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SPIROCYCLIC HETEROCYCLES, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND METHOD FOR THEIR PRODUCTION
专利权人:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人:
HIMMELSBACH, FRANK,JUNG, BIRGIT,LOTZ, RALF
申请号:
NZ58658209
公开号:
NZ586582A
申请日:
2009.02.05
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are spiro (4-(phenylamino)-quinazolin-6-yloxy)-cyclohexane derivatives as represented by the general formula (I), wherein: Ra denotes an optionally substituted phenyl or 1-phenylethyl group A denotes >C(=O) or an optionally substituted alkylene group and wherein the remaining substituents are as defined herein optionally in the form of the tautomers, the racemates, the enantiomers, the diastereoisomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts thereof. Further disclosed is a pharmaceutical formulation which contains a compound of formula (I) as defined above, and which may be formulated for oral administration and wherein said pharmaceutical formulation is for the treatment or prevention of an inflammatory or allergic disease of the airways, and particularly for diseases such as chronic bronchitis, acute bronchitis, bronchitis caused by bacterial or viral infection or fungi or helminths, allergic bronchitis, toxic bronchitis, chronic obstructive bronchitis (COPD), asthma (intrinsic or allergic), paediatric asthma, bronchiectasis, allergic alveolitis, allergic or non-allergic rhinitis, chronic sinusitis, cystic fibrosis or mucoviscidosis, alpha-1-antitrypsin deficiency, cough, pulmonary emphysema, interstitial lung diseases, alveolitis, hyperreactive airways, nasal polyps, pulmonary oedema, pneumonitis of different origins, etc. Representative compounds of formula (I) include syn/anti-8-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy-quinazolin-6-yloxy]-1,3-diaza-spiro[4.5]decan-2,4-dione, anti-9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy-quinazolin-6-yloxy]-1,4-diaza-spiro[5.5]undecan-5-one, anti-9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy-quinazolin-6-yloxy]-4-methyl-1,4-diaza-spiro[5.5]undecan-5-one, anti-9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy-quinazolin-6-yloxy]-1,4-dimethyl-1,4-diaza-spiro[5.5]undecan-5-one and syn/anti-8-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy-quinazolin-6-yloxy]-1,3-d
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