DK2526934T3 - Hæmmere af Brutons tyrosinkinase - Google Patents

Hæmmere af Brutons tyrosinkinase Download PDF

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DK2526934T3
DK2526934T3 DK12166305.8T DK12166305T DK2526934T3 DK 2526934 T3 DK2526934 T3 DK 2526934T3 DK 12166305 T DK12166305 T DK 12166305T DK 2526934 T3 DK2526934 T3 DK 2526934T3
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Lee Honingberg
Zhengying Pan
Tarak Mody
Erik Verner
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Pharmacyclics Llc
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Claims (9)

1. Irreversibel Btk-hæmmer til anvendelse i behandlingen af kronisk lymfatisk leukæmi hvilken er af formel D:
Formula (D) hvor: La er CH2, O, NH eller S; Ar er en substitueret eller usubstitueret aryl, eller en substitueret eller usubstitueret heteroaryl; Y er en eventuelt substitueret gruppe valgt fra alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, og heteroaryl; Z er C(=0), 0C(=0), NHC(=0), C(=S), S(=0)x, 0S(=0)X eller NHS(=0)x, hvor x er 1 eller 2; R7 og Re er uafhængigt valgt fra H, usubstitueret Ci-C4alkyl, substitueret Ci-C4alkyl, usubstitueret Ci-C4heteroalkyl, substitueret Ci-C4heteroalkyl, usubstitueret Cs-Cecycloalkyl, substitueret Cs-Cecycloalkyl, usubstitueret C2-C6heterocycloalkyl, og substitueret C2-C6heterocycloalkyl; eller R7 og Re sammen danner en binding; R6 er H, substitueret eller usubstitueret Ci-C4alkyl, substitueret eller usubstitueret Ci-C4heteroalkyl, Ci-C6alkoxyalkyl, Ci-Csalkylaminoalkyl, substitueret eller usubstitueret C3-C6cycloalkyl, substitueret eller usubstitueret aryl, substitueret eller usubstitueret C2-C8heterocycloalkyl, substitueret eller usubstitueret heteroaryl, Ci-C4alkyl(aryl), Ci-C4alkyl(heteroaryl), Ci-C4alkyl(C3-C8cycloalkyl), eller Ci-C4alkyl(C2-Csheterocycloalkyl); eller et farmaceutisk acceptabelt salt deraf.
2. Irreversibel Btk-hæmmer ifølge krav 1 til anvendelse ifølge krav 1, hvor La er O.
3. Irreversibel Btk-hæmmer ifølge krav 1 til anvendelse ifølge krav 1, hvor Ar er phenyl.
4. Irreversibel Btk-hæmmer ifølge krav 1 hvor Z er CO, NHCO eller SO2.
5. Irreversibel Btk-hæmmer ifølge krav 1 til anvendelse ifølge krav 1, hvilken er l-((R)-3-(4-amino-3-(4-phenoxyphenyl)-lH-pyrazolo[3,4-d]pyrimidin-l-yl)piperidin-l-yl)prop-2-en-l-one eller et farmaceutisk acceptabelt salt deraf.
6. Irreversibel Btk-hæmmer ifølge krav 1 til anvendelse ifølge krav 1, hvilken er i kombination med et andet terapeutisk middel.
7. Irreversibel Btk-hæmmer ifølge et hvilket som helst foregående krav til anvendelse ifølge et hvilket som helst foregående krav ved oral administration.
8. Irreversibel Btk-hæmmer ifølge et hvilket som helst foregående krav til anvendelse ifølge et hvilket som helst foregående krav sammen med et yderligere anticancer middel.
9. Farmaceutisk sammensætning til anvendelse i behandling af kronisk lymfatisk leukæmi som omfatter en irreversibel Btk-hæmmer ifølge et hvilket som helst af kravene 1 til 6.
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