Granted Patent
B2
US 12,213,987 · App. 17/304,201 · Granted Feb 4, 2025
Prodrug salts
Inventors:
Marc F. Pelletier (Shaker Heights, OH); Paul Robert McGuirk (Spring Hill, FL); George William Farr (Rocky River, OH); Robert Zamboni (Beaconsfield, CA); John Colucci (Kirkland, CA); Helmi Zaghdane (Pincourt, CA)
Assignee:
Aeromics, Inc.
View Patent ↗
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Abstract
Provided are novel prodrug salts of selective aquaporin inhibitors, their use as pharmaceuticals, and pharmaceutical compositions comprising them, and novel processes for their synthesis and novel intermediates for use in their synthesis. Also provided is use of a compound for the prophylaxis, treatment, and control of aquaporin-mediated conditions. Aquaporin inhibitors, e.g., inhibitors of AQP4 and/or AQP2, may be of utility in the treatment or control of diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord), hyponatremia, and excess fluid retention, as well as diseases such as epilepsy, retinal ischemia and other diseases of the eye, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines.
Claims (12)
1. A process for synthesizing:
wherein the process comprises deprotecting:
with a deprotecting agent and wherein the process further comprises isolating:
2. The process of claim 1 , wherein the deprotecting agent comprises F.
3. The process of claim 2 , wherein the deprotecting agent is tetra-n-butylammonium fluoride.
4. The process of claim 1 , wherein the deprotecting agent is an acid.
5. The process of claim 4 , wherein the acid is CF 3 COOH (TFA).
6. The process of claim 1 , wherein the deprotection reaction is stirred at room temperature.
7. The process of claim 2 , wherein the deprotection reaction is stirred at room temperature.
8. The process of claim 3 , wherein the deprotection reaction is stirred at room temperature.
9. The process of claim 4 , wherein the deprotection reaction is stirred at room temperature.
10. The process of claim 5 , wherein the deprotection reaction is stirred at room temperature.
Assignments (2)
ASSIGNEE CHANGE OF ADDRESS
Recorded Oct 5, 2023
From: AEROMICS, INC.
To: AEROMICS, INC.
Reel/Frame 065155/0526 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Aug 16, 2021
From: PELLETIER, MARC F.; MCGUIRK, PAUL ROBERT; FARR, GEORGE WILLIAM; ZAMBONI, ROBERT; COLUCCI, JOHN; ZAGHDANE, HELMI
To: AEROMICS, INC.
Reel/Frame 057195/0131 →
Continuity (8)
Continuation
16296663
· Mar 8, 2019
Division
15034274
Provisional Application
61900946
· Nov 6, 2013
Provisional Application
61900878
· Nov 6, 2013
Provisional Application
61900919
· Nov 6, 2013
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