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AR077488A1 - Compuestos heterociclicos nitrogenados inhibidores de autotaxina, medicamentos que los contienen y uso de los mismos para el tratamiento y/o prevencion de cancer y enfermedades tumorales. - Google Patents

Compuestos heterociclicos nitrogenados inhibidores de autotaxina, medicamentos que los contienen y uso de los mismos para el tratamiento y/o prevencion de cancer y enfermedades tumorales.

Info

Publication number
AR077488A1
AR077488A1 ARP100102610A ARP100102610A AR077488A1 AR 077488 A1 AR077488 A1 AR 077488A1 AR P100102610 A ARP100102610 A AR P100102610A AR P100102610 A ARP100102610 A AR P100102610A AR 077488 A1 AR077488 A1 AR 077488A1
Authority
AR
Argentina
Prior art keywords
hal
mono
cona2
so2a
nhcoa
Prior art date
Application number
ARP100102610A
Other languages
English (en)
Inventor
Wolfgang Staehle
Melanie Schultz
Kai Schiemann
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 AR077488A1 publication Critical patent/AR077488A1/es

Links

Classifications

    • 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
    • C07D487/04Ortho-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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C07D487/14Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Los compuestos de la formula (1), R es Hal, Ar o Het1, R1 es SO2A, COOA, COOH, Cyc, Het, Ar, COHet, CONHHet, CONHAr, CHO, CONH2, CONHA, CONA2, (CH2)n2OH, (CH2)n2OA, OAr, NHAr, A, Hal, (CH2)n2NH2, (CH2)n2NHA, (CH2)n2NA2 o NHCOA, R2 es H, (CH2)n3NH2, (CH2)n3NHA, (CH2)n3NA2, (CH2)n3OH, (CH2)n3OA, (CH2)n3Het2, CH2COHet2, CH2CONH2, CH2CONHA, CH2CONA2 o A, X, X1 son cada uno, de modo independiente entre sí, CO, CH(OH), CH(OA), CH(NH2), CH2 o CF2, Y, Y1 son cada uno, de modo independiente entre sí, CH o N, Q es C=O, COO, C=S, C=NH, CH(OH), CH(NH2), SO, SO2 o CF2; E es CO, CH(OH), CA(CH), CH(OA), CA(OA), CH(NH2), Alk, formula (3) o (4); Alk es alquileno lineal o ramificado C1-8, en donde uno o dos grupos CH2 pueden estar reemplazados por O y/o NH, n1 es 0, 1 o 2, n2 es 0, 1,2, 3 o 4, n3 es 1, 2, 3 o 4, Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHSO2A, SO2NH2 y/o SO2A, Het es un heterociclo saturado, insaturado o aromático mono-, bi- o tricíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, Het2, A, OH, OA, NH2, NHA, NA2, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHSO2A, SO2NH2, SO2A, NHCONH2, CHO, COA, =S, =NH, =NA y/o =O (oxígeno del carbonilo), Het1 es un heterociclo aromático mono-, di- o tricíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHSO2A, SO2NH2, SO2A, NHCONH2, CHO y/o COA, Het2 es pirrolidinilo, piperidinilo, tiazolidinilo, morfolinilo, oxazolidinilo, tetrahidroquinazolinilo, tetrahidropiranilo, piperazinilo, tiazolilo, furilo, tienilo, pirrolilo, imidazolilo, pirazolilo, oxazolilo, isoxazolilo, isotiazolilo, piridilo, pirimidinilo, triazolilo, tetrazolilo, oxadiazolilo o tiadiazolilo no sustituido o monosustituido con A, Cyc es alquilo cíclico C3-7, A es alquilo no ramificado o ramificado C1-10, en donde 1-7 átomos de H pueden estar reemplazados por F, Cl y/o Br, y/o en donde uno o dos grupos CH2 pueden estar reemplazados por O y/o NH, o es alquilo cíclico C3-7, Hal es F, Cl, Br o I, así como sus sales y estereoisomeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones, excluyendo los compuestos ôB1ö - ôB27ö, son inhibidores de autotaxina y se pueden utilizar para el tratamiento de tumores.
ARP100102610A 2009-07-16 2010-07-16 Compuestos heterociclicos nitrogenados inhibidores de autotaxina, medicamentos que los contienen y uso de los mismos para el tratamiento y/o prevencion de cancer y enfermedades tumorales. AR077488A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102009033392A DE102009033392A1 (de) 2009-07-16 2009-07-16 Heterocyclische Verbindungen als Autotaxin-Inhibitoren II

Publications (1)

Publication Number Publication Date
AR077488A1 true AR077488A1 (es) 2011-08-31

Family

ID=42646326

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100102610A AR077488A1 (es) 2009-07-16 2010-07-16 Compuestos heterociclicos nitrogenados inhibidores de autotaxina, medicamentos que los contienen y uso de los mismos para el tratamiento y/o prevencion de cancer y enfermedades tumorales.

Country Status (16)

Country Link
US (1) US20120115852A1 (es)
EP (1) EP2454258A1 (es)
JP (1) JP2012532901A (es)
KR (1) KR20120090031A (es)
CN (1) CN102471343A (es)
AR (1) AR077488A1 (es)
AU (1) AU2010272922A1 (es)
BR (1) BR112012000792A2 (es)
CA (1) CA2768095A1 (es)
DE (1) DE102009033392A1 (es)
EA (1) EA201200119A1 (es)
IL (1) IL217466A0 (es)
MX (1) MX2012000609A (es)
SG (1) SG177522A1 (es)
WO (1) WO2011006569A1 (es)
ZA (1) ZA201201124B (es)

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BR112018006034A2 (pt) 2015-09-24 2018-10-09 Hoffmann La Roche compostos bicíclicos como inibidores de atx
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Also Published As

Publication number Publication date
SG177522A1 (en) 2012-02-28
ZA201201124B (en) 2012-11-28
EA201200119A1 (ru) 2012-07-30
DE102009033392A1 (de) 2011-01-20
AU2010272922A1 (en) 2012-03-08
WO2011006569A1 (de) 2011-01-20
CN102471343A (zh) 2012-05-23
JP2012532901A (ja) 2012-12-20
BR112012000792A2 (pt) 2016-02-23
CA2768095A1 (en) 2011-01-20
IL217466A0 (en) 2012-02-29
KR20120090031A (ko) 2012-08-16
EP2454258A1 (de) 2012-05-23
US20120115852A1 (en) 2012-05-10
MX2012000609A (es) 2012-01-27

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