公开(公告)号：US20220380378A1

公开(公告)日：2022-12-01

申请号：US17727054

申请日：2022-04-22

申请人： ESSA Pharma, Inc.

发明人： Han-Jie ZHOU ,  Peter Virsik ,  Berenger Biannic

IPC分类号： C07D487/10 ,  C07D239/47 ,  C07D403/12 ,  C07D405/12 ,  C07D239/42 ,  C07D403/04 ,  C07D471/04 ,  C07D413/12 ,  C07D405/14 ,  C07D471/10

摘要： The present invention relates to compounds of formula (A), (A-I), (A-II), (A-III), (B), (B-I), (C), (D), (E), (E-I), (F), (G), (H), (J), and (K), 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.

公开(公告)号：US20220380325A1

公开(公告)日：2022-12-01

申请号：US17363534

申请日：2021-06-30

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

IPC分类号： C07D263/46 ,  A61P35/00 ,  C07D271/113 ,  C07D261/08 ,  C07D263/48 ,  C07D231/38 ,  C07D239/42 ,  C07D233/74 ,  C07D277/36 ,  C07D277/42 ,  C07D277/56 ,  C07D307/64 ,  C07D241/20 ,  C07D263/38 ,  C07D233/84 ,  C07D233/88 ,  C07D233/80 ,  C07D233/76

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.

公开(公告)号：US20220105093A1

公开(公告)日：2022-04-07

申请号：US17476904

申请日：2021-09-16

申请人： ESSA Pharma, Inc.

发明人： Peter Virsik ,  Han-Jie Zhou

IPC分类号： A61K31/505 ,  A61K31/4164 ,  A61K47/38 ,  A61K31/58 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/573 ,  A61P35/00

摘要： The present disclosure generally relates to pharmaceutical compositions and combinations comprising N-(4-((4-(2-(3-chloro-4-(2-chloroethoxy)-5-cyanophenyl)propan-2-yl)phenoxy) methyl)pyrimidin-2-yOmethanesulfonamideN-(4-((4-(2-(3-chloro-4-(2-chloroethoxy)-5-cyanophenyl) propan-2-yl) phenoxy) methyl)pyrimidin-2-yl)methanesulfonamide or a pharmaceutically acceptable salt, solvate, stereoisomer, or prodrug thereof, and a second therapeutically active agent, such as 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.

公开(公告)号：US20220073472A1

公开(公告)日：2022-03-10

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： 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：US11059795B2

公开(公告)日：2021-07-13

申请号：US16852810

申请日：2020-04-20

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

IPC分类号： C07D263/46 ,  A61P35/00 ,  C07D271/113 ,  C07D261/08 ,  C07D263/48 ,  C07D231/38 ,  C07D239/42 ,  C07D233/74 ,  C07D277/36 ,  C07D277/42 ,  C07D277/56 ,  C07D307/64 ,  C07D241/20 ,  C07D263/38 ,  C07D233/84 ,  C07D233/88 ,  C07D233/80 ,  C07D233/76

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.

公开(公告)号：US20220202780A1

公开(公告)日：2022-06-30

申请号：US17599338

申请日：2020-03-27

申请人： ESSA Pharma, Inc.

发明人： Peter Virsik ,  Han-Jie Zhou ,  Ronan Le Moigne

IPC分类号： A61K31/4164 ,  A61K31/4166 ,  A61K31/4439 ,  A61K31/4155 ,  A61K31/277 ,  A61K31/167 ,  A61K31/635 ,  A61P35/00 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/42 ,  A61K31/415 ,  A61K31/505

摘要： The present disclosure generally relates to pharmaceutical compositions and combinations comprising an androgen receptor modulator or an inhibitor and a second therapeutically active agent, such as 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.

公开(公告)号：US20230078913A1

公开(公告)日：2023-03-16

申请号：US17599341

申请日：2020-03-27

申请人： ESSA Pharma, Inc. ,  The University of British Columbia

发明人： Han-Jie Zhou ,  Raymond John Andersen

IPC分类号： A61K47/55 ,  A61K47/54 ,  C07D239/42

摘要： The present invention relates to bifunctional Proteolysis Targeting Chimeric ligands (Protac compounds) comprising a ligase modulator/binder and a molecule that binds to a protein target of interest, and methods of treating various diseases and conditions with the Protac compounds, including diseases associated with androgen receptors.

公开(公告)号：US11485713B2

公开(公告)日：2022-11-01

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 ,  A61K45/06 ,  C07C69/712 ,  C07C235/74 ,  C07C317/24 ,  C07C317/28 ,  C07D207/24 ,  C07D263/56 ,  C07D295/26 ,  C07D305/06

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：US20220259158A1

公开(公告)日：2022-08-18

申请号：US17732081

申请日：2022-04-28

申请人： ESSA Pharma, Inc.

发明人： Han-Jie Zhou ,  Peter Virsik

IPC分类号： 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：US11518747B2

公开(公告)日：2022-12-06

申请号：US17732081

申请日：2022-04-28

申请人： ESSA Pharma, Inc.

发明人： Han-Jie Zhou ,  Peter Virsik

IPC分类号： A61K31/505 ,  A61K31/4164 ,  C07D239/69 ,  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.