Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Boehringer Ingelheim Pharma Kg

Basf Aktiengesellschaft

Alkahest, Inc.

Rolf Schmid

Matthias Grauert

Bernhard Hauer

Guenter Linz

Peter Sieger

Werner Rall

Gerd Kraemer

Matthias Hoffmann

Ralf Anderskewitz

Rainer Soyka

Juergen Schnaubelt

Rainer Hamm

Svenja Renner

Joerg Brandenburg

Carsten Reichel

Jutta Kroeber

Rolf Herter

Joern Merten

Rolf Bauer

Gunnar Schreiner

Rainer Sobotta

Markus Ostermeier

Adil Duran

Thomas Krueger

Stefan Goepper

Juergen Daeubler

Michael Konrad

Thomas Fachinger

Michael Pangerl

Zeno A Leuter

Emanuel Stehle

Claudia Ochs

Sarah Unger

Markus Matuschek

Bianca Werner

Robert Schiffers

Christiane Buta

Hubert Zipper

Katrin Laemmle

Isabelle Kauffmann

This invention relates to a novel process for making alkyl 7-amino-5-methyl-[1,2,5]-oxadiazolo[3,4-b]pyridine-carboxylate.

Process for manufacturing alkyl 7-amino-5-methyl-[1,2,5]oxadiazolo[3,4-b]pyridine-carboxylate

The present invention relates to a process for preparing CCR3 inhibitors of formula 1, wherein

Process for the manufacturing of CRR inhibitors

The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound 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 its crystallization in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.

Specific salt, anhydrous and crystalline form of a dihydropteridione derivative

The present invention encompasses a process for preparing compounds of formula (1), wherein a compound of formula (2) is reacted in the presence of a catalyst and a solvent under hydrogen pressure to form a compound of formula (1) and wherein A and R&#x2014;Rare defined herein.

Method of preparing chiral cyclic &#x3b2;-aminocarboxamides

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

The present invention relates to a process for the manufacture of a specific indolinone derivative and a pharmaceutically acceptable salt thereof, namely 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone and its monoethanesulfonate, to new manufacturing steps and to new intermediates of this process.

Process for the manufacture of an indolinone derivative

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

Preparation process

Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, processes for preparing them and their use as pharmaceutical compositions.

[object Object]

Ethyl 3-[(2-{[4-(hexyloxycarbonylaminoiminomethyl)phenylamino]methyl}-1-methyl-1H-benzimidazole-5-carbonyl)pyridin-2-ylamino]propionate methanesulfonate in the crystalline modifications I and II and as the hemihydrate and the use thereof as a pharmaceutical composition.

3-[(2-{[4-(hexyloxycarbonylaminoiminomethyl) phenylamino]methyl}-1-methyl-1H-benzimidazol-5-carbonyl)pyridin-2-ylamino]propionic acid ethylester methansulfonate and its use as a medicament

Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]Amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide: processes for preparing them and their use as pharmaceutical compositions with antiproliferative activity.

Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament

The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound 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 its crystallisation in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.

Crystalline forms of the compounds (R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole and the monohydrochloride thereof, processes for the preparation thereof and the use thereof as pharmaceutical compositions.

(R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1(pyrrolidinocarbonyl)-ethyl]-benzimidazole, the monohydrochloride thereof, preparation thereof and the use as pharmaceutical composition

(R) 2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1 (pyrrolidinocarbonyl)-ethyl]-benzimidazole, the monohydrochloride thereof, preparation thereof and the use as pharmaceutical composition

The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I)wherein:

Process for preparing aryl-iminomethyl-carbamino acid esters

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Baltringen, Germany

Rolf Schmid