Circulation-active tetrahydropyridine-3-carbonitrile derivatives
    26.
    发明授权
    Circulation-active tetrahydropyridine-3-carbonitrile derivatives 失效
    循环活性四氢吡啶-3-腈衍生物

    公开(公告)号:US4885303A

    公开(公告)日:1989-12-05

    申请号:US141363

    申请日:1988-01-04

    IPC分类号: C07D211/78 C07D409/04

    CPC分类号: C07D409/04 C07D211/78

    摘要: 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.

    摘要翻译: 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。

    Antihypertensive combination products containing a dihydropyridine and a
pyridazodiazepine
    27.
    发明授权
    Antihypertensive combination products containing a dihydropyridine and a pyridazodiazepine 失效
    含有二氢吡啶和吡咯并二氮杂的抗高血压组合产品

    公开(公告)号:US4859665A

    公开(公告)日:1989-08-22

    申请号:US937867

    申请日:1986-12-02

    IPC分类号: A61K31/50 A61K31/55 A61P9/12

    CPC分类号: A61K31/55 Y10S514/929

    摘要: Compositions for treating hypertension comprising an effective amount of a dihydropyridine of the formula ##STR1## in which X is 1 or 2 identical or different substituents from the group consisting of nitro, chlorine and trifluoromethyl, or together with the phenyl ring, the group ##STR2## R.sup.1 is alkyl of 1 to 4 C atoms, which is optionally substituted by alkoxy of 1 to 4 C atoms,R.sup.2 is alkyl of 1 to 12 C atoms, which is optionally substituted by alkoxy of 1 to 3 C atoms, fluorine or N-methyl-N-benzylamino andR.sup.3 is alkyl of 1 to 4 C atoms, cyano or hydroxymethyl, and a pyridazodiazepine of the formula ##STR3## in which R.sup.4 is aralkyl,R.sup.5 is hydrogen or alkyl of 1 to 8 C atoms,R.sup.6 is hydrogen or alkyl of 1 to 8 C atoms andR.sup.7 and R.sup.8 are hydrogen, or together, an oxo group, are described.

    摘要翻译: 用于治疗高血压的组合物,其包含有效量的式“IMAGE”的二氢吡啶,其中X是与硝基,氯和三氟甲基相同或不同的取代基,或与苯环一起,组IMA IMA > R 1为1〜4个C原子的烷基,其任选被1〜4个C原子的烷氧基取代,R 2为1〜12个C原子的烷基,其任选被1〜3个C原子的烷氧基取代,氟或N - 甲基-N-苄基氨基,R3为1-4个C原子的烷基,氰基或羟甲基,以及其中R 4为芳烷基,R 5为氢或1至8个C原子的烷基的式“IMAGE”的吡咯并二氮杂为R6 氢或1〜8个碳原子的烷基,R7和R8为氢,或一起为氧代基。

    Vaso-dilating and coronary active 4-nitrophenyl-tetrahydropyridines
    28.
    发明授权
    Vaso-dilating and coronary active 4-nitrophenyl-tetrahydropyridines 失效
    血管扩张和冠状动脉的4-硝基苯基 - 四氢吡啶类

    公开(公告)号:US4621093A

    公开(公告)日:1986-11-04

    申请号:US720668

    申请日:1985-04-08

    CPC分类号: C07D211/78 C07D211/90

    摘要: 4-(Nitrophenyl)-1,2,3,4-tetrahydropyridines of the formula ##STR1## in which R.sub.1 and R.sub.2 are identical or different and each represent hydrogen, phenyl or a straight-chain or branched alkyl radical which is optionally substituted by halogen or alkoxy,R.sub.3 represents a straight-chain or branched alkyl radical which is optionally substituted by alkoxy, halogen, alkylamino or aryl,X represents a single bond, an oxygen atom, a sulphur atom or the NH group andY denotes either the nitrile group or the radical ##STR2## wherein X' corresponds to the definition of X and can either be identical to X or different from X, andR.sub.4 corresponds to the definition of R.sub.3 and can be either identical to R.sub.3 or different from R.sub.3,or physiologically acceptable salts thereof, which are active on the circulation system, for example as vasodilators.

    摘要翻译: 式(Ⅰ)的4-(硝基苯基)-1,2,3,4-四氢吡啶,其中R 1和R 2相同或不同,各自表示氢,苯基或直链或支链烷基, 任选被卤素或烷氧基取代,R 3表示任选被烷氧基,卤素,烷基氨基或芳基取代的直链或支链烷基,X表示单键,氧原子,硫原子或NH基,Y表示 腈基或基团“IMAGE”,其中X'对应于X的定义,并且可以与X相同或不同于X,并且R4对应于R3的定义,并且可以与R3相同或不同于R3 或其生理上可接受的盐,其在循环系统上是有活性的,例如作为血管扩张剂。

    Certain nitratoalkyl ester dihydropyridines having antihypertensive
properties
    29.
    发明授权
    Certain nitratoalkyl ester dihydropyridines having antihypertensive properties 失效
    某些具有抗高血压特性的硝基烷基酯二氢吡啶类

    公开(公告)号:US4565824A

    公开(公告)日:1986-01-21

    申请号:US550321

    申请日:1983-11-09

    CPC分类号: C07D211/90

    摘要: Dihydropyridines of the formula ##STR1## in which R is aryl or heterocyclic,R.sup.1, R.sup.2 and R.sup.3 each is hydrogen or various organic radicals,Y is oxygen, or optionally substituted --NH--,Z is --O--NO.sub.2 or --O--NO,X is --COR.sup.4, --COOR.sup.5 or --CO--Y--A--Z,R.sup.4 is alkyl, phenyl, benzyl or an amino radical, andR.sup.5 is an organic radical,or pharmaceutically acceptable acid addition salts thereof, exhibit circulation active properties, e.g. they can be used as antihypertensives, as peripheral and cerebral vasodilators and as coronary therapeutics.

    摘要翻译: 式中,R为芳基或杂环,R 1,R 2和R 3各自为氢或各种有机基团,Y为氧或任选取代的-NH-,Z为-O-NO 2或-O-NO X为-COR 4,-COOR 5或-CO-YAZ,R 4为烷基,苯基,苄基或氨基,R 5为有机基团或其药学上可接受的酸加成盐,具有循环活性,例如 它们可以作为抗高血压药物,作为外周血脑血管扩张剂和冠脉治疗药。