The Medicines Company (leipzig) Gmbh

Privates Institut Fur Biomedizinische Forschung Und Beratung

Arzneimittelerk Dresden G.m.b.h.

The Medicines Company

Siegfried Leistner

Dieter Lohmann

Claudia Reichelt

Alexander Schulze

Mohammed Daghish

Jochen Heinicke

Helmut Vieweg

Michael Gutschow

Karl Drossler

Gunther Wagner

Thomas Strohscheidt

Gunter Laban

Herwart Ambrosius

Angela Siegling

Petra Wippich

Konrad Herrmann

Andreas Krödel

Alexander Ludwig

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

Polycyclic pyrimidine-2,4(1H,3H)-diones with functionalized alkyl residues at the 1-, the 3-, or both position(s); methods for their synthesis, production, and pharmaceutical preparation. The invention concerns the synthesis of the above-described compounds, their chemical and structural characterization, and the analysis of their physiological/pharmacological activities in vitro and in vivo. These goals have been attained by the specification of routes of synthesis, methods for the production of the compounds, and the presentation of compound-specific characteristics. The substances encompassed by the present invention demonstrate pharmacologically significant collangenase/matrix metalloproteinase inhibitory activities. The specific example 1-(3-mercaptoprop-1-yl)-3-methyl-chinazolin-2,4(1H,3H)-dione will be presented in detail.

Polycyclic pyrimidine -2,4(1H,3H)-diones with functionalized alkyl residues at the 1- and/or 3-position(s); methods for their synthesis and pharmaceutical preparation

A compound or its tautomer of Formula I, ##STR1## wherein R.sup.1 is hydrogen, a 6-methyl, 6-fluoro, 6-chloro, 6-bromo, or 6,7-dimethoxy residue,

3-(mercaptoalkyl)quinazoline

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Leipzig, Germany

Siegfried Leistner