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New 1H-pyrazolo(3,4-b)pyridine compounds are guanylate cyclase stimulators useful for treating and/or preventing e.g. heart failure, angina pectoris, hypertonia, pulmonary hypertonia, ischemia, vascular disease, and fibrotic disorder
专利权人:
BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
发明人:
FOLLMANN, MARKUS,STASCH, JOHANNES-PETER,REDLICH, GORDEN,ACKERSTAFF, JENS,GRIEBENOW, NILS,KNORR, ANDREAS,WUNDER, FRANK,MIN-JIAN LI, VOLKHART,KROH, WALTER,BAERFACKER, LARS
申请号:
DE102011003315
公开号:
DE102011003315A1
申请日:
2011.01.28
申请国别(地区):
DE
年份:
2012
代理人:
摘要:
Die vorliegende Anmeldung betrifft neue annellierte Pyrimidine und Triazine, 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.1H-Pyrazolo[3,4-b]pyridine compounds (I) or their N-oxides, salts, solvate, salts of N-oxide and solvates of N-oxides and salts, are new. 1H-Pyrazolo[3,4-b]pyridine compounds of formula (I) or their N-oxides, salts, solvate, salts of N-oxide and solvates of N-oxides and salts, are new. A : N or CR 3> R 3> : H, D, F, CHF 2, CF 3, (1-4C)-alkyl, cyclopropyl or cyclobutyl L : a-CR4AR4B-(CR5AR5B) p-b a : connection point at carbonyl group b : connection point to pyrimidine or triazine ring p : 0-2 either R4A, R5A : H, F, (1-4C)-alkyl or OH and R4B : H, F, (1-4C)-alkyl, CF 3, (1-4C)-alkoxy-carbonylamino or phenyl, where (1-4C)-alkyl is optionally substituted by 1 or 2 F, CF 3, OH, hydroxycarbonyl or (1-4C)-alkoxycarbonyl and R5B : H, F, (1-4C)-alkyl or CF 3 or R4AR4BC : 3-6 membered carbocyclic ring, 4-6 membered heterocyclic ring (both optionally substituted by 1 or 2 F or (1-4C)-alkyl), an oxo group or (2-4C)-alkenyl R 1> : H or F and R 2> : benzyl substituted by 1-3 F. Independent claims are included for: (1) the preparation of (I) (2) a 3-(1H-pyrazolo[3,4-b]pyridin-3-yl)-[1,2,4]triazin-5-ylamine compound of formula (XV) (3) a 3-(1H-pyrazolo[3,4-b]pyridin-3-yl)-[1,2,4]triazin-5-ol compound of formula (XIII) and (4) a medicament comprising (I), inert and non-toxic auxiliary agent and a further active agent, which is an organic nitrate, nitiric 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 Thrombolytic Antiarteriosclero
来源网站:
中国工程科技知识中心
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