EP1178800A4 - Methods for treating neurodegenerative disorders using aspartyl protease inhibitors - Google Patents

Methods for treating neurodegenerative disorders using aspartyl protease inhibitors

Info

Publication number
EP1178800A4
EP1178800A4 EP00916643A EP00916643A EP1178800A4 EP 1178800 A4 EP1178800 A4 EP 1178800A4 EP 00916643 A EP00916643 A EP 00916643A EP 00916643 A EP00916643 A EP 00916643A EP 1178800 A4 EP1178800 A4 EP 1178800A4
Authority
EP
European Patent Office
Prior art keywords
methods
protease inhibitors
neurodegenerative disorders
aspartyl protease
treating neurodegenerative
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.)
Withdrawn
Application number
EP00916643A
Other languages
German (de)
French (fr)
Other versions
EP1178800A1 (en
Inventor
Jonathan A Ellman
Gary Lynch
Irwin D Kuntz
Xiaoning Bi
Christina E Lee
A Geoffrey Skillman
Tasir Haque
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.)
University of California
Original Assignee
University of California
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 University of California filed Critical University of California
Publication of EP1178800A1 publication Critical patent/EP1178800A1/en
Publication of EP1178800A4 publication Critical patent/EP1178800A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4465—Non condensed piperidines, e.g. piperocaine only substituted in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
EP00916643A 1999-03-24 2000-03-24 Methods for treating neurodegenerative disorders using aspartyl protease inhibitors Withdrawn EP1178800A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12595899P 1999-03-24 1999-03-24
US125958P 1999-03-24
PCT/US2000/007804 WO2000056335A1 (en) 1999-03-24 2000-03-24 Methods for treating neurodegenerative disorders using aspartyl protease inhibitors

Publications (2)

Publication Number Publication Date
EP1178800A1 EP1178800A1 (en) 2002-02-13
EP1178800A4 true EP1178800A4 (en) 2002-07-31

Family

ID=22422250

Family Applications (1)

Application Number Title Priority Date Filing Date
EP00916643A Withdrawn EP1178800A4 (en) 1999-03-24 2000-03-24 Methods for treating neurodegenerative disorders using aspartyl protease inhibitors

Country Status (5)

Country Link
EP (1) EP1178800A4 (en)
JP (1) JP2002539260A (en)
AU (1) AU3771700A (en)
CA (1) CA2367112A1 (en)
WO (1) WO2000056335A1 (en)

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KR20080059687A (en) 2000-03-06 2008-06-30 아카디아 파마슈티칼스 인코포레이티드 Azacyclic compounds for use in the treatment of serotonin related diseases
EP1666452A2 (en) 2000-06-30 2006-06-07 Elan Pharmaceuticals, Inc. Compounds to treat Alzheimer's disease
PE20020276A1 (en) 2000-06-30 2002-04-06 Elan Pharm Inc SUBSTITUTE AMINE COMPOUNDS AS ß-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER
WO2002014264A2 (en) 2000-08-11 2002-02-21 The Brigham And Women's Hospital, Inc. (hydroxyethyl)ureas as inhibitors of alzheimer's beta-amyloid production
AU2002314914A1 (en) * 2001-06-01 2002-12-16 Elan Pharmaceuticals, Inc. Hydroxy alkyl amine derivatives as beta-secretase inhibitors and their use for the treatment of alzheimer's disease and similar diseases
BR0213139A (en) 2001-10-04 2004-08-10 Elan Pharm Inc Compound, method of treating or preventing disease and preparing a compound, use of a compound and pharmaceutical composition
BR0214736A (en) * 2001-12-06 2004-11-23 Elan Pharm Inc Compound and its pharmaceutically acceptable salts, pharmaceutical composition and method of treating humans or animals suffering from diseases or conditions
WO2003057698A2 (en) 2001-12-28 2003-07-17 Acadia Pharmaceuticals, Inc. Spiroazacyclic compounds as monoamine receptor modulators
AU2003303141A1 (en) 2002-04-30 2004-07-22 Elan Pharmaceuticals, Inc. Hydroxypropyl amides for the treatment of alzheimer's disease
US7115652B2 (en) 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
US7132568B2 (en) 2002-06-17 2006-11-07 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
US7538222B2 (en) 2002-06-24 2009-05-26 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
US7253186B2 (en) 2002-06-24 2007-08-07 Carl-Magnus Andersson N-substituted piperidine derivatives as serotonin receptor agents
NZ537522A (en) 2002-06-24 2006-07-28 Acadia Pharm Inc N-substituted piperidine derivatives as serotonin receptor agents
MXPA05007568A (en) 2003-01-16 2005-09-21 Acadia Pharm Inc Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases.
AU2003297826A1 (en) * 2003-06-16 2005-01-28 Sunesis Pharmaceuticals, Inc Aspartyl protease inhibitors
TW200524910A (en) * 2003-08-08 2005-08-01 Schering Corp Cyclic amine BACE-1 inhibitors having a heterocyclic substituent
US7820695B2 (en) 2004-05-21 2010-10-26 Acadia Pharmaceuticals, Inc. Selective serotonin receptor inverse agonists as therapeutics for disease
US20050261278A1 (en) 2004-05-21 2005-11-24 Weiner David M Selective serotonin receptor inverse agonists as therapeutics for disease
US7790899B2 (en) 2004-09-27 2010-09-07 Acadia Pharmaceuticals, Inc. Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms
PL2289879T3 (en) 2004-09-27 2015-05-29 Acadia Pharm Inc Synthesis of a crystalline form of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide tartrate salt
WO2008116024A2 (en) 2007-03-19 2008-09-25 Acadia Pharmaceuticals Inc. Combinations of 5-ht2a inverse agonists and antagonists with antipsychotics
JP2011518188A (en) 2008-04-18 2011-06-23 ユニバーシティ オブ コネチカット Compounds for lysosome regulation and methods of use
PT3325444T (en) 2015-07-20 2021-09-22 Acadia Pharm Inc Methods for preparing n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form c
US10953000B2 (en) 2016-03-25 2021-03-23 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome P450 modulators
WO2017165635A1 (en) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome p450 modulators
WO2018118626A1 (en) 2016-12-20 2018-06-28 Acadia Pharmaceuticals Inc. Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis
EP3615028A1 (en) 2017-04-28 2020-03-04 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
WO2019046167A1 (en) 2017-08-30 2019-03-07 Acadia Pharmaceuticals Inc. Formulations of pimavanserin
CA3107352A1 (en) 2018-07-23 2020-01-30 Enclear Therapies, Inc. Methods of treating neurological disorders
WO2020023417A1 (en) * 2018-07-23 2020-01-30 Enclear Therapies, Inc. Methods of treating neurological disorders
JP2022526671A (en) 2019-04-11 2022-05-25 エンクリアー セラピーズ， インク． Methods for improving cerebrospinal fluid and devices and systems for that purpose

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998033795A1 (en) * 1997-02-04 1998-08-06 The Regents Of The University Of California Nanomolar, non-peptide inhibitors of cathepsin d

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998033795A1 (en) * 1997-02-04 1998-08-06 The Regents Of The University Of California Nanomolar, non-peptide inhibitors of cathepsin d

Non-Patent Citations (10)

* Cited by examiner, † Cited by third party
Title
CATALDO A M ET AL: "ENZYMATICALLY ACTIVE LYSOSOMAL PROTEASES ARE ASSOCIATED WITH AMYLOID DEPOSITS IN ALZHEIMER BRAIN", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF USA, NATIONAL ACADEMY OF SCIENCE. WASHINGTON, US, vol. 87, no. 10, 1 May 1990 (1990-05-01), pages 3861 - 3865, XP000602294, ISSN: 0027-8424 *
CATALDO A M ET AL: "LYSOSOMAL HYDROLASES OF DIFFERENT CLASSES ARE ABNORMALLY DISTRIBUTED IN BRAINS OF PATIENTS WITH ALZHEIMER DISEASE", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF USA, NATIONAL ACADEMY OF SCIENCE. WASHINGTON, US, vol. 88, December 1991 (1991-12-01), pages 10998 - 11002, XP002929850, ISSN: 0027-8424 *
CATALDO A M ET AL: "LYSOSOMAL PROTEINASE ANTIGENS ARE PROMINENTLY LOCALIZED WITHIN SENILE PLAQUES OF ALZHEIMER'S DISEASE EVIDENCE FOR A NEURONAL ORIGIN", BRAIN RESEARCH, vol. 513, no. 2, 1990, pages 181 - 192, XP001070394, ISSN: 0006-8993 *
CATALDO ANNE M ET AL: "Colocalization of lysosomal hydrolase and beta-amyloid in diffuse plaques of the cerebellum and striatum in Alzheimer's disease and Down's syndrome.", JOURNAL OF NEUROPATHOLOGY & EXPERIMENTAL NEUROLOGY, vol. 55, no. 6, 1996, pages 704 - 715, XP001070366, ISSN: 0022-3069 *
HAQUE, TASIR S. ET AL: "Potent, Low-Molecular-Weight Non-Peptide Inhibitors of Malarial Aspartyl Protease Plasmepsin II", J. MED. CHEM. (1999), 42(8), 1428-1440, XP000926504 *
KENESSEY AGNES ET AL: "Degradation of tau by lysosomal enzyme cathepsin D: Implication for Alzheimer neurofibrillary degeneration.", JOURNAL OF NEUROCHEMISTRY, vol. 69, no. 5, 1997, pages 2026 - 2038, XP001069801, ISSN: 0022-3042 *
KREUTZBERG G W: "Microglia, the first line of defence in brain pathologies.", ARZNEIMITTEL-FORSCHUNG, vol. 45, no. 3A, 1995, pages 357 - 360, XP001068957, ISSN: 0004-4172 *
LEE, CHRISTINA E. ET AL: "General solid-phase synthesis approach to prepare mechanism-based aspartyl protease inhibitor libraries. Identification of potent cathepsin D inhibitors", J. AM. CHEM. SOC. (1998), 120(38), 9735-9747, XP002197748 *
LI K ET AL: "ABNORMAL DISTRIBUTION OF CATHEPSIN PROTEINASES AND ENDOGENOUS INHIBITORS (CYSTATINS) IN THE HIPPOCAMPUS OF PATIENTS WITH ALZHEIMER'S DISEASE, PARKINSONISM-DEMENTIA COMPLEX ON GUAM, AND SENILE DEMENTIA AND IN THE AGED", VIRCHOWS ARCHIV A. PATHOLOGICAL ANATOMY AND HISTOPATHOLOGY, SPRINGER VERLAG, BERLIN, DE, vol. 423, no. 3, 1 September 1993 (1993-09-01), pages 185 - 194, XP002062087, ISSN: 0174-7398 *
See also references of WO0056335A1 *

Also Published As

Publication number Publication date
EP1178800A1 (en) 2002-02-13
JP2002539260A (en) 2002-11-19
AU3771700A (en) 2000-10-09
WO2000056335A1 (en) 2000-09-28
CA2367112A1 (en) 2000-09-28

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