ECSP099755A - Derivados de pirrolopiridina y su uso como inhibidores de bace - Google Patents

Derivados de pirrolopiridina y su uso como inhibidores de bace

Info

Publication number
ECSP099755A
ECSP099755A EC2009009755A ECSP099755A ECSP099755A EC SP099755 A ECSP099755 A EC SP099755A EC 2009009755 A EC2009009755 A EC 2009009755A EC SP099755 A ECSP099755 A EC SP099755A EC SP099755 A ECSP099755 A EC SP099755A
Authority
EC
Ecuador
Prior art keywords
pirrolopiridine
derivatives
bace inhibitors
neurodegeneration
dementia
Prior art date
Application number
EC2009009755A
Other languages
English (en)
Inventor
Joerg Holenz
Laszlo Rakos
Didier Rotticci
Christopher William Murray
Gianni Chessari
Miles Stuart Congreve
Sahil Patel
Original Assignee
Astrazeneca Ab
Astex Therapeutics Ltd
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 Astrazeneca Ab, Astex Therapeutics Ltd filed Critical Astrazeneca Ab
Publication of ECSP099755A publication Critical patent/ECSP099755A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La invención se refiere a compuestos nuevos que tienen la siguiente fórmula estructural I: y a sus sales, composiciones y métodos de uso farmacéuticamente aceptables. Estos compuestos nuevos proporcionan un tratamiento o una profilaxis de un trastorno cognitivo, la enfermedad de Alzheimer, la neurodegeneración y la demencia.
EC2009009755A 2007-05-15 2009-11-23 Derivados de pirrolopiridina y su uso como inhibidores de bace ECSP099755A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US93800507P 2007-05-15 2007-05-15
US94800707P 2007-07-05 2007-07-05

Publications (1)

Publication Number Publication Date
ECSP099755A true ECSP099755A (es) 2009-12-28

Family

ID=40028127

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2009009755A ECSP099755A (es) 2007-05-15 2009-11-23 Derivados de pirrolopiridina y su uso como inhibidores de bace

Country Status (18)

Country Link
US (2) US20100324072A1 (es)
EP (1) EP2155749A1 (es)
JP (1) JP2010526879A (es)
KR (1) KR20100016534A (es)
CN (1) CN101796052A (es)
AR (1) AR066562A1 (es)
AU (1) AU2008287576A1 (es)
BR (1) BRPI0811542A2 (es)
CA (1) CA2687332A1 (es)
CO (1) CO6241108A2 (es)
EC (1) ECSP099755A (es)
IL (1) IL201836A0 (es)
MX (1) MX2009012168A (es)
PE (1) PE20090290A1 (es)
RU (1) RU2009143105A (es)
TW (1) TW200902499A (es)
UY (1) UY31084A1 (es)
WO (1) WO2009022961A1 (es)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
EP2032542A2 (en) 2006-06-12 2009-03-11 Schering Corporation Heterocyclic aspartyl protease inhibitors
TW200815349A (en) * 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
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.
US8958696B2 (en) * 2008-10-17 2015-02-17 Ciena Corporation Coherent augmented optical add-drop multiplexer
TW201020244A (en) * 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
US20100125081A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 574
US20100125087A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
WO2011002409A1 (en) * 2009-07-02 2011-01-06 Astrazeneca Ab 5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
AU2011263797B2 (en) 2010-06-09 2014-06-05 Janssen Pharmaceutica Nv 5,6-dihydro-2H-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (BACE)
WO2012019056A1 (en) 2010-08-05 2012-02-09 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
JP5834091B2 (ja) 2010-12-22 2015-12-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap ベータ−セクレターゼ(BACE)の阻害剤として有用な5,6−ジヒドロ−イミダゾ[1,2−a]ピラジン−8−イルアミン誘導体
ES2558779T3 (es) 2011-03-01 2016-02-08 Janssen Pharmaceutica, N.V. Derivados de 6,7-dihidro-pirazolo[1,5-a]piracin-4-ilamina útiles como inhibidores de ß-secretasa (BACE)
JP5853035B2 (ja) * 2011-03-09 2016-02-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap β−セクレターゼ(BACE)の阻害剤として有用な3,4−ジヒドロ−ピロロ[1,2−a]ピラジン−1−イルアミン誘導体
GB201212871D0 (en) 2012-07-20 2012-09-05 Eisai Ltd Novel compounds
WO2014127042A1 (en) 2013-02-12 2014-08-21 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
CA2912156C (en) 2013-06-12 2021-07-20 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
CA2911693C (en) 2013-06-12 2021-08-24 Janssen Pharmaceutica Nv 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
AU2014280124B2 (en) * 2013-06-12 2018-11-01 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (BACE)
EP3527569B1 (en) 2014-02-03 2021-08-25 Vitae Pharmaceuticals, LLC Dihydropyrrolopyridine inhibitors of ror-gamma for use in treating drye eye
WO2015188368A1 (en) 2014-06-13 2015-12-17 Merck Sharp & Dohme Corp. Pyrrolo[2,3-c]pyridines as imaging agents for neurofibrilary tangles
TWI675032B (zh) 2014-10-14 2019-10-21 美商維它藥物公司 ROR-γ之二氫吡咯并吡啶抑制劑
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
CA2967164A1 (en) 2014-12-18 2016-06-23 Janssen Pharmaceutica Nv 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase
ES2856931T3 (es) 2015-08-05 2021-09-28 Vitae Pharmaceuticals Llc Moduladores de ROR-gamma
EP3868750A1 (en) 2015-11-20 2021-08-25 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
TW202220968A (zh) 2016-01-29 2022-06-01 美商維它藥物有限責任公司 ROR-γ調節劑
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
MA49685A (fr) 2017-07-24 2021-04-14 Vitae Pharmaceuticals Llc INHIBITEURS DE ROR gamma

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4419849A1 (de) 1994-06-07 1995-12-14 Hoechst Ag Isoindolinpigmente
DE19516804A1 (de) 1995-05-08 1996-11-14 Hoechst Ag Isoindolinpigmente auf Basis von Aminochinoxalindionen
WO1999011643A1 (en) * 1997-09-02 1999-03-11 Du Pont Pharmaceuticals Company Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (crh) antagonists, useful for treating cns and stress-related disorders
TW200613272A (en) 2004-08-13 2006-05-01 Astrazeneca Ab Isoindolone compounds and their use as metabotropic glutamate receptor potentiators
CN101103034A (zh) * 2005-01-14 2008-01-09 惠氏公司 抑制β-分泌酶的氨基-咪唑酮
MX2007011234A (es) 2005-03-14 2007-11-12 Transtech Pharma Inc Derivados de benzazol, composiciones y metodos de uso en la forma de inhibidores de b-secretasa.
CN101228163A (zh) 2005-06-14 2008-07-23 先灵公司 天冬氨酰蛋白酶抑制剂
JP2008543844A (ja) 2005-06-14 2008-12-04 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
AR054510A1 (es) 2005-06-14 2007-06-27 Schering Corp Compuestos heterociclicos como inhibidores de aspartil proteasas y composiciones farmaceuticas que los comprenden.
MX2007016185A (es) * 2005-06-14 2008-03-07 Schering Corp Inhibidores de aspartil proteasa heterociclicos macrociclicos.
CA2610828A1 (en) * 2005-06-14 2006-12-28 Schering Corporation Heterocyclic aspartyl protease inhibitors, preparation and use thereof
US8211904B2 (en) 2005-07-18 2012-07-03 Merck, Sharp & Dohme Corp. Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
US7601751B2 (en) * 2005-09-01 2009-10-13 Bristol-Myers Squibb Company Indole acetic acid acyl guanidines as β-secretase inhibitors
EP2612854B1 (en) 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
ATE478070T1 (de) * 2005-10-27 2010-09-15 Schering Corp Heterozyklische aspartyl-proteasehemmer
EP1943246A1 (en) * 2005-10-31 2008-07-16 Schering Corporation Aspartyl protease inhibitors
TW200734311A (en) 2005-11-21 2007-09-16 Astrazeneca Ab New compounds
EP2032542A2 (en) 2006-06-12 2009-03-11 Schering Corporation Heterocyclic aspartyl protease inhibitors
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds

Also Published As

Publication number Publication date
CA2687332A1 (en) 2009-02-19
KR20100016534A (ko) 2010-02-12
US20090233945A9 (en) 2009-09-17
JP2010526879A (ja) 2010-08-05
EP2155749A1 (en) 2010-02-24
MX2009012168A (es) 2009-12-09
RU2009143105A (ru) 2011-06-20
AU2008287576A1 (en) 2009-02-19
US20080287462A1 (en) 2008-11-20
WO2009022961A1 (en) 2009-02-19
US20100324072A1 (en) 2010-12-23
US7629356B2 (en) 2009-12-08
CO6241108A2 (es) 2011-01-20
PE20090290A1 (es) 2009-04-09
CN101796052A (zh) 2010-08-04
IL201836A0 (en) 2010-06-16
UY31084A1 (es) 2009-01-05
TW200902499A (en) 2009-01-16
BRPI0811542A2 (pt) 2014-11-18
AR066562A1 (es) 2009-08-26

Similar Documents

Publication Publication Date Title
UY31084A1 (es) Compuestos de azaindol para la inhibicion de b-secretasa
ECSP088972A (es) Isoindoles sustituidos como inhibidores de bace y su uso
UY31083A1 (es) Derivados de sulfoximinas para la inhibicion de b-secretasa
ECSP088969A (es) Amino-imidazolones y su uso como medicamento para tratar deficiencias cognitivas, enfermedad de alzheimer, neurodegeneración y demencia
UY29927A1 (es) Derivados sustituidos de la 5-fenil-2-tioxo-imidazolin-4-ona y de la 5-fenil-2-amino-imidazolidin-4-ona y sus sales, composiciones y aplicaciones
UY29919A1 (es) Derivados sustituidos de 3,4-dihidroisoquinolin-1-amino-trifluoroacetato, sus composiciones farmacéuticas y aplicaciones
UY32730A (es) Inhibidores de cyp17
ECSP088970A (es) Amino-imidazolonas y su uso como medicamento para el tratamiento de la deficiencia cognitiva, la enfermedad de alzheimer, la neurodegeneración y la demencia
UA102251C2 (ru) Производные аминодигидротиазина как ингибиторы васе для лечения болезни альцгеймера
EA200800760A1 (ru) ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα
EA201200669A1 (ru) ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα
CL2012000033A1 (es) Compuestos n-(3-(4as,7as)-2-amino-4a,5,7,7a-tetrahidro-4h-furo[3,4-d][1,3] tiazin-7a-il)-4- fluorofenilo) -5-fluoropiconilamida, inhibidor de bace; composicion farmaceutica que los comprende, uso del compuesto para el tratamiento de la enfermedad de alzheimer.
MA37886A1 (fr) Nouvelles pyridinones bicycliques
UA107784C2 (en) Inhibitor of melanin production
UY30025A1 (es) Derivados sustituidos de las 2-amino-5,6-dihidro pirimidin-4(3h)-onas y sus sales farmacéuticamente aceptables, composiciones farmacéuticas conteniéndolos y aplicaciones.
DOP2011000134A (es) Lactamas como inhibidores de beta secretasa
ECSP11010830A (es) Derivados de heteroarilo como inhibidores de dgat1
DE602007011434D1 (de) 1h-indol-5-ylpiperazin-1-ylmethanonderivate
ATE449776T1 (de) Pyrroloä2,3-cüpyridinderivate
UY32852A (es) [4-(5-aminometil-fenil)-piperidin-1-il]-1h-indol-3-il]-metanonas disustituidas.
ATE546448T1 (de) Urotensin-ii-rezeptorantagonisten
NI201200103A (es) NUEVOS DERIVADOS ( HETEROCICLO - TETRAHIDRO - PIRIDIN ) - ( PIPERAZINIL ) - 1 - ALCANONA Y ( HETEROCICLO - DIHIDRO - PIRROLIDIN ) - ( PIPERAZINIL ) - 1 - ALCANONA Y SU UTILIZACIÓN COMO INHIBIDORES DE p75
ATE479691T1 (de) 4,5,6,7-tetrahydrothienoä2,3-cüpyridine als h3- modulatoren
UA96598C2 (ru) Замещенные изоиндолы как ингибиторы васе и их применение
ATE502947T1 (de) 4,5,6,7-tetrahydrothienoä3,2-cüpyridinderivate als h3-modulatoren