AR051195A1 - Piridinas como inhibidores de plk - Google Patents

Piridinas como inhibidores de plk

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Publication number
AR051195A1
AR051195A1 ARP050103502A ARP050103502A AR051195A1 AR 051195 A1 AR051195 A1 AR 051195A1 AR P050103502 A ARP050103502 A AR P050103502A AR P050103502 A ARP050103502 A AR P050103502A AR 051195 A1 AR051195 A1 AR 051195A1
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AR
Argentina
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group
nr4c
nr8c
halogen
alkyl
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ARP050103502A
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English (en)
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Heinz Stadtmueller
Harald Engelhardt
Martin Steegmaier
Anke Baum
Ulrich Guertler
Andreas Schoop
Jens Juergen Quant
Flavio Solca
Rudolf Hauptmann
Ulrich Reiser
Stephan Karl Zahn
Lars Herfurth
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Boehringer Ingelheim Int
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Publication of AR051195A1 publication Critical patent/AR051195A1/es

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    • 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
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    • 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
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    • 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
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    • 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
    • C07D491/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Reivindicacion 1: Compuesto de la formula general (1), en los que significan: W es N o C-R2; X es -NR1a, O o S; Y es CH o N; Z es hidrogeno, halogeno, -NO2, alquiloC1-3-, alqueniloC2-3-, alquiniloC2-3-, halogen-alquiloC1-3-, -COH, -C(=O)-alquiloC1- 3, -C(=O)-alqueniloC2-3, -C(=O)-alquiniloC2-3, -C(=O)alquilC1-3-halogeno y pseudohalogeno; A es seleccionado de las formulas (2), (3) o (4); Q1 es compuestos arilo mono- o bicíclicos; B1, B2, B3 y B4 cada uno, de modo independiente entre sí, C-R9Rh, N-Ri, O o S; R1 y R1a cada uno, de modo independiente entre sí, hidrogeno o metilo; R2 es un radical seleccionado del grupo compuesto por hidrogeno, halogeno, -OR4, -C(=O)R4, -C(=O)NR4R5, -NR4R5, -NR4C(=O)R5, -NR4SO2R5, -N=CR4R5, -C=NRi, -SR4, - SOR4, -SO2R4, -SO2NR4R5 y pseudohalogeno, o un radical eventualmente mono- o polisustituido seleccionado del grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, arilo, heterociclilo y heteroarilo, en donde el o los sustituyen pueden ser iguales o diferentes y están seleccionados del grupo compuesto por halogeno, -NO2, -OR4, -C(=O)R4, -C(=O)OR4, -C(=O)NR4R5, -NR4R5, -NR4C(=O)R5, -NR4C(=O)OR5, -NR4C(=O)NR5R6, -NR4SO2R5, -N=CR4R5, -SR4, -SOR4, -SO2R4, -SO2NR4R5, - NR4SO2NR5R6, -OSO2NR5R6 y pseudohalogeno; Ra, Rb, Rc, Rd, Re, Rf, Rg y Rh cada uno, de modo independiente entre sí, un radical seleccionado del grupo compuesto por hidrogeno, halogeno, =O, -NO2, -OR4, -C(=O)R4, -C(=O)OR4, -C(=O)NR4R5, -NR4R5, - NR4C(=O)R5, -NR4C(=O)OR5, -NR4C(=O)NR5R6, -NR4SO2R5, -N=CR4R5, -C=NRi, -SR4, -SOR4, -SO2R4, -SO2NR4R5, -NR4SO2NR5R6, -OSO2NR5R6 y pseudohalogeno; o un radical eventualmente mono- o polisustituido seleccionado del grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, arilo, heterociclilo y heteroarilo, en donde el o los sustituyen pueden ser iguales o diferentes y están seleccionados del grupo compuesto por halogeno, R8, -NO2, -OR4, -C(=O)R4, -C(=O)OR4, - C(=O)NR4R5, -NR4R5, -NR4C(=O)R5, -NR4C(=O)OR5, -NR4C(=O)NR5R6, -NR4SO2R5, -N=CR4R5, -SR4, -SOR4, -SO2R4, -SO2NR4R5, -NR4SO2NR5R6, -OSO2NR5R6 y pseudohalogeno; o eventualmente Rg y Rh que se hallan en los mismos o en átomos de C adyacentes pueden estar unidos en cualquier combinacion con un puente de alquilo comun de 3-5 miembros saturado o parcialmente insaturado, que eventualmente puede contener uno a dos heteroátomos; Rf un radical seleccionado del grupo compuesto por hidrogeno, =O, -OR4, -C(=O)R4, -C(=O)OR4, -C(=O)NR4R5, -NR4R5, -NR4C(=O)R5, -NR4C(=O)OR5, -NR4C(=O)NR5R6, -NR4SO2R5, -N=CR4R5, -SR4, -SOR4, -SO2R4, -SO2NR4R5, -NR4SO2NR5R6, -OSO2NR5R6 o un radical eventualmente mono- o polisustituido seleccionado del grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, arilo, heterociclilo y heteroarilo, en donde el o los sustituyen pueden ser iguales o diferentes y están seleccionados del grupo compuesto por halogeno, R8, -NO2, -OR4, -C(=O)R4, - C(=O)OR4, -C(=O)NR4R5, -NR4R5, -NR4C(=O)R5, -NR4C(=O)OR5, -NR4C(=O)NR5R6, -NR4SO2R5, -N=CR4R5, -SR4, -SOR4, -SO2R4, -SO2NR4R5, -NR4SO2NR5R6, -OSO2NR5R6 y pseudohalogeno; o eventualmente los Ri que se hallan en átomos de N adyacentes pueden estar unidos entre sí o Ri con Rg o Rh que se hallan en átomos de C adyacentes en cualquier combinacion con un puente de alquilo comun de 3-5 miembros saturado o parcialmente insaturado, que puede contener uno a dos heteroátomos; R3 está seleccionado de las formulas (5)-(11); R4, R5 y R6 cada uno, de modo independiente entre sí, hidrogeno o un radical seleccionado del grupo compuesto por alquilo C1-5, alquenilo C2-5, alquinilo C2-5, cicloalquilo C3-10, arilo, heterociclilo y heteroarilo eventualmente mono- o polisustituido, en donde el o los sustituyentes pueden ser iguales o diferentes y están seleccionados del grupo compuesto por cicloalquilo C3-10, arilo, heterociclilo, heteroarilo, halogeno, -NO2, -OR8, -C(=O)R8, -C(=O)OR8, - C(=O)NR8R9, -NR8R9, -NR8C(=O)R9, -NR8C(=O)OR9, -NR8C(=O)NR9R10, -NR8C(=O)ONR9R10, -NR8SO2R9, -N=CR8R9, -SR8, -SOR8, -SO2R8, -SO2NR8R9, -NR8SO2NR9R10, -OSO2NR8R9 y pseudohalogeno; L es un enlace o un radical seleccionado del grupo compuesto por alquilo C1-16, alquenilo C2-16, alquinilo C2-16, cicloalquilo C3-10, arilo, heterociclilo y heteroarilo eventualmente mono- o polisustituido, en donde el o los sustituyentes pueden ser iguales o diferentes y están seleccionados del grupo compuesto por halogeno, -NO2, -NR2, -OR8, -C(=O)R8, -C(=O)OR8, -C(=O)NR8R9, -NR8R9, -NR8C(=O)R9, -NR8C(=O)OR9, -NR8C(=O)NR9R10, -NR8C(=O)ONR9R10, -NR8SO2R9, -N=CR8R9, -SR8, -SOR8, -SO2R8, -SO2NR8R9, -NR8SO2NR9R10, -OSO2NR8R9 y pseudohalogeno; Q2 y Q3 cada uno, de modo independiente entre sí, un enlace o un radical seleccionado del grupo compuesto eventualmente por alquilo C1-16, alquenilo C2-16, alquinilo C1-16, cicloalquilo C3-10, arilo, heterociclilo y heteroarilo, en donde el o los sustituyentes pueden ser iguales o diferentes y están seleccionados del grupo compuesto por halogeno, -NO2, -OR8 -C(=O)R8 -C(=O)OR8 -C(=O)NR8R9-, NR8R9, -NR8C(=O)R9, -NR8C(=O)OR9, -NR8C(=O)NR8R10, -NR8C(=O)ONR9R10, -NR8SO2R9, -N=CR8R9, -SR8, -SOR8, -SO2R8, - SO2NR8R9, -NR8SO2NR9R10, -OSO2NR8R9 y pseudohalogeno; R7 es hidrogeno o un radical seleccionado del grupo compuesto por alquilo C1-16, alquenilo C2-16, alquinilo C2-16, cicloalquilo C3-10, arilo, heterociclilo y heteroarilo eventualmente mono- o polisustituido, en donde el o los sustituyentes pueden ser iguales o diferentes y están seleccionados del grupo compuesto por halogeno-, NO2, -OR8, -C(=O)R8, -C(=O)OR8, -C(=O)NR8R9, -NR8R9, -NR8COR9, -NR8C(=O)OR9, -NR8C(=O)NR9R10, -NR8C(=O)ONR9R10, - NR8SO2R9, -N=CR8R9, -SR8, -SOR8, -SO2R8, -SO2NR8R9, -NR8SO2NR9R10, -OSO2NR8R9 y pseudohalogeno; R8, R9 y R10 cada uno, de modo independiente entre sí, hidrogeno o un radical seleccionado del grupo compuesto por alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-10, arilo, heterociclilo y heteroarilo eventualmente sustituido, en donde el o los sustituyentes pueden ser iguales o diferentes y están seleccionados del grupo compuesto por halogeno, metilo, etilo, amino, metilamino, dimetilamino, -OH y pseudohalogeno; eventualmente en forma de sus tautomeros, sus racematos, sus enantiomeros, sus diastereoisomeros y sus mezclas, así como eventualmente de sus sales por adicion de ácidos farmacologicamente inocuas.
ARP050103502A 2004-08-20 2005-08-22 Piridinas como inhibidores de plk AR051195A1 (es)

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TW200804364A (en) * 2006-02-22 2008-01-16 Boehringer Ingelheim Int New compounds
EP2007754A1 (en) * 2006-04-10 2008-12-31 Boehringer Ingelheim International GmbH 2, 4-diaminopyrimidine derivatives and their use for the treatment of cancer
US8623887B2 (en) * 2006-05-15 2014-01-07 Boehringer Ingelheim International Gmbh Compounds
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