Otsuka Pharmaceutical Company, Limited

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

Univerzita Palackeho V Olomouci

Palacky University Olomouc

Antonin Sturc

Miroslav Strnad

Libor Havlicek

Vladimir Krystof

Radek Jorda

Petr Zahradnik

Jan Koci

Eva Reznickova

Jiri Malinak

Jiri Tauchman

Tomas Pospisil

Stefan Zahler

Angelika Vollmar

Petr Novak

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

An improved process for preparing 2-chloro-4-nitroimidazole derivatives which are useful intermediates in the preparation of an anti-tuberculosis drug is provided. The process may comprise the step of chlorinating nitroimidazoles with a chlorinating agent and an activating agent to give 2-chloro-4-nitroimidazole derivatives.

Process for production of 2-chloro-4-nitroimidazole derivatives

The present invention relates to a method of production of 4-boronophenylalanine (BPA) from 4-iodophenylalanine, in which all the functional groups of the amino acid are protected by benzyl protection method, and which uses isopropyl magnesium halogenide stabilized by a complexation base, and subsequent condensation of the resulting Grignard reagent with a boric acid ester. The final reaction step, catalytic hydrogenolysis or transfer hydrogenolysis of protecting groups on the amino acid, occurs after hydrolysis of the boronate ester groups.

Method of 4-boronophenylalanine production

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

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Prague, Czechia

Antonin Sturc