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PE20070121A1 - 2,4-diamino-pirimidinas como inhibidores de aurora - Google Patents

2,4-diamino-pirimidinas como inhibidores de aurora

Info

Publication number
PE20070121A1
PE20070121A1 PE2006000752A PE2006000752A PE20070121A1 PE 20070121 A1 PE20070121 A1 PE 20070121A1 PE 2006000752 A PE2006000752 A PE 2006000752A PE 2006000752 A PE2006000752 A PE 2006000752A PE 20070121 A1 PE20070121 A1 PE 20070121A1
Authority
PE
Peru
Prior art keywords
methyl
cyclohexil
ilamino
trifluormethyl
phenylamine
Prior art date
Application number
PE2006000752A
Other languages
English (en)
Inventor
Stephan Zahn
Guido Boehmelt
Ulrich Reiser
Ulrich Guertler
Flavio Solca
Ralph Brueckner
Lars Herfurth
Heinz Stadtmueller
Harald Engelhardt
Oliver Kraemer
Charlotte Reither
Ulrike Tontsch-Grunt
Andreas Schoop
Matthias Treu
Andreas Mantoulidis
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.)
Filing date
Publication date
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20070121A1 publication Critical patent/PE20070121A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • C07D401/14Heterocyclic 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
    • 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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

Landscapes

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

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 ES CICLOALQUILO C3-C10 Y HETEROCICLOALQUILO DE 3 A 8 MIEMBROS SUSTITUIDO CON R5 Y R4, DONDE R4 ES Ra OPCIONALMENTE SUSTITUIDO O Rb, EN DONDE Ra ES ALQUILO(C1-C6), CICLOALQUILO(C3-C10), ARILO(C6-C10), ENTRE OTROS; Rb ES =O, HALOALQUILOXI(C1-C3), OCF3, ENTRE OTROS; R5 ES C(O)Rc, C(O)NRcRc, S(O)2Rc, ENTRE OTROS, DONDE Rc ES ALQUILO(C1-C6), CICLOALQUILO(C3-C10), CICLOALQUILALQUILO(C4-C11) OPCIONALMENTE SUSTITUIDOS, ENTRE OTROS; R2 ES ALQUILO(C1-C6), CICLOALQUILO(C3-C10), ARILO(C6-C15) OPCIONALMENTE SUSTITUIDOS CON R4, ENTRE OTROS; R3 ES H, HALOGENO, CN, NO2, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ( )-N-((1S*,2R*)-2- 2-[4-(4-METIL-PIPERAZIN-1-CARBONIL)-FENILAMINO]-5-TRIFLUORMETIL-PIRIMIDIN-4-ILAMINO -CICLOHEXIL)-ACETAMIDA, ( )-1-METIL-3-((1S*,2R*)-2- 2-[4-(4-METIL-PIPERAZIN-1-CARBONIL)-FENILAMINO]-5-TRIFLUORMETIL-PIRIMIDIN-4-ILAMINO -CICLOHEXIL)-UREA, ESTER METILICO DE ACIDO (( )-(1S*,2R*)-2- 2-[4-(4-METIL-PIPERAZIN-1-CARBONIL)-FENILAMINO]-5-TRIFLUORMETIL-PIRIMIDIN-4-ILAMINO -CICLOHEXIL)-CARBAMICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE QUINASAS DE CICLO CELULAR ESPECIFICA TAL COMO LAS AURORAS SIENDO UTILES EN EL TRATAMIENTO DE CANCER
PE2006000752A 2005-07-01 2006-06-28 2,4-diamino-pirimidinas como inhibidores de aurora PE20070121A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05106007 2005-07-01

Publications (1)

Publication Number Publication Date
PE20070121A1 true PE20070121A1 (es) 2007-03-05

Family

ID=35431858

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006000752A PE20070121A1 (es) 2005-07-01 2006-06-28 2,4-diamino-pirimidinas como inhibidores de aurora

Country Status (30)

Country Link
US (3) US20070032514A1 (es)
EP (1) EP1902037B1 (es)
JP (1) JP5179357B2 (es)
KR (1) KR20080031362A (es)
CN (1) CN101213179A (es)
AR (1) AR057423A1 (es)
AT (1) ATE441639T1 (es)
AU (1) AU2006264958B2 (es)
BR (1) BRPI0613096A2 (es)
CA (1) CA2613664A1 (es)
CY (1) CY1109644T1 (es)
DE (1) DE502006004750D1 (es)
DK (1) DK1902037T3 (es)
EA (1) EA016358B1 (es)
EC (1) ECSP078060A (es)
ES (1) ES2330045T3 (es)
IL (1) IL188452A (es)
MX (1) MX2007015992A (es)
MY (1) MY142496A (es)
NO (1) NO20076059L (es)
NZ (1) NZ565475A (es)
PE (1) PE20070121A1 (es)
PL (1) PL1902037T3 (es)
PT (1) PT1902037E (es)
SI (1) SI1902037T1 (es)
TW (1) TWI369351B (es)
UA (1) UA92355C2 (es)
UY (1) UY29636A1 (es)
WO (1) WO2007003596A1 (es)
ZA (1) ZA200709763B (es)

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Also Published As

Publication number Publication date
PL1902037T3 (pl) 2010-02-26
CA2613664A1 (en) 2007-01-11
UA92355C2 (en) 2010-10-25
BRPI0613096A2 (pt) 2010-12-21
EA016358B1 (ru) 2012-04-30
ATE441639T1 (de) 2009-09-15
MX2007015992A (es) 2008-03-07
DE502006004750D1 (de) 2009-10-15
US20130281429A1 (en) 2013-10-24
US20070032514A1 (en) 2007-02-08
JP2008544972A (ja) 2008-12-11
AU2006264958A1 (en) 2007-01-11
TW200726753A (en) 2007-07-16
JP5179357B2 (ja) 2013-04-10
EP1902037A1 (de) 2008-03-26
DK1902037T3 (da) 2009-12-21
KR20080031362A (ko) 2008-04-08
NZ565475A (en) 2010-01-29
AR057423A1 (es) 2007-12-05
ES2330045T3 (es) 2009-12-03
UY29636A1 (es) 2007-01-31
ZA200709763B (en) 2008-12-31
IL188452A (en) 2012-02-29
PT1902037E (pt) 2009-10-13
WO2007003596A1 (de) 2007-01-11
SI1902037T1 (sl) 2010-01-29
NO20076059L (no) 2008-01-30
AU2006264958B2 (en) 2012-05-03
CN101213179A (zh) 2008-07-02
IL188452A0 (en) 2008-04-13
MY142496A (en) 2010-11-30
ECSP078060A (es) 2008-01-23
US20110251174A1 (en) 2011-10-13
EA200800172A1 (ru) 2008-08-29
TWI369351B (en) 2012-08-01
EP1902037B1 (de) 2009-09-02
CY1109644T1 (el) 2014-08-13

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