PE20090617A1 - Compuestos amino-5-[-4-(difluorometoxi)fenil]-5-fenilimidazolona para la inhibicion de -secretasa - Google Patents
Compuestos amino-5-[-4-(difluorometoxi)fenil]-5-fenilimidazolona para la inhibicion de -secretasaInfo
- Publication number
- PE20090617A1 PE20090617A1 PE2008000502A PE2008000502A PE20090617A1 PE 20090617 A1 PE20090617 A1 PE 20090617A1 PE 2008000502 A PE2008000502 A PE 2008000502A PE 2008000502 A PE2008000502 A PE 2008000502A PE 20090617 A1 PE20090617 A1 PE 20090617A1
- Authority
- PE
- Peru
- Prior art keywords
- phenyl
- amino
- difluorometoxi
- secretase
- difluorometoxy
- Prior art date
Links
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 title abstract 4
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 230000005764 inhibitory process Effects 0.000 title 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 2
- -1 1-FLUORO-PENT-4-ENYL Chemical class 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 206010044688 Trisomy 21 Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/70—One oxygen 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
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
REFERIDO A DERIVADOS DE AMINO-5-[4-(DIFLUOROMETOXI)FENIL]-5-FENILIMIDAZOLONA DE FORMULA (I) DONDE R1 Y R2 SON CADA UNO H, ALQUILO, CICLOALQUILO, ARILO, ENTRE OTROS, O R1 Y R2 SE UNEN JUNTO AL ATOMO DE N PARA FORMAR UN ANILLO DE 5 A 7 MIEMBROS; R3 ES H, ALQUILO, CICLOALQUILO, CICLOHETEROALQUILO, ENTRE OTROS; R4, R5 Y R6 SON CADA UNO H, HALOGENO, NO2, CN, ALQUILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-AMINO-5-[3-(CICLOPROPILO-ETINIL)-4-FLUOROFENIL]-5-[4-(DIFLUOROMETOXI)FENIL]-3-METIL-3,5-DIHIDRO-4H-IMIDAZOL-4-ONA, (5R)-2-AMINO-5-[4-(DIFLUOROMETOXI)FENIL]-5-(4-FLUORO-3-PROP-1-IN-1-ILFENIL)-3-METIL-3,5-DIHIDRO-4H-IMIDAZOL-4-ONA, 2-AMINO-5-[4-DIFLUOROMETOXI-FENIL]-5-[3-(1-FLUORO-PENT-4-ENIL)-FENIL]-3-METIL-3,5-DIHIDRO-IMIDAZOL-4-ONA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA BETA-SECRETASA (BASE) SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER, SINDROME DE DOWN
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US89670707P | 2007-03-23 | 2007-03-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090617A1 true PE20090617A1 (es) | 2009-05-08 |
Family
ID=39734897
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008000502A PE20090617A1 (es) | 2007-03-23 | 2008-03-19 | Compuestos amino-5-[-4-(difluorometoxi)fenil]-5-fenilimidazolona para la inhibicion de -secretasa |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US7723368B2 (es) |
| EP (1) | EP2144884A2 (es) |
| JP (1) | JP2010522237A (es) |
| CN (1) | CN101663281A (es) |
| AR (1) | AR065814A1 (es) |
| AU (1) | AU2008232341A1 (es) |
| BR (1) | BRPI0809162A2 (es) |
| CA (1) | CA2681431A1 (es) |
| CL (1) | CL2008000791A1 (es) |
| MX (1) | MX2009010057A (es) |
| PE (1) | PE20090617A1 (es) |
| TW (1) | TW200901978A (es) |
| WO (1) | WO2008118379A2 (es) |
Families Citing this family (26)
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| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| EP1896478B1 (en) | 2005-06-14 | 2014-05-21 | Merck Sharp & Dohme Corp. | Aspartyl protease inhibitors |
| AR065814A1 (es) * | 2007-03-23 | 2009-07-01 | Wyeth Corp | Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados. |
| US8450308B2 (en) | 2008-08-19 | 2013-05-28 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| BRPI0918449A2 (pt) | 2008-09-11 | 2019-09-24 | Amgen Inc | compostos de anel espiro-tricíclico como moduladores de beta-secretas e métodos de uso |
| ES2571057T3 (es) | 2009-03-13 | 2016-05-23 | Vitae Pharmaceuticals Inc | Inhibidores de beta-secretasa |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| JP5828848B2 (ja) | 2010-02-24 | 2015-12-09 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | ベータセクレターゼインヒビター |
| WO2011115928A1 (en) | 2010-03-15 | 2011-09-22 | Amgen Inc. | Amino -dihydrooxazine and amino - dihydrothiazine spiro compounds as beta - secretase modulators and their medical use |
| CA2791281A1 (en) | 2010-03-15 | 2011-09-22 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators |
| WO2012019056A1 (en) | 2010-08-05 | 2012-02-09 | Amgen Inc. | Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use |
| US8957083B2 (en) | 2010-11-23 | 2015-02-17 | Amgen Inc. | Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use |
| US9346827B2 (en) | 2011-02-07 | 2016-05-24 | Amgen Inc. | 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use |
| EP2675810A1 (en) | 2011-02-15 | 2013-12-25 | Amgen Inc. | Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use |
| US9221839B2 (en) | 2011-04-07 | 2015-12-29 | Merck Sharp & Dohme Corp. | C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use |
| WO2012138590A1 (en) | 2011-04-07 | 2012-10-11 | Merck Sharp & Dohme Corp. | Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| US9309212B2 (en) | 2011-05-24 | 2016-04-12 | The Wistar Institute | Compositions and methods for modulating the activity of Epstein-Barr nuclear antigen 1 |
| RU2014111055A (ru) | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
| WO2013044092A1 (en) | 2011-09-21 | 2013-03-28 | Amgen Inc. | Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| TWI557112B (zh) | 2012-03-05 | 2016-11-11 | 百靈佳殷格翰國際股份有限公司 | β－分泌酶抑制劑 |
| TW201422592A (zh) | 2012-08-27 | 2014-06-16 | Boehringer Ingelheim Int | β－分泌酶抑制劑 |
| JP2015532282A (ja) | 2012-09-28 | 2015-11-09 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | β−セクレターゼの阻害剤 |
| US9725469B2 (en) | 2012-11-15 | 2017-08-08 | Amgen, Inc. | Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use |
| CN103965048B (zh) * | 2014-05-06 | 2016-02-17 | 西北农林科技大学 | 反式肉桂酸酯类化合物及其合成方法和应用 |
| CN108349905A (zh) * | 2015-08-27 | 2018-07-31 | 南顿欧洲有限责任公司 | 用于app选择性bace抑制的组合物及其用途 |
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| US4140493A (en) * | 1976-11-19 | 1979-02-20 | Phillips Petroleum Company | Hydrocarbon steam reforming process |
| DE2901362A1 (de) | 1978-01-25 | 1979-07-26 | Sandoz Ag | Guanidinderivate, ihre herstellung und verwendung |
| GB1588096A (en) | 1978-05-20 | 1981-04-15 | Wyeth & Bros Ltd John | Pyrrole derivatives |
| GB9511694D0 (en) | 1995-06-09 | 1995-08-02 | Fujisawa Pharmaceutical Co | Benzamide derivatives |
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| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| WO2006009655A1 (en) | 2004-06-16 | 2006-01-26 | Wyeth | Diphenylimidazopyrimidine and -imidazole amines as inhibitors of b-secretase |
| MXPA06014793A (es) | 2004-06-16 | 2007-02-16 | Wyeth Corp | Derivados de amino-5, 5-difenilimidazolona para la inhibicion de ??-secretasa. |
| RU2007126570A (ru) | 2005-01-14 | 2009-02-20 | Вайет (Us) | Аминоимидазолоны, применяемые для ингибирования бета-секретазы |
| EP1844035A1 (en) | 2005-02-01 | 2007-10-17 | Wyeth | Amino-pyridines as inhibitors of beta-secretase |
| WO2006088694A1 (en) | 2005-02-14 | 2006-08-24 | Wyeth | SUBSTITUTED THIENYL AND FURYL ACYLGUANIDINES AS β-SECRETASE MODULATORS |
| WO2006088705A1 (en) | 2005-02-14 | 2006-08-24 | Wyeth | Terphenyl guanidines as [beta symbol] -secretase inhibitors |
| JP2008530103A (ja) | 2005-02-14 | 2008-08-07 | ワイス | β−セクレターゼ阻害剤としてのアゾリルアシルグアニジン |
| BRPI0613578A2 (pt) | 2005-06-30 | 2012-01-17 | Wyeth Corp | composito da fórmula i; uso de um composto de fórmula i; e composição farmacêutica |
| TW200738683A (en) | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
| TW200730523A (en) | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
| CN101273018A (zh) | 2005-09-26 | 2008-09-24 | 惠氏公司 | 用于β分泌酶（BACE）抑制剂的氨基-5-[4-(二氟甲氧基)苯基]-5-苯基咪唑酮化合物 |
| JP2009520027A (ja) | 2005-12-19 | 2009-05-21 | ワイス | ２−アミノ−５−ピペリジニルイミダゾロン化合物およびβ−セクレターゼ調節におけるその使用 |
| WO2007100536A1 (en) | 2006-02-24 | 2007-09-07 | Wyeth | DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE |
| US7700606B2 (en) | 2006-08-17 | 2010-04-20 | Wyeth Llc | Imidazole amines as inhibitors of β-secretase |
| MX2009003102A (es) | 2006-09-21 | 2009-04-01 | Wyeth Corp | INDOLILALQUILPIRIDIN-2-AMINAS PARA LA INHIBICION DE ß-SECRETASA. |
| AR065814A1 (es) * | 2007-03-23 | 2009-07-01 | Wyeth Corp | Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados. |
-
2008
- 2008-03-19 AR ARP080101183A patent/AR065814A1/es unknown
- 2008-03-19 CL CL200800791A patent/CL2008000791A1/es unknown
- 2008-03-19 PE PE2008000502A patent/PE20090617A1/es not_active Application Discontinuation
- 2008-03-20 WO PCT/US2008/003783 patent/WO2008118379A2/en not_active Ceased
- 2008-03-20 AU AU2008232341A patent/AU2008232341A1/en not_active Abandoned
- 2008-03-20 CA CA002681431A patent/CA2681431A1/en not_active Abandoned
- 2008-03-20 JP JP2010500946A patent/JP2010522237A/ja not_active Withdrawn
- 2008-03-20 EP EP08727089A patent/EP2144884A2/en not_active Withdrawn
- 2008-03-20 MX MX2009010057A patent/MX2009010057A/es not_active Application Discontinuation
- 2008-03-20 CN CN200880009460A patent/CN101663281A/zh active Pending
- 2008-03-20 BR BRPI0809162-5A patent/BRPI0809162A2/pt not_active Application Discontinuation
- 2008-03-21 US US12/053,086 patent/US7723368B2/en not_active Expired - Fee Related
- 2008-03-21 TW TW097110191A patent/TW200901978A/zh unknown
-
2010
- 2010-03-10 US US12/721,086 patent/US20100168194A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20100168194A1 (en) | 2010-07-01 |
| US20090048320A1 (en) | 2009-02-19 |
| AR065814A1 (es) | 2009-07-01 |
| WO2008118379A3 (en) | 2009-01-29 |
| US7723368B2 (en) | 2010-05-25 |
| WO2008118379A2 (en) | 2008-10-02 |
| CN101663281A (zh) | 2010-03-03 |
| MX2009010057A (es) | 2009-10-12 |
| EP2144884A2 (en) | 2010-01-20 |
| CA2681431A1 (en) | 2008-10-02 |
| BRPI0809162A2 (pt) | 2014-09-16 |
| JP2010522237A (ja) | 2010-07-01 |
| TW200901978A (en) | 2009-01-16 |
| CL2008000791A1 (es) | 2008-05-30 |
| AU2008232341A1 (en) | 2008-10-02 |
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