IP Library Granted Patent US 10,676,432
Granted Patent B2
US 10,676,432 · App. 16/107,836 · Granted Jun 9, 2020

Methods of producing molindone and its salts

Inventors: Martin Hanbauer (Regensburg, DE); Zarghun Nazir (Linz, AT); Peter Hildebrand (Linz, AT); Attilia Figini (Rancate, CH); Likan Liang (Boyds, MD); Tiziano Fumagalli (Pianello del Lario, IT)
Assignee: Supernus Pharmaceuticals, Inc.
C07D209/08C07D295/13
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Quick Facts
Patent No.
US 10,676,432
App. No.
16/107,836
Granted
Jun 9, 2020
Kind
B2
Abstract

The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.

Claims (13)

1. A composition consisting of molindone or its pharmaceutically acceptable salts as the sole active ingredient and comprising formaldehyde, (Z)—N-[(2Z)-2-(hydroxyimino)pentan-3-ylidene]hydroxylamine, (E)-N-ethylidenehydroxylamine, and (2Z)-2-(hydroxyimino)propan-1-ol.

2. The composition of claim 1 , comprising less than 1.5 micrograms per human daily dose of each of formaldehyde, (Z)—N-[(2Z)-2-(hydroxyimino)pentan-3-ylidene]hydroxylamine, (E)-N-ethylidenehydroxylamine, (2Z)-2-(hydroxyimino)propan-1-ol.

3. A composition comprising molindone or its pharmaceutically acceptable salts as the sole active ingredient, formaldehyde, (Z)—N-[(2Z)-2-(hydroxyimino)pentan-3-ylidene]hydroxylamine, (E)-N-ethylidenehydroxylamine, and (2Z)-2-(hydroxyimino)propan-1-ol.

4. The compositions of claim 3 , comprising less than 1.5 micrograms per human daily dose of each of formaldehyde, (Z)—N-[(2Z)-2-(hydroxyimino)pentan-3-ylidene]hydroxylamine, (E)-N-ethylidenehydroxylamine, (2Z)-2-(hydroxyimino)propan-1-ol.

5. A composition comprising molindone or its pharmaceutically acceptable salts as the sole active ingredient and formaldehyde.

6. A composition comprising molindone or its pharmaceutically acceptable salts as the sole active ingredient, formaldehyde, and (Z)—N-[(2Z)-2-(hydroxyimino)pentan-3-ylidene]hydroxylamine.

7. A composition comprising molindone or its pharmaceutically acceptable salts as the sole active ingredient, formaldehyde, (Z)—N-[(2Z)-2-(hydroxyimino)pentan-3-ylidene]hydroxylamine, and (E)-N-ethylidenehydroxylamine.

8. A composition comprising molindone or its pharmaceutically acceptable salts as the sole active ingredient and (Z)—N-[(2Z)-2-(hydroxyimino)pentan-3-ylidene]hydroxylamine.

9. A composition comprising molindone or its pharmaceutically acceptable salts as the sole active ingredient, (Z)—N-[(2Z)-2-(hydroxyimino)pentan-3-ylidene]hydroxylamine, and (E)-N-ethylidenehydroxylamine.

10. A composition comprising molindone or its pharmaceutically acceptable salts as the sole active ingredient, (Z)—N-[(2Z)-2-(hydroxyimino)pentan-3-ylidene]hydroxylamine, (E)-N-ethylidenehydroxylamine, and (2Z)-2-(hydroxyimino)propan-1-ol.

11. A composition comprising molindone or its pharmaceutically acceptable salts as the sole active ingredient and (E)-N-ethylidenehydroxylamine.

12. A composition comprising molindone or its pharmaceutically acceptable salts as the sole active ingredient, (E)-N-ethylidenehydroxylamine, and (2Z)-2-(hydroxyimino)propan-1-ol.

13. A composition comprising molindone or its pharmaceutically acceptable salts as the sole active ingredient and (2Z)-2-(hydroxyimino)propan-1-ol.

Continuity (6)
Continuation 15723515 · Oct 3, 2017
Continuation 15365566 · Nov 30, 2016
Continuation 14608262 · Jan 29, 2015
Division 13834097 · Mar 15, 2013
Provisional Application 61701007 · Sep 14, 2012
Related Publication 20190218179A1 · Jul 18, 2019