Merck Patent Gmbh

Maria Kordowicz

Andree Blaukat

Timo Heinrich

Hartmut Greiner

Frank Zenke

Wolfgang Staehle

Christian Sirrenberg

Lars Thore Burgdorf

Uwe Hofmann

David Bruge

Tadeusz Pacuszka

Andrzej Gardas

The invention relates to compounds of the formula (I), to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumors and/or diseases in the development or course of which kinases are involved. 

Azaheterocyclic compounds as kinase inhibitors

The invention relates to compounds of the formula (I), in which Ar denotes a mono- or bicyclic aromatic homo- or heterocycle having 1 to 4 N, O and/or S atoms and 5 to 10 skeleton atoms, which may be unsubstituted or mono-, di- or trisubstituted by carbonyl oxygen, Hal, A, OH, OA, NH, NHA, NA, NO, CN, OCN, SCN, COOH, COOA, CONH, CONHA, CONA, NHCOA, NHCONH, NHSOA, CHO, COA, SONHand/or S(O)A, A denotes unbranched, branched or cyclic alkyl having 1-14 C atoms, in which one or two CHgroups may be replaced by O or S atoms and/or by &#x2014;CH&#x2550;CH&#x2014; groups and/or in addition 1-7 H atoms may be replaced by F and/or Cl, Hal: F, Cl, Br or I, D: NH, NH, NA, NHA, CH, CH, OH, OA, O or S, E: CH, CH, NH or N, Y: E or a saturated or unsaturated bond, X: CH, O or NH, Q: Hal, A, OH, OA, NH, NHA, NA, NO, CN, OCN, SCN, COOH, COOA, CONH, CONHA, CONA, NHCOA, NHCONH, NHSOA, CHO, COA, SONHor X-M, to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumors and/or diseases in the development or course of which kinases are involved.

(1H-indol-7-yl)-(pyrimidin-2-ylamino)methanone derivatives and related compounds as IGF-R1 inhibitors for the treatment of cancer

The present invention relates to oxindoles of the formula I, their use as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases and their use for the manufacture of a pharmaceutical composition. 

Oxindoles as kinase inhibitors

The present invention relates to the isolation, purification and characterization of a hyaluronidase which derives from the tropical leech. Therefore, according to this invention, the enzyme was called 'manillase'. The invention is furthermore concerned with the recombinant method of production of manillase which includes the disclosure of DNA and amino acid sequences as well as of expression vectors and host systems. Finally, the invention relates to the use of manillase for therapeutic purposes, for example, for the treatment of myocardial diseases, thrombotic events and tumors.

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Griesheim, Germany

Maria Kordowicz