Lead Discovery Center Gmbh

Shire Orphan Therapies Gmbh

Qurient Co., Ltd.

Merck Patent Gmbh

Max-planck-gesellschaft Zur Forderung Der Wissenschaften E.v.

Gunther Zischinsky

Jan Eickhoff

Ulrich Reineke

Frank Osterkamp

Uwe Koch

Gerd Hummel

Roland Stragies

Grit Zahn

Jaeseung Kim

Peter Nussbaumer

Dirk Scharn

Kiyean Nam

Dongsik Park

Yeejin Jeon

Mooyoung Seo

Donghoon Yu

Claudia Christner-Albrecht

Doerte Vossmeyer

Holger Kalkhof

Alfred Jonczyk

Sascha Birkner

Carsten Schultz-Fademrecht

Gerd Rühter

Herbert Waldmann

Javier De Ceballos Cerrajeria

Jochen Knolle

Slava Ziegler

George Karageorgis

Elena Sabrina Reckzeh

Melanie Schwalfenberg

Ulrich Groth

The present invention relates to 2,6-methanobenzo[g][1]oxacin-4-one compounds and their analog compounds and pharmaceutically acceptable salts thereof as selective inhibitor of glucose transporters 1 and 3 (GLUTs 1 and 3), to methods of preparing said compounds, and to the use thereof as pharmaceutically active agents, especially for the prophylaxis and/or treatment of metabolic diseases, immunological diseases, autoimmune diseases, inflammation, graft versus host disease, cancer, and metastasis thereof. Furthermore, the present invention is directed to pharmaceutical composition comprising at least one of 2,6-methanobenzo[g][1]oxacin-4-one compounds and their analog compounds.

Inhibitors of glucose transporters (GLUTs)

The present invention relates to pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.

Pyrazolo-triazine and/or pyrazolo-pxrimidine derivatives as selective inhibitor of cyclin dependent kinase

The present invention relates to pyrazolo [1,5-a][1,3,5]triazine and pyrazolo [1,5-a]pyrimidine derivatives having Formula I: and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.

Substituted pyrazolo[1,5-a]pyrimidines and pyrazolo[1,5-a][1,3,5]triazines as CDK inhibitors

The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.

Pharmaceutically active pyrazolo-triazine derivatives

Pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.

The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; &#x3a8; is a radical of formula (II), Ris a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents. 

Compounds for the inhibition of integrins and use thereof

This invention is directed to compounds of structure (I). Particularly this invention is directed to compounds of structure (VIII) wherein the variables are defined as in the description. These compounds are integrin inhibitors and are useful in the treatment of diseases in which an inhibition of angiogenesis is desired. 

Compounds for the inhibition of angiogenesis and use thereof

The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and &#x3a8; is a radical of formula (II) and their use for the inhibition of integrin. 

Heterocyclic compounds for the inhibition of integrins and use thereof

The invention relates to novel peptides which are biologically active as ligands of blood platelet integrin GPIIbIIIa and the &#x3b1;integrins, preferably the av&#x3b2;s and &#x3b1;&#x3b2;integrin, having the formula (I): R-Arg-X-Asp-Leu-Asp-Ser-Leu-Arg-R(I), in which Rdenotes H, acetyl or acyl and Rdenotes -Oh, ORNH, NHR, N(R)Rdenotes atkyl, aralkyl, aryl, Het and X denotes an amino acid of the formula (II), in which A denotes (CH)Rdenotes H, alkyl, aralkyl or aryl, and n denotes 1, 2, 3, 4, 5 or 6, and the amino acid of the formula (II) is bonded to the adjacent Arg via a peptide bond of the &#x3b1;-amino group and to the &#x3b1;-amino group of the adjacent Asp via a peptide bond of the &#x3b1;-carboxyl group. 

Peptidic sulfonamides

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Datteln, Germany

Gunther Zischinsky