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AssigneeSchering Corporation
InventorsHanns Ahrens, Helmut Biere, Clemens Rufer, Ralph Schmiechen, Eberhard Schroeder, Olaf Loge, Wolfgang Losert, Ekkehard Schillinger
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Thiophene derivatives of the formula ##STR1## WHEREIN R.sub.x is --S-CHR.sub.5 -COOH or --S-CH.sub.2 -CH.sub.2 -OH, R.sub.y is 1-2 of halogen alkoxy of 1-6 carbon atoms, aralkyl of 7-10 carbon atoms, phenyl, halophenyl or alkylcarbonyl of 1-6 carbon atoms in the alkyl group, and R.sub.5 is a hydrogen atom, when R.sub.y is a halogen atom, when R.sub.5 is alkyl, their enantiomers, and their pharmacologically acceptable salts thereof with bases, possess antilipolytic activity.
A pharmaceutical composition in dosage unit form, for inhibiting lypolysis comprising a pharmaceutically acceptable oral or parenteral carrier in admixture with 10 mg to 1g of a thiophene derivative of the formula ##STR5## wherein one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is R.sub.x ;
A method of inhibiting lypolysis which comprises administering systemically to a patient with abnormally high serum triglyceride or FFA level an effective amount of a thiophene derivative of the formula ##STR6## wherein one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is R.sub.x ;
Dependencies are inferred from the claim text.
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Hetero atoms other than halogen: sulfur atoms
Heterocyclic compounds
Term ended 15 Nov 1994 (estimated)
USPTO file history isn’t available for this patent, so only indexed dates are shown.
This invention relates to novel, antilipolytically active thiophene derivatives and to processes for the preparation and use thereof.
Pathologically high blood serum concentrates of triglycerides are held responsible, inter alia, for the origination and progression of arteriosclerotic changes of the blood vessel wall. The triglycerides in the serum originate not only from food intake but also from the liver, where they are synthesized from the blood, in part with the use of free fatty acids (FFA). A lowering of the FFA content in the serum results in a lowering of the triglyceride condentration in the liver and in the blood. BIZZI, VENERONI, and GARATTINI, J. Pharm. Pharmac. 18, 611, 1966; PAOLETTI and PUGLISI, Naunyn-Schmeidebergs Arch. Pharmak., 269, 317, 1971.
Since the FFA concentration in the serum depends primarily on the extent to which the triglyceride is split in the fatty tissue (lipolysis), a pharmacological inhibition of this process represents an effective measure for lowering the triglyceride level in the serum and to prevent arteriosclerotic changes of blood vessels. This was proven by animal experiments. BIZZI, VENERONI, and GARATTINI, J. Pharm. Pharmac. 18, 611, 1966; BIZZI, GARATTINI, VENERONI, HOWARD, GRESHAM, and JENNINGS, Atherosclerosis, in print, 1974. Also in humans, a reduction of the triglyceride concentration in the serum was measured after treatment with agents which inhibit lipolysis. BERLINGER, BAENDER, GLANINGER, MAYRHOFER, and SCHNAK, Horm. Metab. Res. 2, 81, 1970.
Specifically contemplated classes of compounds of this invention include those wherein:
a. R.sub.x is --S-CHR.sub.5 -COOH, especially those wherein R.sub.1 is R.sub.x ;
b. R.sub.x is --S-CH.sub.2 -CH.sub.2 -OH, especially wherein R.sub.1 is R.sub.x ;