[go: up one dir, main page]

WO1999047131A3 - Combination of a gaba-a alpha 5 inverse agonist and an acetylcholinesterase inhibitor - Google Patents

Combination of a gaba-a alpha 5 inverse agonist and an acetylcholinesterase inhibitor Download PDF

Info

Publication number
WO1999047131A3
WO1999047131A3 PCT/GB1999/000778 GB9900778W WO9947131A3 WO 1999047131 A3 WO1999047131 A3 WO 1999047131A3 GB 9900778 W GB9900778 W GB 9900778W WO 9947131 A3 WO9947131 A3 WO 9947131A3
Authority
WO
WIPO (PCT)
Prior art keywords
combination
inverse agonist
gaba
alpha
acetylcholinesterase inhibitor
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.)
Ceased
Application number
PCT/GB1999/000778
Other languages
French (fr)
Other versions
WO1999047131A2 (en
Inventor
Gerard Raphael Dawson
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.)
Organon Pharma UK Ltd
Original Assignee
Merck Sharp and Dohme Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Merck Sharp and Dohme Ltd filed Critical Merck Sharp and Dohme Ltd
Priority to EP99909095A priority Critical patent/EP1061952A2/en
Priority to JP2000536371A priority patent/JP2002506815A/en
Priority to CA002323618A priority patent/CA2323618A1/en
Priority to AU28464/99A priority patent/AU753077B2/en
Publication of WO1999047131A2 publication Critical patent/WO1999047131A2/en
Publication of WO1999047131A3 publication Critical patent/WO1999047131A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present invention relates to a combination of an acetylcholinesterase inhibitor and an inverse agonist of the GABAA α5 receptor subtype, and the use of the combination in treating neurodegenerative conditions such as Alzheimer's Disease.
PCT/GB1999/000778 1998-03-16 1999-03-16 Combination of a gaba-a alpha 5 inverse agonist and an acetylcholinesterase inhibitor Ceased WO1999047131A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP99909095A EP1061952A2 (en) 1998-03-16 1999-03-16 Combination of a gaba-a alpha 5 inverse agonist and an acetylcholinesterase inhibitor
JP2000536371A JP2002506815A (en) 1998-03-16 1999-03-16 Combination of GABAAα5 inverse agonist and acetylcholinesterase inhibitor
CA002323618A CA2323618A1 (en) 1998-03-16 1999-03-16 Combination of a gaba-a alpha 5 inverse agonist and an acetylcholinesterase inhibitor
AU28464/99A AU753077B2 (en) 1998-03-16 1999-03-16 Combination of a GABA-A alpha 5 inverse agonist and an acetylcholinesterase inhibitor

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9805561.9 1998-03-16
GBGB9805561.9A GB9805561D0 (en) 1998-03-16 1998-03-16 A combination of therapeutic agents

Publications (2)

Publication Number Publication Date
WO1999047131A2 WO1999047131A2 (en) 1999-09-23
WO1999047131A3 true WO1999047131A3 (en) 1999-11-04

Family

ID=10828631

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB1999/000778 Ceased WO1999047131A2 (en) 1998-03-16 1999-03-16 Combination of a gaba-a alpha 5 inverse agonist and an acetylcholinesterase inhibitor

Country Status (6)

Country Link
EP (1) EP1061952A2 (en)
JP (1) JP2002506815A (en)
AU (1) AU753077B2 (en)
CA (1) CA2323618A1 (en)
GB (1) GB9805561D0 (en)
WO (1) WO1999047131A2 (en)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6627624B1 (en) 1999-04-02 2003-09-30 Neurogen Corporation Aryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
US6271241B1 (en) 1999-04-02 2001-08-07 Neurogen Corporation Cycloalkyl and aryl fused aminoalkyl-imidazole derivatives: modulators and GLP-1 receptors
US6281237B1 (en) 1999-04-02 2001-08-28 Neurogen Corporation N-phenyl benzimidazolecarboxamide and N-phenyl indolecarboxamide derivatives
US6380210B1 (en) 1999-04-02 2002-04-30 Neurogen Corporation Heteroaryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
US6723332B2 (en) 2000-05-26 2004-04-20 Neurogen Corporation Oxomidazopyridine-carboxamides
US6828329B2 (en) 2000-06-26 2004-12-07 Neurogen Corporation Aryl fused substituted 4-oxy-pyridines
US20020151591A1 (en) * 2000-10-17 2002-10-17 Anabella Villalobos Combination use of acetylcholinesterase inhibitors and GABAa inverse agonists for the treatment of cognitive disorders
IL159811A0 (en) 2001-07-13 2004-06-20 Neurogen Corp Heteroaryl substituted fused bicyclic heteroaryl compounds as gabaa receptor ligands
US20060135403A1 (en) * 2002-12-24 2006-06-22 Francine Gervais Therapeutic formulations for the treatment of beta-amyloid related diseases
GB0322140D0 (en) * 2003-09-22 2003-10-22 Pfizer Ltd Combinations
TW200533371A (en) * 2004-04-15 2005-10-16 Dainippon Pharmaceutical Co Medicament comprising a combination of an acetylcholinesterase inhibitor and a 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1h)-one derivative
WO2005112908A1 (en) * 2004-05-14 2005-12-01 The Johns Hopkins University Method for improving cognitive function
JP5379692B2 (en) 2006-11-09 2013-12-25 プロビオドルグ エージー 3-Hydroxy-1,5-dihydro-pyrrol-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcers, cancer and other diseases
DK2091948T3 (en) 2006-11-30 2012-07-23 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
AU2008220785B2 (en) 2007-03-01 2013-02-21 Vivoryon Therapeutics N.V. New use of glutaminyl cyclase inhibitors
US9656991B2 (en) 2007-04-18 2017-05-23 Probiodrug Ag Inhibitors of glutaminyl cyclase
EP2475428B1 (en) 2009-09-11 2015-07-01 Probiodrug AG Heterocylcic derivatives as inhibitors of glutaminyl cyclase
CA2789014C (en) 2010-02-09 2019-01-15 Michela Gallagher Methods and compositions for improving cognitive function
JP6026284B2 (en) 2010-03-03 2016-11-16 プロビオドルグ エージー Inhibitors of glutaminyl cyclase
EA022420B1 (en) 2010-03-10 2015-12-30 Пробиодруг Аг Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
ES2570167T3 (en) 2011-03-16 2016-05-17 Probiodrug Ag Benzimidazole derivatives as glutaminyl cyclase inhibitors
US20140206667A1 (en) 2012-11-14 2014-07-24 Michela Gallagher Methods and compositions for treating schizophrenia
WO2014144663A1 (en) 2013-03-15 2014-09-18 The Johns Hopkins University Methods and compositions for improving cognitive function
CN105142623A (en) 2013-03-15 2015-12-09 艾吉因生物股份有限公司 Methods and compositions for improving cognitive function
JP6899043B2 (en) 2015-05-22 2021-07-07 エージンバイオ, インコーポレイテッド Sustained release pharmaceutical composition of levetiracetam
KR101743960B1 (en) * 2015-07-06 2017-06-08 서울대학교산학협력단 G 19 Pharmaceutical composition for preventing treating or retarding Alzheimers disease or dementia comprising G protein-Coupled Receptor19 agonist as an active ingredient
ES2812698T3 (en) 2017-09-29 2021-03-18 Probiodrug Ag Glutaminyl cyclase inhibitors

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4647580A (en) * 1985-07-18 1987-03-03 Syntex (U.S.A.) Inc. Treatment of Alzheimer's disease
WO1996025948A1 (en) * 1995-02-23 1996-08-29 Merck Sharp & Dohme Limited PREPARATION AND USE OF A SPECIFIC GABA-Aα5 RECEPTOR LIGAND FOR TREATMENT OF ALZHEIMER'S DISEASE
WO1998004560A1 (en) * 1996-07-25 1998-02-05 Merck Sharp & Dohme Limited SUBSTITUTED TRIAZOLO PYRIDAZINE DERIVATIVES AS INVERSE AGONISTS OF THE GABAAα5 RECEPTOR SUBTYPE

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4647580A (en) * 1985-07-18 1987-03-03 Syntex (U.S.A.) Inc. Treatment of Alzheimer's disease
WO1996025948A1 (en) * 1995-02-23 1996-08-29 Merck Sharp & Dohme Limited PREPARATION AND USE OF A SPECIFIC GABA-Aα5 RECEPTOR LIGAND FOR TREATMENT OF ALZHEIMER'S DISEASE
WO1998004560A1 (en) * 1996-07-25 1998-02-05 Merck Sharp & Dohme Limited SUBSTITUTED TRIAZOLO PYRIDAZINE DERIVATIVES AS INVERSE AGONISTS OF THE GABAAα5 RECEPTOR SUBTYPE

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ROSENBERG D R ET AL: "COGNITIVE ENHANCING AGENTS FOR THE TREATMENT OF SENILE DEMENTIA OF THE ALZHEIMER'S TYPE", DRUGS OF TODAY / MEDICAMENTOS DE ACTUALIDAD, vol. 26, no. 7, 1 October 1990 (1990-10-01), pages 449 - 471, XP000616601, ISSN: 0025-7656 *

Also Published As

Publication number Publication date
AU753077B2 (en) 2002-10-10
WO1999047131A2 (en) 1999-09-23
CA2323618A1 (en) 1999-09-23
GB9805561D0 (en) 1998-05-13
AU2846499A (en) 1999-10-11
JP2002506815A (en) 2002-03-05
EP1061952A2 (en) 2000-12-27

Similar Documents

Publication Publication Date Title
WO1999047131A3 (en) Combination of a gaba-a alpha 5 inverse agonist and an acetylcholinesterase inhibitor
AU2001293936A1 (en) Association of the CB1 receptor antagonist and sibutramin, for treating obesity
DE69528823D1 (en) Morpholinwirkstoffvorläufer als tachykininreceptorantagonisten
TR200002773T2 (en) Smilagen and anzurogenin-D and their use for the treatment of Alzheimer's.
GC0000046A (en) Compositions for use in well construction, repair and/or abandonment.
PL323490A1 (en) Tetralinic compounds exibiting acitity against multgiple-drug refractoriness
AU2002366641A1 (en) Methods for inhibiting ocular processes
DE69931975D1 (en) FSH mimetics for the treatment of infertility
AU2002213336A1 (en) Substituted heterocyclic compounds for treating multidrug resistance
MX9804588A (en) Use of halogen bleach-comprising compositions for improved mildness to the skin.
EP1201268A3 (en) Combinations of D4 dopamine receptor antagonists with acetylcholine esterase inhibitors
SG167670A1 (en) Aminocyclohexyl ether compounds and uses thereof
CA2418167A1 (en) Compositions and methods of preventing or reducing the risk or incidence of skeletal injuries in horses
HU9503625D0 (en) Use of p antagonist for producing pharmaceutical compositions for treating acne, rosacea and/or pubic arythema
AU1604001A (en) Use of an aldosterone antagonist for the treatment or prohpylaxis of aldosterone-mediated pathogenic effects
NO992504L (en) Compositions for the treatment of soil, process for its preparation, and use
GB9805559D0 (en) A combination of therapeutic agents
IL152908A0 (en) USE OF (+)-a- (2,3-DIMETHOXYPHENYL)-1-[2-(4-FLUOROPHENYL) ETHYL] -4-PIPERIDINEMETHANOL OR ITS PRODRUG IN THE TREATMENT OF SYMPTOMS OF DEMENTIA AND DOPAMINE INDUCED PSYCHOSIS
PL331882A1 (en) Substituted 1,2,3,4-tetrahydro-2-dibenzofurane amines and 2-amino cyclohepta[b]benzofuranes
AU3896899A (en) Compositions for the treatment of tumors, and uses thereof
GB2340256B (en) Use of alkoxy N-Hydroxyalkyl alkanamide as resist removing agent composition for removing resist method for preparing the same and resist removing method.
CA2369825A1 (en) Microstructured components
WO1999051779A3 (en) Glaucoma therapeutics and diagnostics
IL129622A0 (en) Novel CIS-3,4-chroman derivatives useful in the prevention or treatment of estrogen related diseases or syndromes
IL129624A0 (en) Novel (+)-enantiomers of CIS-3,4-chroman derivatives useful in the prevention or treatment of estrogen related diseases or syndromes

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW SD SL SZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

AK Designated states

Kind code of ref document: A3

Designated state(s): AE AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW SD SL SZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
WWE Wipo information: entry into national phase

Ref document number: 1999909095

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 09622954

Country of ref document: US

WWE Wipo information: entry into national phase

Ref document number: 28464/99

Country of ref document: AU

ENP Entry into the national phase

Ref document number: 2323618

Country of ref document: CA

Ref country code: CA

Ref document number: 2323618

Kind code of ref document: A

Format of ref document f/p: F

NENP Non-entry into the national phase

Ref country code: KR

WWP Wipo information: published in national office

Ref document number: 1999909095

Country of ref document: EP

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWG Wipo information: grant in national office

Ref document number: 28464/99

Country of ref document: AU

WWW Wipo information: withdrawn in national office

Ref document number: 1999909095

Country of ref document: EP