UY25279A1 - Un proceso para la preparacion de intermediarios de epotilona de anillo abierto utiles para la preparacion de analogos de epotilona - Google Patents

Un proceso para la preparacion de intermediarios de epotilona de anillo abierto utiles para la preparacion de analogos de epotilona

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Publication number
UY25279A1
UY25279A1 UY25279A UY25279A UY25279A1 UY 25279 A1 UY25279 A1 UY 25279A1 UY 25279 A UY25279 A UY 25279A UY 25279 A UY25279 A UY 25279A UY 25279 A1 UY25279 A1 UY 25279A1
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Uruguay
Prior art keywords
preparation
epotilone
formula
alkyl
analogs
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UY25279A
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English (en)
Inventor
Kim Soong-Hoon
M Borzilleri Robert
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Bristol Myers Squibb Co
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Publication of UY25279A1 publication Critical patent/UY25279A1/es

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    • C07D303/02—Compounds containing oxirane rings
    • C07D303/38—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • 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
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Abstract

La presente invención se refiere a un proceso para preparar compuestos de la fórmula (I), figura 1. Dichos compuestos son nuevos intermediarios para la preparación de análogos de la epotilona, útiles en el tratamiento de una variedad de cánceres y otras enfermedades proliferativas anormales. Los compuestos de la fórmula (I) pueden ser usados para preparar, por ejemplo, análogos de la fórmula (II), figura 2, que son agentes anticáncer. Un compuesto de la fórmula (II) en donde: Q es seleccionado del grupo de estructuras indicadas en la figura 3; R1, R2, R3, R4 y R5 son seleccionados del grupo H, alquilo, alquilo substituido, o arilo y en donde R1 y R2 son alquilo pueden ser unidos para formar un cicloalquilo; R6 se selecciona del grupo que consiste en H, alquilo, alquilo substituido, arilo, heteroarilo, cicloalquilo, o heterociclo; R7 es hidrógeno ó SO2R9. Se caracteriza porque comprende llevar a cabo una reacción de macrolactamización en un compuesto de la fórmula (I), en donde: X es NR7R8, N3, N(COR11)COR12 y NR9SO2R10; Q, R1, R2, R3, R4 y R5 son como se indico anteriormente; R6 y R7 son seleccionados del grupo que consiste en H, alquilo, alquilo substituido, arilo, cicloalquilo, o heterociclo. Por ejemplo: (1S-(1R*,3R*(E),7R*,10S*,11R*,12R*,16S*))-7,11-dihidroxi-8,8,10,12,16-pentametil-3-(1-metil-2-(2-metil-4-tiazolil)etenil)-4-aza-17-oxibiciclo(14.1.0)heptadecano-5,9-diona.
UY25279A 1997-12-04 1998-12-03 Un proceso para la preparacion de intermediarios de epotilona de anillo abierto utiles para la preparacion de analogos de epotilona UY25279A1 (es)

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US6755097P 1997-12-04 1997-12-04

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US (1) US6365749B1 (es)
EP (1) EP1035824A4 (es)
JP (1) JP2003522722A (es)
AR (1) AR017808A1 (es)
AU (1) AU739380B2 (es)
CA (1) CA2312098C (es)
PE (1) PE134099A1 (es)
UY (1) UY25279A1 (es)
WO (1) WO1999027890A2 (es)
ZA (1) ZA9810993B (es)

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