AU2006201188B2 - New use of iloperidone - Google Patents
New use of iloperidone Download PDFInfo
- Publication number
- AU2006201188B2 AU2006201188B2 AU2006201188A AU2006201188A AU2006201188B2 AU 2006201188 B2 AU2006201188 B2 AU 2006201188B2 AU 2006201188 A AU2006201188 A AU 2006201188A AU 2006201188 A AU2006201188 A AU 2006201188A AU 2006201188 B2 AU2006201188 B2 AU 2006201188B2
- Authority
- AU
- Australia
- Prior art keywords
- treatment
- benzisoxazol
- ethanone
- piperidinyl
- methoxyphenyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
P/00/011 Regulation 3.2
AUSTRALIA
Patents Act 1990 COMPLETE SPECIFICATION STANDARD PATENT
(ORIGINAL)
Name of Applicant: Actual Inventor: Address for Service: Invention Title: Novartis AG, of Lichtstrasse 35, CH-4056 Basel, Switzerland Hans O Kalkman DAVIES COLLISON CAVE, Patent Trademark Attorneys, of 1 Nicholson Street, Melbourne, 3000, Victoria, Australia Ph: 03 9254 2777 Fax: 03 9254 2770 Attorney Code: DM "New use of iloperidone" The following statement is a full description of this invention, including the best method of performing it known to us:- P \OPER\M4a2006\I 2744170 div claims 081 doc-22/03/06 0-1- E NEW USE OF ILOPERIDONE N, This is a divisional of Australian patent application No. 2002231766 (2002231766), the entire contents of which are incorporated herein by reference.
00 00 The present invention relates to a new pharmaceutical use of 1-[4-[3-[4-(6-fluoro-1,2- O benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxyphenyl]ethanone (iloperidone), and its \O pharmaceutically acceptable acid addition salts, hereinafter referred to as "agents of the invention".
The agents of the invention and their production process are known e.g. from EP 402 644. This patent also discloses the use of the agents of the invention as antipsychotics.
In accordance with the present invention, it has now surprisingly been found that the agents of the invention are useful in the treatment of affective disorders including bipolar mood disorders.
The activity of the agents of the invention in said treatment is evidenced, for example, in the following tests suitable for detecting drugs having potential behavioral disinhibitory and/or sociotropic effects which are thought to be relevant for recovery from social withdrawal, a cardinal feature of depression and related psychiatric conditions.
a) The Half Enclosed Platform Test This test is basically as described in Psychopharmacology, 1986, 89:31-37.
Groups of 12 male OF-1 mice are given vehicle or the substance 1 hour before being tested on the platform. The apparatus consists of a transparent platform perforated with 25 equally-spaced 1 cm holes. The platform is divided into equal halves by a 15 cm high, semi-rectangular wall enclosing one half of the platform, the other half having open edges. The whole platform rests on four 15 cm high legs. A line down the middle runs from the edge of one wall to the edge of the opposite wall. The experiment consists of placing a mouse on the midline and recording their behaviour for 5 minutes as they explore the platform. In particular, the mean frequencies and durations of the behavioral elements are recorded and statistical comparisons are determined using the Kruskal-Wallis test followed by paired comparisons between control and treatment groups using the Mann-Whitney U-test.
C Probabilities quoted are 2-tailed.
00 At doses of about 0.3 to about 10 mg/kg the agents of the invention 00 0 significantly increase exploratory behaviour, such as stretched attend posture, head raising and forward locomotion, in the open half of the platform, which decreasing rCl the frequency of stationary elements, such as sitting still and inactivity, in the Senclosed half of the platform.
b) The Elevated Plus-maze Paradigm in mice This test is basically as described in Behav. Pharmacol., 1998, 8: 477-496.
At doses of about 1 to about 10mg/kg the agents of the invention significantly increase the time spent on the open arms. These findings are consistent with the Half Enclosed Platform test results.
c) The amphetamine-induced hypermotility test This test is performed according to the method described by Arnt J in Eur. J.
Pharmacol, 283, 55-62 (1995).
At doses of about 0,01 to about 10 mg/kg the agents of the invention significantly inhibit the amphetamine-induced locomotion in the animals.
In view of their behavioral desinhibitory anxiolytic or antidepressant- like) and sociotropic activity, the agents of the invention are useful in the treatment of affective disorders including bipolar disorders, e.g. manic and depressive disorders, cyclothymia, schizo-affective disorders and excessive mood swings where behavioral stabilization is desired. In addition, the compounds are indicated in ADHD (attention deficit hyperactivity disorders) and behavioral disorders associated with dementia and Parkinson's disease.
As evidenced by the elevated.maze test, an effect is anticipated in anxiety disorders, (e.g.
generalized anxiety, social phobia and agoraphobia), as well as those behavioral states Scharacterized by social withdrawal autism and psychoses with predominant negative Ssymptoms [hebephrenia]).
00 For the above-mentioned indications the appropriate dosage will vary depending upon, for 00 example, the compound employed, the host, the mode of administration and the nature and severity of the condition being treated. However, in general, satisfactory results in O animals are indicated to be obtained at a daily dosage of from about 1 to about 50 mg/kg O animal body weight. Daily doses in larger mammals, such as humans, depend on the outcome of clinical studies in the different behavioral disorders and vary from about 1 to (about 50mg of an agent of the invention, conveniently administered in divided doses up to two times a day.
The agents of the invention may be administered in any usual manner, e.g. orally, for example in the form of tablets or capsules, or parenterally, for example in the form of injection solutions or suspensions.
The present invention also provides pharmaceutical compositions comprising an agent of the invention in association with at least one pharmaceutical carrier or diluent, for use in the treatment of affective and attention disorders. Such compositions may be manufactured in conventional manner. Unit dosage forms may contain for example from about 0.1 mg to about 25 mg of the compound of formula I.
The invention further provides the use of an agent of the invention for the manufacture of a pharmaceutical composition for the treatment of affective and attention/behavioral disorders.
The invention furthermore provides a method for the treatment of affective and attention disorders in a subject in need of such treatment, which comprises administering to said subject a therapeutically effective amount of an agent of the invention.
P:\OPERMaIU206\1 2744170 div claims 081.doc-22A)3/06 -4- Throughout this specification and the claims which follow, unless the context requires ,I otherwise, the word "comprise", and variations such as "comprises" and "comprising", will be understood to imply the inclusion of a stated integer or step or group of integers or steps but not the exclusion of any other integer or step or group of integers or steps.
00 00 The reference in this specification to any prior publication (or information derived from it), or IC to any matter which is known, is not, and should not be taken as an acknowledgment or admission or any form of suggestion that that prior publication (or information derived from it) C or known matter forms part of the common general knowledge in the field of endeavour to which this specification relates.
Claims (4)
1. 1 -[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-I -piperidinyl]propoxy]-3- 00 5 methoxyphenyl]ethanone and its pharmaceutically acceptable acid addition salts, when used in the treatment of a bipolar disorder.
O S2. The use of 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-l-piperidinyl]propoxy]-3- C1 methoxyphenyl]ethanone or a pharmaceutically acceptable acid addition salt thereof, in the manufacture of a pharmaceutical composition for the treatment of a bipolar disorder.
3. A method for the treatment of a bipolar disorder in a subject in need of such treatment, which comprises administering to said subject a therapeutically effective amount of 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3- methoxyphenyl]ethanone or a pharmaceutically acceptable acid addition salt thereof.
4. A use according to claim 1 or claim 2 or a method according to claim 3 substantially as hereinbefore described. DATED this 22nd day of March, 2006 Novartis AG By DAVIES COLLISON CAVE Patent Attorneys for the Applicant
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU2006201188A AU2006201188B2 (en) | 2001-02-05 | 2006-03-22 | New use of iloperidone |
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0102841.4A GB0102841D0 (en) | 2001-02-05 | 2001-02-05 | Organic compounds |
GB0102841.4 | 2001-02-05 | ||
AU2002231766A AU2002231766B2 (en) | 2001-02-05 | 2002-02-04 | New use of iloperidone |
PCT/EP2002/001130 WO2002064141A1 (en) | 2001-02-05 | 2002-02-04 | New use of iloperidone |
AU2006201188A AU2006201188B2 (en) | 2001-02-05 | 2006-03-22 | New use of iloperidone |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AU2002231766A Division AU2002231766B2 (en) | 2001-02-05 | 2002-02-04 | New use of iloperidone |
Publications (2)
Publication Number | Publication Date |
---|---|
AU2006201188A1 AU2006201188A1 (en) | 2006-04-13 |
AU2006201188B2 true AU2006201188B2 (en) | 2007-11-15 |
Family
ID=36251981
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AU2006201188A Expired AU2006201188B2 (en) | 2001-02-05 | 2006-03-22 | New use of iloperidone |
Country Status (1)
Country | Link |
---|---|
AU (1) | AU2006201188B2 (en) |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0402644B1 (en) * | 1989-05-19 | 1995-08-16 | Hoechst-Roussel Pharmaceuticals Incorporated | N-(aryloxyalkyl)heteroarylpiperidines and -heteroarylpiperazines,a process for their preparation and their use as medicaments |
US5955459A (en) * | 1997-11-26 | 1999-09-21 | Neuromedica, Inc. | Fatty acid-antipsychotic compositions and uses thereof |
WO2000023057A2 (en) * | 1998-10-16 | 2000-04-27 | Janssen Pharmaceutica N.V. | Atypical antiphsychotic in combination with acetylcholinesterase inhibitor for improving cognition |
-
2006
- 2006-03-22 AU AU2006201188A patent/AU2006201188B2/en not_active Expired
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0402644B1 (en) * | 1989-05-19 | 1995-08-16 | Hoechst-Roussel Pharmaceuticals Incorporated | N-(aryloxyalkyl)heteroarylpiperidines and -heteroarylpiperazines,a process for their preparation and their use as medicaments |
US5955459A (en) * | 1997-11-26 | 1999-09-21 | Neuromedica, Inc. | Fatty acid-antipsychotic compositions and uses thereof |
WO2000023057A2 (en) * | 1998-10-16 | 2000-04-27 | Janssen Pharmaceutica N.V. | Atypical antiphsychotic in combination with acetylcholinesterase inhibitor for improving cognition |
Also Published As
Publication number | Publication date |
---|---|
AU2006201188A1 (en) | 2006-04-13 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CA2359877A1 (en) | Combination treatment for dementia or cognitive deficits associated with alzheimer's disease and parkinson's disease | |
JP2008538583A (en) | Methods for treating apathy syndrome | |
CA2694866A1 (en) | Novel use of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and its physiologically acceptable salts | |
EP1541197B1 (en) | Use of pipamperone and an SNDRI, SNRI or SSRI for the treatment of mood or anxiety disorders | |
US20090131477A1 (en) | New use of iloperidone | |
US8168785B2 (en) | Benzothiazole derivatives | |
AU2006201188B2 (en) | New use of iloperidone | |
JP6830895B2 (en) | Triazolopyridine and triazolopyrimidines that reduce stress-induced p-tau | |
AU2002231766A1 (en) | New use of iloperidone | |
Marzanatti et al. | Effects of nonsedating histamine H1-antagonists on EEG activity and behavior in the cat | |
AU704695B2 (en) | Pyridyl-and pyrimidyl-piperazines in the treatment of substance abuse disorders | |
CN1247578C (en) | Dementia remedies containing 2-aryl-8-oxodihydropurine derivatives as the active ingredient | |
US11840731B2 (en) | Method for diagnosing and treating subjects having single nucleotide polymorphisms in chromosome 2, 2:107,510,000-107,540,000 locus | |
Shopsin et al. | Serotonin and depression | |
US20240068035A1 (en) | Method for diagnosing and treating subjects having single nucleotide polymorphisms in chromosome 2, 2:107,510,000-107,540,000 locus | |
Neshkes et al. | Pharmacologic approach to the treatment of senile dementia | |
JP2014507370A (en) | Treatment of cognitive impairment using certain alpha-7 nicotinic acid receptor agonists in combination with acetylcholinesterase inhibitors | |
Bai et al. | Psychopharmacotherapy in Patients with Tics and Other Motor Disorders | |
Scates et al. | Focus on citalopram: A selective serotonin reuptake inhibitor for the treatment of depression | |
Post-MI | IV. MEDICAL CAUSES OF DEPRESSION | |
JP2005060286A (en) | Treatment of schizophrenia |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FGA | Letters patent sealed or granted (standard patent) | ||
MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |