Hoechst Aktiengesellschaft

Gunther Wess

Gerhard Beck

Wilhelm Bartmann

Werner Kramer

Hans-Hermann Lau

Heiner Glombik

Alfons Enhsen

Kurt Kesseler

Heiner Jendralla

Ernold Granzer

Dirk Seiffge

Ekkehard Baader

Bela Kerekjarto

Klaus-Ulrich Weithmann

Stefan Mullner

Hiristo Anagnostopulos

Horst Neubauer

Alfons Ehnsen

Klaus Bock

Bile acid derivatives, processes for their preparation, and use as

Bile acid conjugates of proline hydroxylase inhibitors

The invention relates to linker-modified bile acid derivatives of the formula I: ##STR1## wherein the radicals X.sup.1, X.sup.2, X.sup.3 and Y and n are as defined in the claims, and to a process for their preparation. The compounds according to the invention are therapeutically active and are thus suitable as drugs, especially as hypolipldemics. The invention further relates to the use of the bile acid derivatives according to the invention as drugs.

Modified bile acids process for their preparation and their use

nor-Bile acid derivatives, processes for their preparation and the use of these compounds as medicaments nor-Bile acid derivatives of the formula I

Nor-bile acid derivatives, processes for their preparation and the use

Lipid-selective antioxidants of the formula I

Lipid-selective antioxidants and their preparation and use

Process for the preparation of 3.beta.-aminocholanic acid derivatives A process for the preparation of 3.beta.-aminocholanic acid derivatives of the formula II ##STR1## wherein R(1), R(2) and R(3) have the meanings given, starting from the corresponding 3.beta.-hydroxycholanic acid esters, is described.

Process for the preparation of 3.beta.-aminocholanic acid derivatives

The invention relates to tetrazole derivatives of bile acids, processes for their preparation, and use of these compounds as medicaments and cholesterol lowering agents. The tetrazole-bile acid derivatives are of the formula G1--X--G2, where G1 is H, a bile acid radical, or a bile acid radical which is modified on the hydroxyl functions and/or on the carboxyl group, X is a single bond or a bridge group between G1 and G2, and G2 is of the formula: ##STR1##

Tetrazole derivatives of bile acids, and their use as lipid level

Bile acid derivatives, processes for their preparation and use as pharmaceuticals Bile acid derivatives of the formula I

Modified bile acid conjugates, and their use as pharmaceuticals

Bile acid derivatives, process for their preparation and use of these

4-Hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, process for their preparation, their use as pharmaceuticals, and pharmaceutical preparations and precursors. Compounds of the formula I ##STR1## and the corresponding open-chain dihydroxycarboxylic acids of the formula II ##STR2## in which X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings indicated, and also their pharmacologically tolerable salts with bases and their pharmacologically tolerable esters, processes for the preparation of these compounds, their use as pharmaceuticals and pharmaceutical preparations are described. In addition, compounds of the formula III ##STR3## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X and Y have the meanings indicated are described.

4-hydroxytetrahydropyran-2-ones and the corresponding

The invention relates to bile acid derivatives of the formula I

6-Fluoro-3,5-dihydroxy carboxylic acid derivatives of the formula I and the corresponding lactones of the formula II ##STR1## in which R.sup.1 and R.sup.2 have the specified meanings, a process for the preparation of these compounds, the use thereof as medicinal agents and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formula I or formula II are described.

6-fluoro-3,5-dihydroxy carboxylic acids and derivatives thereof

6-Phenoxymethyl-4-hydroxytetrahydropyran-2-ones and 6-thiophenoxymethyl-4-hydroxytetrahydropyran-2-ones and the corresponding dihydroxycarboxylic acid derivatives, salts and esters, processes for the preparation of these compounds, their use as pharmaceuticals, pharmaceutical preparations and novel phenols and thiophenols Compounds of the general formula I ##STR1## and the corresponding open-chain dihydroxycarboxylic acids of the formula II ##STR2## in which X, Y and Z have the meanings given, and pharmacologically tolerated salts thereof with bases and pharmacologically tolerated esters thereof, processes for the preparation of these compounds, their use as pharmaceuticals and pharmaceutical preparations are described. Novel phenols and thiophenols of the formula III ##STR3## in which X, Y and Z have the meanings given, are also described.

6-phenoxymethyl-4-hydroxytetrahydropyran-2-ones and

7-Substituted 3,5-dihydroxyhept-6-ynoic acids and the derivatives thereof of the formula I ##STR1## as well as the corresponding lactones of the formula II ##STR2## in which R and R.degree. have the specified meanings, a process for the preparation of these compounds, the use thereof as pharmaceuticals and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formula I or formula II are described.

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Erlensee, Germany

Gunther Wess