Genentech, Inc.

Hoffmann-la Roche Inc.

Harvard College

F. Hoffmann-la Roche Ag

Pirmin Hidber

Reinhard Reents

Francis Gosselin

Peter Steidle

Martin Wunderlich

Marie Pepelnjak

Andre Hell

Edward Yost

Ursula Hoffmann

George M Whitesides

Enoch Kim

Urs Schwitter

Srinivasan Babu

Qingping Tian

Remo Anton Hochstrasser

Dieter Voegelin

Herbert Yajima

Zhigang Cheng

Franziska E Rohrer

Goesta Rimmler

Michael Hennig

Andre Bubendorf

Dennis A Smith

Theresa Humphries

Declan Costello

Gerard John Hamett

Thomas McCarthy

Timothy Smyth

Gerard John Harnett

Alexander Bausch

Wolfgang Helbig

Andre Gerard Bubendorf

Thomas Mccarthy

André Hell

André Gerard Bubendorf

The present invention relates to pharmaceutical compositions comprising Akt protein kinase inhibitors with therapeutic activity against diseases such as cancer as well as processes for their preparation and their use as medicament.

Pharmaceutical compositions comprising AKT protein kinase inhibitors

Pharmaceutical compositions comprising Akt protein kinase inhibitors

Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure:  and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof.

Process for making thienopyrimidine compounds

The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]2-methylthiopropionate which is a useful pharmaceutical active compound.

Process

A multi-well filtration device for filtering a suspension comprises a filtration plate with a filtration chamber and a collecting plate with a collecting well. The filtration chamber is connected to the collecting well and a filter element is arranged between the filtration chamber and the collecting well. A separation layer is arranged between the filtration plate and the collecting plate adjacent to the filter element. The use such of a separation layer allows an easy detachment of the filtration plate from the collecting plate. The detached filtration plate can comfortably be transferred into an analysis device, in which the solid phase of the filtration chamber can separately be analyzed through the separation layer, without any replacement of the solid phase.

Multi-well filtration device

The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. The [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride is an inhibitor of tyrosine kinase enzymes, and are useful in the treatment of cancer. Also disclosed are methods of making and using the novel polymorph, as well as pharmaceutical compositions containing the novel polymorph.

[6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride polymorph

The present invention relates to a process for manufacturing a pulverous preparation of a submicron-sized biologically active compound comprising the steps of dissolving a biologically active compound under elevated pressure in a compressed gas, liquid or supercritical fluid containing a surface modifier; and rapidly expanding the compressed solution thereby precipitating the dissolved compound. An alternative process comprises dissolving the biologically active compound in compressed dimethylether, which may optionally contain a surface modifier; and spraying the compressed solution into an antisolvent phase, optionally containing a surface modifier, under vacuum, atmospheric pressure or elevated pressure. An optional third step involves converting the antisolvent phase into a pulverous preparation using conventional powder processing.

Process for making submicron particles

A method of transferring a chemical activating agent from an applicator to a substrate surface involves providing an applicator having a raised application surface, applying a chemical activating agent to the application surface, contacting the substrate surface with the application surface, and removing the applicator. The chemical activating agent is transferred in a form in which it is capable of effecting a chemical reaction, such as catalysis, at the surface. Thus, following transfer of the chemical activating agent to the surface in a pattern, a metal can be plated at the substrate surface in the pattern. The applicator can be an elastomeric stamp having a raised portion defining a stamping surface.

Microcontact printing of catalytic colloids

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Basel, Switzerland

Pirmin Hidber