Univerzita Palackeho V Olomouci

Ustav Experimentalni Botaniky Av Cr, V.v.i.

Biopatterns, S.r.o.

Palacky University Olomouc

Radek Jorda

Miroslav Strnad

Vladimir Krystof

Libor Havlicek

Antonin Sturc

Eva Reznickova

Karel Dolezal

Marek Zatloukal

Igor Popa

Tereza Radosova Muchova

Vladimir Divoky

Tomas Gucky

Tomas Pospisil

Stefan Zahler

Angelika Vollmar

Wolfgang Mikulits

Ladislava Vymetalova

5-alkylthio-7-[(4-arylbenzyl)amino]-1(2)H-pyrazolo[4,3-d]pyrimidine derivatives of formula I that are effective inhibitors of kinases and exhibit strong antiproliferative and proapoptotic properties on lymphoma cells. Derivatives in the treatment of blood hyperproliferative diseases, such as Non-Hodgkin lymphomas are also disclosed.

5-alkylthio-7-[(4-arylbenzyl)amino]-1(2)H-pyrazolo[4,3-d]pyrimidines for treatment of lymphoma

The present invention relates to novel 2,6-disubstituted-9-cyclopentyl-9H-purines of general formula I, capable of inhibiting the activity of kinases such as FLT3, CDKs and PDGFRs in cancer and other related proliferative diseases. The invention further includes pharmaceutical compositions containing the 2,6-disubstituted-9-cyclopentyl-9H-purines. Compounds of the present invention can be used as active ingredients of a pharmaceutical compositions for treating acute myeloid leukemia (AML).

2,6-disubstituted-9-cyclopentyl-9H-purines, use thereof as medicaments, and pharmaceutical compositions

5-substituted-7-[4-(2-pyridyl)phenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidines are potent inhibitors of protein kinases, especially cyclin-dependent kinases such as CDK2 and CDK5, and display antileukemic, pro-apoptotic, antiangiogenic and anticancer activities. The invention also relates to processes for their preparation, to pharmaceutical compositions and to their use as medicaments, particularly in the treatment of disorders involving cell proliferation, apoptosis, angiogenesis and inflammation, such as leukemia and metastatic solid cancer.

5-substituted 7- [4-(2-pyridyl)phenylmethylamino] -3-isopropylpyrazolo4,3-D]pyrimidine derivatives, use thereof as medicaments, and pharmaceutical compositions

The invention relates to substituted 6-(2-hydroxybenzylamino)purines of general formula I, to their activity as cyclin-dependent kinases 2, 5, 7 and 9 inhibitors and to their use as medicaments, particularly in the treatment of disorders involving cell proliferation or inflammation. The invention further includes pharmaceutical compositions containing the substituted 6-(2-hydroxybenzylamino)purines. 

Substituted 6-(2-hydroxybenzylamino)purine derivatives, their use as medicaments and compositions containing these derivatives

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Olomouc, Czechia

Radek Jorda