EP 2037930 A1 20090325 - THE USE OF 1,4-DIARYL-DIHYDROPYRIMIDINE-2-ON DERIVATIVES FOR TREATING PULMONARY ARTERIAL HYPERTENSION
Title (en)
THE USE OF 1,4-DIARYL-DIHYDROPYRIMIDINE-2-ON DERIVATIVES FOR TREATING PULMONARY ARTERIAL HYPERTENSION
Title (de)
VERWENDUNG VON 1,4-DIARYL-DIHYDROPYRIMIDIN-2-ON-DERIVATEN ZUR BEHANDLUNG DER PULMONALEN ARTERIELLEN HYPERTONIE
Title (fr)
UTILISATION DE DÉRIVÉS DE 1,4-DIARYL-DIHYDROPYRIMIDIN-2-ONE POUR LE TRAITEMENT DE L'HYPERTENSION ARTÉRIELLE PULMONAIRE
Publication
Application
Priority
- EP 2007005579 W 20070625
- DE 102006031314 A 20060701
Abstract (en)
[origin: DE102006031314A1] Use of 1,4-diaryl-dihydropyrimidin-2-one derivative (I) or its salts, solvates or solvates of the salts, for producing a medicament for the treatment and/or prophylaxis of pulmonary arterial hypertension. Use of 1,4-diaryl-dihydropyrimidin-2-one derivative of formula (I) or its salts, solvates or solvates of the salts, for producing a medicament for the treatment and/or prophylaxis of the pulmonary arterial hypertension. R 1>H, -(CH 2) nC(=O)-O-R 5> or benzoic acid of formula (a) or (b); R 5>H or 1-4C-alkyl; R 2>CN or -C(=O)-R 6> or -C(=O)-O-R 6>; R 6>1-6C-alkyl or 3-6C-cycloalkyl (which is partially or substituted two times with hydroxy, 1-4C-alkoxy, hydroxycarbonyl, amino, mono- and/or di-1-4C-alkylamino, where respectively, CH 2 is replaced with an O-atom); R 3>, R 4>H, F or Cl; X : CH or N; and asterisk : connecting place with the N-atom. Independent claims are included for: (1) a combination comprising (I) and an active substance from kinase-inhibitor, stimulator and activator of the soluble guanylate cyclase, prostacyclin-analogues, endothelium receptor-antagonist and phosphodiesterase-inhibitors; (2) a medicament comprising the combination; and (3) method for the treatment and/or prophylaxis of the pulmonary arterial hypertension with humans and animals by administering (I), the combination or the medicament in combination with inert, non-toxic auxiliary materials. [Image] ACTIVITY : Hypotensive; Respiratory-Gen; Vulnerary; Respiratory-gen.; CNS-Gen; Thrombolytic; Antiinflammatory. MECHANISM OF ACTION : Neutrophile elastase inhibitor. The neutrophile elastase inhibitory activity of (I) was tested using human neutrophile elastase. The result showed that (I) exhibited a median inhibitory concentration (IC 5 0) of 14.8 nM.
IPC 8 full level
A61K 31/513 (2006.01); C07D 239/22 (2006.01); C07D 401/02 (2006.01)
CPC (source: EP)
A61P 9/12 (2017.12); A61P 11/00 (2017.12); A61P 43/00 (2017.12); C07D 239/22 (2013.01)
Citation (search report)
See references of WO 2008003412A1
Citation (examination)
PETKOV V: "Pulmonary hypertension", JOURNAL FUER HYPERTONIE, vol. 7, no. 3, 2003, pages 7 - 15
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC MT NL PL PT RO SE SI SK TR
Designated extension state (EPC)
AL BA HR MK RS
DOCDB simple family (publication)
DE 102006031314 A1 20080103; CA 2656307 A1 20080110; EP 2037930 A1 20090325; JP 2009541384 A 20091126; WO 2008003412 A1 20080110
DOCDB simple family (application)
DE 102006031314 A 20060701; CA 2656307 A 20070625; EP 07764815 A 20070625; EP 2007005579 W 20070625; JP 2009516962 A 20070625