DK2134374T3 - Btk-hæmmere til anvendelse ved behandling af kemoterapeutiske lægemiddelresistente epiteliale tumorer - Google Patents

Btk-hæmmere til anvendelse ved behandling af kemoterapeutiske lægemiddelresistente epiteliale tumorer Download PDF

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DK2134374T3
DK2134374T3 DK08717840T DK08717840T DK2134374T3 DK 2134374 T3 DK2134374 T3 DK 2134374T3 DK 08717840 T DK08717840 T DK 08717840T DK 08717840 T DK08717840 T DK 08717840T DK 2134374 T3 DK2134374 T3 DK 2134374T3
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btk
cells
gene
leu
tumour
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DK08717840T
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Marialuisa Lavitrano
Kristian Helin
Emanuela Grassilli
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Bionsil S R L In Liquidazione
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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Claims (8)

1. Isoleret protein af aminosyresekvensen SEQ ID NO:2, der koder for en BTK-proteinisoform.
2. Isoleret polynukleotid, der koder for det isolerede protein ifølge krav 1.
3. Polynukleotid ifølge krav 2 med sekvensen af det første exon svarende til SEQ ID NO:1
4. In-vitro-fremgangsmåde til reduktion af lægemiddelresistensen af tumorceller af den epiteliale type, hvilken fremgangsmåde omfatter trinnet med funktionelt og selektivt at blokere for et BTK-gen ved hjælp af: a. et oligonukleotidmolekyle af en lille interferens-RNA (siRNA); eller b. LFM-A13, hvor BTK-genet koder for en proteinisoform med en molekylvægt mellem 65 og 68 kDa af aminosyresekvensen SEQ ID NO:2
5. Fremgangsmåde ifølge krav 4, hvor tumorcellerne er stamceller.
6. Forbindelse, som funktionelt kan blokere for BTK-genet, til anvendelse ved formindskelsen af modstanden over for kemoterapeutiske lægemidler ved den terapeutiske behandling af epiteliale tumorpatologier, hvor forbindelsen er et oligonukleotidmolekyle af en lille interferens-RNA (siRNA) eller LFM-A13.
7. Farmaceutisk kit, omfattende et oligonukleotidmolekyle af en lille interferens-RNA (siRNA) eller LFM-A13, som funktionelt og selektivt kan blokere for et BTK-gen, og et kemoterapeutisk lægemiddel, valgt fra gruppen, bestående af 5-fluoruracil, oxaliplatin eller oxaliplatin i blanding med 5-fluoruracil, hvor kittet er til anvendelse ved behandlingen af epiteliale tumorpatologier.
8. Farmaceutisk kit til anvendelse ifølge krav 7, hvor de epiteliale tumorpatologier er valgt fra gruppen, bestående af colon-, bryst-, lunge- og ovarietumor.
DK08717840T 2007-03-14 2008-03-14 Btk-hæmmere til anvendelse ved behandling af kemoterapeutiske lægemiddelresistente epiteliale tumorer DK2134374T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ITPD20070088 ITPD20070088A1 (it) 2007-03-14 2007-03-14 Composti modulatori della resistenza farmacologica in cellule epiteliali tumorali
EP07106119 2007-04-13
PCT/EP2008/053099 WO2008110624A2 (en) 2007-03-14 2008-03-14 Sirna-mediated silencing of genes for treating chemotherapeutic drug-resistant epithelial tumors

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DK2134374T3 true DK2134374T3 (da) 2014-02-24

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US (6) US8232085B2 (da)
EP (3) EP2550976A3 (da)
JP (1) JP5832721B2 (da)
KR (1) KR101791981B1 (da)
CA (1) CA2680589A1 (da)
CY (1) CY1115141T1 (da)
DK (1) DK2134374T3 (da)
ES (1) ES2447868T3 (da)
HR (1) HRP20140160T1 (da)
PL (1) PL2134374T3 (da)
PT (1) PT2134374E (da)
RS (1) RS53165B (da)
SI (1) SI2134374T1 (da)
WO (1) WO2008110624A2 (da)

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ES2660418T3 (es) 2008-07-16 2018-03-22 Pharmacyclics Llc Inhibidores de la tirosina quinasa de Bruton para el tratamiento de tumores sólidos
US9095592B2 (en) * 2008-11-07 2015-08-04 The Research Foundation For The State University Of New York Bruton's tyrosine kinase as anti-cancer drug target
US20100261776A1 (en) * 2008-11-07 2010-10-14 The Research Foundation Of State University Of New York Bruton's tyrosine kinase as anti-cancer drug target
US8178307B2 (en) * 2009-09-02 2012-05-15 National Tsing Hua University Methods and compositions for detection of lethal cell and uses thereof
KR101580714B1 (ko) 2010-06-03 2016-01-04 파마싸이클릭스 엘엘씨 브루톤 티로신 인산화효소(ｂｔｋ)의 억제제의 용도
US20120040361A1 (en) * 2010-07-22 2012-02-16 National Tsing Hua University Methods and compositions for detection of lethal system and uses thereof
EP2729466B1 (en) 2011-07-08 2015-08-19 Novartis AG Novel pyrrolo pyrimidine derivatives
JP2014520863A (ja) 2011-07-13 2014-08-25 ファーマサイクリックス，インク． Ｂｒｕｔｏｎ型チロシンキナーゼの阻害剤
CN104704129A (zh) 2012-07-24 2015-06-10 药品循环公司 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变
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