Nycomed Gmbh

Polyphor Ag

Unversität Zürich

Altana Pharma Ag

4sc Ag

Takeda Gmbh

Astrazeneca Ab

Steffen Weinbrenner

Beate Schmidt

Dieter Flockerzi

Hans-Peter Kley

Raimund Külzer

Daniel Obrecht

Thomas Maier

Armin Hatzelmann

Thomas Stengel

Thomas Beckers

Geert Jan Sterk

Raimund Kuelzer

Hermann Tenor

Christian Ludin

John Anthony Robinson

Ulrich Kautz

Gerhard Grundler

Alexander Lederer

Anatol Luther

Kerstin Moehle

Degenhard Marx

Astrid Zimmermann

Christian Hesslinger

Volker Gekeler

Frank Otto Gombert

Stefan Fischer

Petra Gimmnich

Mathias Schmidt

Christof Zitt

Andreas Pahl

Josef Stadlwieser

Christian Bisang

Torsten Dunkern

Clemens Braun

Alexander Weber

Odile Sellier-Kessler

Ewald Benediktus

Florian Dehmel

William J Drury, Iii

Christian Steuer

Harald Ohmer

Alexander Mann

Manuella Schmitt-Billet

William J Drury Iii

Herrmann Tenor

Raimund c/o Nycomed Gmbh Külzer

Novel backbone-cyclized peptidomimetics of the general formulacyclo[-P-P-P-P-P-P-P-P-T-T-]&#x2003;&#x2003; (I)wherein the single elements T or P are &#x3b1;-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to modulate the GLP-1 receptor. They can be used as medicaments to treat, prevent, or delay the onset of diseases, disorders or conditions in which modulation of the human GLP-1 receptor is beneficial, such as type 2 diabetes. These backbone-cyclized peptidomimetics can be manufactured by a process which is based on a mixed solid&#x2014;and solution phase synthetic strategy.

Backbone-cyclized peptidomimetics with GLP-1R modulating activity

&#x3b2;-Hairpin peptidomimetics of the general formula cyclo(-Xaa-Xaa-Thr-Xaa-Ser-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-) and pharmaceutically acceptable salts thereof, with Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaa, Xaaand Xaabeing amino acid residues of certain types which are defined in the description and the claims, have elastase inhibitory properties, especially against human neutrophil elastase, and can be used for preventing infections or diseases related to such infections in healthy individuals or for slowing infections in infected patients. The compounds of the invention can further be used where cancer, or immunological diseases, or pulmonary diseases, or cardiovascular diseases, or neurodegenerative diseases, or inflammation, or diseases related to inflammation, are mediated or resulting from elastase activity. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Beta-hairpin peptidomimetics as selective elastase inhibitors

The compounds of Formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.

3,4,4a,10b-Tetrahydro-1H-thiopyrano-[44,3-c] isoquinoline derivatives

The invention relates to thiophene-imidazopyridine compounds according to formula (I), wherein the substituents and symbols are as defined in the description. The compounds are inhibitors of PIk1. 

Thiophene-imidazopyridines

The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors.

Triazolophthalazines

The compounds of formula I in which R1 and R2 have the meanings as given in the description are novel effective PDE2 inhibitors.

3,4-Dihydroisoquinoline and isoquinoline compounds of formula I, in which Ar represents a phenyl raidcal of the formulae IIa, IIb or IIc are novel effective PDE7 inhibitors.

(Dihydro) isoquinoline derivatives as phosphodiesterase inhibitors

Growing community of inventors

Constance, Germany

Steffen Weinbrenner