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1. US20180265482 - Methods for producing viloxazine salts and novel polymorphs thereof

Office United States of America
Application Number 15988190
Application Date 24.05.2018
Publication Number 20180265482
Publication Date 20.09.2018
Grant Number 10160733
Grant Date 25.12.2018
Publication Kind B2
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
265
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
28
1,4-Oxazines; Hydrogenated 1,4-oxazines
30
not condensed with other rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
265
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
28
1,4-Oxazines; Hydrogenated 1,4-oxazines
30
not condensed with other rings
32
with oxygen atoms directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
215
Compounds containing amino and hydroxy groups bound to the same carbon skeleton
02
having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
04
the carbon skeleton being saturated
06
and acyclic
08
with only one hydroxy group and one amino group bound to the carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
217
Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
02
having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
04
the carbon skeleton being acyclic and saturated
28
having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines
30
having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring
32
the six-membered aromatic ring or condensed ring system containing that ring being further substituted
34
by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms
C07D 265/30
C07D 265/32
C07C 215/08
C07C 217/34
CPC
C07C 215/08
C07C 217/34
C07D 265/30
C07D 265/32
Applicants Supernus Pharmaceuticals, Inc.
Inventors Likan Liang
Padmanabh P. Bhatt
David Dain
Jean-Philippe Taquet
Aleksandr Pechenov
Alexei Tchesnokov
Reynold Mariaux
Agents Foley & Lardner LLP
Sunit Talapatra
Title
(EN) Methods for producing viloxazine salts and novel polymorphs thereof
Abstract
(EN)

Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.