公开(公告)号：US10173978B2

公开(公告)日：2019-01-08

申请号：US15749383

申请日：2016-08-02

Applicant: GEORGETOWN UNIVERSITY

Inventor： Milton L. Brown ,  Shujie Hou ,  Partha Banerjee ,  Karishma Amin

IPC: A61K31/403 ,  C07D209/88 ,  A61P35/00 ,  A61K45/06

Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.

公开(公告)号：US20200247751A1

公开(公告)日：2020-08-06

申请号：US16661510

申请日：2019-10-23

Applicant: GEORGETOWN UNIVERSITY

Inventor： Milton L. Brown ,  Shujie Hou ,  Partha Banerjee ,  Karishma Amin

IPC: C07D209/88 ,  A61K45/06 ,  A61P35/00 ,  A61K31/403

Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.

公开(公告)号：US11104646B2

公开(公告)日：2021-08-31

申请号：US16661510

申请日：2019-10-23

Applicant: GEORGETOWN UNIVERSITY

Inventor： Milton L. Brown ,  Shujie Hou ,  Partha Banerjee ,  Karishma Amin

IPC: C07D209/88 ,  A61K45/06 ,  A61P35/00 ,  A61K31/403

Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.

公开(公告)号：US20180215712A1

公开(公告)日：2018-08-02

申请号：US15749383

申请日：2016-08-02

Applicant: GEORGETOWN UNIVERSITY

Inventor： Milton L. Brown ,  Shujie Hou ,  Partha Banerjee ,  Karishma Amin

IPC: C07D209/88 ,  A61K31/403 ,  A61P35/00 ,  A61K45/06

CPC classification number: C07D209/88 ,  A61K31/403 ,  A61K45/06 ,  A61P35/00 ,  A61K2300/00

Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.

公开(公告)号：US11053255B2

公开(公告)日：2021-07-06

申请号：US15189512

申请日：2016-06-22

Applicant: Georgetown University

Inventor： Milton L. Brown ,  Shujie Hou

IPC: C07D491/052 ,  C07D491/048

Abstract: Disclosed herein are methods of synthesizing mahanine and related compounds. The synthesis features an intramolecular aryl-alkyne isomerization, transition metal catalyzed cross-coupling and intramolecular carbazole forming reaction.

公开(公告)号：US10023551B2

公开(公告)日：2018-07-17

申请号：US15573183

申请日：2016-05-12

Applicant: GEORGETOWN UNIVERSITY

Inventor： Milton L. Brown ,  Yali Kong ,  Jacqueline Smith ,  Kan Wang ,  Shujie Hou

IPC: C07D311/58 ,  C07D311/02 ,  A61P35/00 ,  G01N21/64 ,  A61K47/69 ,  C07C321/14 ,  C07C69/017 ,  C07C69/003 ,  C07C271/28

Abstract: A glutathione-cleavable prodrug is provided herein, as well as methods for its use in treating cancer, including triple negative breast cancer. The prodrug can be cleaved by glutathione under physiological conditions to generate a biologically active agent. The compound described herein is advantageous as the compound is fluorescent and can therefore be monitored within a subject.

公开(公告)号：US20190077755A1

公开(公告)日：2019-03-14

申请号：US16182720

申请日：2018-11-07

Applicant: GEORGETOWN UNIVERSITY

Inventor： Milton L. Brown ,  Shujie Hou ,  Partha Banerjee ,  Karishma Amin

IPC: C07D209/88 ,  A61K45/06 ,  A61K31/403 ,  A61P35/00

Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.

公开(公告)号：US20180105505A1

公开(公告)日：2018-04-19

申请号：US15573183

申请日：2016-05-12

Applicant: GEORGETOWN UNIVERSITY

Inventor： Milton L. Brown ,  Yali Kong ,  Jacqueline Smith ,  Kan Wang ,  Shujie Hou

IPC: C07D311/02 ,  C07C271/28 ,  C07C321/14 ,  C07C69/017 ,  C07C69/003 ,  A61K47/69 ,  A61P35/00 ,  G01N21/64

CPC classification number: C07D311/02 ,  A61K31/352 ,  A61K47/6957 ,  A61P35/00 ,  C07C69/003 ,  C07C69/017 ,  C07C271/28 ,  C07C321/14 ,  C07D311/18 ,  C07D311/58 ,  G01N21/64

Abstract: A glutathione-cleavable prodrug is provided herein, as well as methods for its use in treating cancer, including triple negative breast cancer. The prodrug can be cleaved by glutathione under physiological conditions to generate a biologically active agent. The compound described herein is advantageous as the compound is fluorescent and can therefore be monitored within a subject.

公开(公告)号：US20160368927A1

公开(公告)日：2016-12-22

申请号：US15189512

申请日：2016-06-22

Applicant: Georgetown University

Inventor： Milton L. Brown ,  Shujie Hou

IPC: C07D491/048

CPC classification number: C07D491/048

Abstract: Disclosed herein are methods of synthesizing mahanine and related compounds. The synthesis features an intramolecular aryl-alkyne isomerization, transition metal catalyzed cross-coupling and intramolecular carbazole forming reaction.

Abstract translation: 本文公开了合成马汉酸和相关化合物的方法。 该合成具有分子内芳基炔异构化，过渡金属催化的交叉偶联和分子内咔唑形成反应。