Max-planck-gesellschaft Zur F&#xf6;rderung Der Wissenschaften E. V.

Sugen Incorporated

Other

University of California

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.

Pecsi Tudomanyegyetem

Medizinische Universitat Innsbruck

Bio-signal Corporation Ltd.

Vichem Chemie Kutató Kft.

Virostatics Srl

Vichem Chemie Kutato Korlatolt Felelossegu Tarsasag

László Örfi

Axel Ullrich

György Kéri

Istvan Szekely

Aviv Gazit

Klaus Peter Hirth

Alex Levitzki

Elaina Mann

Reiner Lammers

Janis Haimichael

Tamas Bajor

Peng Cho Tang

Laura Kay Shawver

Donna Pruess Schwartz

Yixiang Zhang

István Szabadkai

Dennis J Slamon

Zoltán Varga

Zoltán Greff

Gyorgi Keri

Fairooz F Kabbinavar

Robert Torka

Franco Lori

Gábor Németh

Pjotr Knyazev

Antonio Solinas

Péter Bánhegyi

Anna Sípos

James Chafouleas

Davide De Forni

Lukas A Huber

Csaba Szántai-kis

Zsuzsanna Helyes

Frigyes Wáczek

Tamás Szüts

Laura K Shawyer

Johann Jakob Leban

János Szolcsányi

János Pató

Erika Pintér

Kéri György

Éva Szöke

Winfried Wunderlech

Wáczek Frigyes

Csaba Szántai Kis

The present invention relates to 3-amino-pyrazolo[3,4-d]pyrimidin-4-ones, such as for example, N-{4-[1-(2,6-dichloro-4-sulfamoyl-phenyl)-3-dimethylamino-4-oxo-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-ylmethyl]-phenyl}-2-diethylamino-acetamide, particularly useful as cyclin dependent kinase (CDK) inhibitors, pharmaceutical compositions comprising the same and the use thereof in particular in the prophylaxis and/or treatment of cancer and other proliferative diseases. Furthermore, the present invention relates to processes for the synthesis of said 3-aminopyrazolo[3,4d]pyrimidin-4-ones and intermediates to be used in the processes of the present invention.

3-amino-1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-ones as cyclin dependent kinase inhibitors

The present invention relates to 4-phenetylamino-7H-pyrrolo[2,3-d]pyrimidine derivatives of the and solvates, hydrates and pharmaceutically acceptable salts thereof, processes for manufacturing of them, the use of them, as well as pharmaceutical compositions containing at least one of them as pharmaceutically active agent(s) together with pharmaceutically acceptable carrier, excipient and/or diluents, especially for the prevention and/or treatment of acute neurogenic inflammation and/or neuropathic hyperalgesia. Said 4-phenetylamino-7H-pyrrolo[2,3-d]pyrimidine compounds have been identified as new drug candidates for the prevention and/or treatment of acute neurogenic inflammation and/or neuropathic hyperalgesia.

Agents for treating neurogenic inflammation and neuropathic hyperalgesia related disorders

Novel 4,6-disubstituted aminopyrimidine derivatives with the following structure (I) have anti-HIV activity.

4,6-disubstituted aminopyrimidine derivatives have anti-HIV activity

Novel compounds which are inhibitors of receptor tyrosine kinases of the AXL receptor family are described herein. These compounds are suitable for the treatment or prevention of disorders associated with, accompanied by or caused by hyperfunction of a receptor of the AXL family. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly cancer metastases.

Quinoline derivatives as AXL kinase inhibitors

The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.

Quinolinyloxyphenylsulfonamides

The invention relates compounds of general formula (I) and pharmaceutically acceptable salts and solvates thereof wherein Furthermore, the present invention is directed to pharmaceutical composition containing at least one compound of general formula (I) and/or pharmaceutically acceptable salts or solvates thereof and for the use of them for the preparation of pharmaceutical compositions for the prophylaxis and/or the treatment of protein kinase related, especially CDK9-related diseases e.g. cell proliferative disease, infectious disease, pain, cardiovascular disease and inflammation.

4-phenylamino-pyrimidine derivatives having protein kinase inhibitor activity

The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG.,), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.

Treatment of platelet derived growth factor related disorders such as cancers

The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.

Treatment of platelet derived growth factor related disorders such as

Method for treating a patient inflicted with a cell proliferation disorder, such as a cancer, characterized by inappropriate PDGF-R activity. The method involves the step of administering to the patient a therapeutically effective amount of a composition described in application.

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Budapest, Hungary

László Örfi