DE602004011255D1 - Phosphinsäurederivate, inhibitoren von beta-sekretase zur behandlung von alzheimer-krankheit - Google Patents

Phosphinsäurederivate, inhibitoren von beta-sekretase zur behandlung von alzheimer-krankheit

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Publication number
DE602004011255D1
DE602004011255D1 DE602004011255T DE602004011255T DE602004011255D1 DE 602004011255 D1 DE602004011255 D1 DE 602004011255D1 DE 602004011255 T DE602004011255 T DE 602004011255T DE 602004011255 T DE602004011255 T DE 602004011255T DE 602004011255 D1 DE602004011255 D1 DE 602004011255D1
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DE
Germany
Prior art keywords
sup
treatment
beta
acid derivatives
phosphinic acid
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Application number
DE602004011255T
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English (en)
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DE602004011255T2 (de
Inventor
Hans Hilpert
Roland Humm
Dietmar Knopp
Peter Weiss
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Publication of DE602004011255D1 publication Critical patent/DE602004011255D1/de
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Publication of DE602004011255T2 publication Critical patent/DE602004011255T2/de
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/30Phosphinic acids R2P(=O)(OH); Thiophosphinic acids, i.e. R2P(=X)(XH) (X = S, Se)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/30Phosphinic acids R2P(=O)(OH); Thiophosphinic acids, i.e. R2P(=X)(XH) (X = S, Se)
    • C07F9/301Acyclic saturated acids which can have further substituents on alkyl
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • C07F9/5728Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/60Quinoline or hydrogenated quinoline ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6527Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07F9/653Five-membered rings
DE602004011255T 2003-11-11 2004-11-02 Phosphinsäurederivate, inhibitoren von beta-sekretase zur behandlung von alzheimer-krankheit Active DE602004011255T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP03025852 2003-11-11
EP03025852 2003-11-11
PCT/EP2004/012371 WO2005044830A1 (en) 2003-11-11 2004-11-02 Phosphinic acids derivatives, beta-secretase inhibitors for the treatment of alzheimer’s disease

Publications (2)

Publication Number Publication Date
DE602004011255D1 true DE602004011255D1 (de) 2008-02-21
DE602004011255T2 DE602004011255T2 (de) 2009-01-08

Family

ID=34560161

Family Applications (1)

Application Number Title Priority Date Filing Date
DE602004011255T Active DE602004011255T2 (de) 2003-11-11 2004-11-02 Phosphinsäurederivate, inhibitoren von beta-sekretase zur behandlung von alzheimer-krankheit

Country Status (14)

Country Link
US (1) US7345082B2 (de)
EP (1) EP1685142B1 (de)
JP (1) JP4451449B2 (de)
KR (1) KR100782618B1 (de)
CN (1) CN100497355C (de)
AT (1) ATE383160T1 (de)
AU (1) AU2004287586A1 (de)
BR (1) BRPI0416450A (de)
CA (1) CA2544203A1 (de)
DE (1) DE602004011255T2 (de)
ES (1) ES2298837T3 (de)
PL (1) PL1685142T3 (de)
RU (1) RU2367666C2 (de)
WO (1) WO2005044830A1 (de)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
JP5379692B2 (ja) 2006-11-09 2013-12-25 プロビオドルグ エージー 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての3−ヒドロキシ−1,5−ジヒドロ−ピロール−2−オン誘導体
US9126987B2 (en) 2006-11-30 2015-09-08 Probiodrug Ag Inhibitors of glutaminyl cyclase
CN101668525A (zh) 2007-03-01 2010-03-10 前体生物药物股份公司 谷氨酰胺酰环化酶抑制剂的新用途
FR2913886B1 (fr) 2007-03-22 2012-03-02 Guerbet Sa Utilisation de nanoparticules metalliques dans le diagnostique de la maladie d'alzheimer
DK2142514T3 (da) 2007-04-18 2015-03-23 Probiodrug Ag Thioureaderivater som glutaminylcyclase-inhibitorer
CN102177164B (zh) 2008-11-05 2015-02-11 科莱恩金融(Bvi)有限公司 利用烯丙醇/丙烯醛制备二烷基次膦酸、二烷基次膦酸酯和二烷基次膦酸盐的方法,以及它们的用途
DE102008056341A1 (de) 2008-11-07 2010-05-12 Clariant International Limited Verfahren zur Herstellung von monoaminofunktionalisierten Dialkylphosphinsäuren, -estern und -salzen mittels Acrylnitrilen und ihre Verwendung
DE102008056339A1 (de) * 2008-11-07 2010-05-12 Clariant International Limited Verfahren zur Herstellung von mono-aminofunktionalisierten Dialkylphosphinsäuren, -estern und -salzen und ihre Verwendung
DE102008060035A1 (de) 2008-12-02 2010-06-10 Clariant International Limited Verfahren zur Herstellung von mono-hydroxyfunktionalisierten Dialkylphosphinsäuren, -estern und -salzen mittels Vinylester einer Carbonsäure und ihre Verwendung
DE102008060535A1 (de) 2008-12-04 2010-06-10 Clariant International Limited Verfahren zur Herstellung von mono-carboxyfunktionalisierten Dialkylphosphinsäuren, -estern und -salzen mittels Vinylether und ihre Verwendung
DE102008063668A1 (de) 2008-12-18 2010-07-01 Clariant International Limited Verfahren zur Herstellung von Alkylphosponsäuren, -estern und -salzen mittels Oxidation von Alkylphosphonigsäuren und ihre Verwendung
DE102008063627A1 (de) 2008-12-18 2010-06-24 Clariant International Limited Verfahren zur Herstellung von monohydroxyfunktionalisierten Dialkylphosphinsäuren,-estern und -salzen mittels Ethylenoxid und ihre Verwendung
ES2446666T3 (es) 2008-12-18 2014-03-10 Clariant Finance (Bvi) Limited Procedimiento para la preparación de ácidos etilen-dialquil-fosfínicos, o de sus ésteres y sales, mediante acetileno, y su utilización
DE102008063642A1 (de) 2008-12-18 2010-06-24 Clariant International Limited Verfahren zur Herstellung von monocarboxyfunktionalisierten Dialkylphosphinsäuren, -estern und -salzen mittels Alkylenoxiden und ihre Verwendung
DE102008064003A1 (de) 2008-12-19 2010-06-24 Clariant International Limited Verfahren zur Herstellung von mono-funktionalisierten Dialkylphosphinsäuren, -estern und -salzen und ihre Verwendung
JP5934645B2 (ja) 2009-09-11 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
CN102791704B (zh) 2010-03-10 2015-11-25 前体生物药物股份公司 谷氨酰胺酰环化酶(qc, ec 2.3.2.5)的杂环抑制剂
EP2560953B1 (de) 2010-04-21 2016-01-06 Probiodrug AG Hemmer der glutaminylzyklase
JP6050264B2 (ja) 2011-03-16 2016-12-21 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
DK3461819T3 (da) 2017-09-29 2020-08-10 Probiodrug Ag Inhibitorer af glutaminylcyklase
NO345530B1 (en) * 2020-03-20 2021-03-29 Axichem As Synthesis of capsaicin derivatives

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2788525B1 (fr) 1999-01-19 2002-11-29 Commissariat Energie Atomique Pseudo-peptides phosphiniques, utilisables comme inhibiteurs des metalloproteases a zinc matricielles
US7176242B2 (en) * 2001-11-08 2007-02-13 Elan Pharmaceuticals, Inc. N,N′-substituted-1,3-diamino-2-hydroxypropane derivatives
AR037460A1 (es) * 2001-11-30 2004-11-10 Smithkline Beecham Plc Compuesto de hidroxietileno, composicion farmaceutica que lo comprende, uso del mismo para la fabricacion de un medicamento y procedimiento para su preparacion
CN101090883A (zh) * 2002-02-27 2007-12-19 艾伦药物公司 取代羟基乙胺

Also Published As

Publication number Publication date
KR20060083230A (ko) 2006-07-20
RU2006120078A (ru) 2008-01-20
ES2298837T3 (es) 2008-05-16
US7345082B2 (en) 2008-03-18
BRPI0416450A (pt) 2007-03-06
ATE383160T1 (de) 2008-01-15
JP2007510684A (ja) 2007-04-26
EP1685142A1 (de) 2006-08-02
CN100497355C (zh) 2009-06-10
WO2005044830A1 (en) 2005-05-19
CN1878781A (zh) 2006-12-13
DE602004011255T2 (de) 2009-01-08
PL1685142T3 (pl) 2008-06-30
JP4451449B2 (ja) 2010-04-14
EP1685142B1 (de) 2008-01-09
AU2004287586A1 (en) 2005-05-19
RU2367666C2 (ru) 2009-09-20
CA2544203A1 (en) 2005-05-19
KR100782618B1 (ko) 2007-12-06
US20050107341A1 (en) 2005-05-19

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