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AR073551A1 - Pirimidinas macrociclicas como inhibidores de proteina cinasa - Google Patents

Pirimidinas macrociclicas como inhibidores de proteina cinasa

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Publication number
AR073551A1
AR073551A1 ARP090103426A ARP090103426A AR073551A1 AR 073551 A1 AR073551 A1 AR 073551A1 AR P090103426 A ARP090103426 A AR P090103426A AR P090103426 A ARP090103426 A AR P090103426A AR 073551 A1 AR073551 A1 AR 073551A1
Authority
AR
Argentina
Prior art keywords
independently
aryl
compounds
heteroaryl
bridge
Prior art date
Application number
ARP090103426A
Other languages
English (en)
Inventor
Benny C Askew
Andreas Goutopoulos
Henry Yu
Selm Lizbeth Celeste De
Xuliang Jiang
Srinivasa R Karra
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR073551A1 publication Critical patent/AR073551A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • A61P5/00Drugs for disorders of the endocrine 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D515/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/08Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Se proporcionan compuestos derivados macrocíclicos que inhiben las enzimas proteína cinasa junto con composiciones farmacéuticas que comprenden estos compuestos y métodos para sintetizar los mismos. Dichos compuestos tienen utilidad en el tratamiento de enfermedades proliferativas que resultan de una actividad de cinasa no regulada y/o alterada tales como cánceres, psoriasis, infecciones virales y bacterianas, y enfermedades inflamatorias y autoinmunitarias. Reivindicacion 1: Un compuesto de la formula (1) caracterizado porque: X es H; halogeno; preferiblemente F; CF3 CN, NO2, N(RR'), C(O)N(RR'); C(O)OR; C(O)H; S(O)2; S(OH); S(O); o S(O)NRR'; Los anillos A y B, cada uno independientemente es arilo, un heterociclo saturado o insaturado o un unicarbociclo, bicarbociclo o tricarbociclo saturado o insaturado, que forma un puente o que no forma un puente, cualquiera de los cuales opcionalmente puede estar sustituido; ---------- representa la presencia o ausencia de un enlace doble; L1, L2, L2', L2ö, L2'ö y L3, cada uno independientemente es CH2, CH, CH(OH); C(=O), O, S, S(O), S(OH), S(O)2, NR2 o NH; R y R', cada uno independientemente es H, alquilo C1-6, heteroalquilo C1-6, arilo; heteroarilo; heterociclo; (CH2)2OH, (CH2)2-O-(CH2)2-; (CH2)2-NH2; (CH2)2NRx o (CH2)2-Ry, en donde Rx, y Ry, cada uno independientemente es CH3 o C2F5; R2 es arilo, heteroarilo o alquilo; n, p y q, cada uno independientemente, es 0 o 1; r es 0, 1, 2, 3 o 4; o una sal, profármaco, hidrato, solvato, tautomero, enantiomero o mezcla racémica farmacéuticamente aceptable de los mismos.
ARP090103426A 2008-09-08 2009-09-07 Pirimidinas macrociclicas como inhibidores de proteina cinasa AR073551A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19150508P 2008-09-08 2008-09-08

Publications (1)

Publication Number Publication Date
AR073551A1 true AR073551A1 (es) 2010-11-17

Family

ID=41403411

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090103426A AR073551A1 (es) 2008-09-08 2009-09-07 Pirimidinas macrociclicas como inhibidores de proteina cinasa

Country Status (14)

Country Link
US (1) US8815872B2 (es)
EP (1) EP2334301B1 (es)
JP (1) JP5749645B2 (es)
KR (1) KR20110073500A (es)
CN (1) CN102143750B (es)
AR (1) AR073551A1 (es)
AU (1) AU2009288021B2 (es)
CA (1) CA2735420C (es)
EA (1) EA201100450A1 (es)
ES (1) ES2668834T3 (es)
IL (1) IL211584A (es)
MX (1) MX2011002470A (es)
WO (1) WO2010028116A1 (es)
ZA (1) ZA201101243B (es)

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US9073944B2 (en) 2012-02-21 2015-07-07 Merck Patent Gmbh Cyclic diaminopyrimidine derivatives
ES2621220T3 (es) * 2012-03-06 2017-07-03 Pfizer Inc. Derivados macrocíclicos para el tratamiento de enfermedades proliferativas
WO2014008636A1 (en) * 2012-07-11 2014-01-16 Merck Sharp & Dohme Corp. Macrocyclic compounds as hiv integrase inhibitors
LT2953952T (lt) * 2013-02-07 2017-08-25 Merck Patent Gmbh Makrocikliniai piridazinono dariniai
WO2015112806A2 (en) * 2014-01-24 2015-07-30 Tp Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
TWI736134B (zh) * 2014-09-11 2021-08-11 美商特普醫葯公司 作為蛋白質激酶之調節劑的二芳基巨環
ES2864839T3 (es) 2015-07-02 2021-10-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales como moduladores de proteína quinasas
ES2979111T3 (es) * 2015-07-06 2024-09-24 Turning Point Therapeutics Inc Polimorfo de macrociclo de diarilo
MX383823B (es) * 2015-07-21 2025-03-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales y usos de los mismo.
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TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
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Publication number Publication date
AU2009288021B2 (en) 2015-06-18
US8815872B2 (en) 2014-08-26
ZA201101243B (en) 2012-05-30
EP2334301A1 (en) 2011-06-22
AU2009288021A1 (en) 2010-03-11
KR20110073500A (ko) 2011-06-29
ES2668834T3 (es) 2018-05-22
CN102143750B (zh) 2014-04-02
CN102143750A (zh) 2011-08-03
IL211584A (en) 2017-04-30
JP5749645B2 (ja) 2015-07-15
HK1158947A1 (en) 2012-07-27
WO2010028116A1 (en) 2010-03-11
US20110294801A1 (en) 2011-12-01
CA2735420A1 (en) 2010-03-11
MX2011002470A (es) 2011-04-05
EA201100450A1 (ru) 2011-10-31
JP2012502043A (ja) 2012-01-26
CA2735420C (en) 2016-06-28
EP2334301B1 (en) 2018-02-14

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