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AR037460A1 - Compuesto de hidroxietileno, composicion farmaceutica que lo comprende, uso del mismo para la fabricacion de un medicamento y procedimiento para su preparacion - Google Patents

Compuesto de hidroxietileno, composicion farmaceutica que lo comprende, uso del mismo para la fabricacion de un medicamento y procedimiento para su preparacion

Info

Publication number
AR037460A1
AR037460A1 ARP020104587A ARP020104587A AR037460A1 AR 037460 A1 AR037460 A1 AR 037460A1 AR P020104587 A ARP020104587 A AR P020104587A AR P020104587 A ARP020104587 A AR P020104587A AR 037460 A1 AR037460 A1 AR 037460A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
groups
cycloalkyl
aryl
Prior art date
Application number
ARP020104587A
Other languages
English (en)
Original Assignee
Smithkline Beecham Plc
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
Priority claimed from GB0128748A external-priority patent/GB0128748D0/en
Priority claimed from GB0214090A external-priority patent/GB0214090D0/en
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Publication of AR037460A1 publication Critical patent/AR037460A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/267—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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
    • C07D223/08—Oxygen atoms
    • C07D223/10—Oxygen atoms attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic 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
    • C07D263/16—Heterocyclic 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/22—Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Compuestos de hidroxietileno que tienen actividad inhibidora de Asp2 (b-secretasa, BACE1 o Memapsina). Procedimiento para su preparación, composiciones farmacéuticas que los contienen y a su uso en el tratamiento de enfermedades individualizadas por niveles elevados de b-amiloide o depósitos de b-amiloide, en particular, a la enfermedad de Alzheimer. Reivindicación 1: Un compuesto de hidroxietileno caracterizado porque responde a la fórmula (1), en la que: R1 representa un grupo de fórmula (2) ó (3); A1 representa CH2, O, S o NR5; A2 representa O, S o NR5; n1 representa un número entero de 1 a 3; R5 representa hidrógeno, alquilo C1-6 opcionalmente sustituido con uno o más grupos R11, cicloalquilo C3-8 opcionalmente sustituido con uno o más grupos R11, -(alquil C1-2)(cicloalquilo C3-8) o arilo; Ra representa halógeno; Rb representa -(alquilo C1-6) opcionalmente sustituido con uno o más grupos R11 o -(alquil C1-6)arilo; X1 representa N, -C(-R6)- o -C(-O-R7)-; X2 representa N, -C(R8)- o -C(-Y-R9)-; Y representa un enlace, CH2, O, S, CO, NR10, -N(R10)C(O)-, -C(O)N(R10)-, COO, arilo, heterociclilo o heteroarilo; R6 representa hidrógeno, halógeno, -(alquilo C1-6) opcionalmente sustituido con uno o más grupos R11, -(alquenilo C2-6), -(cicloalquilo C3-8), opcinalmente sustituido con uno o más grupos R11, -(alquil C1-2) (cicloalquilo C3-8), heteroarilo, heterociclilo o arilo; R8 representa halógeno o trifluorometilo; R7, R9 y R10 representan independientemente hidrógeno, -(alquilo C1-6) opcionalmente sustituido con uno o más grupos R11, -(alquenilo C2-6), -(cicloalquilo C3-8) opcionalmente sustituido con uno o más grupos R11, -(alquil C1-2) (cicloalquilo C3-8), heteroarilo, heterociclilo o arilo; W1 representa CO ó SO2; R2 representa -(alquilo C5-8), -(alquil C1-6)arilo, -(alquil C1-6)heteroarilo, -(alquil C1-6)heterociclilo, -(alquil C1-6)(cicloalquilo C3-8), -(alquil C1-6)-S-arilo, -(alquil C1-6)-O-arilo, -(alquil C1-6)-S-heteroarilo o -(alquil C1-6)-O-heteroarilo; R3 representa -(alquilo C1-6) opcionalmente sustituido con uno o más grupos R11 o propargilo; R4 representa -(alquilo C1-6) opcionalmente sustituido con uno o más grupos R11, -(alquil C1-6)arilo, -(alquil C1-6)heteroarilo, -(alquil C1-6)heterociclilo, -(alquil C1-6) (cicloalquilo C3-8), -(cicloalquilo C3-8) opcionalmente sustituido con uno o más grupos seleccionados de R11 y alquilo C1-6, o propargilo; w y x representan independientemente un número entero de 0 a 2; R11 representa halógeno, hidroxi, -COOH, -COOCH3, alcoxi C1-6, ciano o amino; o una de sus sales o solvatos farmacéuticamente aceptables.
ARP020104587A 2001-11-30 2002-11-28 Compuesto de hidroxietileno, composicion farmaceutica que lo comprende, uso del mismo para la fabricacion de un medicamento y procedimiento para su preparacion AR037460A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0128748A GB0128748D0 (en) 2001-11-30 2001-11-30 Novel compounds
GB0214090A GB0214090D0 (en) 2002-06-18 2002-06-18 Novel compounds

Publications (1)

Publication Number Publication Date
AR037460A1 true AR037460A1 (es) 2004-11-10

Family

ID=26246821

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020104587A AR037460A1 (es) 2001-11-30 2002-11-28 Compuesto de hidroxietileno, composicion farmaceutica que lo comprende, uso del mismo para la fabricacion de un medicamento y procedimiento para su preparacion

Country Status (7)

Country Link
US (1) US6992103B2 (es)
EP (1) EP1448520A1 (es)
JP (1) JP2005514373A (es)
AR (1) AR037460A1 (es)
AU (1) AU2002365516A1 (es)
TW (1) TW200304374A (es)
WO (1) WO2003045913A1 (es)

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GB0314302D0 (en) * 2003-06-19 2003-07-23 Glaxo Group Ltd Novel compounds
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EP1673078B1 (en) * 2003-10-03 2008-05-28 Merck & Co., Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease
EP1694635A2 (en) * 2003-10-30 2006-08-30 Elan Pharmaceuticals, Inc. HYDROXYPROPYL AMIDES FOR THE TREATMENT OF ALZHEIMER’S DISEASE
PL1685142T3 (pl) 2003-11-11 2008-06-30 Hoffmann La Roche Pochodne kwasu fosfinowego, inhibitory beta-sekterazy do leczenia choroby Alzheimera
AU2004293416B2 (en) * 2003-11-24 2009-09-24 Merck & Co., Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of Alzheimer's disease
EP1697308B1 (en) * 2003-12-19 2014-03-19 Merck Sharp & Dohme Corp. Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease
JP2007533743A (ja) * 2004-04-20 2007-11-22 メルク　エンド　カムパニー　インコーポレーテッド アルツハイマー病治療のためのβ−セクレターゼ阻害薬として有用な１，３，５−置換フェニル誘導体化合物
ITTO20040343A1 (it) 2004-05-24 2004-08-24 Rotta Res Lab Spa Uso di neboglamine (cr2249) come neuropsicotico e neuroprotettivo
US7872009B2 (en) 2005-11-21 2011-01-18 Amgen Inc. Beta-Secretase modulators and methods of use
WO2007061670A1 (en) 2005-11-21 2007-05-31 Amgen Inc. Beta-secretase modulators and methods of use
US7838676B2 (en) * 2005-11-21 2010-11-23 Amgen Inc. Beta-secretase modulators and methods of use
US7745484B2 (en) * 2005-11-21 2010-06-29 Amgen Inc. Beta-secretase modulators and methods of use
EP2038264B1 (en) * 2006-06-29 2016-10-26 F.Hoffmann-La Roche Ag Tetrazole-substituted arylamides
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JP5539235B2 (ja) 2008-02-29 2014-07-02 エボテック・アーゲー アミド化合物、組成物およびそれらの使用
CN102209721A (zh) * 2008-09-11 2011-10-05 安姆根有限公司 作为β-分泌酶调节剂的螺四环化合物及其使用方法
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ES2450568T3 (es) 2010-03-15 2014-03-25 Amgen Inc. Compuestos espiero de amino-dihidrooxazina y amino-dihidrotiazina como moduladores de beta-secretasa y su uso médico
EP2547685A1 (en) 2010-03-15 2013-01-23 Amgen Inc. Spiro-tetracyclic ring compounds as beta - secretase modulators
EP2673279A1 (en) 2011-02-07 2013-12-18 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
EP2758406A1 (en) 2011-09-21 2014-07-30 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
EP2740474A1 (en) 2012-12-05 2014-06-11 Instituto Europeo di Oncologia S.r.l. Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a
US10233165B2 (en) 2014-05-30 2019-03-19 Istituto Europeo Di Oncologia S.R.L. Cyclopropylamine compounds as histone demethylase inhibitors
EP2949648A1 (en) 2014-05-30 2015-12-02 IEO - Istituto Europeo di Oncologia Srl Cyclopropylamine derivatives as histone demethylase inhibitors
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Also Published As

Publication number Publication date
US6992103B2 (en) 2006-01-31
JP2005514373A (ja) 2005-05-19
AU2002365516A1 (en) 2003-06-10
US20050085520A1 (en) 2005-04-21
WO2003045913A1 (en) 2003-06-05
TW200304374A (en) 2003-10-01
EP1448520A1 (en) 2004-08-25

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