Boehringer Ingelheim International Gmbh

Guenther Huchler

Markus Ostermeier

Werner Rall

Stefan Goepper

Uwe Joerg Ries

Marco Santagostino

Juergen Ramharter

Andreas Gollner

Christiane Kofink

Harald Weinstabl

Joachim Broeker

Manuel Henry

Nina Kerres

Annika Gille

Juergen Daeubler

Waldemar F Pfrengle

Peter Sieger

Stephan Kling

Andreas Zopf

Uwe Reis

Ulrike Werthmann

Thomas Krueger

Jean-Nicolas Desrosiers

Michael Konrad

Kathrin Pachur

Michael Pangerl

Sonja Sproll

Waldermar Pfrengle

Guanghua Lu

Stefan Braith

Kathrin Maier

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 application includes a description of novel intermediates, of new manufacturing steps resulting in a novel and improved process for producing the intermediates and the final compounds, i.e., 6-alkynyl-pyridine derivatives. The intermediates of the invention are useful to produce 6-alkynyl-pyridine derivatives, which compounds are useful for the treatment of cancer.

Process for the manufacture of 6-alkynyl-pyridine derivatives

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 process for the stereoselective preparation of compounds of formulae (1A) and (1B) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.

Stereoselective synthesis of bicyclic heterocycles

The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.

9-[4-(3-chloro-2-fluoro-phenylamino-7-methoxy-quinazoline-6-yloxy]-1,4-diaza-spiro[5.5]undecane-5-one dimaleate, use thereof as a medicament and method for the production thereof

9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy-quinazoline-6-yloxy]-1,4-diaza-spiro[5.5] undecane-5-one dimaleate, use thereof as a medicament and method for the production thereof

The present invention relates to a process for the stereoselective preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.

Process for the stereoselective preparation of bicyclic heterocycles

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

Preparation process

The present invention relates to a process for preparing compounds of general formula I wherein Rand Rare defined as in claim, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein Ris defined as in claim

Production method

The present invention relates to a process for preparing compounds of general formula I wherein Rand Rare defined as in claimthe pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein Ris defined as in claim

The present invention relates to the new crystalline compounds A of general formula I wherein A, A, A, X, Y, Yand Yare defined as in claim, and which are present in the form of their physiologically acceptable salts with acids, the acids being selected from the group B comprising hydrochloric acid, hydrobromic acid, sulphuric acid, phosphoric acid, benzenesulphonic acid, p-toluenesulphonic acid, maleic acid, succinic acid, fumaric acid, D-(&#x2212;)-tartaric acid, L-(+)-tartaric acid, naphthalene-2-sulphonic acid and naphthalene-1,5-disulphonic acid, and the polymorphs, the corresponding solvates and hydrates thereof.

Crystalline compounds

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Hochdorf, Germany

Guenther Huchler