Paxil Patent 6063927 With Pediatric Extention

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Patent Family
paroxetine (product, mesilate, 1998)

Trade Name(s)
CASBOL
SEROXAT
AROPAX
PAXIL
TAGONIS
FROSINOR
DEROXAT
SEREUPIN
MOTIVAN

Generic Name(s)
paroxetine (INN)
paroxetine hydrochloride (INN)
paroxetine mesylate (USAN)

Lab Code(s)
FR 7051
BRL 29060
BRL 29060A
SI 211103

CAS Number
61869-08-7 paroxetine
110429-35-1 paroxetine hydrochloride hemihydrate (1:1:0.5)
78246-49-8 paroxetine hydrochloride (1:1)
121368-57-8 paroxetine hydrobromide (1:1)
64006-44-6 paroxetine maleate (1:1)
217797-14-3 paroxetine mesylate (1:1)
63952-24-9 replaced by 61869-08-7
172501-13-2 replaced by 78246-49-8
217797-12-1 replaced by 64006-44-6

Chemical Name
(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine

Class Description
SSRI antidepressants (N6A4)
Tranquillisers (N5C)

Indication
depression
obsessive compulsive disorder
anxiety
panic disorder

Action
5HT reuptake inhibitor

Latest Phase
Marketed

Company
GlaxoSmithKline, UK

Patentee
SmithKline Beecham, UK

Patent Country
USA

Priority Details
02 Jul 1998 : UK, 14316
06 Oct 1998 : UK, 21732
10 Feb 1999 : UK, 2935
22 Jun 1999 : UK, 14601
23 Jun 1999 : UK, 14709
23 Jun 1999 : UK, 14712
28 Jun 1999 : UK, 15096
19 Nov 1999 : UK, 27498
19 Nov 1999 : UK, 27501
03 Dec 1999 : UK, 28693

Patent Number
6063927

Patent Date
16 May 2000

Patent Type
Process

Filing Date
23 Apr 1999

Est. Expiry Date
23 Oct 2019

Expiry Comment
Extended

Country Comment
US 6063927 claims paroxetine mesilate in crystalline form and claims paroxetine hydrochloride formed by reacting this with hydrochloric acid.Pediatric exclusivity of 6 months has been granted in the USA for US 6063927. The new expiry date is 23 October 2019 from 23 April 2019.US 6063927 was quoted by the FDA Orange Book as relating to the PAXIL 10 mg, 20 mg, 30 mg and 40 mg oral tablet formulations, the PAXIL CR 12.5 mg, 25 mg a nd 37.5 mg oral extended release tablet formulations and the PAXIL 10 mg/5 ml oral suspension formulation of paroxetine hydrochloride equivalent to paroxetine base.All of these formulations have since been delisted from the FDA Orange Book.US marketing exclusivity for the PAXIL oral suspension for the treatment of social anxiety disorder expired on 17 May 2002.US marketing exclusivities for the PAXIL extended release tablet formulations expire on 16 February 2002. US marketing exclusivities for the PAXIL oral tablet formulations expired on 17 May 2002 for the treatment of social anxiety disorder and on 13 April 2004 for the treatment of generalised anxiety disorder.

General Comment
The patent family here is quite complex with 10 inter-related priorities and give rise to 4 PCT applications:WO 00/1692 which quotes UK priority 14316 and claims paroxetine acid salts where the acid is from a defined list of several thousand named acids. The salts claimed can be non-crystalline or crystalline. Also claimed is the use of each salt as an alternative to the currently marketed hydrochloride or as an intermediate in the preparation of the hydrochloride.WO 00/1694 which quotes UK priorities 14316, 21732 and 14601 and has specific product claims to paroxetine mesilate, in crystalline or non-crystalline form. The preparation of paroxetine hydrochloride from paroxetine mesilate is also claimed.WO 00/78290 which quotes UK priorities 14601, 14712, 27498 and 28693 claims compositions of paroxetine salts which are more water soluble than paroxetine hydrochloride hemihydrate. Compositions of paroxetine mesilate are specifically claimed.WO 00/78291 which quotes UK priorities 14601, 14709 and 27501 and claims compositions of paroxetine mesilate.The patent family listed here relates to the PAXIL and PAXIL CR formulations of paroxetine.Last reviewed: June 2009