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AU2002310788A1 - Treatment of dementia and neurodegenerative diseases with intermediate doses of LHRH antagonists - Google Patents

Treatment of dementia and neurodegenerative diseases with intermediate doses of LHRH antagonists

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Publication number
AU2002310788A1
AU2002310788A1 AU2002310788A AU2002310788A AU2002310788A1 AU 2002310788 A1 AU2002310788 A1 AU 2002310788A1 AU 2002310788 A AU2002310788 A AU 2002310788A AU 2002310788 A AU2002310788 A AU 2002310788A AU 2002310788 A1 AU2002310788 A1 AU 2002310788A1
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AU
Australia
Prior art keywords
use according
lhrh antagonist
methyl
treatment
monthly
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.)
Granted
Application number
AU2002310788A
Other versions
AU2002310788B2 (en
Inventor
Jurgen Engel
Rainer Voegeli
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Aeterna Zentaris GmbH
Original Assignee
Zentaris AG
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Filing date
Publication date
Application filed by Zentaris AG filed Critical Zentaris AG
Priority claimed from PCT/EP2002/004677 external-priority patent/WO2002102401A1/en
Publication of AU2002310788A1 publication Critical patent/AU2002310788A1/en
Application granted granted Critical
Publication of AU2002310788B2 publication Critical patent/AU2002310788B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Description

Treatment of dementia and neurodegenerative diseases with intermediate doses of LHRH antagonists
The present invention relates to the treatment of dementia and neurodegenerative diseases with intermediate doses of LHRH antagonists which do not cause a castration.
FURUYA, Shuichi et al. in WO 01/78780 teach preventives and remedies for Alzheimer's disesase containing a compound having GnRH antagonism have effects of preventing and treating Alzheimer's disease with little toxicity.
It has been shown in a study by Bowen R.L et al. that serum concentrations of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were significantly higher in individuals suffering of dementia , e.g. Alzheimer's disease. Bowen R.L. et al. propose in their patent application CA 2,309,395 (US priority June 4, 1999, 09/326,180) to lower FSH and LH to minimal levels by the use of castrating doses of analogues of the LH-releasing hormone (LHRH), either super-agonists or antagonists.
This treatment would be accompanied by highly undesirable side effects as lowering sex hormone levels to castration levels would result in loss or reduction of libido, sexual desire and sexual potency. In men and pre-menopausal women this treatment would also result in the typical symptoms of drop of sex hormones like hot flushes, etc. Women would additionally suffer from loss of bone minerals that would limit the treatment. These side effects could be reduced by hormone replacement therapy.
It has been found now that the treatment with intermediate doses of LHRH antagonists results in a sub-maximal lowering of FSH and LH to normal levels that leaves sex hormone levels above the castration treshold. This treatment is highly advantageous as it gives the desired results of normalising FSH and LH levels without the undesirable side-effects of sex hormone blockade. Thus the additional treatment of sex hormone replacement becomes superfluous. The present invention relates to the treatment of dementia and neurodegenerative diseases with intermediate doses of LHRH antagonists, wherein the antagonist is preferably cetrorelix, teverelix, antide or abarelix. The antagonist can also be the LHRH antagonist D-63 153 (Ac-D-Nal-D-pCI-Phe-D-Pal-Ser-N-Me-Tyr-D-Hci-Nle- Arg-Pro-D-Ala-NH2) as described in the PCT application WO 00/55190 A1.
The mentioned LHRH antagonists can also exhibit a heterocyclic skeletal structure. Such peptidomimetics can be for example
- 1 -[7-Chloro-3-(3,5-dimethyl-phenyl)-2-oxo-4-(2-piperidin-2-yl-ethoxy)-1 ,2- dihydro-quinolin-6-yl]-3-pyridin-2-yl-urea (described in WO 97/44339),
- 3-[Benzyl-methyl-amino)-methyl]-2-tørf-butyl-8-(2-fluoro-benzyl)-6-(3-methoxy- phenyl)-7-methyl-8H-imidazo[1 ,2-a]pyrimidin-5-one (described in WO 01/29044),
- 2-(2,5-Dimethyl-furan-3-yl)-8-(2-fluoro-benzyl)-3-([methyl-(2-pyridin-2-yl-ethyl)- amino]-methyl)-5-oxo-5,8-dihydro-imidazo[1 ,2-a]pyrimidine-6-carboxylic acid 1- ethyl-propylester (described in WO 00/69859),
- 3-((2-[2-(3,5-Difluoro-phenyl)-1-(2-methoxy-benzoyl)-2-oxo-ethylidene]-2,3- dihydro-1/7-benzoimidazol-5-yl-amino)-methyl)-benzonitrile (described in WO 02/02533).
The LHRH antagonist is given in a monthly dose of 10 to 100 mg per month and the treatment is repeated monthly, two-monthly or lasting several months.
In a preferred embodiment the LHRH antagonist is given in a monthly dose of 30 to 60 mg per month and the treatment is repeated monthly, two-monthly or lasting several months.
Pharmaceutical formulations of the LHRH antagonist suitable for the therapeutic management of dementia and neurodegenerative diseases may be for example a) acetate salt formulations of the active compounds in the concentration of 1 mg/1 ml or lower where the lyophilisate powder may be dissolved in water for injection or in gluconic acid;
b) acetate salt formulations of the active compounds in the concentration of 1.5 mg/1 ml to 5.0 mg/1 ml, preferably 2.5 mg/1 ml where the lyophilisate powder may be dissolved in water for injection or in gluconic acid;
c) pamoate salt formulations of the active compounds in the concentration of 10 mg/1 ml to 30 mg/1 ml, preferably 15 mg/1 ml where the lyophilisate powder may be dissolved in gluconic acid or in water for injection.
Suitable excipients and dosage forms are for example described by K.H. Bauer, K.-H. Frδmming and C. Fϋhrer, Lehrbuch der Pharmazeutischen Technologie, 6th edition, Stuttgart 1999, pages 163-186 (excipients) and pages 227-386 (dosage forms), including the references as cited therein.
The LHRH antagonist can be administered for example subcutaneous, oral, intramuscular or inhalative.
The disease as mentioned, for example can be treated in accordance with the following scheme.
Example
In one embodiment of the invention a single dose of 30-60 mg of cetrorelix is administered by injection per month. The treatment is continued monthly. In another embodiment the treatment is continued two-mothly or lasting several months after the administration of the single dose.

Claims

Claims
1. Use of a LHRH antagonist for the preparation of a medicament for the treatment of dementia and neurodegenerative diseases in humans by administration of intermediate doses, which do not cause a castration.
2. Use according to claim 1 , characterized in that the monthly single dose is in the range of 10 - 100 mg LHRH antagonist.
3. Use according to claims 1 and 2, characterized in that the monthly single dose is about 30 to about 60 mg LHRH antagonist.
4. Use according to one of claims 1 to 3, characterized in that the administration is continued on a monthly or two-monthly or lasting several months base.
5. Use according to one of claims 1 to 4, characterized in that the treated disease is Alzheimer's disease.
6. Use according to one of claims 1 to 5, characterized in that the LHRH antagonist is cetrorelix.
7. Use according to one of claims 1 to 5, characterized in that the LHRH antagonist is teverelix.
8. Use according to one of claims 1 to 5, characterized in that the LHRH antagonist is antide.
9. Use according to one of claims 1 to 5, characterized in that the LHRH antagonist is abarelix.
10. Use according to one of claims 1 to 5, characterized in that the LHRH antagonist is D-63 153 (Ac-D-Nal-D-pCI-Phe-D-Pal-Ser-N-Me-Tyr-D-Hci-Nle- Arg-Pro-D-Ala-NH2).
11. Use according to one of claims 1 to 5, characterized in that the LHRH antagonist is a peptidomimetic.
12. Use according to claim 11 in which the peptidomimetic is a compound
- 1 -[7-Chloro-3-(3,5-dimethyl-phenyl)-2-oxo-4-(2-piperidin-2-yl-ethoxy)-1 ,2- dihydro-quinolin-6-yl]-3-pyridin-2-yl-urea
- 3-[Benzyl-methyl-amino)-methyl]-2-te/ϊ-butyl-8-(2-fluoro-benzyl)-6-(3- methoxy-phenyl)-7-methyl-8H-imidazo[1,2-a]pyrimidin-5-one
- 2-(2,5-Dimethyl-furan-3-yl)-8-(2-fluoro-benzyl)-3-([methyl-(2-pyridin-2-yl- ethyl)-amino]-methyl)-5-oxo-5,8-dihydro-imidazo[1(2-a]pyrimidine-6- carboxylic acid 1-ethyl-propylester or
- 3-((2-[2-(3,5-Difluoro-phenyl)-1-(2-methoxy-benzoyl)-2-oxo-ethylidene]-2,3- dihydro-1H-benzoimidazol-5-yl-amino)-methyl)-benzonitrile.
AU2002310788A 2001-04-30 2002-04-27 Treatment of dementia and neurodegenerative diseases with intermediate doses of LHRH antagonists Ceased AU2002310788B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US28743401P 2001-04-30 2001-04-30
US60/287,434 2001-04-30
PCT/EP2002/004677 WO2002102401A1 (en) 2001-04-30 2002-04-27 Treatment of dementia and neurodegenerative diseases with intermediate doses of lhrh antagonists

Publications (2)

Publication Number Publication Date
AU2002310788A1 true AU2002310788A1 (en) 2003-05-15
AU2002310788B2 AU2002310788B2 (en) 2007-04-05

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2002310788A Ceased AU2002310788B2 (en) 2001-04-30 2002-04-27 Treatment of dementia and neurodegenerative diseases with intermediate doses of LHRH antagonists

Country Status (27)

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US (1) US7288517B2 (en)
EP (1) EP1392348B1 (en)
JP (1) JP2004529207A (en)
KR (1) KR20040000446A (en)
CN (1) CN1317030C (en)
AT (1) ATE400287T1 (en)
AU (1) AU2002310788B2 (en)
BG (1) BG108339A (en)
BR (1) BR0209290A (en)
CA (1) CA2444876A1 (en)
CZ (1) CZ20033167A3 (en)
DE (1) DE60227507D1 (en)
DK (1) DK1392348T3 (en)
ES (1) ES2307760T3 (en)
HU (1) HUP0400067A2 (en)
IL (1) IL156777A0 (en)
MX (1) MXPA03008666A (en)
NO (1) NO20034322L (en)
NZ (1) NZ544417A (en)
PL (1) PL362319A1 (en)
PT (1) PT1392348E (en)
RU (1) RU2319501C2 (en)
SI (1) SI1392348T1 (en)
SK (1) SK14512003A3 (en)
UA (1) UA80679C2 (en)
WO (1) WO2002102401A1 (en)
ZA (1) ZA200305326B (en)

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US20020077327A1 (en) * 1999-09-23 2002-06-20 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
EP1300398B1 (en) 2000-07-05 2006-04-05 Astellas Pharma Inc. Propane-1,3-dione derivatives
DE10137174A1 (en) * 2001-07-31 2003-02-13 Zentaris Ag Use of LHRH antagonists in non-castrating doses to improve T cell-mediated immunity
US7709519B2 (en) * 2004-06-04 2010-05-04 Astellas Pharma Inc. Benzimidazolylidene propane-1,3 dione derivative or salt thereof
US20080171736A1 (en) * 2004-12-23 2008-07-17 Gregory Christopher W Treatment of Alzheimer's Disease and Mild Cognitive impairment using GnRH-I analogs and one or more of acetylcholinesterase inhibitors and NMDA receptor antagonists
CA2590997A1 (en) * 2004-12-23 2006-07-06 Voyager Pharmaceutical Corporation Leuprolide acetate and acetylcholinesterase inhibitors or nmda receptor antagonists for the treatment of alzheimer`s disease
BRPI0609625A2 (en) 2005-03-31 2010-04-20 Astellas Pharma Inc propane-1,3-dione derivatives or salt thereof
BRPI0717618A2 (en) 2006-10-21 2013-10-22 Abbott Gmbh & Co Kg HYPEROCYCLIC COMPOUNDS AND USE OF THE SAME AS GLYCOGEN SYNTASE KINASE 3 INHIBITORS
WO2009043437A2 (en) * 2007-09-11 2009-04-09 Mondobiotech Laboratories Ag Use of a peptide as a therapeutic agent
EP2187917A2 (en) * 2007-09-11 2010-05-26 Mondobiotech Laboratories AG Use of neuropeptide sf, alone or in combination with glp-2, as a therapeutic agent
EP2095818A1 (en) * 2008-02-29 2009-09-02 AEterna Zentaris GmbH Use of LHRH antagonists at non-castrating doses
US20110129532A1 (en) * 2008-05-29 2011-06-02 Isr Immune System Regulation Ab Method and means for treating viral disease, in particular hiv/aids
CN103119035B (en) 2010-09-27 2015-09-30 雅培股份有限两合公司 Heterogeneous ring compound and they are as the purposes of GSK-3 inhibitor
US9090592B2 (en) 2010-12-30 2015-07-28 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
EP3560555A1 (en) * 2018-04-26 2019-10-30 LifeArc A composition for treating one or more estrogen related diseases
WO2025155903A1 (en) * 2024-01-19 2025-07-24 Temple University-Of The Commonwealth System Of Higher Education Compositions of antioxidant translation modulators for treating neurodegenerative disorders

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US3135743A (en) 1960-06-29 1964-06-02 Sterling Drug Inc Steroido[2. 3-d]isoxazoles and preparation thereof
EP0901489A1 (en) 1996-05-20 1999-03-17 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
DE19911771B4 (en) * 1999-03-17 2006-03-30 Zentaris Gmbh LHRH antagonist, process for its preparation and its use
WO2000069859A1 (en) * 1999-05-14 2000-11-23 Neurocrine Biosciences, Inc. Imidazo- and pyrrolo[1,2-a]pyrimid-4-ones as gonadotropin-releasing hormone receptor antagonists
CA2309395A1 (en) * 1999-06-04 2000-12-04 Richard Lloyd Bowen Methods for preventing and treating alzheimer's disease
KR20020045609A (en) * 1999-10-15 2002-06-19 추후기재 Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
WO2001078780A1 (en) 2000-04-13 2001-10-25 Takeda Chemical Industries, Ltd. Preventives/remedies for alzheimer's disease
EP1300398B1 (en) 2000-07-05 2006-04-05 Astellas Pharma Inc. Propane-1,3-dione derivatives

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