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PE20090160A1 - COMPUESTOS AMINO-5-[4-(DIFLUOROMETOXI)FENIL SUSTITUIDO]-5-FENILIMIDAZOLONA COMO INHIBIDORES DE ß-SECRETASA - Google Patents

COMPUESTOS AMINO-5-[4-(DIFLUOROMETOXI)FENIL SUSTITUIDO]-5-FENILIMIDAZOLONA COMO INHIBIDORES DE ß-SECRETASA

Info

Publication number
PE20090160A1
PE20090160A1 PE2008000494A PE2008000494A PE20090160A1 PE 20090160 A1 PE20090160 A1 PE 20090160A1 PE 2008000494 A PE2008000494 A PE 2008000494A PE 2008000494 A PE2008000494 A PE 2008000494A PE 20090160 A1 PE20090160 A1 PE 20090160A1
Authority
PE
Peru
Prior art keywords
amino
secretase inhibitors
difluorometoxi
compounds
difluorometoxy
Prior art date
Application number
PE2008000494A
Other languages
English (en)
Inventor
Michael Sotirios Malamas
Albert Jean Robichaud
Alexander Michael Porte
William Ronald Solvibile
Koi Michele Morris
Schuyler Adam Antane
Ji-In Kim
Robert Emmett Mcdevitt
Original Assignee
Wyeth Corp
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 Wyeth Corp filed Critical Wyeth Corp
Publication of PE20090160A1 publication Critical patent/PE20090160A1/es

Links

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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

REFERIDA A UN DERIVADO DE IMIDAZOLONA DE FORMULA (I), DONDE R1 Y R2 SON H, ALQUILO, CICLOALQUILO, ENTRE OTROS; R3 ES H, ALQUILO, CICLOALQUILO, ARILO, ENTRE OTROS; R4, R5 Y R6 SON H, HALOGENO, NO2, CN, ALQUILO, ENTRE OTROS; R7 Y R8 SON H, HALOGENO, ALQUILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (5R)-2-AMINO-5-[3-(CICLOPROPILETINIL)-4-FLUOROFENIL]-5-[4-(DIFLUOROMETOXI)-3-METILFENIL]-3-METIL-3,5-DIHIDRO-4H-IMIDAZOL-4-ONA, 2-AMINO-5-[4-(DIFLUOROMETOXI)-3-METILFENIL]-3-METIL-5-FENIL-3,5-DIHIDRO-4H-IMIDAZOL-4-ONA, 2-AMINO-4-(4-(DIFLUOROMETOXI)-3-METILFENIL)-4-(4-FLUOROFENIL)-1-METIL-1H-IMIDAZOL-5(4H)-ONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE BETA-SECRETASA Y SON UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER, TRISOMIA 21, ENTRE OTROS
PE2008000494A 2007-03-20 2008-03-18 COMPUESTOS AMINO-5-[4-(DIFLUOROMETOXI)FENIL SUSTITUIDO]-5-FENILIMIDAZOLONA COMO INHIBIDORES DE ß-SECRETASA PE20090160A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US91908707P 2007-03-20 2007-03-20

Publications (1)

Publication Number Publication Date
PE20090160A1 true PE20090160A1 (es) 2009-02-11

Family

ID=39564223

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000494A PE20090160A1 (es) 2007-03-20 2008-03-18 COMPUESTOS AMINO-5-[4-(DIFLUOROMETOXI)FENIL SUSTITUIDO]-5-FENILIMIDAZOLONA COMO INHIBIDORES DE ß-SECRETASA

Country Status (24)

Country Link
US (1) US20090042964A1 (es)
EP (1) EP2137161A1 (es)
JP (1) JP2010522235A (es)
KR (1) KR20100015376A (es)
CN (1) CN101641335A (es)
AR (1) AR065811A1 (es)
AU (1) AU2008229327A1 (es)
BR (1) BRPI0808944A2 (es)
CA (1) CA2681243A1 (es)
CL (1) CL2008000784A1 (es)
CO (1) CO6140056A2 (es)
CR (1) CR11020A (es)
EC (1) ECSP099639A (es)
GT (1) GT200900241A (es)
IL (1) IL200961A0 (es)
MX (1) MX2009009699A (es)
NI (1) NI200900164A (es)
PA (1) PA8772701A1 (es)
PE (1) PE20090160A1 (es)
RU (1) RU2009133807A (es)
SV (1) SV2009003373A (es)
TW (1) TW200845965A (es)
WO (1) WO2008115552A1 (es)
ZA (1) ZA200906542B (es)

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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
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
TW201004961A (en) 2005-06-14 2010-02-01 Schering Corp Aspartyl protease inhibitors
US8450308B2 (en) 2008-08-19 2013-05-28 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
EP2184276A1 (en) * 2008-11-07 2010-05-12 Universite Paul Cezanne Aix-Marseille Iii Process to prepare new substituted 1H-Benzo(d) imidazol-2(3h)-Ones, New intermediates and their use as bace 1 inhibitors
AP2866A (en) 2009-03-13 2014-03-31 Vitae Pharmaceuticals Inc Inhibitors of beta-secretase
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US8889703B2 (en) 2010-02-24 2014-11-18 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US9145426B2 (en) 2011-04-07 2015-09-29 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
WO2012138734A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2013028670A1 (en) 2011-08-22 2013-02-28 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their 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
DK2956443T3 (da) * 2013-02-12 2020-01-20 Buck Inst Res Aging Hydantoiner som modulatorer af BACE-medieret APP-forarbejdning
US20160298151A1 (en) 2015-04-09 2016-10-13 Sher Ali Butt Novel Method for the cheap, efficient, and effective production of pharmaceutical and therapeutic api's intermediates, and final products
CN112423756B (zh) 2018-04-23 2024-08-13 默沙东有限责任公司 用于合成苯氧基二氨基嘧啶化合物的新方法
CN109289696B (zh) * 2018-10-29 2022-03-22 天津先光化工有限公司 一种咪唑啉两性表面活性剂的制备方法

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE45198B1 (en) * 1976-06-05 1982-07-14 Wyeth John & Brother Ltd Guanidine derivatives
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
TW544448B (en) * 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
US6492408B1 (en) * 1999-07-21 2002-12-10 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammatory disease
DE10046993A1 (de) * 2000-09-22 2002-04-11 Aventis Pharma Gmbh Substituierte Zimtsäureguanidide, Verfahren zur ihrer Herstellung, ihre Verwendung als Medikament sowie sie enthaltendes Medikament
AU2003229024A1 (en) * 2002-05-07 2003-11-11 Elan Pharmaceuticals, Inc. Succinoyl aminopyrazoles and related compounds
US7700603B2 (en) * 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
DE602005017033D1 (de) * 2004-06-16 2009-11-19 Wyeth Corp Amino-5,5-diphenylimidazolon-derivate zur beta-sekretase-hemmung
DE602005012825D1 (de) * 2004-06-16 2009-04-02 Wyeth Corp Diphenylimidazopyrimidin- und -imidazolamine als b-sekretase-inhibitoren
AU2006205127A1 (en) * 2005-01-14 2006-07-20 Wyeth Amino-imidazolones for the inhibition of beta-secretase
BRPI0607094A2 (pt) * 2005-02-01 2009-08-04 Wyeth Corp composto da fórmula i; uso do composto para o tratamento de uma doença ou distúrbio associado à atividade excessiva de bace em um paciente que dele necessita; uso do composto para modular a atividade de bace; e composição farmacêutica
WO2006088705A1 (en) * 2005-02-14 2006-08-24 Wyeth Terphenyl guanidines as [beta symbol] -secretase inhibitors
WO2006088694A1 (en) * 2005-02-14 2006-08-24 Wyeth SUBSTITUTED THIENYL AND FURYL ACYLGUANIDINES AS β-SECRETASE MODULATORS
CN101146769A (zh) * 2005-02-14 2008-03-19 惠氏公司 作为β-分泌酶抑制剂的唑基酰基胍
CA2613435A1 (en) * 2005-06-30 2007-01-11 Wyeth Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for .beta.-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
JP2009509957A (ja) * 2005-09-26 2009-03-12 ワイス β−セクレターゼ阻害剤としてのアミノ−５−［４−（ジフルオロメトキシ）フェニル］−５−フェニルイミダゾロン化合物
EP1966185A2 (en) * 2005-12-19 2008-09-10 Wyeth a Corporation of the State of Delaware 2-AMINO-5-PIPERIDINYLIMIDAZOLONE COMPOUNDS AND USE THEREOF FOR ß-SECRETASE MODULATION
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
EP2064201A2 (en) * 2006-09-21 2009-06-03 Wyeth Indolylalkylpyridin-2-amines for the inhibition of beta-secretase

Also Published As

Publication number Publication date
RU2009133807A (ru) 2011-04-27
TW200845965A (en) 2008-12-01
PA8772701A1 (es) 2008-11-19
MX2009009699A (es) 2009-09-24
AR065811A1 (es) 2009-07-01
NI200900164A (es) 2010-07-29
US20090042964A1 (en) 2009-02-12
SV2009003373A (es) 2010-08-10
AU2008229327A8 (en) 2009-10-15
CN101641335A (zh) 2010-02-03
CA2681243A1 (en) 2008-09-25
AU2008229327A1 (en) 2008-09-25
ECSP099639A (es) 2009-10-30
IL200961A0 (en) 2010-05-17
JP2010522235A (ja) 2010-07-01
BRPI0808944A2 (pt) 2014-09-02
EP2137161A1 (en) 2009-12-30
GT200900241A (es) 2010-05-07
CL2008000784A1 (es) 2008-05-30
CR11020A (es) 2009-10-06
ZA200906542B (en) 2010-06-30
CO6140056A2 (es) 2010-03-19
WO2008115552A1 (en) 2008-09-25
KR20100015376A (ko) 2010-02-12

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