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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole 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)

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)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0314302D0 (en) * 2003-06-19 2003-07-23 Glaxo Group Ltd Novel compounds
ATE402921T1 (de) 2003-08-08 2008-08-15 Schering Corp Cyclische amine mit einem heterocyclischen substituenten als bace-1-inhibitoren
AU2004277981B2 (en) * 2003-10-03 2009-10-01 Merck & Co., Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of Alzheimer's disease
US20070225374A1 (en) * 2003-10-30 2007-09-27 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
WO2005051914A1 (en) * 2003-11-24 2005-06-09 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
AU2005236020A1 (en) * 2004-04-20 2005-11-03 Merck & Co., Inc. 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
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
US7745484B2 (en) * 2005-11-21 2010-06-29 Amgen Inc. Beta-secretase modulators and methods of use
JP5274258B2 (ja) 2005-11-21 2013-08-28 アムジエン・インコーポレーテツド β−セクレターゼ調節物質及び使用方法
US7838676B2 (en) 2005-11-21 2010-11-23 Amgen Inc. Beta-secretase modulators and methods of use
CA2654915C (en) * 2006-06-29 2015-07-28 F.Hoffmann-La Roche Ag Tetrazole-substituted arylamides
US20080277393A1 (en) * 2007-05-07 2008-11-13 True Charles W Collapsible, stackable, semi-rigid universal cotainer for hazardous and non-hazardous goods
US8163909B2 (en) 2007-05-25 2012-04-24 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
US8173810B2 (en) * 2007-05-25 2012-05-08 Amgen Inc. Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
US7803809B2 (en) 2008-11-12 2010-09-28 Amgen Inc. Substituted pyrano [2,3-b] pyridinamine compounds as beta-secretase modulators and methods of use
CA2715835C (en) 2008-02-29 2017-03-21 Renovis, Inc. Amide compounds, compositions and uses thereof
MX2011002705A (es) * 2008-09-11 2011-09-09 Amgen Inc Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso.
US20110237578A1 (en) 2008-09-18 2011-09-29 Zhi-Liang Wei Amide compounds, compositions and uses thereof
EP2504330A1 (en) 2009-11-23 2012-10-03 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
WO2011063233A1 (en) 2009-11-23 2011-05-26 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
WO2011090911A1 (en) 2010-01-19 2011-07-28 Amgen Inc. Amino heteroaryl compounds as beta-secretase modulators and methods of use
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.
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
WO2013044092A1 (en) 2011-09-21 2013-03-28 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
EP2949648A1 (en) 2014-05-30 2015-12-02 IEO - Istituto Europeo di Oncologia Srl Cyclopropylamine derivatives as histone demethylase inhibitors
BR112016028219B1 (pt) 2014-05-30 2022-12-06 Istituto Europeo Di Oncologia S.R.L Composto ou composição farmacêutica para uso no tratamento ou prevenção do câncer, de uma doença infecciosa, ou de uma doença designada por aberração de metabolismo de energia celular em um indivíduo, processo para obtenção de um composto de fórmula (i) e uso do composto ou composição farmacêutica na fabricação de um medicamento para uso no tratamento ou prevenção do câncer, de uma doença infecciosa, ou de uma doença designada por aberração de metabolismo de energia celular em um indivíduo
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
CN106699594B (zh) * 2016-12-29 2018-11-06 山东诚汇双达药业有限公司 一种碘普罗胺的制备方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5869024A (en) * 1989-11-29 1999-02-09 Bracco International B.V. Methods and compositions for using non-ionic contrast agents to reduce the risk of clot formation in diagnostic procedures
CA2029830A1 (en) * 1989-11-29 1991-05-30 Ramachandran S. Ranganathan Nonionic radiographic contrast agents
PL335484A1 (en) * 1997-02-26 2000-04-25 Pfizer Derivatives of heteroarylhexamide, their production and application as selective inhibitors of mip-1a being assimilated by its ccr1 receptor
US7119085B2 (en) * 2000-03-23 2006-10-10 Elan Pharmaceuticals, Inc. Methods to treat alzheimer's disease
NZ533107A (en) * 2001-11-08 2007-04-27 Upjohn Co N, N'-substituted-1,3-diamino-2-hydroxypropane derivatives

Also Published As

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

Similar Documents

Publication Publication Date Title
AR037460A1 (es) Compuesto de hidroxietileno, composicion farmaceutica que lo comprende, uso del mismo para la fabricacion de un medicamento y procedimiento para su preparacion
ATE397605T1 (de) Nebivolol und dessen pharmazeutisch unbedenkliche salze, herstellungsverfahren und pharmazeutische zusammensetzungen von nebivolol
NO20031331L (no) Substituerte amino-aza-cykloalkaner anvendelige mot malaria
NO20091892L (no) Krystallinsk form av (3S)-3-(N-(N`-(2-tert-butylfenyl)oksamyl) alaninyl)amino-5-(2`,3`,5`,6`-tetrafluorfenoksy)-4 oksopentanoisk syre
CR9314A (es) Derivado de espirocetal y uso del mismo como medicina para la diabetes
NO20056192L (no) Kapaseinhibitorer og anvendelse derav
NO20050741L (no) Ny fremgangsmate for syntesen og ny krystallinsk form av agomelatin og farmasoytiske sammensetninger inneholdende den
MY145075A (en) Tetrazole compounds and their use as metabotropic glutamate receptor antagonists.
IL151172A0 (en) Amine derivatives, their preparation and use as bax modulators
AR035320A1 (es) Compuestos activadores de hppardelta, composicion farmaceutica, su uso en la preparacion de medicamentos, metodo para el tratamiento de enfermedades mediadas por hppardelta
NO20023932D0 (no) Nye forbindelser
DK1263722T3 (da) Farmaceutiske sammensætninger, som indeholder azetidinderivat, nye azetidinderivater og fremstilling deraf
TN2010000026A1 (fr) Nouveaux derives de 6-triazolopyridazine-sulfanyl benzothiazole et benzimidazole, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de met
NO20070224L (no) 2-karbamid-4-fenyltiazolderivater, fremstilling og terapeutisk anvendelse derav
NO20090327L (no) Nye forbindelser 384
AR034268A1 (es) Compuestos derivados de piperidina, su uso en preparacion de medicamentos, composicion farmaceutica, metodo de tratamiento y proceso para su preparacion
UY29312A1 (es) Piperazin-1-carboxamidas n,4,sustituidas y sus derivados, composiciones que los contienen, procedimientos de preparación y aplicaciones
NO20052683L (no) Nye pyridopyrimidinonforbindelser, fremgangsmate for deres fremstilling og farmasoytiske sammensetninger inneholdende dem
SE0403171D0 (sv) New compounds
TW200740781A (en) Novel compounds
UY27424A1 (es) Agentes antidiabéticos
MXPA05011176A (es) Derivados de carboxamida como agentes antidiabeticos.
NO20034215D0 (no) Nye amider, fremstilling og terapeutisk anvendelse av modulatorer av CCR-reseptoraktivitet
HUP0300235A2 (hu) Heterociklikus oldalláncot tartalmazó, N-szubsztituált metalloproteáz inhibitorok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
SE0401763D0 (sv) Compounds

Legal Events

Date Code Title Description
FA Abandonment or withdrawal