FOLLMANN, MARKUS, DR.,Markus, Dr. Follmann,STASCH, JOHANNES-PETER, PROF. DR.,Johannes-Peter, Prof. Dr. Stasch,REDLICH, GORDEN,Gorden Redlich,ACKERSTAFF, JENS,Jens Ackerstaff,GRIEBENOW, NILS, DR.,Nils,
申请号：
DE102011007891
公开号：
DE102011007891A1
申请日:
2011.04.21
申请国别(地区):
DE
年份:
2012
代理人:
摘要：
Die vorliegende Anmeldung betrifft neue annellierte 4-Aminopyrimidine, Verfahren zu ihrer Herstellung, ihre Verwendung allein oder in Kombinationen zur Behandlung und/oder Prophylaxe von Krankheiten sowie ihre Verwendung zur Herstellung von Arzneimitteln zur Behandlung und/oder Prophylaxe von Krankheiten, insbesondere zur Behandlung und/oder Prophylaxe von Herz-Kreislauf-Erkrankungen.Ring-fused 4-aminopyrimidine compounds (I) and their N-oxides, salts, solvates, salts of N-oxides or solvates of N-oxides and salts, are new. Ring-fused 4-aminopyrimidine compounds of formula (I) and their N-oxides, salts, solvates, salts of N-oxides or solvates of N-oxides and salts, are new. A : 1-3C-alkandiyl (optionally substituted by 1 or 2 F, CF 3, OH, amino or 1-4C-alkyl (optionally substituted by 1-3 F, CF 3or OH)) or a cyclic group of formula (AA)； a : connection point with pyrimidine ring； b : connection point with the carbonyl group； R 1>； : H or F； R 2>； : 1-6C-alkyl (substituted by CF 3or optionally substituted by 1-3 F) or benzyl substituted by 1-3 F； and ring Q : 4-6 membered heterocyclic ring. Independent claims are included for: (1) the preparation of (I)； and (2) a medicament comprising (I) in combination with an inert, non-toxic auxiliary agent and a further active agent comprising organic nitrate, nitric oxide donors, cGMP-phosphodiesterase inhibitors, anti-thrombotic active agents, blood pressure lowering agents and/or fat metabolism modifying agent. [Image] ACTIVITY : Cardiant； Antianginal； Muscular-Gen.； Vasotropic； Nephrotropic； Thrombolytic； Antiarteriosclerotic； Antiarrhythmic； Antiparkinsonian； Antiinflammatory； Endocrine-Gen.； Antilipemic； Anorectic； Uropathic； Hypotensive； Respiratory-Gen.； CNS-Gen.； Nootropic； Neuroprotective； Cerebroprotective； Anticonvulsant； Antidepressant； Antibacterial； Immunosuppressive； Gastrointestinal-Gen.； Antiarthritic； Antirheumatic； Vulnerary； Hepatotropic； Virucide； Osteopathic； Ophthalmological. MECHANISM OF ACTION :
