IP Library Granted Patent US 8,324,273
Granted Patent B2
US 8,324,273 · App. 12/904,960 · Granted Dec 4, 2012

Catechol protected levodopa diester prodrugs, compositions, and methods of use

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Quick Facts
Patent No.
US 8,324,273
App. No.
12/904,960
Granted
Dec 4, 2012
Kind
B2
Abstract

Catechol protected levodopa diester prodrugs pharmaceutical, compositions comprising catechol protected levodopa diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.

Claims (14)

1. A compound chosen from:

(1R)-1-methyl-2-phenylcarbonyloxyethyl (2S)-2-amino-3-[3,4-bis(ethoxycarbonyloxy)phenyl]propanoate hydrochloride;

(1R,2R)-2-acetyloxy-1-methylpropyl (2S)-2-amino-3-[3,4-bis(ethoxycarbonyloxy)phenyl]propanoate-hydrochloride-;

(1R,2R)-1-methyl-2-(2-methylpropanoyloxy)propyl (2S)-2-amino-3-[3,4-bis(ethoxycarbonyloxy)phenyl]propanoate hydrochloride;

(1R,2R)-2-isopropoxycarbonyloxy-1-methylpropyl (2S)-2-amino-3-[3,4-bis(ethoxycarbonyloxy)phenyl]propanoate hydrochloride;

(2R)-2-acetyloxypropyl (2S)-2-amino-3-[3,4-bis(ethoxycarbonyloxy)phenyl]propanoate hydrochloride;

(1R)-2-acetyloxy-1-methylethyl (2S)-2-amino-3-[3,4-bis(ethoxycarbonyloxy)phenyl]propanoate hydrochloride;

(1R)-2-acetyloxy-1-methylethyl (2S)-2-amino-3-[3,4-bis(ethoxycarbonyloxy)phenyl]propanoate hydrogen fumarate;

(1R)-1-methyl-2-(2-methylpropanoyloxy)ethyl (2S)-2-amino-3-[3,4-bis(ethoxycarbonyloxy)phenyl]propanoate hydrochloride, and

other pharmaceutically acceptable salts of any of the foregoing.

2. A pharmaceutical composition comprising at least one pharmaceutically acceptable vehicle and a therapeutically effective amount for treating a disease in a patient of at least one compound of claim 1 ; wherein the disease is chosen from schizophrenia, cognitive impairment disorders, restless legs syndrome, periodic limb movement disorders, tardive dyskinesia, Huntington's disease, hypertension, stroke, excessive daytime sleepiness, dystonia, and memory and learning deficit or loss.

3. The pharmaceutical composition of claim 2 , wherein the pharmaceutical composition is a sustained release oral dosage formulation.

4. A pharmaceutical composition comprising at least one pharmaceutically acceptable vehicle and a therapeutically effective amount for treating Parkinson's disease in a patient of at least one compound of claim 1 .

5. The pharmaceutical composition of claim 4 , wherein the pharmaceutical composition is a sustained release oral dosage formulation.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 25, 2018
From: XENOPORT, INC.
To: ARBOR PHARMACEUTICALS, LLC
Reel/Frame 046633/0753 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2018
From: ARBOR PHARMACEUTICALS, LLC
To: XENOPORT, INC.
Reel/Frame 046449/0306 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 29, 2012
From: XIANG, JIA-NING; ZHOU, CINDY X.; YAO, FENMEI; NGUYEN, MARK Q.
To: XENOPORT, INC.
Reel/Frame 029206/0174 →