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New Conjugates, their Preparation and therapeutic Application
专利权人:
SANOFI - ADVENTIS
发明人:
BOUCHARD, HERVE,COMMERCON, ALAIN,BRUN, MARIE-PRISCILLE,ZHANG, JIDONG
申请号:
ECSP11011553
公开号:
ECSP11011553A
申请日:
2011.12.26
申请国别(地区):
EC
年份:
2012
代理人:
摘要:
The Invention relates to a selection of the target Agent is connected to at least one of criptoficina Derivative of formula (i), which represents a Halogen Atom, R1 and R2 represents an - Oh Group.An acyl Group of an amino acid or a derivative alcanoiloxi AA Group (C1 - C4); or R1 and R2 together form a reason epoxide; AA indicates a natural or non natural amino acid; R3 represents alkyl group (C1 - C6); R4 and R5 H represent the two together form a double Bond or CH = CH between C13 and C14; R6 and R7 represent independently of each other (H or an alkyl group (C1 - C6); R8 and R9 reprIndependently of each other esentan H or an alkyl group (C1 - C6); R10 represents at least a Substituent of the phenyl Nucleus chosen from: H, an Oh Group, alkoxy (c1-c4), a Halogen Atom, or a Group, - NH2,- nhalquilo (C1 - C6) or N (alkyl (C1 - C6); 2 R11 represents at least one of the core phenyl Substituent selected from H or an alkyl group (C1 - C4); being United, the selection of the target Agent and the Derivative of criptoficina covalently with the Union position orto (or target), or (m) For (P) of the phenyl NucleusLa invención se refiere a un agente de selección de la diana al que está unido al menos un derivado de criptoficina de la fórmula (I), en la que: R1 representa un átomo de halógeno y R2 representa un grupo -OH, un grupo acilo derivado de un aminoácido AA o un grupo alcanoiloxi(C1-C4); o bien R1 y R2 forman conjuntamente un motivo epóxido; AA indica un aminoácido natural o no natural; R3 representa un grupo alquilo(C1-C6); R4 y R5 representan los dos H o forman conjuntamente un doble enlace CH=CH entre C13 y C14; R6 y R7 representan independientemente uno de otro H o un grupo alquilo(C1-C6); R8 y R9 representan independientemente uno de otro H o un grupo alquilo(C1-C6); R10 representa al menos un sustituyente del núcleo fenilo elegido entre: H, un grupo OH, alcoxi(C1-C4), un átomo de halógeno o bien un grupo -NH2, -NHalquilo(C1-C6) o N(alquilo(C1-C6))2; R11 representa
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