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Annellierte 4-Aminopyrimidine und ihre Verwendung
专利权人:
BAYER SCHERING PHARMA AG
发明人:
Erfinder wird später genannt werden
申请号:
DE102010031148
公开号:
DE102010031148A1
申请日:
2010.07.09
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.1-(2-Fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridine compounds (I) and their N-oxides, salts, solvates, salts of N-oxides or solvates of N-oxides and salts, are new. 1-(2-Fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridine 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 3or 1-4C-alkyl) or a cyclic group of formula (AA) a : connection point with pyrimidine ring b : connection point with the carbonyl group ring Q : 4-6 membered heterocycle, preferably azetidinyl, oxetanyl, pyrrolidinyl, tetrahydrofuranyl, piperidinyl or tetrahydropyranyl ring and R 1>H or F. 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. - ACTIVITY : Cardiant Antianginal Muscular-Gen. Vasotropic Thrombolytic Antiarteriosclerotic Antiarrhythmic Antiparkinsonian Antiinflammatory Endocrine-Gen. Antilipemic Anorectic Uropathic Nephrotropic Neuroprotective Hypotensive Respiratory-Gen. CNS-Gen. Nootropic Cerebroprotective Anticonvulsant Antidepressant Antibacterial Immunosuppressive Gastrointestinal-Gen. Antiarthritic Antirheumatic Vulnerary Hepatotropic Virucide Osteopathic Ophthalmological. - MECHANISM OF ACTION : Guanylate cyclase stimulator. The ability of (I) to stimulate guanylate cyclase w
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