
摘要： The present invention concerns pharmaceutical formulations of abiraterone actetate and ARN-509, which can be administered to a mammal, in particular a human, suffering from an androgen receptor (AR)-related disease or condition, in particular cancer, more in particular prostate cancer, including but not limited to castration-resistant prostate cancer, metastatic castration resistant prostate cancer, chemotherapy-naive metastatic castration resistant prostate cancer, biochemically relapsed hormone sensitive prostate cancer, or high-risk, non-metastatic castration-resistant prostate cancer. In one aspect, these formulations comprise abiraterone acetate and a solid dispersion of ARN-509 and a polymer selected from HPMCAS, a poly(meth)acrylate copolymer, and mixtures thereof. In one aspect, these formulations comprise a granulate of abiraterone acetate and a solid dispersion of ARN-509 and a polymer selected from HPMC AS, a poly(meth)acrylate copolymer, and mixtures thereof.
摘要翻译：本发明涉及阿比特酸阿替酯和ARN-509的药物制剂，其可以给药于患有雄激素受体（AR）相关疾病或病症的哺乳动物，特别是人，特别是癌症，更特别是前列腺癌，包括但不限于去势抵抗性前列腺癌，转移性去势抵抗性前列腺癌，未经化学治疗的转移性去势抵抗性前列腺癌，生化复发的激素敏感性前列腺癌或高风险非转移性去势抵抗性前列腺癌。在一个方面，这些制剂包含乙酸阿比特龙酯和ARN-509和选自HPMCAS，聚（甲基）丙烯酸酯共聚物及其混合物的聚合物的固体分散体。在一个方面，这些制剂包含醋酸阿比特龙的颗粒和ARN-509和选自HPMC AS，聚（甲基）丙烯酸酯共聚物及其混合物的聚合物的固体分散体。

7. 发明申请

WO2016090101A1 ANTICANCER COMPOSITIONS 审中-公开
标题翻译： ANTICANCER组合物
公开(公告)号：WO2016090101A1
公开(公告)日：2016-06-09
申请号：PCT/US2015/063667
申请日：2015-12-03
申请人： ARAGON PHARMACEUTICALS, INC.
发明人： VERRECK, Geert
IPC分类号： A61K9/14 , A61K9/20
CPC分类号： A61K9/141 , A61K9/2027
摘要： The present invention concerns pharmaceutical formulations of ARN-509, which can be administered to a mammal, in particular a human, suffering from an androgen receptor (AR)-related disease or condition, in particular cancer, more in particular prostate cancer, including but not limited to castration-resistant prostate cancer, metastatic castration resistant prostate cancer, chemotherapy-naive metastatic castration resistant prostate cancer, biochemically relapsed hormone sensitive prostate cancer, or high-risk, non-metastatic castration-resistant prostate cancer. In one aspect, these formulations comprise a solid dispersion of ARN-509 and a poly(meth)acrylate copolymer. In one aspect, the solid dispersion of ARN-509 and a poly(meth)acrylate copolymer is obtainable, in particular is obtained, by melt-extruding a mixture comprising ARN-509 and a poly(meth)acrylate copolymer and optionally subsequently milling said melt-extruded mixture. In one aspect, the solid dispersion of ARN-509 and a poly(meth)acrylate copolymer is obtainable, in particular is obtained, by spray drying a mixture comprising ARN-509 and a poly(meth)acrylate copolymer in a suitable solvent.
摘要翻译：本发明涉及ARN-509的药物制剂，其可以施用于患有雄激素受体（AR）相关疾病或病症，特别是癌症，特别是前列腺癌的哺乳动物，特别是人，包括但不限于不限于去势抗性前列腺癌，转移性阉割抗性前列腺癌，化疗初次转移性阉割抗性前列腺癌，生化复发性激素敏感前列腺癌或高风险，非转移性去阉割抗性前列腺癌。一方面，这些制剂包含ARN-509和聚（甲基）丙烯酸酯共聚物的固体分散体。一方面，通过熔融挤出包含ARN-509和聚（甲基）丙烯酸酯共聚物的混合物，并任选随后研磨所述的（甲基）丙烯酸酯共聚物，可以获得ARN-509和聚（甲基）丙烯酸酯共聚物的固体分散体，熔融挤出混合物。一方面，通过在合适的溶剂中将包含ARN-509和聚（甲基）丙烯酸酯共聚物的混合物喷雾干燥，可以获得ARN-509和聚（甲基）丙烯酸酯共聚物的固体分散体。

8. 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.

9. 发明申请

WO2012037411A2 ESTROGEN RECEPTOR MODULATORS AND USES THEREOF 审中-公开
公开(公告)号：WO2012037411A2
公开(公告)日：2012-03-22
申请号：PCT/US2011051845
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 , A61K31/416 , A61K31/4192 , A61P35/00 , C07D249/18 , C07D401/06 , C07D409/06
CPC分类号： C07D231/56 , A61K31/416 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7105 , C07C215/10 , C07D209/08 , C07D215/227 , C07D217/24 , C07D249/18 , C07D265/18 , C07D277/68 , C07D279/16 , C07D401/10 , C07D401/12 , C07D403/10 , C07D409/10 , C07D413/10 , C07D417/10 , C07D471/04 , C07D495/04
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.

10. 发明申请

WO2022195407A1 METHODS FOR TREATING PROSTATE CANCER 审中-公开
公开(公告)号：WO2022195407A1
公开(公告)日：2022-09-22
申请号：PCT/IB2022/052105
申请日：2022-03-09
申请人： ARAGON PHARMACEUTICALS, INC.
发明人： MUNDLE, Suneel D. , SALEH, Mohamed Samir , ANTONI, Laurent Paul
IPC分类号： A61K31/4439 , A61P35/00
摘要： The disclosure provides methods of treating prostate cancer in a patient in need thereof, the methods comprising performing an imaging technique that is selected from an ultrasound imaging, magnetic resonance imaging, positron emission tomography imaging, computed tomography imaging, bone imaging, or a combination thereof on the patient; generating a conventional imaging result from the conventional imaging technique, wherein the conventional imaging result does not indicate metastasis of the prostate cancer; performing prostate -specific membrane antigen-positron emission tomography (PSMA-PET) on the patient; generating a first PSMA-PET result of the PSMA-PET, wherein the first PSMA-PET result indicates metastasis of the prostate cancer and is generated at substantially the same time as the conventional imaging result; and administering a therapeutically effective amount of apalutamide to the patient following generation of said first PSMA-PET result.

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