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    • 5. 发明授权
    • Circulation-active tetrahydropyridine-3-carbonitrile derivatives
    • 循环活性四氢吡啶-3-腈衍生物
    • US4885303A
    • 1989-12-05
    • US141363
    • 1988-01-04
    • Horst MeyerEckhard SchwennerAndreas Knorr
    • Horst MeyerEckhard SchwennerAndreas Knorr
    • C07D211/78C07D409/04
    • C07D409/04C07D211/78
    • Circulation active tetrahydropyridines of the formula ##STR1## in which R.sup.1 represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical which has up to 20 carbon atoms and can be interrupted in the chain by an oxygen atom or a sulphur atom and/or can be substituted by halogen, cyano, hydroxyl, acyloxy, nitro or nitrooxy, or by a phenyl, phenoxy, phenylthio or phenylsulphonyl group which is optionally substituted by halogen, cyano, dialkylamino with in each case 1 or 2 carbon atoms per alkyl group, alkoxy with 1 to 4 carbon atoms, alkyl with 1 to 4 carbon atoms, trifluoromethyl or nitro, or by an .alpha.-, .beta.- or .gamma.-pyridyl group, or by an amino group, this amino group carrying 2 identical or different substituents from the group comprising alkyl with up to 4 carbon atoms, alkoxyalkyl with up to 4 carbon atoms, phenyl and aralkyl, and these substitutents optionally forming, with the nitrogen atom, a 5- to 7-membered ring which can contain, as a further hetero atom, an oxygen or sulphur atom or an N-phenyl or N-alkyl grouping, this alkyl group containing 1 to 3 carbon atoms,R.sup.2 represents phenyl, naphthyl, thienyl, furyl, pyrryl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyridazinyl, pyrimidyl, pyrazinyl, indolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzoxadiazolyl, benzothiadiazolyl, quinolyl, isoquinolyl, quinazolyl or quinoxalyl;whereinm denotes a number from 0 to 2 and alkyl contains 1 to 4 carbon atoms with optionally 1 to 3 fluorine atoms,R.sup.3 represents a group of the formula --CN or --COOR.sup.5, whereinR.sup.5 has the same meaning as R.sup.1 and can be identical to or different from this radical, andR.sup.4 represents hydrogen, or represents phenyl or naphthyl, and their pharmaceutically acceptable acid addition salts.
    • 式“IMAGE”的循环活性四氢吡啶,其中R1表示直链,支链或环状,饱和或不饱和的烃基,其具有至多20个碳原子并且可以被氧原子或硫原子中断, 或可以被卤素,氰基,羟基,酰氧基,硝基或硝基氧基取代,或被任选被卤素,氰基,二烷基氨基取代的苯基,苯氧基,苯硫基或苯基磺酰基,在每种情况下,每个烷基具有1或2个碳原子 具有1至4个碳原子的烷氧基,具有1至4个碳原子的烷基,三氟甲基或硝基,或由α,β或γ-吡啶基或氨基组成,该氨基带有2个相同或不同的 含有至多4个碳原子的烷基,至多4个碳原子的烷氧基烷基,苯基和芳烷基的取代基,这些取代基任选地与氮原子一起形成5-至7-元环,其可以含有作为 furt 其杂原子,氧或硫原子或N-苯基或N-烷基,该含有1至3个碳原子的烷基,R 2表示苯基,萘基,噻吩基,呋喃基,吡咯基,吡唑基,咪唑基,恶唑基,异恶唑基, 噻唑基,吡啶基,哒嗪基,嘧啶基,吡嗪基,吲哚基,苯并咪唑基,苯并恶唑基,苯并异恶唑基,苯并恶二唑基,苯并噻二唑基,喹啉基,异喹啉基,喹唑啉基或喹喔啉基。 其中m表示0至2的数,烷基含有1至4个碳原子,可选地具有1至3个氟原子,R 3表示式-CN或-COOR 5的基团,其中R 5具有与R 1相同的含义并且可以相同 R 4表示氢,或表示苯基或萘基,以及它们的药学上可接受的酸加成盐。