IP Library › Granted Patent US 12,747,218
Granted Patent B2
US 12,747,218 · App. 18/740,059 · Granted Sep 29, 2026

Derivatives of substituted morpholines and uses thereof

Inventors: Janak Khimchand Padia (Germantown, MD); Chungping Yu (Gaithersburg, MD)
Assignee: Supernus Pharmaceuticals, Inc.
C07D265/30A61K31/5375A61K31/5377C07D413/14
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Quick Facts
Patent No.
US 12,747,218
App. No.
18/740,059
Granted
Sep 29, 2026
Kind
B2
Abstract

A compound of Formula I includes a stereoisomer thereof and/or a salt thereof; wherein R 1 is a substituted alkane group, a heterocylic group, or a pyridine group; X is hydrogen, a halogen, an amino acid residue, a substituted amino acid residue, an alkyl group, or an ester. Such compounds may be used in pharmaceutical compositions and for the treatment of central nervous system (CNS) disorders:

Claims (24)

1 . A method for treating a central nervous system disorder, the method comprising administering to a subject in need thereof a compound of Formula I, a stereoisomer thereof, or a salt thereof:

wherein:

R 1 is alkyl, heterocyclyl, or a pyridyl;

R 2 is alkyl, aryl, heteroaryl, or heterocyclyl;

R 3 -R 14 are each independently H, F, Cl, Br, I, CN, NO 2 , alkyl, aryl, heteroaryl, or heterocyclyl; and

X is halogen, an amino acid residue, a substituted amino acid residue, or ester, wherein X may also be H but only when R 1 is pyridyl.

2 . The method of claim 1 , wherein X is an amino acid residue.

3 . The method of claim 2 , wherein the amino acid residue is valine.

4 . The method of claim 3 , wherein R 1 is CH 2 , CH 3 CH, or (CH 3 ) 2 CHCH.

5 . The method of claim 1 , wherein the compound has the following structure:

6 . The method of claim 1 , comprising administering to the subject a salt of a compound having the following structure:

7 . The method of claim 1 , wherein the compound has the following structure:

8 . The method of claim 1 , wherein the compound has the following structure:

9 . The method of claim 1 , wherein the compound has the following structure:

10 . The method of claim 1 , wherein the compound has the following structure:

11 . The method of claim 1 , wherein the disorder is selected from the group consisting of depression, attention deficit hyperactivity disorder (ADHD), sleep disorders, apathy, cognition, anxiety, orthostatic hypotension, pain, and neurological disorders.

12 . The method of claim 1 , wherein the disorder is a sleep disorder.

13 . The method of claim 12 , wherein the administering is performed during an inactive or sleep phase.

14 . The method of claim 12 , wherein the sleep disorder is narcolepsy, cataplexy, or a REM sleep behavior disorder.

15 . The method of claim 1 , wherein the disorder is ADHD.

16 . The method of claim 1 , wherein the disorder is a neurological disorder selected from the group consisting of Parkinson's disease, Alzheimer's disease, Lewy body dementia, and multiple system atrophy.

17 . The method of claim 1 , wherein the disorder comprises pain.

18 . The method of claim 1 , wherein the disorder is a neuropsychiatric disorder.

19 . The method of claim 1 , wherein the disorder is anxiety or depression.

Continuity (3)
Continuation 18617255 · Mar 26, 2024
Provisional Application 63454930 · Mar 27, 2023
Related Publication 20240343699A1 · Oct 17, 2024
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