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AR076810A1 - Compuestos anticancerigenos de amino pirimidina - Google Patents

Compuestos anticancerigenos de amino pirimidina

Info

Publication number
AR076810A1
AR076810A1 ARP100101897A ARP100101897A AR076810A1 AR 076810 A1 AR076810 A1 AR 076810A1 AR P100101897 A ARP100101897 A AR P100101897A AR P100101897 A ARP100101897 A AR P100101897A AR 076810 A1 AR076810 A1 AR 076810A1
Authority
AR
Argentina
Prior art keywords
halogen
independently
optionally substituted
compounds
alkoxy
Prior art date
Application number
ARP100101897A
Other languages
English (en)
Original Assignee
Osi Pharm 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 Osi Pharm Inc filed Critical Osi Pharm Inc
Publication of AR076810A1 publication Critical patent/AR076810A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509Six-membered rings
    • C07F9/6512Six-membered rings having the nitrogen atoms in positions 1 and 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6544Six-membered rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Sus formulaciones, y su uso en el tratamiento de enfermedades con dichos compuestos, que abarcan tipos de cáncer mediados, al menos en parte, por FAK. Reivindicacion 1: Un compuesto de la Formula 1: donde: R1 es halogeno, -CF3 , o -CCH; por lo menos uno de Q2-Q4 es -C-X1-R2; Q1 y los restantes Q2-Q4 son, de manera independiente, CH, CF, N, o N-oxido; X1 y X2 son, de manera independiente, -(CR7R8)0-2-; cada R7 y R8 es, de modo independiente, halogeno, alifático C0-3, o -OalifáticoC0-3, cualquiera de los cuales está opcionalmente sustituido con halogeno, excepto que en el caso de X2, R7 y R8 no son halogeno u -OalifáticoC0-3; R6 es halogeno, -OalifáticoC0-3 o -alifáticoC0-3, cualquiera de los cuales está opcionalmente sustituido con uno o más halogeno o -OCF3 R2 es P(O)R9R10; R9 y R10 son, de modo independiente, alcoxi C0-3, cualquiera de los cuales pueden tomarse juntos en cualquiera de sus átomos a fin de formar un anillo, donde cualquiera de los anteriores puede estar adicionalmente sustituido con uno o más halogeno, alcoxi C0-3 o cíclico 3-6; R es un compuesto de la formula 2; uno de Q6, Q7, o A es -CR4; Q5 y los restantes Q6-Q7 y A son, de manera independiente, CH, CF, N, o N-oxido; R3 es alifático C0-6, -S(O)2R11, -S(O)2NR11R12, -C(O)NR11R12, -C(O)OR11 -NR11S(O)2R12, o -NR11R12; R11 y R12 son, de manera independiente, alquilo C0-6, y pueden tomarse juntos en cualquiera de sus átomos a fin de formar un anillo que contiene 1-3 heteroátomos; o, alternativamente, R3 y A definen cualquier cíclico 5-6 opcionalmente sustituido que contiene uno o más heteroátomos; R4 es cíclico4-6, alcoxi C0-6 o alifático C0-6, cada uno, opcionalmente sustituido; o halogeno; o una de sus sales farmacéuticamente aceptables.
ARP100101897A 2009-06-01 2010-05-31 Compuestos anticancerigenos de amino pirimidina AR076810A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18289809P 2009-06-01 2009-06-01
US29834910P 2010-01-26 2010-01-26

Publications (1)

Publication Number Publication Date
AR076810A1 true AR076810A1 (es) 2011-07-06

Family

ID=43298430

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101897A AR076810A1 (es) 2009-06-01 2010-05-31 Compuestos anticancerigenos de amino pirimidina

Country Status (18)

Country Link
US (2) US8399433B2 (es)
EP (1) EP2438056B1 (es)
JP (1) JP5718324B2 (es)
KR (1) KR20120034676A (es)
CN (1) CN102448955B (es)
AR (1) AR076810A1 (es)
AU (1) AU2010256865A1 (es)
BR (1) BRPI1013760A2 (es)
CA (1) CA2757083A1 (es)
EA (1) EA021801B1 (es)
ES (1) ES2655882T3 (es)
IL (1) IL215490A0 (es)
MX (1) MX2011012797A (es)
PL (1) PL2438056T3 (es)
PT (1) PT2438056T (es)
TW (1) TW201100441A (es)
WO (1) WO2010141406A2 (es)
ZA (1) ZA201108721B (es)

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Publication number Publication date
US20130231306A1 (en) 2013-09-05
MX2011012797A (es) 2012-01-27
EP2438056A4 (en) 2012-12-19
KR20120034676A (ko) 2012-04-12
WO2010141406A3 (en) 2011-04-21
AU2010256865A1 (en) 2011-11-03
US9096624B2 (en) 2015-08-04
WO2010141406A2 (en) 2010-12-09
BRPI1013760A2 (pt) 2016-04-05
IL215490A0 (en) 2011-12-29
PL2438056T3 (pl) 2018-03-30
TW201100441A (en) 2011-01-01
PT2438056T (pt) 2018-01-19
ZA201108721B (en) 2012-10-31
CN102448955B (zh) 2014-06-18
JP2012528864A (ja) 2012-11-15
US8399433B2 (en) 2013-03-19
US20110136764A1 (en) 2011-06-09
JP5718324B2 (ja) 2015-05-13
EP2438056A2 (en) 2012-04-11
EA021801B1 (ru) 2015-09-30
ES2655882T3 (es) 2018-02-22
CN102448955A (zh) 2012-05-09
CA2757083A1 (en) 2010-12-09
EA201171489A1 (ru) 2012-05-30
EP2438056B1 (en) 2017-12-20

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