公开(公告)号：US20220218632A1

公开(公告)日：2022-07-14

申请号：US17599329

申请日：2020-03-27

申请人： ESSA Pharma, Inc. ,  The University of British Columbia ,  Provincial Health Services Authority

发明人： Peter Virsik ,  Han-Jie Zhou ,  Marianne Dorothy Sadar ,  Raymond John Andersen ,  Kunzhong Jain ,  Daniel Andrew Golec

IPC分类号： A61K31/145 ,  A61K31/519 ,  A61K31/203

摘要： The present disclosure generally relates to pharmaceutical compositions and combinations comprising an androgen receptor N-terminal domain inhibitor or an inhibitor and a second therapeutically active agent, such as an CDK4/6 inhibitor, a Pin1 inhibitor (inhibitor of peptidyl-prolyl cis/trans isomerases), or an antiandrogen. In particular, the present disclosure relates to pharmaceutical compositions and combinations useful for treatment of various cancers, for example breast cancer and prostate cancer. Further, the present disclosure relates administering an androgen receptor N-terminal domain inhibitor in combination with radiation therapy for treatment of various cancers.

公开(公告)号：US11358938B2

公开(公告)日：2022-06-14

申请号：US17526660

申请日：2021-11-15

申请人： ESSA Pharma, Inc.

发明人： Han-Jie Zhou ,  Peter Virsik

IPC分类号： A61K31/505 ,  A61K31/4164 ,  C07D239/69 ,  A61K45/06 ,  C07D239/42

摘要： The present invention relates to a crystalline form of Compound I, a salt, a solvate, or a solvate salt thereof or an amorphous form of Compound I, a salt, a solvate, or a solvate salt thereof. The present invention also provides compositions comprising the crystalline form and/or the amorphous form, therapeutic uses of the crystalline forms and/or the amorphous forms, and the compositions thereof.

公开(公告)号：US11242324B2

公开(公告)日：2022-02-08

申请号：US17342923

申请日：2021-06-09

申请人： ESSA Pharma, Inc.

发明人： Han-Jie Zhou ,  Peter Virsik

IPC分类号： C07D239/08 ,  A61K31/505 ,  C07D239/69 ,  A61K45/06 ,  C07D239/42

摘要： The present invention relates to a crystalline form of Compound I, a salt, a solvate, or a solvate salt thereof or an amorphous form of Compound I, a salt, a solvate, or a solvate salt thereof. The present invention also provides compositions comprising the crystalline form and/or the amorphous form, therapeutic uses of the crystalline forms and/or the amorphous forms, and the compositions thereof.

公开(公告)号：US20210332016A1

公开(公告)日：2021-10-28

申请号：US17342923

申请日：2021-06-09

申请人： ESSA Pharma, Inc.

发明人： Han-Jie Zhou ,  Peter Virsik

IPC分类号： C07D239/42 ,  A61K45/06

摘要： The present invention relates to a crystalline form of Compound I, a salt, a solvate, or a solvate salt thereof or an amorphous form of Compound I, a salt, a solvate, or a solvate salt thereof. The present invention also provides compositions comprising the crystalline form and/or the amorphous form, therapeutic uses of the crystalline forms and/or the amorphous forms, and the compositions thereof.

公开(公告)号：US20210323931A1

公开(公告)日：2021-10-21

申请号：US17233161

申请日：2021-04-16

申请人： ESSA Pharma, Inc.

发明人： Han-Jie Zhou ,  Peter Virsik

IPC分类号： C07D239/69 ,  A61K45/06

摘要： The present invention relates to a crystalline form of Compound I, a salt, a solvate, or a solvate salt thereof or an amorphous form of Compound I, a salt, a solvate, or a solvate salt thereof. The present invention also provides compositions comprising the crystalline form and/or the amorphous form, therapeutic uses of the crystalline forms and/or the amorphous forms, and the compositions thereof.

公开(公告)号：US20210198213A1

公开(公告)日：2021-07-01

申请号：US17058481

申请日：2019-05-24

申请人： ESSA Pharma, Inc. ,  The University of British Columbia ,  Provincial Health Services Authority

发明人： Han-Jie Zhou ,  Peter Virsik ,  Raymond John Andersen ,  Marianne Dorothy Sadar ,  Kunzhong Jian ,  Daniel Andrew Golec

IPC分类号： C07D239/34 ,  C07C317/28 ,  C07D305/06 ,  C07D295/26 ,  C07C317/24 ,  C07C69/712 ,  C07D263/56 ,  C07D207/24 ,  C07C235/74 ,  A61K45/06

摘要： Compounds having a structure of formula (I), (I-A), (Ia)-(Ie), (A)-(E), and (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of disorders including prostate cancer are also provided.

公开(公告)号：US20200247763A1

公开(公告)日：2020-08-06

申请号：US16852810

申请日：2020-04-20

申请人： ESSA Pharma, Inc.

发明人： Han-Jie Zhou ,  Peter Virsik

IPC分类号： C07D263/46 ,  C07D233/84 ,  C07D263/38 ,  C07D241/20 ,  C07D307/64 ,  C07D277/56 ,  C07D277/42 ,  C07D277/36 ,  C07D233/74 ,  C07D239/42 ,  C07D231/38 ,  C07D263/48 ,  C07D261/08 ,  C07D271/113 ,  A61P35/00

摘要： The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.