New 2-pyridin-2-yl-pyrazol-3(2H)-one compounds are hypoxia inducible factor activators, useful for the treatment of hypertension, heart failure, diabetes, anemia, angina pectoris or myocardial infarction and pulmonary hypertension

摘要

2-Pyridin-2-yl-pyrazol-3(2H)-one compounds (I) and their base or acid addition salts are new. 2-Pyridin-2-yl-pyrazol-3(2H)-one compounds of formula (I) and their base or acid addition salts are new. n : 1-4; m, o : 0 or 1; X : -CHR1a-, -NHR1a-, or heteroatom comprising O or S; R1a : 1-5C alkyl, 1-5C alkoxy, -CH 2-aryl, -COR 5> or -COOR 5>; R 1> : oxo; R 2> : H, 1-5C alkyl, 1-5C alkoxy, -COOR 5>, NR 5>R 6>, CONR 5>R 6>, or SO 2NR 3>R 4>; either R 3>, R 4> : H, 1-5C alkyl, 3-6C cycloalkyl, (hetero)aryl, -CH 2-heteroaryl, -1-5C alkyl-NR 5>R 6>; or NR 3>R 4> : heterocycloalkyl optionally substituted by 1-5C alkyl or -CH 2-aryl; and R 5>, R 6> : H or 1-5C alkyl. Independent claims are included for: (1) the preparation of (I); (2) a combination of (I) with other active compounds useful in the treatment of hypertension, heart failure, diabetes and anemia; and (3) phenyl-hydrazine ester compounds of formula (IVa) or (IVb). [Image] [Image] ACTIVITY : Cardiovascular-Gen.; Vasotropic; Cardiant; Antianginal; Antiarteriosclerotic; Cerebroprotective; Hypotensive; Respiratory-Gen.; Antidiabetic; Antianemic; Ophthalmological; Nephrotropic; Neuroprotective. MECHANISM OF ACTION : Hypoxia inducible factor (HIF) activator. Tests details are described but no results given.