IP Library › Granted Patent US 11,241,418
Granted Patent B2
US 11,241,418 · App. 16/796,448 · Granted Feb 8, 2022

Salts of selective estrogen receptor degraders

Inventors: Xing Dai (Short Hills, NJ); Yueheng Jiang (Belmont, MA)
Assignee: INVENTISBIO CO., LTD.
A61K31/4375A61K45/06C07D471/04C07B2200/13
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Quick Facts
Patent No.
US 11,241,418
App. No.
16/796,448
Granted
Feb 8, 2022
Kind
B2
Abstract

Provided herein are compounds, salts, crystalline forms, and pharmaceutical compositions that are related to Selective Estrogen Receptor Degraders, as well as methods of preparing the same. Also provided herein are methods of using the compounds, salts, crystalline forms, and pharmaceutical compositions for the treatment of diseases or disorders, such as breast cancer.

Claims (17)

1. A meglumine salt of Compound FA represented by the structure below:

2. A pharmaceutical composition comprising the meglumine salt of claim 1 , and optionally a pharmaceutically acceptable excipient.

3. The pharmaceutical composition of claim 2 , which is free or substantially free of Compound FA in free acid form.

4. A method of treating breast cancer, the method comprising administering to a subject in need thereof an effective amount of the meglumine salt of claim 1 .

5. A method of treating ER+ breast cancer, the method comprising administering to a subject in need thereof an effective amount of the meglumine salt of claim 1 .

6. The method of claim 5 , further comprising administering to the subject an effective amount of an additional antiproliferative agent.

7. A method of preparing Compound FA or an amine salt thereof, the method comprising:

a) reacting a tryptamine compound, or a salt thereof, with an

aldehyde, or a salt thereof, under suitable conditions to form

Compound FA or a salt thereof;

b) optionally converting Compound FA or a salt thereof into an amine salt of Compound FA.

8. The method of claim 7 , wherein the amine salt is a diisopropylethyl amine salt, and the method comprises reacting Compound FA or a salt thereof with diisopropylethyl amine to provide the diisopropylethyl amine salt of Compound FA:

9. The method of claim 7 , wherein the amine salt is a meglumine amine salt, and the method comprises reacting Compound FA or a salt thereof with meglumine to provide the meglumine salt of Compound FA:

10. The method of claim 9 , comprising reacting a diisopropylethyl amine salt of Compound FA with meglumine to provide the meglumine salt of Compound FA.

11. The method of claim 7 , wherein the tryptamine compound is prepared by a process comprising reacting

with

in the presence of a base.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 19, 2021
From: DAI, XING; JIANG, YUEHENG
To: INVENTISBIO CO., LTD.
Reel/Frame 055647/0673 →
Priority Claims (1)
WO PCT/CN2018/123031 · Dec 24, 2018 · international
Continuity (1)
Related Publication 20200197375A1 · Jun 25, 2020
Cited By (2)
US 12,187,736 US 12,746,229