BRPI0416450A - derivados de ácido fosfìnico, inibidores de beta - secretase para o tratamento de mal de alzheimer - Google Patents
derivados de ácido fosfìnico, inibidores de beta - secretase para o tratamento de mal de alzheimerInfo
- Publication number
- BRPI0416450A BRPI0416450A BRPI0416450-4A BRPI0416450A BRPI0416450A BR PI0416450 A BRPI0416450 A BR PI0416450A BR PI0416450 A BRPI0416450 A BR PI0416450A BR PI0416450 A BRPI0416450 A BR PI0416450A
- Authority
- BR
- Brazil
- Prior art keywords
- treatment
- alzheimer
- acid derivatives
- disease
- alkyl
- Prior art date
Links
- 208000024827 Alzheimer disease Diseases 0.000 title abstract 2
- 239000002439 beta secretase inhibitor Substances 0.000 title abstract 2
- 229940042400 direct acting antivirals phosphonic acid derivative Drugs 0.000 title 1
- 150000003007 phosphonic acid derivatives Chemical class 0.000 title 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- ACVYVLVWPXVTIT-UHFFFAOYSA-N phosphinic acid Chemical class O[PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-N 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 1
- -1 C1-6- Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
- C07F9/301—Acyclic saturated acids which can have further substituents on alkyl
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/572—Five-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/572—Five-membered rings
- C07F9/5728—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/58—Pyridine rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/60—Quinoline or hydrogenated quinoline ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
- C07F9/653—Five-membered rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
"DERIVADOS DE áCIDO FOSFìNICO, INIBIDORES DE BETA - SECRETASE PARA O TRATAMENTO DE MAL DE ALZHEIMER". A presente invenção refere-se a derivados de ácido fosfínico de fórmula (I) onde R¬ 1¬ é arila ou heteroarila, R¬ 2¬ é C~ 1-5~ alquila ou fenila, R¬ 3¬ é hidrogênio, C~ 1-5~ alquila, O-C~ 1-5~ alquila ou fenila, R¬ 4¬ é C~ 1-6~ alquila, C~ 3-6~, cicloalquila, fenila, piridila ou indolila, e seus sais farmaceuticamente aceitáveis. Os compostos podem ser usados no tratamento ou prevenção de uma doença relacionada à inibição de beta - secretase, inter alia para o tratamento de mal de Alzheimer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
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 (1)
Publication Number | Publication Date |
---|---|
BRPI0416450A true BRPI0416450A (pt) | 2007-03-06 |
Family
ID=34560161
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI0416450-4A BRPI0416450A (pt) | 2003-11-11 | 2004-11-02 | derivados de ácido fosfìnico, inibidores de beta - secretase para o tratamento de mal de alzheimer |
Country Status (14)
Country | Link |
---|---|
US (1) | US7345082B2 (pt) |
EP (1) | EP1685142B1 (pt) |
JP (1) | JP4451449B2 (pt) |
KR (1) | KR100782618B1 (pt) |
CN (1) | CN100497355C (pt) |
AT (1) | ATE383160T1 (pt) |
AU (1) | AU2004287586A1 (pt) |
BR (1) | BRPI0416450A (pt) |
CA (1) | CA2544203A1 (pt) |
DE (1) | DE602004011255T2 (pt) |
ES (1) | ES2298837T3 (pt) |
PL (1) | PL1685142T3 (pt) |
RU (1) | RU2367666C2 (pt) |
WO (1) | WO2005044830A1 (pt) |
Families Citing this family (22)
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 |
WO2008055945A1 (en) | 2006-11-09 | 2008-05-15 | Probiodrug Ag | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
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 |
EP2142514B1 (en) | 2007-04-18 | 2014-12-24 | Probiodrug AG | Thiourea derivatives as glutaminyl cyclase inhibitors |
WO2010051883A1 (de) | 2008-11-05 | 2010-05-14 | Clariant International Ltd | Verfahren zur herstellung von dialkylphosphinsäuren, -estern und -salzen mittels allylalkoholen/acroleinen und ihre verwendung |
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 |
US9181487B2 (en) | 2008-12-18 | 2015-11-10 | Clariant Finance (Bvi) Limited | Process for preparing ethylenedialkylphosphinic acids, esters and salts by means of acetylene and use thereof |
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 |
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 |
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 |
DE102008064003A1 (de) | 2008-12-19 | 2010-06-24 | Clariant International Limited | Verfahren zur Herstellung von mono-funktionalisierten Dialkylphosphinsäuren, -estern und -salzen und ihre Verwendung |
SG178953A1 (en) | 2009-09-11 | 2012-04-27 | Probiodrug Ag | Heterocylcic derivatives as inhibitors of glutaminyl cyclase |
ES2586231T3 (es) | 2010-03-03 | 2016-10-13 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
DK2545047T3 (da) | 2010-03-10 | 2014-07-28 | Probiodrug Ag | Heterocycliske inhibitorer af glutaminylcyclase (QC, EC 2.3.2.5) |
WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel inhibitors |
ES2570167T3 (es) | 2011-03-16 | 2016-05-17 | Probiodrug Ag | Derivados de benzimidazol como inhibidores de glutaminil ciclasa |
PL3461819T3 (pl) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitory cyklazy glutaminylowej |
Family Cites Families (4)
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 |
MXPA04004428A (es) * | 2001-11-08 | 2004-09-10 | Elan Pharm Inc | Derivados de 2,3-diamino-2-hidroxipropano n,n`-sustituidos. |
TW200304374A (en) * | 2001-11-30 | 2003-10-01 | Smithkline Beecham Plc | Novel compounds |
US7498436B2 (en) * | 2002-02-27 | 2009-03-03 | Pharmacia & Upjohn Company Llc | Substituted hydroxyethylamines |
-
2004
- 2004-11-02 WO PCT/EP2004/012371 patent/WO2005044830A1/en active IP Right Grant
- 2004-11-02 AT AT04797517T patent/ATE383160T1/de not_active IP Right Cessation
- 2004-11-02 EP EP04797517A patent/EP1685142B1/en not_active Not-in-force
- 2004-11-02 KR KR1020067009049A patent/KR100782618B1/ko not_active IP Right Cessation
- 2004-11-02 JP JP2006538727A patent/JP4451449B2/ja not_active Expired - Fee Related
- 2004-11-02 CN CNB2004800332302A patent/CN100497355C/zh not_active Expired - Fee Related
- 2004-11-02 DE DE602004011255T patent/DE602004011255T2/de active Active
- 2004-11-02 ES ES04797517T patent/ES2298837T3/es active Active
- 2004-11-02 AU AU2004287586A patent/AU2004287586A1/en not_active Abandoned
- 2004-11-02 CA CA002544203A patent/CA2544203A1/en not_active Abandoned
- 2004-11-02 RU RU2006120078/04A patent/RU2367666C2/ru not_active IP Right Cessation
- 2004-11-02 BR BRPI0416450-4A patent/BRPI0416450A/pt not_active IP Right Cessation
- 2004-11-02 PL PL04797517T patent/PL1685142T3/pl unknown
- 2004-11-08 US US10/983,363 patent/US7345082B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
CN1878781A (zh) | 2006-12-13 |
CN100497355C (zh) | 2009-06-10 |
PL1685142T3 (pl) | 2008-06-30 |
KR20060083230A (ko) | 2006-07-20 |
CA2544203A1 (en) | 2005-05-19 |
US20050107341A1 (en) | 2005-05-19 |
JP4451449B2 (ja) | 2010-04-14 |
ATE383160T1 (de) | 2008-01-15 |
JP2007510684A (ja) | 2007-04-26 |
RU2006120078A (ru) | 2008-01-20 |
KR100782618B1 (ko) | 2007-12-06 |
EP1685142A1 (en) | 2006-08-02 |
RU2367666C2 (ru) | 2009-09-20 |
EP1685142B1 (en) | 2008-01-09 |
WO2005044830A1 (en) | 2005-05-19 |
ES2298837T3 (es) | 2008-05-16 |
DE602004011255T2 (de) | 2009-01-08 |
DE602004011255D1 (de) | 2008-02-21 |
AU2004287586A1 (en) | 2005-05-19 |
US7345082B2 (en) | 2008-03-18 |
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Legal Events
Date | Code | Title | Description |
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B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 7A ANUIDADE. |
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B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2158 DE 15/05/2012. |