IP Library Granted Patent US 7,763,638
Granted Patent B2
US 7,763,638 · App. 10/598,449 · Granted Jul 27, 2010

Substituted 1,2,3,4-tetrahydroisoquinoline derivatives

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Quick Facts
Patent No.
US 7,763,638
App. No.
10/598,449
Granted
Jul 27, 2010
Kind
B2
Abstract

The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to a mammal.

Claims (8)

1. The compound (2R)-2-{(1S)-6,7-dimethoxy-1-[2-(4-trifluoromethyl-phenyl)-ethyl]-3,4-dihydro-1H-isoquinolin-2-yl}-N-methyl-2-phenyl-acetamide, structurally represented by formula (II):

in free or pharmaceutically acceptable salt form.

2. The compound according to claim 1 which is (2R)-2-{(1S)-6,7-dimethoxy-1-[2-(4-trifluoromethyl-phenyl)-ethyl]-3,4-dihydro-1H-isoquinolin-2-yl}-N-methyl-2-phenyl-acetamide in free base form.

3. The compound according to claim 1 which is (2R)-2-{(1S)-6,7-dimethoxy-1-[2-(4-trifluoromethyl-phenyl)-ethyl]-3,4-dihydro-1H-isoquinolin-2-yl}-N-methyl-2-phenyl-acetamide in pharmaceutically acceptable acid addition salt form;

wherein the acidic component of the acid addition salt is selected from the group consisting of hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, phosphoric acid, nitric acid, citric acid, formic acid, acetic acid, maleic acid, tartaric acid, fumaric acid, benzoic acid, pamoic acid, stearic acid, methanesulfonic acid, p-toluenesulfonic acid, salicylic acid, succinic acid, and trifluoroacetic acid.

4. The compound according to claim 1 which is (2R)-2-{(1S)-6,7-dimethoxy-1-[2-(4-trifluoromethyl-phenyl)-ethyl]-3,4-dihydro-1H-isoquinolin-2-yl}-N-methyl-2-phenyl-acetamide hydrochloric acid salt.

5. A pharmaceutical composition comprising at least one compound according to any one of claims 1 - 4 and a pharmaceutically acceptable carrier material.

6. A method of preventing or treating insomnia comprising administering to a subject in need thereof an effective amount of the compound according to any one of claims 1 - 4 .

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE ASSIGNEE ADDRESS PREVIOUSLY RECORDED AT REEL: 042464 FRAME: 0407. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jun 28, 2017
From: ACTELION PHARMACEUTICALS LTD
To: IDORSIA PHARMACEUTICALS LTD
Reel/Frame 043017/0022 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 13, 2017
From: ACTELION PHARMACEUTICALS LTD
To: IDORSIA PHARMACEUTICALS LTD
Reel/Frame 042464/0407 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 1, 2006
From: AISSAOUI, HAMED; CLOZEL, MARTINE; FISCHLI, WALTER; KOBERSTEIN, RALF; WELLER, THOMAS
To: ACTELION PHARMACEUTICALS, LTD.
Reel/Frame 018261/0266 →