IP Library Granted Patent US 11,591,327
Granted Patent B2
US 11,591,327 · App. 16/877,284 · Granted Feb 28, 2023

Acid addition salts of piperazine derivatives

Inventors: Anna Quattropani (Rolle, CH); Santosh S. Kulkarni (Bangalore, IN); Awadut Gajendra Giri (Bangalore, IN); Dawn V. Toronto (Saint Lamain, FR); David Malcolm Crowe (Reading, GB)
Assignee: Asceneuron SA
C07D417/14C07D405/12C07D405/14C07D417/12C07D513/04
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Quick Facts
Patent No.
US 11,591,327
App. No.
16/877,284
Granted
Feb 28, 2023
Kind
B2
Abstract

The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glycosidase inhibitors.

Claims (10)

1. An acid addition salt of hydrochloric acid, maleic acid, tartaric acid, sulfuric acid, or p-toluolsufonic acid with one of the following compounds:

2. An acid addition salt selected from the group consisting of:

N-(5-{4-[(1 S)-1-(2,3-dihydro-1-benzofuran-6-yl)ethyl]piperazin-1-yl}-1,3,4-thiadiazol-2-yl)acetamide, mono-hydrochloride;

N-(5-{4-[(1 S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}-1,3,4-thiadiazol-2-yl)acetamide, mono-hydrochloride;

2-{4-[(1S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}-N-methyl-1,3-thiazole-5-carboxamide, mono-hydrochloride;

2-{4-[(1S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}-N-methylpyrimidine-5-carboxamide, mono-hydrochloride;

N-(2-{4-[(1 S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}pyrimidin-5-yl)acetamide, mono-hydrochloride; and

2-{4-[(1S)-1-(2,3-dihydro-1-benzofuran-6-yl)ethyl]piperazin-1-yl}-4H,5H,6H,7H-[1,3]thiazolo[5,4-c]pyridin-4-one, mono-hydrochloride.

3. A solid oral dosage form comprising the acid addition salt of claim 1 .

4. A solid oral dosage form comprising the acid addition salt of claim 2 .

Assignments (3)
RELEASE OF SECURITY INTEREST Recorded Feb 23, 2023
From: KREOS CAPITAL VI (UK) LIMITED
To: ASCENEURON SA
Reel/Frame 062789/0477 →
SECURITY INTEREST Recorded Mar 22, 2022
From: ASCENEURON SA
To: KREOS CAPITAL VI (UK) LIMITED
Reel/Frame 059337/0849 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 19, 2020
From: QUATTROPANI, ANNA; KULKARNI, SANTOSH S.; GIRI, AWADUT GAJENDRA; TORONTO, DAWN V.; CROWE, DAVID MALCOLM
To: ASCENEURON SA
Reel/Frame 052697/0099 →
Priority Claims (1)
IN 201621006638 · Feb 25, 2016 · national
Continuity (2)
Division 16079162
Related Publication 20200385375A1 · Dec 10, 2020
Cited By (3)
US 12,187,741 US 12,195,455 US 12,398,130