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AR083169A1 - Compuestos para tratar enfermedades neurodegenerativas - Google Patents

Compuestos para tratar enfermedades neurodegenerativas

Info

Publication number
AR083169A1
AR083169A1 ARP110103476A ARP110103476A AR083169A1 AR 083169 A1 AR083169 A1 AR 083169A1 AR P110103476 A ARP110103476 A AR P110103476A AR P110103476 A ARP110103476 A AR P110103476A AR 083169 A1 AR083169 A1 AR 083169A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
carbocycle
sulfanyl
alkoxycarbonyl
Prior art date
Application number
ARP110103476A
Other languages
English (en)
Inventor
Tony P Tang
Kevin W Hunt
Allen A Thomas
Original Assignee
Array Biopharma Inc
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 Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of AR083169A1 publication Critical patent/AR083169A1/es

Links

Classifications

    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61P25/28Drugs 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
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20Spiro-condensed systems

Landscapes

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

Abstract

Estos compuestos tricíclicos de la fórmula (1) que inhiben el clivaje de b-secretasa de APP son de utilidad como agentes terapéuticos para el tratamiento de enfermedades neurodegenerativas. Se reivindica el compuesto y composiciones farmacéuticas.Reivindicación 1: Un compuesto seleccionado de la fórmula (1) y sus estereoisómeros, diastereómeros, enantiómeros, tautómeros y sales farmacéuticamente aceptables, en donde: X1 está seleccionado de O, S, S(O), SO2, NR10 y CHR10; X2 está seleccionado de CR5R6, NR7 y O; X3 está seleccionado de CR8R9 y O; X4 está seleccionado de CR11 y N; X5 está seleccionado de CR12R13 y O, en donde dos de X2, X3 y X5 deben contener C; R1 está seleccionado de hidrógeno, alquilo, aralquilo, heteroarilo y heteroaralquilo; R2 y R3 están seleccionados, de modo independiente, de hidrógeno, halógeno y alquilo; R4 está seleccionado de hidrógeno, hidroxi, halógeno, amino, ciano, nitro, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, un carbociclo y un heterociclo, en donde dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, carbociclo y heterociclo están opcionalmente sustituidos con hidroxi, halógeno, amino, ciano, nitro, oxo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, sulfanilo, acilo, alcoxicarbonilo, haloalquilo o carbociclo opcionalmente sustituido; R5 y R6 están seleccionados, de modo independiente, de hidrógeno, hidroxi, halógeno, amino, ciano, nitro, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, un carbociclo y un heterociclo, en donde dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, carbociclo y heterociclo están opcionalmente sustituidos con hidroxi, halógeno, amino, ciano, nitro, oxo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, sulfanilo, acilo, alcoxicarbonilo, haloalquilo o carbociclo opcionalmente sustituido, o R5 y R6 tomados juntos forman un grupo oxo, o R5 y R6 junto con el átomo al que están unidos forman un carbociclo o heterociclo; R7 está seleccionado de hidrógeno, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, un carbociclo y un heterociclo, en donde dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, carbociclo y heterociclo están opcionalmente sustituidos con hidroxi, halógeno, amino, ciano, nitro, oxo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, sulfanilo, acilo, alcoxicarbonilo, haloalquilo o carbociclo opcionalmente sustituido; R8 y R9 están seleccionados, de modo independiente, de hidrógeno, hidroxi, halógeno, amino, ciano, nitro, alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, un carbociclo y un heterociclo, en donde dicho alquilo, alcoxi, acilo, aciloxi, alcoxicarbonilo, sulfonilo, sulfinilo, sulfanilo, ariloxi, carbociclo y heterociclo están opcionalmente sustituidos con hidroxi, halógeno, amino, ciano, nitro, oxo, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, sulfanilo, acilo, alcoxicarbonilo, haloalquilo o carbociclo opcionalmente sustituido, o R8 y R9 tomados juntos forman un oxo o grupo alquenilo, en donde el enlace doble del grupo alquenilo se une inmediatamente al átomos de carbono al que están unidos R8 y R9, o R8 y R9 junto con el átomo al que están unidos forman un carbociclo o heterociclo; R10 está seleccionado de hidrógeno, halógeno y alquilo; R11 está seleccionado de hidrógeno, halógeno y alquilo; y R12 y R13 están seleccionados, de modo independiente, de hidrógeno y alquilo.
ARP110103476A 2010-09-24 2011-09-23 Compuestos para tratar enfermedades neurodegenerativas AR083169A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US38629610P 2010-09-24 2010-09-24

Publications (1)

Publication Number Publication Date
AR083169A1 true AR083169A1 (es) 2013-02-06

Family

ID=45874425

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110103476A AR083169A1 (es) 2010-09-24 2011-09-23 Compuestos para tratar enfermedades neurodegenerativas

Country Status (5)

Country Link
US (1) US20120083501A1 (es)
AR (1) AR083169A1 (es)
TW (1) TW201219400A (es)
UY (1) UY33627A (es)
WO (1) WO2012040641A2 (es)

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RU2540424C2 (ru) 2007-10-02 2015-02-10 Теранос, Инк. Патрон для автоматического обнаружения аналита в пробе телесной жидкости и содержащая его система
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US8957083B2 (en) 2010-11-23 2015-02-17 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
US8415483B2 (en) 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
CN106323876B (zh) 2011-01-21 2020-02-14 西拉诺斯知识产权有限责任公司 样品使用最大化的系统和方法
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
WO2012112462A1 (en) 2011-02-15 2012-08-23 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
EP2694521B1 (en) 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2694489B1 (en) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
CA2844988A1 (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
US8840838B2 (en) 2011-09-25 2014-09-23 Theranos, Inc. Centrifuge configurations
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US20140170735A1 (en) 2011-09-25 2014-06-19 Elizabeth A. Holmes Systems and methods for multi-analysis
US9619627B2 (en) 2011-09-25 2017-04-11 Theranos, Inc. Systems and methods for collecting and transmitting assay results
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US8475739B2 (en) 2011-09-25 2013-07-02 Theranos, Inc. Systems and methods for fluid handling
US9664702B2 (en) 2011-09-25 2017-05-30 Theranos, Inc. Fluid handling apparatus and configurations
EP2758406A1 (en) 2011-09-21 2014-07-30 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9810704B2 (en) 2013-02-18 2017-11-07 Theranos, Inc. Systems and methods for multi-analysis
US9250229B2 (en) 2011-09-25 2016-02-02 Theranos, Inc. Systems and methods for multi-analysis
US10012664B2 (en) 2011-09-25 2018-07-03 Theranos Ip Company, Llc Systems and methods for fluid and component handling
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BR112014029597A2 (pt) 2012-05-30 2017-11-07 Comentis Inc compostos de cromano
US9000184B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000183B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000182B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab 2H-imidazol-4-amine compounds and their use as BACE inhibitors
US9000185B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cycloalkyl ether compounds and their use as BACE inhibitors
US10548882B2 (en) 2012-06-21 2020-02-04 Astrazeneca Ab Camsylate salt
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US11576900B2 (en) 2017-09-25 2023-02-14 Case Western Reserve University Compositions and methods of reducing serum cholesterol and PCSK9
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Also Published As

Publication number Publication date
WO2012040641A3 (en) 2012-06-07
TW201219400A (en) 2012-05-16
US20120083501A1 (en) 2012-04-05
WO2012040641A2 (en) 2012-03-29
UY33627A (es) 2013-04-30

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