FOLLMANN, MARKUS, DR.,Markus, Dr. Follmann,STASCH, JOHANNES-PETER, PROF. DR.,Johannes-Peter, Prof. Dr. Stasch,REDLICH, GORDEN,Gorden Redlich,GRIEBENOW, NILS, DR.,Nils, Dr. Griebenow,WUNDER, FRANK,Fran
申请号：
DE102011007890
公开号：
DE102011007890A1
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 Fluoralkyl-substituierte Pyrazolopyridine, 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.Fluoroalkyl-substituted pyrazolopyridine compounds (I) are new. Fluoroalkyl-substituted pyrazolopyridine compounds of formula (I) and their N-oxides, salts, solvates, salts of N-oxides and solvates of the N-oxides or their salts are new. A : N or CR3； R3 : H, D, F, difluoromethyl, trifluoromethyl, 1-4C-alkyl, cyclopropyl or cyclobutyl； L : a1-CR4AR4B-(CR5AR5B) p-a2； a1 : point of attachment to the carbonyl group； a2 : point of attachment to the pyrimidine or triazine ring； p : 0-2； either R4A : H, F, 1-4C-alkyl, hydroxy or amino； and R4B : H, F, 1-4C-alkyl (optionally substituted with 1-3 substituents comprising F, trifluoromethyl, hydroxy, hydroxycarbonyl or 1-4C-alkoxycarbonyl), trifluoromethyl, 1-4C-alkoxycarbonylamino or phenyl； or R4A+C+R4B : 3-6 membered carbocycle or 4-6 membered heterocycle (both optionally substituted with 1 or 2 substituents comprising F or 1-4C-alkyl), oxo-group or 2-4C-alkenyl； R5A : H, F, 1-4C-alkyl or hydroxy； R5B : H, F, 1-4C-alkyl or trifluoromethyl； R1 : H or F； R2 : a3-(CR6AR6B) qCF 3； a3 : point of attachment to the pyrazolopyridine； R6A, R6B : H or F； and q : 1-3. Independent claims are included for: (1) the preparation of (I)； and (2) a drug comprising (I) in combination with further active agents comprising organic nitrates, nitric oxide donors, cyclic guanosine monophosphate-phosphodiesterase inhibitors, antithrombotic agents, blood pressure lowering agents or lipid modifying agents. [Image] ACTIVITY : Cardiant； Antianginal； Hypotensive； Respiratory-Gen.； Vasotropic； Nephrotropic； Thrombolytic； Antiinflammatory； Antiarterioscleroti
