PE20160996A1 - Conjugados de farmacos anticuerpo (adcs) con inhibidores de ksp - Google Patents

Conjugados de farmacos anticuerpo (adcs) con inhibidores de ksp

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Publication number
PE20160996A1
PE20160996A1 PE2016000837A PE2016000837A PE20160996A1 PE 20160996 A1 PE20160996 A1 PE 20160996A1 PE 2016000837 A PE2016000837 A PE 2016000837A PE 2016000837 A PE2016000837 A PE 2016000837A PE 20160996 A1 PE20160996 A1 PE 20160996A1
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PE
Peru
Prior art keywords
binder
ksp
mod
alkyl
antibody
Prior art date
Application number
PE2016000837A
Other languages
English (en)
Inventor
Sandra Berndt
Grande Yolanda Cancho
Simone Greven
Nils Griebenow
Hans-Georg Lerchen
Sven Wittrock
Christoph Mahlert
Anette Sommer
Beatrix Stelte-Ludwig
Carsten Terjung
Mario Lobell
Original Assignee
Bayer Pharma AG
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Publication date
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of PE20160996A1 publication Critical patent/PE20160996A1/es

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    • C07K16/2875—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the NGF/TNF superfamily, e.g. CD70, CD95L, CD153, CD154
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Abstract

Se refiere a conjugados de acuerdo con la formula general BINDER–[L–[KSP]n]m, donde BINDER es un aglomerante (preferentemente un anticuerpo); L es un enlazante; KSP es un inhibidor de KSP (proteina de husillo de quinesina); m es 1 o 2; y n es un numero de 1 a 50. En un aspecto preferido, BINDER es un anticuerpo anti–TWEARK, o un anticuerpo anti–EGFR (cetuximab o nimotuzumab), entre otros; KSP es ispinesib, filanesib (ARRY–520), entre otros, y mas particularmente un compuesto de Formula (IIa) donde X1 es N, X2 es N y X3 es C; o X1 es N, X2 es C y X3 es N; o mas preferentemente X1 es CH, X2 es C y X3 es N, entre otros; R1 es H, –L–#1 o –MOD, entre otros; R2 H, –L–#1 o –MOD, entre otros; A es CO, SO, SO2, SO2NH o CNNH; R3 es –L–#1, –MOD o alquilo C1–C10, entre otros; R4 es H, –L–#1, –C(O)–CH2NH2, –CH2OH, –CH2NH2, entre otros; R5 es H, NH2, NO2, halogeno, CN; –L–#1, entre otros; R6 y R7 son independientemente H, CN, alquilo C1–10, entre otros; R8 es alquilo C1–10, alquenilo C2–10, alquinilo C2–10, entre otros; R9 es H, F, CH3, CF3, CH2F o CHF2; #1 es la union con el aglomerante; y MOD es –(NR10)n–(G1)o–G2–H, donde R10 es H o alquilo C1–3; G es –NHCO– o –CONH–, entre otros; n es 0 o 1; o es 0 o 1; y G2 es una cadena de hidrocarburo C1–10 que puede estar interrumpido una o mas veces por uno o mas de O, S, SO, SO2, NH, entre otros. Dichos conjugados son utiles para el tratamiento o prevencion de enfermedades hiperproliferativas y angiogenicas, como cancer
PE2016000837A 2013-12-23 2014-12-10 Conjugados de farmacos anticuerpo (adcs) con inhibidores de ksp PE20160996A1 (es)

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EP13199358 2013-12-23
EP14170585 2014-05-30

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EP (1) EP3086814B1 (es)
JP (1) JP6721507B2 (es)
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