Aminothiophene carboxylic acid amides and the use thereof as phosphodiesterase inhibitors
AssigneeMerck Patent GmbH
InventorsRochus Jonas, Pierre Schelling, Franz-Werner Kluxen, Maria Christadler
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Abstract
Aminothiophenecarboxamides of the formula I ##STR1## and their physiologically acceptable salts, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, A and n have the meanings stated in claim 1, exhibit phosphodiesterase V inhibition and can be used for the treatment of diseases of the cardiovascular system and for the therapy of disturbances of potency.
Claims19
Compounds of the formula I ##STR6## where R.sup.1 and R.sup.2, independently of one another, are each H, A, OA, alkenyl, alkynyl, CF.sub.3 or Hal, one of the radicals R.sup.1 or R.sup.2 always being.noteq.H,
- R.sup.1 and R.sup.2 together are also alkylene having 3-5 C atoms,
- R.sup.3 and R.sup.4, independently of one another, are each H, A, OA, NO.sub.2, NH.sub.2 or Hal,
- R.sup.3 and R.sup.4 together are also --O--CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 --O-- or --O--CH.sub.2 --CH.sub.2 --O--,
- A and A', independently of one another, are each H or alkyl having 1 to 6 C atoms,
- R.sup.5 is --X--Y,
- X is CO, CS or SO.sub.2,
- Y is a saturated or unsaturated 5- to 7-membered isocyclic or heterocyclic ring which is unsubstituted or monosubstituted or disubstituted by COOH, COOA, CONH.sub.2, CONAA', CONHA, CN, NHSO.sub.2 A, N(SO.sub.2 A).sub.2 or SO.sub.2 A,
- Hal is F, Cl, Br or I and
- n is 0, 1, 2 or 3,
- and their physiologically acceptable salts excluding the compound 2-benzoylamino- 4,5,6,7-tetrahydro-benzo[b]thiophen-3-carboxylic acid N-phenylamide.
A pharmaceutical formulation according to claim 16, further comprising at least one pharmaceutically acceptable excipient.
Dependencies are inferred from the claim text.