IP Library Granted Patent US 8,609,641
Granted Patent B2
US 8,609,641 · App. 10/587,637 · Granted Dec 17, 2013

(S)-2-N-propylamino-5-hydroxytetralin as a D3-agonist

Inventors: Dieter Scheller (Neuss, DE); Klaus Hansen (Grevenbroich-Münchrath, DE)
Assignee: UCB Pharma GmbH
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Quick Facts
Patent No.
US 8,609,641
App. No.
10/587,637
Granted
Dec 17, 2013
Kind
B2
Abstract

The invention relates to a medicament containing (S)-2-N-propylamino-5-hydroxytetralin, the salts or prodrugs thereof. As a D3 agonist, (S)-2-N-propylamino-5-hydroxytetralin is suitable particularly for the treatment of dopa-sensitive movement disorders.

Claims (14)

1. A pharmaceutical composition comprising (S)-2-N-propylamino-5-hydroxytetralin or a pharmaceutically acceptable salt or prodrug thereof, and at least one pharmaceutically acceptable carrier or adjuvant, wherein the prodrug is of the formula

or a salt thereof;

wherein R 1 is selected from the group consisting of acyl, alkoxycarbonyl, cycloalkoxycarbonyl, aryloxycarbonyl, acetal, ketal, —C(O)NR 2 R 3 , —C(O)NHR 2 , —P(O 2 H)OR 2 and —P(O 2 H)R 2 , wherein R 2 and R 3 are independently selected from H, C 1-6 alkyl, C 3-10 cycloalkyl, benzyl and phenyl and

wherein the at least one pharmaceutically acceptable carrier or adjuvant is selected from the group consisting of fillers, disintegrants, binders, lubricants, stabilizers, flavors, antioxidants, preservatives, dispersants, buffers and electrolytes; and

wherein the pharmaceutical composition is in a form selected from the group consisting of an infusion solution, an injection solution, an oil, a suppository, a patch, a microcapsule and a microparticle.

2. The composition of claim 1 , comprising (S)-2-N-propylamino-5-hydroxytetralin or a pharmaceutically acceptable salt thereof.

3. The composition of claim 1 , comprising a prodrug or a salt thereof wherein R 1 is selected from C 1-6 alkylcarbonyl, C 3-10 cycloalkylcarbonyl, benzoyl, —C(O)NR 2 R 3 and —C(O)NHR 2 .

4. The composition of claim 1 , wherein the (S)-2-N-propylamino-5-hydroxytetralin or salt or prodrug thereof is present as a pure (S)-enantiomer.

5. A compound having the formula

or a salt thereof;

wherein R 1 is selected from the group consisting of acyl, alkoxycarbonyl, cycloalkoxycarbonyl, aryloxycarbonyl, acetal, ketal, —C(O)NR 2 R 3 , —C(O)NHR 2 , —P(O 2 H)OR 2 and —P(O 2 H)R 2 , wherein R 2 and R 3 are independently selected from H, C 1-6 alkyl, C 3-10 cycloalkyl, benzyl and phenyl;

said compound being in the (S)-configuration; and

wherein said compound, when administered to a human body, is cleaved, processed or metabolized to (S)-2-N-propylamino-5-hydroxytetralin.

6. The compound of claim 5 , wherein R 1 is selected from C 1-6 alkylcarbonyl, C 3-10 cycloalkylcarbonyl, benzoyl, —C(O)NR 2 R 3 and —C(O)NHR 2 .

Assignments (3)
MERGER Recorded Jul 12, 2012
From: SRZ PROPERTIES, INC.
To: UCB MANUFACTURING, INC.
Reel/Frame 028535/0465 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2012
From: UCB MANUFACTURING, INC.
To: UCB PHARMA GMBH
Reel/Frame 028535/0510 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 4, 2009
From: SCHELLER, DIETER; HANSEN, KLAUS
To: SRZ PROPERTIES, INC.
Reel/Frame 022341/0995 →
Priority Claims (1)
DE 103 59 528 · Dec 18, 2003 · national
Continuity (1)
Related Publication 20070197480A1 · Aug 23, 2007