Oxazolidinone For The Treatment And Prophylaxis Of Pulmonary Hypertension
AssigneeBayer Schering Pharma Aktiengesellschaft
InventorsGeorges Von Degenfeld, Martina Klein, Elisabeth Perzborn, Joachim Hütter, Gerrit Weimann
Life of this patent
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Abstract
The present invention relates to the use of factor Xa inhibitors, especially of oxazolidinones of the formula (I), for the treatment and/or prophylaxis of pulmonary hypertension, and to the use thereof for the manufacture of medicaments for the treatment and/or prophylaxis of pulmonary hypertension.
Claims11
A method for the treatment and/or prophylaxis of pulmonary hypertension comprising administering a therapeutically effective amount of a compound of the formula
- in which
- R1 is 2-thiophene which is substituted in position 5 by a radical selected from the group of chlorine, bromine, methyl and trifluoromethyl,
- R2 is D-A-,
- where
- the radical “A” is phenylene,
- where
- the group “A” may be substituted where appropriate once or twice in the meta position relative to the linkage to the oxazolidinone by a radical selected from the group of fluorine, chlorine, nitro, amino, trifluoromethyl, methyl and cyano,
- and
- the radical “D” is a saturated 5- or 6-membered heterocycle which is linked via a nitrogen atom to “A” and has in the direct vicinity of the linking nitrogen atom a carbonyl group, and in which one ring carbon member may be replaced by a heteroatom from the series S, N and O,
- or one of the salts, solvates and solvates of the salts thereof
- to a human or animal patient in need thereof.
-6. (canceled)
A method for the treatment and/or prophylaxis of pulmonary arterial hypertension comprising administering a therapeutically effective amount of a compound of the formula
- in which
- R1 is 2-thiophene which is substituted in position 5 by a radical selected from the group of chlorine, bromine, methyl and trifluoromethyl,
- R2 is D-A-,
- where
- the radical “A” is phenylene,
- where
- the group “A” may be substituted where appropriate once or twice in the meta position relative to the linkage to the oxazolidinone by a radical selected from the group of fluorine, chlorine, nitro, amino, trifluoromethyl, methyl and cyano,
- and
- the radical “D” is a saturated 5- or 6-membered heterocycle which is linked via a nitrogen atom to “A” and has in the direct vicinity of the linking nitrogen atom a carbonyl group, and in which one ring carbon member may be replaced by a heteroatom from the series S, N and O,
- or one of the salts, solvates and solvates of the salts thereof
- to a human or animal patient in need thereof.
A method for the treatment and/or prophylaxis of idiopathic pulmonary arterial hypertension, familial pulmonary arterial hypertension (FPAH) and associated pulmonary arterial hypertension (APAH) which is associated with collagenoses, congenital systemic-pulmonary shunts, portal hypertension, HIV infections, intake of particular drugs and medicaments, with other disorders such as thyroid disorders, glycogen storage diseases, Gaucher's disease, hereditary telangiectasia, haemoglobinopathies, myeloproliferative disorders and splenectomy, or with disorders with significant venous/capillary involvement such as pulmonary venoocclusive disease and pulmonary capillary haemangiomatosis, and persistent pulmonary hypertension of newborns comprising administering a therapeutically effective amount of a compound of the formula
- in which
- R1 is 2-thiophene which is substituted in position 5 by a radical selected from the group of chlorine, bromine, methyl and trifluoromethyl,
- R2 is D-A-,
- where
- the radical “A” is phenylene,
- where
- the group “A” may be substituted where appropriate once or twice in the meta position relative to the linkage to the oxazolidinone by a radical selected from the group of fluorine, chlorine, nitro, amino, trifluoromethyl, methyl and cyano,
- and
- the radical “D” is a saturated 5- or 6-membered heterocycle which is linked via a nitrogen atom to “A” and has in the direct vicinity of the linking nitrogen atom a carbonyl group, and in which one ring carbon member may be replaced by a heteroatom from the series S, N and O,
- or one of the salts, solvates and solvates of the salts thereof
- to a human or animal patient in need thereof.
A method for the treatment and/or prophylaxis of pulmonary hypertension associated with chronic obstructive pulmonary disorders, interstitial lung disease, sleep apnoea syndrome, alveolar hypoventilation, chronic altitude sickness and constitutional abnormalities comprising administering a therapeutically effective amount of a compound of the formula
- in which
- R1 is 2-thiophene which is substituted in position 5 by a radical selected from the group of chlorine, bromine, methyl and trifluoromethyl,
- R2 is D-A-,
- where
- the radical “A” is phenylene,
- where
- the group “A” may be substituted where appropriate once or twice in the meta position relative to the linkage to the oxazolidinone by a radical selected from the group of fluorine, chlorine, nitro, amino, trifluoromethyl, methyl and cyano,
- and
- the radical “D” is a saturated 5- or 6-membered heterocycle which is linked via a nitrogen atom to “A” and has in the direct vicinity of the linking nitrogen atom a carbonyl group, and in which one ring carbon member may be replaced by a heteroatom from the series S, N and O,
- or one of the salts, solvates and solvates of the salts thereof
- to a human or animal patient in need thereof.
A method for controlling pulmonary hypertension in humans and animals comprising administering an effective amount of a medicament comprising at least one compound of formula
- in which
- R1 is 2-thiophene which is substituted in position 5 by a radical selected from the group of chlorine, bromine, methyl and trifluoromethyl,
- R2 is D-A-,
- where
- the radical “A” is phenylene,
- where
- the group “A” may be substituted where appropriate once or twice in the meta position relative to the linkage to the oxazolidinone by a radical selected from the group of fluorine, chlorine, nitro, amino, trifluoromethyl, methyl and cyano,
- and
- the radical “D” is a saturated 5- or 6-membered heterocycle which is linked via a nitrogen atom to “A” and has in the direct vicinity of the linking nitrogen atom a carbonyl group, and in which one ring carbon member may be replaced by a heteroatom from the series S, N and O,
- or one of the salts, solvates and solvates of the salts thereof
- in combination with an inert, non-toxic, pharmaceutically suitable excipient to a human or animal patient in need thereof.
Dependencies are inferred from the claim text.