AR084444A1 - Oxindolpirimidinas bencilicas y las preparaciones farmaceuticas que las contienen - Google Patents

Oxindolpirimidinas bencilicas y las preparaciones farmaceuticas que las contienen

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Publication number
AR084444A1
AR084444A1 ARP110104829A ARP110104829A AR084444A1 AR 084444 A1 AR084444 A1 AR 084444A1 AR P110104829 A ARP110104829 A AR P110104829A AR P110104829 A ARP110104829 A AR P110104829A AR 084444 A1 AR084444 A1 AR 084444A1
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AR
Argentina
Prior art keywords
group
nrfc
nrere
nrcrc
alkyl
Prior art date
Application number
ARP110104829A
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English (en)
Inventor
Heather Tye
Stephan Karl Zahn
Patricia Amouzegh
Matthias Treu
Cristina Lecci
Original Assignee
Boehringer Ingelheim Int
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.)
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Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR084444A1 publication Critical patent/AR084444A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Son apropiados para el tratamiento de enfermedades que se caracterizan por proliferación celular excesiva o anormal, preparaciones farmacéuticas que contienen tales compuestos, así como su uso como medicamentos.Reivindicación 1: Oxindolpirimidinas bencílicas caracterizadas porque tienen la fórmula general (1), en la cual R5 está seleccionado del grupo compuesto por trifluorometilo y halógeno; R6, R7 y R8 están seleccionados cada uno, de modo independiente, del grupo compuesto por hidrógeno y alquilo C1-4 o R6 y R7 junto con el átomo de carbono al que están unidos forman un anillo hidrocarbonado de 3 - 5 miembros saturado; el sistema de anillos A está seleccionado del grupo compuesto por arilo C6-10, heterociclilo de 3 - 14 miembros y heteroarilo de 5 - 12 miembros; cada R9 están seleccionados cada uno, de modo independiente, del grupo compuesto por alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-5, halógeno y -CN; m representa 0, 1, 2 ó 3; L1 está seleccionado del grupo compuesto por un enlace, -(CH2)n-O-, -(CH2)n-NH-, -(CH2)n-NH-C(O)-, -(CH2)n-C(O)-NH-, -(CH2)n- y -(CH2)n-C(O)-, en donde en la presente forma de escritura el grupo ligador L1 se une a la derecha al sistema de anillos A; n representa 0, 1, 2 ó 3; el sistema de anillos B está seleccionado del grupo compuesto por heterociclilo saturado o insaturado de 4 - 10 miembros y fenilo; cada R10 están seleccionados cada uno, de modo independiente, del grupo compuesto por Ra y Rb; p representa 0, 1, 2 ó 3; cada Ra, en cada caso de manera independiente entre sí, es un radical, eventualmente sustituido con uno o varios Rb y/o Rc, iguales o diferentes, seleccionado del grupo consistente en alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquenilo C4-10, arilo C6-10, heteroarilo de 5 - 12 eslabones y heterociclilo de 3 - 14 eslabones; cada Rb está seleccionado cada uno, de modo independiente, del grupo compuesto por -ORc, -SRc, -NRcRc, halógeno, -CN, -NO2, -C(O)Rc, -C(O)ORc, -C(O)NRcRc, -C(NRf)NRcRc, -OC(O)Rc, -OC(O)ORc, -S(O)2Rc, -S(O)2NRcRc, -NRfC(O)Rc, -NRfC(O)ORc, -NRfC(O)NRcRc, -NRfC(NRf)NRcRc y -NRfS(O)2Rc, así como el sustituyente bivalente =O, en donde el último mencionado sólo puede ser sustituyente en sistemas de anillos no aromáticos; cada Rc, en cada caso de manera independiente entre sí, es hidrógeno o un radical, eventualmente sustituido con uno o varios Rd y/o Re, iguales o diferentes, seleccionado del grupo consistente en alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquenilo C4-10, arilo C6-10, heteroarilo de 5 - 12 eslabones y heterociclilo de 3 - 14 eslabones; cada Rd están seleccionados cada uno, de modo independiente, del grupo compuesto por -ORe, -SRe, -NReRe, halógeno, -CN, -NO2, -C(O)Re, -C(O)ORe, -C(O)NReRe, -C(NRf)NReRe, -OC(O)Re, -OC(O)ORe, -S(O)2Re, -S(O)2NReRe, -NRfC(O)Re, -NRfC(O)ORe, -NRfC(O)NReRe, -NRfC(NRf)NReRe y -NRfS(O)2Re, así como el sustituyente bivalente =O, en donde el último mencionado sólo puede ser sustituyente en sistemas de anillos no aromáticos; cada Re en cada caso de modo independiente entre sí son hidrógeno o un radical Rf eventualmente sustituido con uno o varios iguales o diferentes, seleccionado del grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, cicloalquenilo C4-10, arilo C6-10, heteroarilo de 5 - 12 miembros y heterociclilo de 3 - 14; y cada Rf está seleccionado cada uno, de modo independiente, del grupo compuesto por hidrógeno y alquilo C1-6; pudiendo presentarse los compuestos de fórmula (1) eventualmente también en forma de sus tautómeros, sus racematos, sus enantiómeros, sus diastereómeros o sus mezclas, o también como sales respectivas de todas las formas mencionadas en lo que antecede.
ARP110104829A 2010-12-21 2011-12-20 Oxindolpirimidinas bencilicas y las preparaciones farmaceuticas que las contienen AR084444A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10196277 2010-12-21
EP11189723 2011-11-18

Publications (1)

Publication Number Publication Date
AR084444A1 true AR084444A1 (es) 2013-05-15

Family

ID=45507665

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104829A AR084444A1 (es) 2010-12-21 2011-12-20 Oxindolpirimidinas bencilicas y las preparaciones farmaceuticas que las contienen

Country Status (6)

Country Link
US (1) US8546443B2 (es)
EP (1) EP2655358B1 (es)
JP (1) JP5809288B2 (es)
AR (1) AR084444A1 (es)
UY (1) UY33817A (es)
WO (1) WO2012085126A1 (es)

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Also Published As

Publication number Publication date
US20120329771A1 (en) 2012-12-27
JP2014500295A (ja) 2014-01-09
JP5809288B2 (ja) 2015-11-10
EP2655358B1 (en) 2014-11-19
UY33817A (es) 2012-07-31
EP2655358A1 (en) 2013-10-30
WO2012085126A1 (en) 2012-06-28
US8546443B2 (en) 2013-10-01

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