MX2010011808A - Conjugados potentes y enlazadores hidrofilicos. - Google Patents

Conjugados potentes y enlazadores hidrofilicos.

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Publication number
MX2010011808A
MX2010011808A MX2010011808A MX2010011808A MX2010011808A MX 2010011808 A MX2010011808 A MX 2010011808A MX 2010011808 A MX2010011808 A MX 2010011808A MX 2010011808 A MX2010011808 A MX 2010011808A MX 2010011808 A MX2010011808 A MX 2010011808A
Authority
MX
Mexico
Prior art keywords
cell
linkers
hydrophilic linkers
binding
conjugates
Prior art date
Application number
MX2010011808A
Other languages
English (en)
Inventor
Singh Rajeeva
V J Chari Ravi
D Wilhelm Sharon
Kovtun Yalena
Original Assignee
Immunogen Inc
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 Immunogen Inc filed Critical Immunogen Inc
Publication of MX2010011808A publication Critical patent/MX2010011808A/es

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    • 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
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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    • 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
    • A61K31/537Heterocyclic 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 spiro-condensed or forming part of bridged ring systems
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    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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    • A61K47/6889Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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Abstract

Los enlazadores para enlazar fármacos a agentes de enlace celular son modificados para enlazadores hidrofílicos mediante la incorporación de un separador de polietilen glicol. La potencia o eficacia de los conjugados de agente de enlace celular-fármaco se mejora varias veces de modo sorprendente en una variedad tipos de célula de cáncer, que incluyen a aquellas que expresan un bajo número de antígenos en la superficie celular o células de cáncer que son resistentes a tratamiento.
MX2010011808A 2008-04-30 2009-04-30 Conjugados potentes y enlazadores hidrofilicos. MX2010011808A (es)

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