JP2013503824A5 - - Google Patents

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JP2013503824A5
JP2013503824A5 JP2012527219A JP2012527219A JP2013503824A5 JP 2013503824 A5 JP2013503824 A5 JP 2013503824A5 JP 2012527219 A JP2012527219 A JP 2012527219A JP 2012527219 A JP2012527219 A JP 2012527219A JP 2013503824 A5 JP2013503824 A5 JP 2013503824A5
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mitotic checkpoint
compounds
schmidt
inhibition
pharmacological
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JP2012527219A
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JP2013503824A (ja
JP5728683B2 (ja
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Priority claimed from PCT/EP2010/005183 external-priority patent/WO2011026579A1/en
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異数性および腫瘍形成と不完全ではないが低下した有糸分裂チェックポイント機能とを関連づける十分な証拠がある[Weaver BA and Cleveland DW, Cancer Research, 2007, 67, 10103-5；King RW, Biochimica et Biophysica Acta, 2008, 1786, 4-14]。これに対して、有糸分裂チェックポイントの完全な阻害は、重度の染色体誤分配および腫瘍細胞におけるアポトーシスの誘導をもたらすと認識されている[Kops GJ et al., Nature Reviews Cancer, 2005, 5, 773-85；Schmidt M and Medema RH, Cell Cycle, 2006, 5, 159-63； Schmidt M and Bastians H, Drug Resistance Updates, 2007, 10, 162-81]。それ故に、有糸分裂チェックポイントのMps-1キナーゼまたは他の成分の薬理阻害による有糸分裂チェックポイントの停止は、固体腫瘍、例えば、癌腫および肉腫および白血病およびリンパ性悪性疾患または制御されていない細胞性増殖に関連する他の疾患をふくむ増殖性疾患の処置のための新規方法を示す。
しかしながら、上記した本分野の先行技術の記述には、後記“本発明の化合物”またはその薬理活性として本明細書に記述かつ規定したような本発明の一般式(Ｉ)の置換アミノキノキサリン化合物、またはその立体異性体、互変異性体、Ｎ-オキシド、水和物、溶媒和物または塩、あるいはそれらの混合物を記述したものはない。これは本発明の基礎を構成するものであり、本発明の該化合物は驚くべきかつ有利な特性を有するということが見出された。
様々なタイプの異性体を互いに限定するために、IUPAC Rules Section E (Pure Appl Chem 45, 11-30, 1976)を参照されたい。
JP2012527219A 2009-09-04 2010-08-24 チロシンスレオニンキナーゼ阻害剤としての置換アミノキノキサリン Expired - Fee Related JP5728683B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09075415.1 2009-09-04
EP09075415 2009-09-04
PCT/EP2010/005183 WO2011026579A1 (en) 2009-09-04 2010-08-24 Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors

Publications (3)

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JP2013503824A JP2013503824A (ja) 2013-02-04
JP2013503824A5 true JP2013503824A5 (ja) 2013-10-10
JP5728683B2 JP5728683B2 (ja) 2015-06-03

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JP2012527219A Expired - Fee Related JP5728683B2 (ja) 2009-09-04 2010-08-24 チロシンスレオニンキナーゼ阻害剤としての置換アミノキノキサリン

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US (1) US9340528B2 (ja)
EP (1) EP2473498A1 (ja)
JP (1) JP5728683B2 (ja)
CN (1) CN102596932A (ja)
CA (1) CA2772790C (ja)
WO (1) WO2011026579A1 (ja)

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