1,3,7-Trisubstitued xanthine peripheral vasodilators
    1.
    发明授权
    1,3,7-Trisubstitued xanthine peripheral vasodilators 失效
    1,3,7-三位置黄嘌呤外周血管扩张剂

    公开(公告)号:US3998953A

    公开(公告)日:1976-12-21

    申请号:US641550

    申请日:1975-12-17

    摘要: Compounds of the formula ##STR1## wherein R is methyl or ethyl,R.sub.1 is methyl, ethyl or ##STR2## and R.sub.2 is methyl, ethyl, ##STR3## where Alk is alkyl of 1 to 4 carbon atoms,Q is ethyl, propyl, isopropyl or 2-hydroxy-propyl,A is 3-phenoxy-2-hydroxy-propyl, where the phenyl ring is substituted in the o-position by hydroxy, methoxy, n-hexyloxy or benzyloxy,B is alkyl of 1 to 4 carbon atoms, phenyl, p-methyl-phenyl, 3-phenyl-3-hydroxy-isopropyl or A, as defined above, andn is an integer from 2 to 6, inclusive,Provided, however, that one of R.sub.1 and R.sub.2 must be methyl or ethyl and the other has one of the other respective meanings indicated; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as peripheral vasodilators.

    摘要翻译: 其中R 1为甲基或乙基,R 1为甲基,乙基或R 2为甲基,乙基,其中Alk为1至4个碳原子的烷基, Q是乙基,丙基,异丙基或2-羟基丙基,A是3-苯氧基-2-羟基丙基,其中苯环在o位被羟基,甲氧基,正己氧基或苄氧基取代,B是 1至4个碳原子的烷基,苯基,对甲基 - 苯基,3-苯基-3-羟基 - 异丙基或A,如上所定义,N是2至6的整数,包括但不限于此 R 1和R 2必须是甲基或乙基,另一个具有所指示的其它各自的含义之一; 和无毒的,药学上可接受的酸加成盐。 化合物以及盐可用作外周血管扩张剂。

    Hydroxyphenylhydroxyalkylaminoalkyltheophyllines
    2.
    发明授权
    Hydroxyphenylhydroxyalkylaminoalkyltheophyllines 失效
    羟基苯甲酰基羟基烷基氨基甲酰氯

    公开(公告)号:US3728346A

    公开(公告)日:1973-04-17

    申请号:US3728346D

    申请日:1971-07-16

    申请人: DEGUSSA

    发明人: KLINGLER K

    CPC分类号: C07D473/08

    摘要: Compounds are prepared having the formula

    Where R1 and R2 are alkyl of one to four carbon atoms or one of them is hydrogen, R3 is hydrogen or alkyl of one to two and n is 1 or 2 or a salt thereof. The compounds have outstanding broncholytic activity.

    摘要翻译: 制备具有下式的化合物,其中R 1和R 2是1至4个碳原子的烷基或其中一个是氢,R 3是氢或一至二个的烷基,n是1或2或其盐。 该化合物具有优异的支气管分解活性。

    Pyridinecarbonyl derivatives of 7-(omega-(n-alkyl-n-optionally hydroxyalkyl substituted amino) - hydroxyalkyl)theophylline
    3.
    发明授权
    Pyridinecarbonyl derivatives of 7-(omega-(n-alkyl-n-optionally hydroxyalkyl substituted amino) - hydroxyalkyl)theophylline 失效
    7-(OMEGA-(N-烷基-N-选择性羟基烷基取代氨基) - 羟基烷基)的吡啶并吡啶衍生物THEOPHYLLINE

    公开(公告)号:US3565896A

    公开(公告)日:1971-02-23

    申请号:US3565896D

    申请日:1969-12-08

    IPC分类号: C07D473/08 C07D57/48

    CPC分类号: C07D473/08 Y10S514/826

    摘要: THE PRESENT PYRIDINECARBONYL DERIVATIVES OF 7-(W-(NALKYL-N-OPTIONALLY HYDROXYALKYL SUBSTITUTED AMINO)-HYDROXYALKYL)THEOPHYLLINE POSSESS DIURETIC, BRONCHIOLAR DILATING, MYOCARDINAL STIMULATING, SMOOOTH MUSCLE RELAXING, LIPOTROPIC AND VASODILATING ACTIVITY AND ARE USEFUL AS CARDIOTONIC AGENTS. THE COMPOUNDS ARE PREPARED BY REACTION OF THE CORRESPONDING 7 - (W - (N-ALKYLAMINO)-HYDROXYALKYL) THEOPHYLLINE OR 7-(W-(N-ALKYL-(-HYDROXYALKYLAMINO)-HYDROXYALKYL)THEOPHYLLINE WITH A PYRIDINECARBOXYLIC ACID OR A REACTIVE DERIVATIVE THEREOF SUCH AS THE PYRIDINECARBONYL HALIDES. ALTERNATIVELY THE COMPOUNDS CAN BE PREPARED BY REACTION OF THEOPHYLLINE WITH THE APPROPRIATE PYRIDINECARBONYL DERIVATIVE OF AN W-(N-ALKYL-N-OPTIONALLY HYDROXYALKYL SUBSTITUTED AMINO)-HYDROXYALKYL HALIDE OR BY REACTION OF AN APPROPRIATE 7-(W-HALO-HYDROXYALKYL)THEOPHYLLINE DERIVATIVE WITH THE APPROPRIATE SECONDARY AMINE.

    Dialkyl-xanthine derivatives
    7.
    发明授权
    Dialkyl-xanthine derivatives 失效
    二盐酸衍生物

    公开(公告)号:US3734911A

    公开(公告)日:1973-05-22

    申请号:US3734911D

    申请日:1970-03-23

    申请人: BESTIAN W

    发明人: BESTIAN W

    摘要: DIALKYL-XANTHINE DERIVATIVES INCLUDING THE PHARMACEUTICALLY ACCEPTABLE SALTS AND QUATERNARY AMMONIUM SALTS CHARACTERIZED BY THEIR CORONARY DILATING AND CENTRAL INHIBITING ACTIVITY AND HAVE THE FORMULA:

    A-CH2-CH(-O-R1)-CH2-N
    WHEREIN A DESIGNATES A 1,3-DIMETHYL-XANTHINE OR A 3,7,DIMETHYL-XANTHINE RADICAL, R1 AND R2 EACH DESIGNATE HYDROGEN, AN ALIPHATIC, CYCLOALIPHATIC, HETEROCYCLIC OR AROMATIC ACYL RADICAL, X DESIGNATES ALKYLENE HAVING 2 TO 3 CARBON ATOMS AND Y DESIGNATES ALKYLENE HAVING 2 TO 4 CARBON ATOMS,

    Theophylline derivatives
    9.
    发明授权
    Theophylline derivatives 失效
    THEOPHYLLINE衍生物

    公开(公告)号:US3896127A

    公开(公告)日:1975-07-22

    申请号:US37880673

    申请日:1973-07-13

    IPC分类号: C07D473/08 C07D57/48

    CPC分类号: C07D473/08 Y10S514/929

    摘要: Theophylline compounds of the formula,

    WHEREIN X is oxycarbonyl, carboxyl or carbonyl and R is a lower alkyl group containing from 1 to 5 carbon atoms which have excellent coronary vasodilating effects are produced by reacting a compound having the formula

    WHEREIN A is hydroxyl, or a carboxyl containing group or a halogenide, acid anhydride or ester thereof, with a compound having the formula

    WHEREIN B is hydrogen, hydroxyl, or a carboxyl containing group or a halogenide, acid anhydride or ester thereof, and R is defined as before.

    2-(n-cycloalkyl-phenylamino)-2-imidazolines-(2) and salts thereof
    10.
    发明授权
    2-(n-cycloalkyl-phenylamino)-2-imidazolines-(2) and salts thereof 失效
    2-(N-环己基 - 苯基)-2-咪唑啉酮(2)及其盐

    公开(公告)号:US3740401A

    公开(公告)日:1973-06-19

    申请号:US3740401D

    申请日:1970-11-18

    CPC分类号: C07D233/50

    摘要: COMPOUND OF THE FORMULA

    2-((CYCLOPENTYL)-N(-Y)-)-2-IMIDAZOLINE, OR 2-((CYCLO-

    HEPTYL)-N(-Z)-)-2-IMIDAZOLINE

    WHEREIN 1 IS 2,6-DICHLORO-PHENYL, 2-CHLORO-L-METHY6-PHENYL, 2CHLORO-4-METHYL-PHENYL, 2-METHYL-4-CHLORO-PHENYL,2CHLORO-PHENYL, 2,4-DICHLORO-PHENYL, 2-METHYL-PHENYL. 2,6-DIETHYL-PHENYL, 4-BROMO-PHENYL, 2,6- DICHLORO-4BROMO-PHENYL, 4-CYANO-PHENYL, 4-FLUORO-PHENYL OR 2-TRI FLUOROMETHYL-PHENYL, 2-METHOXY-4-CHLORO-PHENYL OR 2CHLORO-3-METHYL-PHENYL, AND Z IS

    (2-CL,6-R7-PHENYL)-

    WHERE R7 IS CHLORINE OR METHYL, AND THEIR NON-TOXIC, PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS, THE COMPOUNDS AS WELL AS THEIR SALTS ARE USEFUL AS ANALGESICS.