Hoffmann-la Roche Inc.

Covagen Ag

F. Hoffmann-la Roche Ag

Michael Hennig

David Banner

Urs Schwitter

Dragan Grabulovski

Olaf Grassmann

Pirmin Hidber

Remo Anton Hochstrasser

Julian Bertschinger

René Trussardi

Goesta Rimmler

Franziska E Rohrer

Simon Brack

Sarah Batey

Pierre Goldbach

Andre Bubendorf

Jörg Benz

Ines Sauer

Daniel Schlatter

André Bubendorf

Andre Gerard Bubendorf

André Gerard Bubendorf

Olaf Grassman

The present invention relates to a polypeptide binding to a chymase (EC 3.4.21.39), wherein the polypeptide comprises or consists of an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDY(X)A(X)(X)(X)(X)(X)LSFHKGEKFQIL(X)(X)(X)(X) (X)(X)G(X)(X)WEARSLTTGETGYIPSNYVAPVDSIQ (SEQ ID NO: 1), wherein (X) is R, N, Q, E, K, H, S, T, C, or D; (X) is E, T, D, Q, L, P, A, S, C, M, N, E, G, A, V or I; (X) is R, T, H, N, K, S, C, N or Q; (X) is S, W, T, C, N, Q, F or Y; (X) is T, H, L, F, C, S, M, N, Q, R, K, G, A, V, I, P, Y or W; (X) is D, Q, H, E, S, T, C, N, R or K; (X) is D, N, R, E, Q, S, T, C, K or D; (X) is M, W, G, F, A, T, C, S, N, Q, Y, V, L, I or P; (X) is T, H, S, D, C, N, Q, R, K, E or absent; (X) is V, T, Q, G, A, L, I, P, S, C, M, N or absent; (X) is P, A, D, G, K, V, L, I, E, R, M, H or absent; (X) is N, V, P, I, E, T, S, A, G, L, C, M, Q or D; (X) is D, E, T, P, G, A, V, L, I, S, C, M, N or Q, and (X) is W, Y, L, G, A, V, I, P, M, or F; (b) an amino acid sequence which is at least 85% identical to the amino acid sequence of (a), wherein the identity determination excludes amino acid positions (X) to (X).

Chymase binding compounds and medical uses thereof

Methods for transmission mode X-ray diffraction analysis of a sample by means of apparatuses comprising an X-ray radiation source that provides X-ray radiation for irradiating the sample and a detector for detecting X-ray radiation transmitted through and diffracted by the sample. The methods include: (a) placing a sample to be analyzed on a substrate, (b) generating X-ray radiation by means of an X-ray radiation source, (c) positioning the substrate and the sample in an initial position, (d) rotating the substrate and the sample with respect to the initial position around a rotation axis over a predetermined rotation angle, (e) tilting the substrate and the sample with respect to the initial position around a tilting axis over a tilting angle, (f) detecting with a detector the X-ray radiation transmitted through and diffracted by the sample during a time interval, and (g) analyzing the X-ray radiation that is detected.

Methods of transmission mode X-ray diffraction analysis and apparatuses therefor

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

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Weil am Rhein, Germany

Michael Hennig