1,4-Dihydropyridine hydroxyamines, process for the

专利名称：1,4-Dihydropyridine hydroxyamines, process

for their preparation and their use aspharmaceutical agents

发明人：TRIGGLE, DAVID, PROF. DR.,SCHWENNER,

ECKHARD, DR.,KINAST, GUNTHER,DR.,KAZDA, STANISLAV, DR.,KNORR,ANDREAS, DR.,GARTHOFF, BERNWARD, DR.

申请号：EP85113060.9申请日：19851015公开号：EP0179386A2公开日：19860430

摘要：1. Compounds of the general formula (I) see diagramm : EP0179386,P26,F3 inwhich R represents phenyl, pyridyl or the benzoxadiazolyl radical, the phenyl radicalcontaining 1 or 2 identical or different substituents from the group comprising nitro,trifluoromethyl, fluorine, chlorine and cyano, R**1 and R**3 are identical of different andeach represent alkyl with 1 to 4 carbon atoms, or one of the substituents R**1 or R**3represents hydroxymethyl, amino or cyano, R**2 represents hydrogen or alkyl with 1 or 2carbon atoms, A either represents an alkylene group which has up to 12 carbon atomsand is substituted by methyl, ethyl or propyl, and which is optionally substituted orinterrupted by a phenyl group and/or is optionally interrupted by an oxygen or sulphuratom or a grouping of the formula -NR**6 , or A represents a straight-chain or branchedalkylene group which has up to 12 carbon atoms and is optionally interrupted by anoxygen or sulphur atom or a grouping of the formula -NR**6 when a) R**4 represents

phenyl, benzyl, CO-R**6 , CO2 -R**6' , CO-NR**6 R**7 , SO2 R6 or -CH2 -CHOH-CH2 -OR**8, or b) R represents pyridyl or benzoxadiazolyl, or c) R**5 represents indolyl, or d) thealkylene chain is interrupted by a sulphur atom or the group -NR**6 or e) X representsCOR**9 , wherein R**6 und R**7 are identical or different and each represent hydrogen,alkyl with up to 4 C atoms, benzyl or phenyl and wherein R**8 has the meaning given forR**5 and can be identical or different from this radical wherein R**9 represents alkylwhich has 1 to 7 C atoms and is optionally substituted by halogen, cyano, alkoxy ordialkylamino with in each case 1-4 C atoms, or denotes phenyl, naphthyl, phenylalkyl oranilino or an amino, monoalkylamino or dialkylamino group with in each case 1 to 4 Catoms, the alkyl groups optionally forming, with the nitrogen atom a 5-membered to 7-membered ring which can contain an oxygen atom as a further hetero-atom and whereinR**6' has the meaning of R**6 , but does not denote hydrogen, R**4 representshydrogen, or represents straight-chain or branched alkyl with 1 to 3 carbon atoms, orrepresents phenyl or benzyl, or represents a radical of the formula CO-R**6 , CO2 -R**6' ,CO-NR**6 R**7 , SO2 -R**6 or -CH2 -CHOH-CH2 -OR**8 , wherein R**6 , R**6' , R**7 , R**8und R**9 have the abovementioned meaning, R**5 represents phenyl, naphthyl or indolyl,the phenyl radical optionally being substituted by 1 or 2 identical or different

substituents from the group comprising fluorine, chlorine, nitro, cyano, alkyl with 1 or 2 Catoms, NR**6 , R**7 , NR**6 COR**7 , the group CH2 -CO-NH2 or acetyl and X representsthe group COOR**10 , wherein R**10 represents a straight-chain, branched or cyclic alkylradical which has up to 12 C atoms and is optionally interrupted in the chain by an oxygenatom and/or is optionally substituted by fluorine, chlorine, hydroxyl, pyridyl, phenyl oramino, or represents the group COR**9 , wherein R**9 has the abovementioned meaning,and pharmaceutically acceptable acid addition salts thereof.

申请人：BAYER AG

地址：51368 Leverkusen DE

国籍：DE

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