PE20091466A1 - Derivados de 4,5-dihidro-oxazol-2-il-amina - Google Patents

Derivados de 4,5-dihidro-oxazol-2-il-amina

Info

Publication number
PE20091466A1
PE20091466A1 PE2009000228A PE2009000228A PE20091466A1 PE 20091466 A1 PE20091466 A1 PE 20091466A1 PE 2009000228 A PE2009000228 A PE 2009000228A PE 2009000228 A PE2009000228 A PE 2009000228A PE 20091466 A1 PE20091466 A1 PE 20091466A1
Authority
PE
Peru
Prior art keywords
dihydro
oxazole
ilamine
biphenyl
phenyl
Prior art date
Application number
PE2009000228A
Other languages
English (en)
Inventor
Matteo Andreini
Emanuele Gabellieri
Wolfgang Guba
Guido Marconi
Robert Narquizian
Eoin Christopher Power
Massimiliano Travagli
Thomas Woltering
Wolfgang Wostl
Original Assignee
Hoffmann La Roche
Siena Biotech Spa
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 Hoffmann La Roche, Siena Biotech Spa filed Critical Hoffmann La Roche
Publication of PE20091466A1 publication Critical patent/PE20091466A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/28Nitrogen atoms not forming part of a nitro radical
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/10Heterocyclic 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 carbon chain containing aromatic rings

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 4,5-DIHIDRO-OXAZOL-2-IL-AMINA DE FORMULA (I) DONDE R1 Y R1' SON CADA UNO H, HALOGENO, ALCOXI INFERIOR, ENTRE OTROS; R2 ES H, HALOGENO, CN, ALCOXI INFERIOR, ENTRE OTROS; R3 ES H, CN, ALQUILO INFERIOR, ENTRE OTROS; R4 ES H O ALQUILO INFERIOR; X ES UN ENLACE, -NH-C(O)-, -NH- O -O-CH2; Ar ES ARILO O HETEROARILO; m ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: (RS)-4-(3'-CLORO-BIFENIL-3-IL)-4-(4-METOXI-FENIL)-4,5-DIHIDRO-OXAZOL-2-ILAMINA, (RS)-4-(6-FLUOR-3'-METOXI-BIFENIL-3-IL)-4-(4-METOXI-3-METIL-FENIL)-4,5-DIHIDRO-OXAZOL-2-ILAMINA, (RS)-4-(4-DIFLUORMETOXI-3-METIL-FENIL)-4-(2'-FLUOR-5'-METOXI-BIFENIL-3-IL)-4,5-DIHIDRO-OXAZOL-2-ILAMINA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ASP2 (B-SECRETASA, BACE 1 O MEMAPSINA-2) SIENDO UTILES PARA EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMER
PE2009000228A 2008-02-18 2009-02-16 Derivados de 4,5-dihidro-oxazol-2-il-amina PE20091466A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08151546 2008-02-18

Publications (1)

Publication Number Publication Date
PE20091466A1 true PE20091466A1 (es) 2009-09-24

Family

ID=40545768

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2009000228A PE20091466A1 (es) 2008-02-18 2009-02-16 Derivados de 4,5-dihidro-oxazol-2-il-amina

Country Status (16)

Country Link
US (1) US7989449B2 (es)
EP (1) EP2245019B1 (es)
JP (1) JP5258904B2 (es)
KR (1) KR101259240B1 (es)
CN (1) CN101952260B (es)
AR (1) AR070395A1 (es)
AU (1) AU2009216825A1 (es)
BR (1) BRPI0907563A2 (es)
CA (1) CA2712228C (es)
CL (1) CL2009000349A1 (es)
ES (1) ES2398017T3 (es)
IL (1) IL206765A0 (es)
MX (1) MX2010008347A (es)
PE (1) PE20091466A1 (es)
TW (1) TW200938537A (es)
WO (1) WO2009103626A1 (es)

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CN102119161B (zh) 2008-06-13 2015-07-08 盐野义制药株式会社 具有β分泌酶抑制作用的含硫杂环衍生物
EP2324032B1 (en) * 2008-08-19 2014-10-01 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
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AR075854A1 (es) * 2009-03-13 2011-05-04 Vitae Pharmaceuticals Inc Inhibidores de beta- secretasa
US20110065695A1 (en) * 2009-09-11 2011-03-17 Jeremy Beauchamp Use of aminodihydrothiazines for the treatment or prevention of diabetes
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US8354441B2 (en) * 2009-11-11 2013-01-15 Hoffmann-La Roche Inc. Oxazoline derivatives
WO2011070781A1 (ja) 2009-12-09 2011-06-16 塩野義製薬株式会社 置換アミノチアジン誘導体
UA103272C2 (uk) * 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
UA110467C2 (uk) 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
JPWO2011077726A1 (ja) 2009-12-24 2013-05-02 塩野義製薬株式会社 4−アミノ−1,3−チアジンまたはオキサジン誘導体
EP2539322B1 (en) 2010-02-24 2014-01-01 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
MX2012010657A (es) 2010-03-15 2013-02-07 Amgen Inc Compuestos de espiro amino-dihidrooxazina y amino-dihidrotiazina como moduladores de beta-secretasa y su uso medico.
CA2791281A1 (en) 2010-03-15 2011-09-22 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators
US8815881B2 (en) * 2010-08-09 2014-08-26 Hoffmann-La Roche Inc. 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
US9018219B2 (en) 2010-10-29 2015-04-28 Shionogi & Co., Ltd. Fused aminodihydropyrimidine derivative
WO2012057248A1 (ja) 2010-10-29 2012-05-03 塩野義製薬株式会社 ナフチリジン誘導体
PL2663561T3 (pl) * 2011-01-13 2016-10-31 Nowe pochodne heterocykliczne i ich zastosowanie w leczeniu zaburzeń neurologicznych
US8399459B2 (en) 2011-02-02 2013-03-19 Hoffmann-La Roche Inc. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
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
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
EP2758406A1 (en) 2011-09-21 2014-07-30 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
DE102011055815A1 (de) 2011-11-29 2013-05-29 Aicuris Gmbh & Co. Kg Carboxamid-substituierte Heteroaryl-Pyrazole und ihre Verwendung
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
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TW201422592A (zh) 2012-08-27 2014-06-16 Boehringer Ingelheim Int β-分泌酶抑制劑
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EP3463359A4 (en) * 2016-06-02 2020-08-26 Purdue Pharma LP SPURENAMINE-ASSOCIATED RECEPTOR-1 AGONISTS AND PARTIAL AGONISTS FOR PAIN MANAGEMENT
CN113729026A (zh) * 2021-10-09 2021-12-03 合肥巨卓农业技术开发有限公司 一种包含啶磺草胺和异丙隆的复合除草剂
TW202342013A (zh) * 2022-02-10 2023-11-01 英屬開曼群島商百濟神州有限公司 雜環化合物、其組成物及用其進行治療之方法

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TW200602045A (en) * 2004-06-16 2006-01-16 Wyeth Corp Amino-5, 5-diphenylimidazolone derivatives for the inhibition of β-secretase
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TW200734311A (en) * 2005-11-21 2007-09-16 Astrazeneca Ab New compounds
EP2114906B1 (en) * 2007-02-02 2014-08-06 F. Hoffmann-La Roche AG 2-aminooxazolines as taar1 ligands for cns disorders

Also Published As

Publication number Publication date
CA2712228A1 (en) 2009-08-27
JP2011512378A (ja) 2011-04-21
KR20100130595A (ko) 2010-12-13
AU2009216825A1 (en) 2009-08-27
ES2398017T3 (es) 2013-03-13
WO2009103626A1 (en) 2009-08-27
CN101952260A (zh) 2011-01-19
CN101952260B (zh) 2013-02-13
CA2712228C (en) 2013-04-16
AR070395A1 (es) 2010-03-31
MX2010008347A (es) 2010-11-12
US20090209529A1 (en) 2009-08-20
US7989449B2 (en) 2011-08-02
JP5258904B2 (ja) 2013-08-07
IL206765A0 (en) 2010-12-30
EP2245019B1 (en) 2012-11-14
BRPI0907563A2 (pt) 2015-08-04
TW200938537A (en) 2009-09-16
CL2009000349A1 (es) 2010-02-19
KR101259240B1 (ko) 2013-04-29
EP2245019A1 (en) 2010-11-03

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