Univerzita Palackeho V Olomouci

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

Institute of Experimental Botany

Biopatterns, S.r.o.

Institute of Experimental Botany Ascr

Palacky University Olomouc

Bioapex, S.r.o.

Kauno Technologijos Universitetas

Vladimir Krystof

Miroslav Strnad

Libor Havlicek

Radek Jorda

Karel Dolezal

Marek Zatloukal

Rene Lenobel

Peter Martin Fischer

Lukas Spichal

Antonin Sturc

Eva Reznickova

Borivoj Vojtesek

René Lenobel

Igor Popa

Kveta Fuksova

Jan Slouka

Daniela Moravcová

Iveta Frysova

Petr Cankar

Stefan Zahler

Tomas Pospisil

Algirdas Sackus

Vladimir Divoky

Tereza Radosova Muchova

Tomas Gucky

Angelika Vollmar

Ladislava Vymetalova

Hana Kolarova

Barbora Hosikova

Lukas Malina

Gabriele Varvuolyte

Helena Simerska

Aurimas Bieliauskas

Neringa Kleiziene

Egle Arbaciauskiene

Wolfgang Mikulits

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 new substituted 6-(2-aminobenzylamino)purines, represented by the general formula I, which can be used in CDK inhibition, in particular, in the treatment of viral infections and diseases involving cell proliferation. The invention further includes pharmaceutical preparations containing substituted 6-(2-aminobenzylamino)purines.

Substituted 6-(2-aminobenzylamino)purine derivatives, their use as medicaments and preparations containing these compounds

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

A series of mono- and binuclear 4-arylazo-3,5-diamino-pyrazoles which are useful for inhibition of cyclin-dependent kinases (preferably CDK9). Hence they can be used as antimitotic-, pro-apoptotic and antiinflammatory drugs, in particular, in chemotherapy of cancer and asthma, therapy of psoriasis and parasitoses as those caused by fungi or protists, treatment of Alzheimer's disease or as antineurodegenerative drugs, or to suppress immunostimulation. These compounds are useful in a variety of utilities, including as intermediates in the preparation of flame-retardants, diagnostic reagents and therapeutics, including antivirals and immunosuppressors.

4-arylazo-3,5-diamino-pyrazole compounds and use thereof

The present invention relates to a compound of formula I, or a pharmaceutically acceptable acid salt thereof.  The invention further relates to the use of such compounds in the treatment of hyperproliferative skin disorders, viral infections, cancer, rheumatoid arthritis, lupus, type I diabetes, multiple sclerosis, restenosis, polycystic kidney disease, graft rejection, graft versus host disease and gout, or for psoriasis, parasitoses such as those caused by fungi or protists, or Alzheimer's disease. Further aspects of the invention relate to the use of such compounds in the inhibition of cell proliferation, in the induction of apoptosis, to modulate the activity of adrenergic and/or purinergic receptors or to suppress immunostimulation. The invention also relates to the use of 2,6,9-trisubstituted 8-azapurines in maintaining mammalian ooctyes at the germinal vesicle stage.

Substituted [1,2,3] triazolo[4,5-D]pyrimidines as cdk inhibitors

The invention relates to 3-, 5-, 7-trisubstituted pyrazolo[4,3-d]pyrimidines represented by the general formula I and pharmaceutically acceptable salts thereof, whereinR3 is an optionally substituted alkyl, cycloalkyl, cycloheteroalkyl, cycloalkyl alkyl, aryl or alkylaryl group;R5 is halogen, &#x2014;NHNH, &#x2014;NHOH, NHCONH, guanylo (NH&#x2014;C(NH)NH) an optionally substituted C-Calkyl, alkenyl, alkynyl, C-Ccycloalkyl, R(C-Ccycloalkyl), heterocyclyl, heteroalkyl, aryl, heteroaryl, arylalkylene, arylalkenylene, arylalkynylene, cycloheteroalkyl, cycloheteroalkyl alkyl, heteroarylalkylene, heteroarylalkenylene, heteroarylalkynylene group, the group &#x2014;C(O)&#x2014;R, &#x2014;C(O)NRR, &#x2014;SOR, or &#x2014;NHC(O)R, wherein Rand Rare an optionally substituted C-Calkyl, alkenyl, or alkynyl group, R, R, and Rare independently selected from the group consisting of H, optionally substituted C-Calkyl, alkenyl, or alkynyl group, and Ris a hydroxy, amino, alkoxy, alkylamino, optionally substituted C-Calkyl, alkenyl or alkynyl group; or the group &#x2014;X&#x2014;R, wherein X is &#x2014;NH&#x2014;, &#x2014;O&#x2014;, &#x2014;S&#x2014; or &#x2014;N(alkyl)- and R' is hydrogen, an optionally substituted C-Calkyl, alkenyl, alkynyl, C-Ccycloalkyl, Rf(C-Ccycloalkyl), aryl, heterocyclyl, hetero C-Calkyl, arylalkylene, arylalkenylene, arylalkynylene, heteroaryl, cycloheteroalkyl, cycloheteroalkyl alkyl, or heteroarylalkylene, heteroarylalkenylene, heteroarylalkynylene group, the group &#x2014;C(O)&#x2014;R, &#x2014;C(O)NRR, &#x2014;SOR, or &#x2014;NHC(O)R, wherein R, R, R, R, Rand Rhave the above meaning, andR7 is halogen, &#x2014;NHNH, NHOH, NHCONH, guanylo (NH&#x2014;C(NH)NH) or the group &#x2014;X&#x2014;R, wherein X has the above meaning and the meaning of Ris as defined for R.

Pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy

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Olomouc, Czechia

Vladimir Krystof