CA2367112A1 - Traitement des maladies neurodegeneratives par des inhibiteurs de l'aspartyl protease - Google Patents

Traitement des maladies neurodegeneratives par des inhibiteurs de l'aspartyl protease Download PDF

Info

Publication number
CA2367112A1
CA2367112A1 CA002367112A CA2367112A CA2367112A1 CA 2367112 A1 CA2367112 A1 CA 2367112A1 CA 002367112 A CA002367112 A CA 002367112A CA 2367112 A CA2367112 A CA 2367112A CA 2367112 A1 CA2367112 A1 CA 2367112A1
Authority
CA
Canada
Prior art keywords
substituted
group
member selected
alkyl
aryl
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.)
Abandoned
Application number
CA002367112A
Other languages
English (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
Individual
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 Individual filed Critical Individual
Publication of CA2367112A1 publication Critical patent/CA2367112A1/fr
Abandoned 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)
  • Psychology (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)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

L'invention concerne (i) des inhibiteurs non peptidiques de l'aspartyl protéase; (ii) des méthodes permettant de moduler la maturation d'une protéine précurseur amyloïde (APP); (iii) des méthodes permettant de moduler la maturation d'une protéine tau (protéine ~); et (iv) des méthodes permettant de traiter les maladies neurodégénératives.
CA002367112A 1999-03-24 2000-03-24 Traitement des maladies neurodegeneratives par des inhibiteurs de l'aspartyl protease Abandoned CA2367112A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12595899P 1999-03-24 1999-03-24
US60/125,958 1999-03-24
PCT/US2000/007804 WO2000056335A1 (fr) 1999-03-24 2000-03-24 Traitement des maladies neurodegeneratives par des inhibiteurs de l'aspartyl protease

Publications (1)

Publication Number Publication Date
CA2367112A1 true CA2367112A1 (fr) 2000-09-28

Family

ID=22422250

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002367112A Abandoned CA2367112A1 (fr) 1999-03-24 2000-03-24 Traitement des maladies neurodegeneratives par des inhibiteurs de l'aspartyl protease

Country Status (5)

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

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4664564B2 (ja) 2000-03-06 2011-04-06 アカディア ファーマシューティカルズ，インコーポレーテッド セロトニン関連疾患の治療に使用する含窒素環式化合物
PE20020276A1 (es) 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
EP1666452A2 (fr) 2000-06-30 2006-06-07 Elan Pharmaceuticals, Inc. Composés pour le traitement de la maladie d'Alzheimer
WO2002014264A2 (fr) 2000-08-11 2002-02-21 The Brigham And Women's Hospital, Inc. (hydroxyethyl)urees utilisees en tant qu'inhibiteurs de la production de beta-amyloide de la maladie d'alhzeimer
MXPA03011046A (es) * 2001-06-01 2004-06-25 Elan Pharm Inc Hidroxialquilaminas.
BR0213139A (pt) * 2001-10-04 2004-08-10 Elan Pharm Inc Composto, método de tratamento ou prevenção de doenças e de preparação de um composto, uso de um composto e composição farmacêutica
BR0214736A (pt) * 2001-12-06 2004-11-23 Elan Pharm Inc Composto e seus sais farmaceuticamente aceitáveis, composição farmacêutica e método de tratar seres humanos ou animais que sofrem de doenças ou condições
EP1461339B1 (fr) 2001-12-28 2010-04-28 Acadia Pharmaceuticals Inc. Composes spiroazacycliques utilises comme modulateurs du recepteur de monoamine
WO2004058686A1 (fr) * 2002-04-30 2004-07-15 Elan Pharmaceuticals, Inc. Amides hydroxypropyle pour le traitement de la maladie d'alzheimer
US7115652B2 (en) 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
AU2003276047A1 (en) 2002-06-17 2003-12-31 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
NZ537522A (en) 2002-06-24 2006-07-28 Acadia Pharm Inc N-substituted piperidine derivatives as serotonin receptor agents
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
SG170617A1 (en) 2003-01-16 2011-05-30 Acadia Pharm Inc Selective serotonin 2a/2c receptor inverse agonists as therapeutics for neurodegenerative diseases
CA2529739A1 (fr) * 2003-06-16 2005-01-20 Sunesis Pharmaceuticals, Inc. Inhibiteurs d'aspartyl-protease
ATE402921T1 (de) 2003-08-08 2008-08-15 Schering Corp Cyclische amine mit einem heterocyclischen substituenten als bace-1-inhibitoren
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
WO2006037043A1 (fr) 2004-09-27 2006-04-06 Acadia Pharmaceuticals Inc. Synthese de n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide, tartrate de ce compose et ses formes cristallines
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
JP2010522198A (ja) 2007-03-19 2010-07-01 アカドイア プハルマセウチカルス インコーポレーテッド ５−ｈｔ２ａインバースアゴニスト及びアンタゴニストの抗精神病薬との併用
JP2011518188A (ja) 2008-04-18 2011-06-23 ユニバーシティ オブ コネチカット リソソーム調節のための化合物および使用方法
US10597363B2 (en) 2015-07-20 2020-03-24 Acadia Pharmaceuticals 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 (fr) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Association de pimavansérine et de modulateurs du cytochrome p450
WO2018118626A1 (fr) 2016-12-20 2018-06-28 Acadia Pharmaceuticals Inc. Pimavansérine seule ou en association pour une utilisation dans le traitement de la psychose liée à la maladie d'alzheimer
WO2018200977A1 (fr) 2017-04-28 2018-11-01 Acadia Pharmaceuticals Inc. Pimavansérine pour le traitement d'un trouble de contrôle des impulsions
US20210077479A1 (en) 2017-08-30 2021-03-18 Acadia Pharmaceuticals Inc. Formulations of pimavanserin
EP3826649A4 (fr) * 2018-07-23 2022-07-20 Enclear Therapies, Inc. Méthodes de traitement de troubles neurologiques
WO2020023418A1 (fr) 2018-07-23 2020-01-30 Enclear Therapies, Inc. Méthodes de traitement de troubles neurologiques
EP3952947A1 (fr) 2019-04-11 2022-02-16 Enclear Therapies, Inc. Procédés d'amélioration du liquide céphalorachidien et dispositifs et systèmes à cet effet

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6150416A (en) * 1997-02-04 2000-11-21 The Regents Of The University Of California Nanomolar, non-peptide inhibitors of cathepsin D

Also Published As

Publication number Publication date
AU3771700A (en) 2000-10-09
WO2000056335A1 (fr) 2000-09-28
EP1178800A1 (fr) 2002-02-13
EP1178800A4 (fr) 2002-07-31
JP2002539260A (ja) 2002-11-19

Similar Documents

Publication Publication Date Title
CA2367112A1 (fr) Traitement des maladies neurodegeneratives par des inhibiteurs de l'aspartyl protease
US6150416A (en) Nanomolar, non-peptide inhibitors of cathepsin D
JP7419486B2 (ja) τリン酸化を阻害する方法
Kreft et al. Recent advances in the identification of γ-secretase inhibitors to clinically test the Aβ oligomer hypothesis of Alzheimer’s disease
Wolfe γ‐Secretase inhibitors and modulators for Alzheimer’s disease
CN102123763B (zh) 富马酸氢甲酯的前体药物、其药物组合物、及其使用方法
Costanzo et al. Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone
Andersson et al. Disulfide cyclized tripeptide analogues of angiotensin IV as potent and selective inhibitors of insulin-regulated aminopeptidase (IRAP)
Schiefer et al. Design, synthesis, and optimization of novel epoxide incorporating peptidomimetics as selective calpain inhibitors
AU2002239727C1 (en) Inhibitors of memapsin 2 and use thereof
WO2009137597A1 (fr) Composés inhibant la production de sappβ et d’aβ et leurs utilisations
Hoang et al. Discovery of conformationally restricted human glutaminyl cyclase inhibitors as potent anti-Alzheimer’s agents by structure-based design
MXPA02002578A (es) Compuestos de union a ciclofilina no peptidicos, y su uso.
US20040157896A1 (en) Methods for treating neurodegenerative disorders using aspartyl protease inhibitors
WO2011076854A1 (fr) Clivage de protéine précurseur de β-amyloïde
AU2005201481A1 (en) Methods for treating neurodegenerative disorders using aspartyl protease inhibitors
JP2011518188A (ja) リソソーム調節のための化合物および使用方法
US20080167387A1 (en) Microglia Facilitated Amyloidogenesis Assay
Al-Nadaf et al. Haloperidol inhibits Memapsin 2: Innovation by docking simulation and in vitro assay
AU2006202400A1 (en) Nanomolar, non-peptide inhibitors of cathepsin D
Greig et al. Dissociation between the potent β-amyloid protein pathway inhibition and cholinergic actions of the Alzheimer drug candidates phenserine and cymserine
KR20090034009A (ko) 글라이신 모액을 포함하는 신규한 베타-세크리타제 저해용화합물
WO2004041211A2 (fr) Inhibiteurs de la $g(b)-secretase et leur utilisation pour la prevention ou le traitement de la maladie d'alzheimer ou d'une deficience intellectuelle legere

Legal Events

Date Code Title Description
EEER Examination request
FZDE Dead