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דיהידרותיאנופירימידינים לטיפול במחלות דלקתיות ושימושים בהם
专利权人:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人:
申请号:
IL18674907
公开号:
IL186749A
申请日:
2007.10.18
申请国别(地区):
IL
年份:
2014
代理人:
摘要:
Dihydrothienopyrimidine derivatives (I) are new. Dihydrothienopyrimidine derivatives of formula (I) and their salts, diastereomers, enantiomers, racemates, hydrates or solvates are new. X : O, S, SO or SO 2; either R 1>; : H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 6-10C aryl or 6-10C aryl-1-6C-alkylene, 5-10C heteroaryl-1-6C-alkylene; and R 2>; : 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl (all optionally substituted), optionally one or more bridged mono- or bicyclic 3-10C cycloalkyl, 6-10C aryl, aromatic or non-aromatic, 3-10C heterocyclic ring, a bicyclic ring or 3-10C heterocycle condensed 6-10C aryl, or H; or NR 1>;R 2>; : heterocyclic ring, optionally with one or more of 1-4C-alkyl, 2-6C-alkenyl, 2-6C-alkynyl, 1-6C alkanol or oxo; R 3>; : 6-10C heterocyclic ring, 3-7C cycloalkyl, 6-10C aryl-1-6C alkylene, 5-10C heteroaryl-1-6C-alkylene, a condensed bicyclic ring (optionally containing 1-4 heteroatoms of N, O or S), optionally substituted phenyl, COR 37>;, COCH 2R 38>;, CONHR 38>; or SO 2R 38>;; R 37>; : H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl or 6-10C aryl; R 38>; : 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, 3-7C cycloalkyl, 6-10C aryl, 3-10C heterocyclic ring and a bicyclic ring, optionally substituted with one or more of 1-6C-alkyl, 2-6C alkenyl, 2-6C alkynyl, halo, NR-38aR-38b, 6-10C aryl or 3-10C heterocyclic ring; R-38a, R-38b : H, 1-6C alkyl, 2-6C alkenyl or 2-6C alkynyl; R 4>; : H, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl or oxo; R 5>;, R 6>; : H, 1-4C alkyl, 2-4C alkenyl or 2-4C alkynyl; and either R 7>;, R 8>; : H, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 6-10C aryl or OH; or R 7>;+R 8>; : oxo. An independent claim is included for 50 intermediate compounds e.g. pyrimidine derivatives of formula (VIII), (IV) or (V). [Image] [Image] ACTIVITY : Respiratory-Gen.; Gastrointestinal-Gen.; Antiinflammatory; Cytostatic; CNS-Gen.; Antiasthmatic; Antiulcer.Antidepressant; Neuroleptic; Antimanic; Neuroprotective; Nootropic; Antiparkinso
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