New substituted heteroaryl compounds are hypoxia-inducible factor prolyl-4-hydroxylase inhibitors useful to treat and/or prevent e.g. circulatory heart diseases, heart failure, anemia, chronic kidney diseases and renal failure

摘要

Substituted heteroaryl compounds (I) and their salts, solvates or solvates of the salts, are new. Substituted heteroaryl compounds of formula (I) and their salts, solvates or solvates of the salts, are new. A : O or S; D 1N or CR 3; R 3H, (1-6C)-alkyl or (3-7C)-cycloalkyl; R 1phenyl, 5- or 6-membered heteroaryl, naphthyl or 8-10-membered heteroaryl (optionally substituted); either m, n : 0-3; or m+n : greater than 4; R2a, R2b, R2c, R2d : H, F, (1-4C)-alkyl, CF 3, OH, (1-4C)-alkoxy or amino; L : e.g. O, S, SO 2, C(=O)-O or O-C(=O); and Het 1, Het 2heteroaryl groups. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. [Image] ACTIVITY : Cardiant; Antianemic; Nephrotropic; Cardiovascular-Gen.; Vasotropic; Antianginal; Cerebroprotective; Antiarteriosclerotic; Muscular-Gen.; Antimicrobial; Anti-HIV; Antiinflammatory; Antiarthritic; Antirheumatic; Respiratory-Gen.; Cytostatic; Immunosuppressive; Ophthalmological; Antiparkinsonian; Neuroprotective; Nootropic; Analgesic; Anabolic; Endocrine-Gen.; Antidiabetic; Vulnerary; Hepatotropic. MECHANISM OF ACTION : Hypoxia-inducible factor prolyl-4-hydroxylase inhibitor. The ability of (I) to inhibit hypoxia-inducible factor prolyl-4-hydroxylase was tested in vitro. The results showed that (I) exhibited an IC 5 0value of = 30 mu M.