Boehringer Ingelheim International Gmbh

Stefan Goepper

Juergen Ramharter

Guenther Huchler

Christiane Kofink

Annika Gille

Andreas Gollner

Harald Weinstabl

Joachim Broeker

Manuel Henry

Nina Kerres

Michael Konrad

Guenter Linz

Uwe Joerg Ries

Peter Sieger

Marco Santagostino

Tobias Wunberg

Werner Rall

Anke Baum

Heinz Stadtmueller

Markus Ostermeier

Rolf Schmid

Adil Duran

Dorothea Ingrid Rudolph

Markus Frank

Marco Hans Hofmann

Michael Gmachl

Kathrin Pachur

Andreas Zopf

Julian Wippich

Joerg Halmer

Kathrin Maier

Fabio Savarese

The present invention encompasses intermediates for preparing compounds of formula (I) wherein the groups Rto R, R, A, D, E, F, V, W, X, Y, n, r and q are defined in claim, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.

Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-P53 inhibitors

The present invention encompasses compounds of formula (1) wherein the groups Rto R, A and p have the meanings given in the claims and specification, their use as inhibitors of SOS1, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors

The present invention encompasses compounds of formula (I) wherein the groups Rto R, R, A, D, E, F, V, W, X, Y, n, r and q are defined in claim, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.

The present invention relates to a method of making pyrimidines of formula (III), wherein X1, X2, R1 and R2 have the meanings as defined herein.

Regioselective preparation of substituted pyrimidines

The present invention relates to a crystalline form a dihydropteridione derivative, namely a crystalline form of the free base N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.

Crystalline form of the free base N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7r)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide

A process for preparing compounds of the formula (I) in which R, R, Rand Rare as defined in the description.

Preparation process

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Biberach, Germany

Stefan Goepper