公开(公告)号：US20230373904A1

公开(公告)日：2023-11-23

申请号：US18203678

申请日：2023-05-31

申请人： Radius Pharmaceuticals, Inc.

发明人： Michael Paul Cruskie, JR. ,  Joshua Kyle Bolger ,  Jonathan Blake McKenzie ,  Pratik Sheth ,  Richard Edwards ,  Alex Eberlin ,  Michael Markey

IPC分类号： C07C217/84 ,  A61P35/00 ,  C07C213/10

CPC分类号： C07C217/84 ,  A61P35/00 ,  C07C213/10 ,  C07B2200/13

摘要： Various polymorphic forms of RAD1901-2HCl, including three crystalline and amorphous forms, are prepared and characterized. Uses of the various polymorphic forms of RAD1901-2HCl for cancer treatment are also disclosed.

公开(公告)号：US11413258B2

公开(公告)日：2022-08-16

申请号：US16580914

申请日：2019-09-24

申请人： Radius Pharmaceuticals, Inc.

发明人： Gary Hattersley

IPC分类号： A61K31/137 ,  A61K31/519 ,  A61P35/00 ,  A61P35/04 ,  A61K31/436 ,  A61K45/06 ,  A61K31/675

摘要： Disclosed herein are methods of inhibiting tumor growth or producing tumor regression in a subject by administering to the subject a therapeutically effective amount of a combination of palbociclib and RAD1901.

公开(公告)号：US20220125932A1

公开(公告)日：2022-04-28

申请号：US17519844

申请日：2021-11-05

申请人： RADIUS PHARMACEUTICALS, INC.

发明人： Kiran Kumar VANGARA ,  Huaguang Li ,  Ningxin Yan ,  Hung Q. Nguyen ,  Venkat R. Goskonda

IPC分类号： A61K47/44 ,  A61K9/08 ,  A61K31/05 ,  A61K31/352 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22

摘要： The present invention is generally directed to substantially pure cannabidiol, stable cannabinoid pharmaceutical formulations, and methods of their use.

公开(公告)号：US20210330612A1

公开(公告)日：2021-10-28

申请号：US17299948

申请日：2019-12-06

申请人： Radius Pharmaceuticals, Inc.

发明人： Hitisha PATEL ,  Teeru BIHANI ,  Heike ARLT ,  Nianjun TAO

IPC分类号： A61K31/137 ,  A61P35/00 ,  C12Q1/6886

摘要： Disclosed herein are methods of treating a CDK4/6 inhibitor resistant estrogen receptor alpha-positive cancer in a subject having either a wild-type estrogen receptor alpha and/or a mutant estrogen receptor alpha, the method comprising administering to the subject a therapeutically effective amount of elacestrant, or a pharmaceutically acceptable salt or solvate thereof, wherein the mutant estrogen receptor alpha comprises one or more mutations selected from the group consisting of D538G, Y537X1, L536X2, P535H, V534E, S463P, V392I, E380Q and combinations thereof, wherein: X1 is S, N, or C; and X2 is R or Q. In some embodiments, the CDK4/6 inhibitor resistant estrogen receptor alpha-positive cancer is selected from the group consisting of breast cancer, uterine cancer, ovarian cancer, and pituitary cancer.

公开(公告)号：US20200347032A1

公开(公告)日：2020-11-05

申请号：US16963794

申请日：2019-01-22

申请人： Radius Pharmaceuticals, Inc.

发明人： Chris Miller

IPC分类号： C07D403/10 ,  C07D487/04 ,  C07D209/30 ,  C07D333/64 ,  C07D409/12 ,  C07D495/04 ,  A61P35/04

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.

公开(公告)号：US20180169101A1

公开(公告)日：2018-06-21

申请号：US15794861

申请日：2017-10-26

申请人： RADIUS PHARMACEUTICALS, INC.

发明人： Gary HATTERSLEY

IPC分类号： A61K31/519 ,  A61K31/137 ,  A61P35/00

CPC分类号： A61K31/137 ,  A61K31/436 ,  A61K31/519 ,  A61K31/675 ,  A61K45/06 ,  A61K2300/00 ,  A61P35/00 ,  A61P35/04

摘要： Disclosed herein are methods of inhibiting tumor growth or producing tumor regression in a subject by administering to the subject a therapeutically effective amount of a combination of palbociclib and RAD1901.

公开(公告)号：US20180153828A1

公开(公告)日：2018-06-07

申请号：US15794774

申请日：2017-10-26

申请人： RADIUS PHARMACEUTICALS, INC.

发明人： Fiona GARNER ,  Gary HATTERSLEY

IPC分类号： A61K31/137 ,  A61P35/04 ,  A61P35/00

CPC分类号： A61K31/137 ,  A61K31/436 ,  A61K31/519 ,  A61K31/675 ,  A61K45/06 ,  A61K2300/00 ,  A61P35/00 ,  A61P35/04

摘要： Disclosed herein are methods of inhibiting tumor growth or producing tumor regression in a subject having a drug-resistant estrogen receptor alpha positive cancer or a mutant estrogen receptor alpha positive cancer. The methods entail administering to the subject a therapeutically effective amount of RAD1901 having the structure: or a salt or solvate thereof.

公开(公告)号：US20240308986A1

公开(公告)日：2024-09-19

申请号：US18661960

申请日：2024-05-13

申请人： RADIUS PHARMACEUTICALS, INC.

发明人： Chris MILLER

IPC分类号： C07D403/10 ,  A61P35/04 ,  C07D209/30 ,  C07D333/64 ,  C07D409/12 ,  C07D487/04 ,  C07D495/04

CPC分类号： C07D403/10 ,  A61P35/04 ,  C07D209/30 ,  C07D333/64 ,  C07D409/12 ,  C07D487/04 ,  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.

公开(公告)号：US11911361B2

公开(公告)日：2024-02-27

申请号：US15712515

申请日：2017-09-22

申请人： RADIUS PHARMACEUTICALS, INC.

发明人： Kiran Kumar Vangara ,  Huaguang Li ,  Ningxin Yan ,  Hung Q. Nguyen ,  Venkat R. Goskonda

IPC分类号： A61K31/352 ,  A61K9/00 ,  A61K31/05 ,  A61K47/44 ,  A61K47/10 ,  A61K47/22 ,  A61K31/355 ,  A61K9/08 ,  A61P25/08 ,  A61K47/14 ,  A61P25/28 ,  A61K47/26 ,  A61K31/365

CPC分类号： A61K31/352 ,  A61K9/0095 ,  A61K9/08 ,  A61K31/05 ,  A61K31/355 ,  A61K31/365 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/26 ,  A61K47/44 ,  A61P25/08 ,  A61P25/28 ,  A61K31/05 ,  A61K2300/00 ,  A61K31/355 ,  A61K2300/00 ,  A61K31/365 ,  A61K2300/00

摘要： The present invention is generally directed to substantially pure cannabidiol, stable cannabinoid pharmaceutical formulations, and methods of their use.

公开(公告)号：US11857518B2

公开(公告)日：2024-01-02

申请号：US17510050

申请日：2021-10-25

申请人： Radius Pharmaceuticals, Inc.

发明人： Gary Hattersley

IPC分类号： A61K31/137 ,  A61K31/436 ,  A61K31/675 ,  A61K45/06 ,  A61P35/04 ,  A61P35/00 ,  A61K31/519

CPC分类号： A61K31/137 ,  A61K31/436 ,  A61K31/519 ,  A61K31/675 ,  A61K45/06 ,  A61P35/00 ,  A61P35/04 ,  A61K2300/00 ,  A61K31/137 ,  A61K2300/00 ,  A61K31/436 ,  A61K2300/00 ,  A61K31/675 ,  A61K2300/00

摘要： Disclosed herein are methods of treating one or more tumors by administering to the subject a therapeutically effective amount of a combination of RAD1901 or solvates (e.g., hydrate) or salts thereof and one or more second therapeutic agent(s) (e.g., everolimus). The cancer is an estrogen-dependent cancer, such as breast cancer, ovarian cancer, colon cancer, endometrial cancer, or prostate cancer.