ECSP088286A - COMPUESTOS DE AMINO-5-[4-(DIFLUOROMETOXI)FENIL]-5-FENILIMIDAZOLONA PARA LA INHIBICIÓN DE LA ß-SECRETASA - Google Patents
COMPUESTOS DE AMINO-5-[4-(DIFLUOROMETOXI)FENIL]-5-FENILIMIDAZOLONA PARA LA INHIBICIÓN DE LA ß-SECRETASAInfo
- Publication number
- ECSP088286A ECSP088286A EC2008008286A ECSP088286A ECSP088286A EC SP088286 A ECSP088286 A EC SP088286A EC 2008008286 A EC2008008286 A EC 2008008286A EC SP088286 A ECSP088286 A EC SP088286A EC SP088286 A ECSP088286 A EC SP088286A
- Authority
- EC
- Ecuador
- Prior art keywords
- secretase
- phenyl
- amino
- difluorometoxi
- inhibition
- Prior art date
Links
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract 2
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- -1 2-amino-5- [4- (difluoromethoxy) phenyl] -5-3,5-dihydro-phenylimidazol-4-one compound Chemical class 0.000 abstract 1
- 208000037259 Amyloid Plaque Diseases 0.000 abstract 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- 102100021257 Beta-secretase 1 Human genes 0.000 abstract 1
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 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
- C07D233/88—Nitrogen atoms, e.g. allantoin
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
-
- 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
- A61P25/28—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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención suministra un compuesto de 2-amino-5-[4-(difluorometoxi)fenil]-5-3,5-dihidro-fenilimidazol-4-ona de fórmula I. La presente invención también suministra métodos para el uso del mismo para inhibir la ß-secretasa (BACE) y tratar los depósitos ß-amiloides y las marañas neurofibrilares.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72058905P | 2005-09-26 | 2005-09-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP088286A true ECSP088286A (es) | 2008-04-28 |
Family
ID=37693581
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2008008286A ECSP088286A (es) | 2005-09-26 | 2008-03-17 | COMPUESTOS DE AMINO-5-[4-(DIFLUOROMETOXI)FENIL]-5-FENILIMIDAZOLONA PARA LA INHIBICIÓN DE LA ß-SECRETASA |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US7423158B2 (es) |
| EP (2) | EP1928841A1 (es) |
| JP (1) | JP2009509957A (es) |
| KR (1) | KR20080050430A (es) |
| CN (1) | CN101273018A (es) |
| AR (1) | AR056536A1 (es) |
| AU (1) | AU2006294620A1 (es) |
| BR (1) | BRPI0616757A2 (es) |
| CA (1) | CA2623245A1 (es) |
| CR (1) | CR9830A (es) |
| EC (1) | ECSP088286A (es) |
| GT (1) | GT200600432A (es) |
| IL (1) | IL189650A0 (es) |
| NO (1) | NO20080942L (es) |
| PE (1) | PE20070461A1 (es) |
| RU (1) | RU2008106936A (es) |
| TW (1) | TW200808735A (es) |
| WO (1) | WO2007038271A1 (es) |
| ZA (1) | ZA200802636B (es) |
Families Citing this family (67)
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| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7592348B2 (en) | 2003-12-15 | 2009-09-22 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700603B2 (en) | 2003-12-15 | 2010-04-20 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| ATE423121T1 (de) | 2004-06-16 | 2009-03-15 | Wyeth Corp | Diphenylimidazopyrimidin- und -imidazolamine als b-sekretase-inhibitoren |
| ES2332659T3 (es) * | 2004-06-16 | 2010-02-10 | Wyeth | Derivados de amino-5,5-difenilimidazolona para la inhibicion de beta-secretasa. |
| WO2006014944A1 (en) | 2004-07-28 | 2006-02-09 | Schering Corporation | Macrocyclic beta-secretase inhibitors |
| CN101103034A (zh) * | 2005-01-14 | 2008-01-09 | 惠氏公司 | 抑制β-分泌酶的氨基-咪唑酮 |
| MX2007009313A (es) * | 2005-02-01 | 2007-09-12 | Wyeth Corp | Amino-piridinas como inhibidores de ????-secretasa. |
| BRPI0606902A2 (pt) | 2005-02-14 | 2009-07-28 | Wyeth Corp | composto; método para o tratamento de uma doença ou distúrbio associado a atividade excessiva de bace em um paciente que dele necessite; método para modular a atividade de bace; composição farmacêutica |
| CN101228163A (zh) | 2005-06-14 | 2008-07-23 | 先灵公司 | 天冬氨酰蛋白酶抑制剂 |
| CA2610828A1 (en) * | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
| TW200738683A (en) * | 2005-06-30 | 2007-10-16 | Wyeth Corp | Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation |
| EP1896448A1 (en) * | 2005-06-30 | 2008-03-12 | Wyeth | AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION |
| TW200730523A (en) * | 2005-07-29 | 2007-08-16 | Wyeth Corp | Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation |
| CA2620136A1 (en) * | 2005-09-05 | 2007-03-15 | Jun Fujita | Sequence capable of enhancing the expression of gene under moderately low temperature |
| EP2612854B1 (en) | 2005-10-25 | 2015-04-29 | Shionogi&Co., Ltd. | Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors |
| CN101360737A (zh) * | 2005-12-19 | 2009-02-04 | 惠氏公司 | 2-氨基-5-哌啶咪唑酮化合物和其用于β分泌酶调节的用途 |
| 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 |
| EP2032542A2 (en) * | 2006-06-12 | 2009-03-11 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US7700606B2 (en) * | 2006-08-17 | 2010-04-20 | Wyeth Llc | Imidazole amines as inhibitors of β-secretase |
| EP2064201A2 (en) * | 2006-09-21 | 2009-06-03 | Wyeth | Indolylalkylpyridin-2-amines for the inhibition of beta-secretase |
| JP2010512389A (ja) | 2006-12-12 | 2010-04-22 | シェーリング コーポレイション | アスパルチルプロテアーゼ阻害剤 |
| KR20090090364A (ko) * | 2006-12-12 | 2009-08-25 | 쉐링 코포레이션 | 트리사이클릭 환 시스템을 함유하는 아스파르틸 프로테아제 억제제 |
| WO2008076043A1 (en) * | 2006-12-20 | 2008-06-26 | Astrazeneca Ab | Novel 2-amino-5,5-diaryl-imidazol-4-ones |
| CL2008000784A1 (es) * | 2007-03-20 | 2008-05-30 | Wyeth Corp | Compuestos amino-5-[-4-(diflourometoxi) fenil sustituido]-5-fenilmidazolona, inhibidores de b-secretasa; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar alzheimer, deterioro cognitivo, sindrome de down, disminucion co |
| CL2008000791A1 (es) * | 2007-03-23 | 2008-05-30 | Wyeth Corp | Compuestos derivados de 2-amino-5-(4-difluorometoxi-fenil)-5-fenil-imidazolidin-4-ona; composicion farmaceutica que comprende a dichos compuestos; y su uso en el tratamiento de una enfermedad asociada con la actividad bace excesiva, tales como enferm |
| WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
| TW200902526A (en) | 2007-04-24 | 2009-01-16 | Shionogi & Amp Co Ltd | Aminodihydrothiazin derivative substituted with a cyclic group |
| CL2009000954A1 (es) * | 2008-04-22 | 2010-12-31 | Schering Corp | Compuestos derivados de 2-imino-3-metil pirrolo pirimidinona,inhibidores de bace-1; composicion farmaceutica; y su uso para tratar, prevenir y/o retardar el inicio de una patologia de beta-amiloide seleccionada de enfermedad de alzheimer, enfermedad de parkinson, perdida de la memoria, sindrome de down, entre otras. |
| WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
| WO2010021680A2 (en) | 2008-08-19 | 2010-02-25 | Vitae Pharmaceuticals, Inc. | Inhibitors of beta-secretase |
| CA2736130C (en) | 2008-09-11 | 2014-01-14 | Amgen Inc. | Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use |
| JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体 |
| KR101908255B1 (ko) | 2009-03-13 | 2018-10-15 | 비타이 파마슈티컬즈, 인코포레이티드 | 베타세크리타아제 저해제 |
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| 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 |
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| KR20140054295A (ko) | 2011-08-22 | 2014-05-08 | 머크 샤프 앤드 돔 코포레이션 | Bace 억제제로서의 2-스피로-치환된 이미노티아진 및 그의 모노- 및 디옥시드, 조성물 및 그의 용도 |
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| US9290477B2 (en) | 2012-09-28 | 2016-03-22 | Vitae Pharmaceuticals, Inc. | Inhibitors of β-secretase |
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| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
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| WO2014127042A1 (en) | 2013-02-12 | 2014-08-21 | Buck Institute For Research On Aging | Hydantoins that modulate bace-mediated app processing |
| CN103408573B (zh) * | 2013-07-12 | 2015-12-23 | 上海工程技术大学 | 硼酸衍生物及其制备方法和应用 |
| KR20180090778A (ko) * | 2015-08-27 | 2018-08-13 | 난트뉴로, 엘엘씨 | App-선택적 bace 억제를 위한 조성물 및 그의 용도 |
| CN106749033A (zh) * | 2015-11-25 | 2017-05-31 | 中国人民解放军军事医学科学院毒物药物研究所 | 乙内酰脲类化合物及其作为β-分泌酶抑制剂的用途 |
| CN113087667B (zh) * | 2021-03-24 | 2022-06-24 | 五邑大学 | 一种咪唑啉酮衍生物的合成方法 |
| WO2024201390A1 (en) * | 2023-03-29 | 2024-10-03 | Simon Fraser University | Methods and reagents for synthesizing haloaldehydes, and uses thereof |
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| MX2007009313A (es) | 2005-02-01 | 2007-09-12 | Wyeth Corp | Amino-piridinas como inhibidores de ????-secretasa. |
| 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 |
| BRPI0606902A2 (pt) | 2005-02-14 | 2009-07-28 | Wyeth Corp | composto; método para o tratamento de uma doença ou distúrbio associado a atividade excessiva de bace em um paciente que dele necessite; método para modular a atividade de bace; composição farmacêutica |
| EP1896448A1 (en) | 2005-06-30 | 2008-03-12 | Wyeth | AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION |
| 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 |
| CN101360737A (zh) | 2005-12-19 | 2009-02-04 | 惠氏公司 | 2-氨基-5-哌啶咪唑酮化合物和其用于β分泌酶调节的用途 |
| 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 |
-
2006
- 2006-09-22 KR KR1020087007179A patent/KR20080050430A/ko not_active Withdrawn
- 2006-09-22 WO PCT/US2006/036985 patent/WO2007038271A1/en not_active Ceased
- 2006-09-22 CN CNA2006800353948A patent/CN101273018A/zh active Pending
- 2006-09-22 AU AU2006294620A patent/AU2006294620A1/en not_active Abandoned
- 2006-09-22 CA CA002623245A patent/CA2623245A1/en not_active Abandoned
- 2006-09-22 EP EP06815185A patent/EP1928841A1/en not_active Withdrawn
- 2006-09-22 RU RU2008106936/04A patent/RU2008106936A/ru not_active Application Discontinuation
- 2006-09-22 EP EP10172623A patent/EP2256107A1/en not_active Withdrawn
- 2006-09-22 PE PE2006001150A patent/PE20070461A1/es not_active Application Discontinuation
- 2006-09-22 JP JP2008532416A patent/JP2009509957A/ja not_active Withdrawn
- 2006-09-22 BR BRPI0616757-8A patent/BRPI0616757A2/pt not_active IP Right Cessation
- 2006-09-25 US US11/526,511 patent/US7423158B2/en not_active Expired - Fee Related
- 2006-09-26 GT GT200600432A patent/GT200600432A/es unknown
- 2006-09-26 AR ARP060104191A patent/AR056536A1/es unknown
- 2006-09-26 TW TW095135587A patent/TW200808735A/zh unknown
-
2008
- 2008-02-21 IL IL189650A patent/IL189650A0/en unknown
- 2008-02-25 NO NO20080942A patent/NO20080942L/no not_active Application Discontinuation
- 2008-03-17 EC EC2008008286A patent/ECSP088286A/es unknown
- 2008-03-25 ZA ZA200802636A patent/ZA200802636B/xx unknown
- 2008-03-26 CR CR9830A patent/CR9830A/es not_active Application Discontinuation
- 2008-08-29 US US12/201,026 patent/US20090012139A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| PE20070461A1 (es) | 2007-05-10 |
| EP1928841A1 (en) | 2008-06-11 |
| KR20080050430A (ko) | 2008-06-05 |
| WO2007038271A9 (en) | 2008-05-08 |
| CR9830A (es) | 2008-05-21 |
| US20090012139A1 (en) | 2009-01-08 |
| US20070072925A1 (en) | 2007-03-29 |
| CA2623245A1 (en) | 2007-04-05 |
| WO2007038271A1 (en) | 2007-04-05 |
| TW200808735A (en) | 2008-02-16 |
| JP2009509957A (ja) | 2009-03-12 |
| AU2006294620A1 (en) | 2007-04-05 |
| US7423158B2 (en) | 2008-09-09 |
| CN101273018A (zh) | 2008-09-24 |
| AR056536A1 (es) | 2007-10-10 |
| ZA200802636B (en) | 2009-03-25 |
| RU2008106936A (ru) | 2009-11-10 |
| GT200600432A (es) | 2007-05-28 |
| IL189650A0 (en) | 2008-06-05 |
| EP2256107A1 (en) | 2010-12-01 |
| BRPI0616757A2 (pt) | 2011-06-28 |
| NO20080942L (no) | 2008-04-07 |
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