The Medicines Company (leipzig) Gmbh

The Medicines Company

Jochen Heinicke

Claudia Reichelt

Alexander Schulze

Friedrich-Alexander Ludwig

Mohammed Daghish

Torsten Steinmetzer

Andrea Schweinitz

Joerg Stuerzebecher

Jörg Stürzebecher

Andreas Van De Locht

Silke Nicklisch

Anett Soeffing

Peter Steinmetzer

Siegfried Leistner

Mohammed Daghisch

Alexander Ludwig

Andreas Krödel

Joseph DeAngelo

Kenneth Mugridge

Sven Letschert

Maj Schuster

Konrad Herrmann

Anett Söffing

Joseph Deangelo

The invention relates to compounds of general formula 1 to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts and/or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as inductors of apoptosis in the case of non-solid malignant tumors of the hematopoietic system, in particular in the case of leukemias and lymphomas, more particularly in the case of leukemic B lymphocytes.

Substituted 5H-pyrimido[5,4-B]indoles, method for the production thereof and use thereof for treating non-solid malignant tumors of the blood-producing system

The invention relates to inhibitors of trypsin-like serine proteases, including those of the general formula (IV) which, as well as plasmin, also inhibit plasma kallikrien, and to their use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.

Trypsin-like serine protease inhibitors, and their preparation and use

The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrein, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.

The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrien, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.

The invention relates to compounds of general formula (I); 1a, 1 b, 1 c and 1 d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNF&#x3b1;-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes. 

Substituted pyrido [3', 2&#x2032;: 4, 5] thieno [3, 2-D] pyrimidines and pyrido [3&#x2032;, 2&#x2032;: 4, 5] furo [3, 2-D] pyrimidines used as inhibitors of the PDE-4 and/or the release of TNF-ALPHA

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Leipzig, Germany

Jochen Heinicke