• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    Compounds of the formula <IMAGE> wherein A is =CH- or =N-; R1 is (a) hydrogen, lower alkyl, lower alkoxy or a fused benzene ring, or (b) -CO-R4, tetrazol-5-yl or cyano in the 4- or 5-position; R2 is -CO-R4, tetrazol-5-yl, cyano or, when R1 has one of the meanings included in (b), also hydrogen, lower alkyl, lower alkoxy or a fused benzene ring; R3 is hydrogen or lower alkanoyl; and R4 is hydroxyl, amino, hydroxy-amino, tetrazol-5-yl-amino or lower alkoxy; internal salts thereof, and non-toxic salts thereof formed with a basic substance. The compounds as well as their salts are useful as antiallergics.
    公开号:SU886743A3
    申请号:SU792765447
    申请日:1979-05-21
    公开日:1981-11-30
    发明作者:Шромм Курт；Ментруп Антон；Рент Эрнст-Отто；Фюгнер Армин；Якоби Фолькер
    申请人:К.Х.Берингер Зон (Фирма)；
    IPC主号:
    专利说明:

    (54) METHOD FOR OBTAINING SALTS OF ALKALINE METALS DERIVATIVES
    2-PIRIDSh1-OR a-pyrimidyl-amino-benzoic acid 38 is subjected to alkaline interaction and the target product is isolated as an alkali metal salt. Target products can be used for therapeutic purposes, for example, as anti-allergic agents, for the treatment of allergic diseases such as asthma, senile fever, conjunctivitis, nettle fever, eczema, and atonic dermatat. The novel compounds, in addition, have bronchodilatory and vasodilating effects. Example 1. Disodium salt of 4- (2-pyridylamino-isophthalic acid. 5.24 g of cathrium salt II-H-11-oxo-pyrido-2, 1-in quinazoline-2-carboxylic acid and 20 ml of 1N; sodium hydroxide The water is aggravated in a water bath for 1 h. The resulting clear yellow solution is removed and the azeotrope with chloroform is removed. The crystals obtained are suspended in a small amount of ether, filtered and dried in a vacuum at 4.86 g (72% of the Theoretical. Calculated,%: C 46.15; H 55; N 8.28; 10.65. Found,%: C 46.04; H 3.34 |: MB, 15; 11.1 &amp; UV-UVHelup log4.18 4.30 Example 2. Di atrieva sol 2- (2-pyridylamins) -5- (. 1 H-tetrazol-5g-yl) -benzoic acid. 8 g of P-H-11-oxopyrido-f 2,1-BJ-2- (1H-tetrazole-5 -yl-quinazoline and 60.6 ml of I H. sodium hydroxide are heated to 70 ° C for 2 hours, water is distilled off and the crystals are suspended in a small amount of ether, filtered and dried under vacuum.You gives 76% of theoretical} Calculated%: C 41.05; H 3.68; N22.10.;, HgW. X MN ,, 0 Iideko,%: C 41.98; H 3.54; And 22.18. UV spectrum: Hu YAH, nm 290 317 dogge 4.24 4.27 Example 3. Dikaliev salt of 4- (. 2-pyrindylamino) -isophthalic acid. 5.56 g (about, 02 mol of potassium salt 11-N-1 Noxo-pyrido-p, IB quinazoline-2-carboxylic acid is heated for 1 hour with 20 ml of potassium hydroxide. Water is azeotropically removed from the corresponding solution. Residue Suspended in ether, sucked off and existed at 60 ° C. The yield of the compound is 85%. UV spectrum: A, α1HM 288 328 log g 4.18 4.30 The sodium salt of the compounds listed in the table is obtained in the same way.
    f
    HH-
    (JOOdH;
    4.18
    80 4.40
    4- (2-Quinolinylamino) isophthalic acid
    Nz y xx-CJOOH .j j ss x CJOOH
    chakn-4, 25 84
    320
    left acid 4- (5-Acetamido-.2-eH-pyridiAmino) -iso-, -pmpyN minh 1 phthalic acid
    Irodol Table (J-NK. ,, HDOd, C.OOH,, and I TVt and .Lo 4.25. -L 4.30. L MoHo-N- (w-tetraf zolg3-yl-carboxamide 4- (2-pyridylWx JJHamino) - isophthalic, acid
    Hood ,,, / g
     VCOOH
    jT
    f -NH886743
    8 Continuation of the table.
    Hood
    4.30 75
    325
    54.6
    with the UN
    4.18
    78.4 4.30
    sbon
    2.24
    290
    65, P: F- K b-iJH-f 11 to
    权利要求:
    Claims (1)
    [1]
    Invention Formula
    Method for preparing alkali metal salts of 2-pyridyl- or 2-pyrimidylaminobenzoic acid derivatives of general formula I
    TERM
    a benzene ring or a —CO — R group at the 4 or 5 position of the ring;
     rpyjtina -CO-DCH tetrazol-5-yl, cyan in the 4th or 5th position of the benzene Ring shsh, if R is a -COR group, then R is hydrogen, methyl, methoxy, or a condensed benzene ring;
    ft is hydroxy, amino, hydroxyamino, tetrazol-5-yl-amino or methoxy, characterized in that the compound of general formula 11
    wherein
    A - group GSN- or
    R is hydrogen, methyl, methoxy, amino, acetamino, condensed.
    988674. , 0
    where l yfl and a have the indicated value - sources of information,
    nor, is interacting with shch-. taken into account when examining with a scab and the target product is singled out in 1. Great Britain Patent No. 1064259, in the form of an alkali metal salt. C 071 31/24, published 1967.
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    同族专利:
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    ES480622A1|1980-01-01|
    IE47228B1|1984-01-25|
    NZ188101A|1981-01-23|
    YU191678A|1983-01-21|
    GB2002764B|1982-08-04|
    PL208942A1|1979-12-03|
    BG30472A1|1981-06-15|
    AU3877278A|1980-02-14|
    NL7808319A|1979-02-13|
    US4241068A|1980-12-23|
    DK148019B|1985-02-04|
    PT68407A|1978-09-01|
    FI71555B|1986-10-10|
    YU40832B|1986-06-30|
    NO152605B|1985-07-15|
    AU520240B2|1982-01-21|
    DD140351A5|1980-02-27|
    FI782039A|1979-02-11|
    ES475456A1|1979-05-01|
    MX5672E|1983-12-08|
    DK148019C|1985-07-01|
    DE2735919C2|1988-10-27|
    CS202506B2|1981-01-30|
    CH649289A5|1985-05-15|
    ES480623A1|1980-01-01|
    ES475457A1|1979-11-16|
    LU80094A1|1979-09-07|
    HU179933B|1983-01-28|
    FR2400017A1|1979-03-09|
    IT7850642D0|1978-08-08|
    IE781618L|1979-02-10|
    PL115778B1|1981-04-30|
    NO782707L|1979-02-13|
    SE7808530L|1979-02-11|
    SE444170B|1986-03-24|
    FI71555C|1987-01-19|
    BE869640A|1979-02-09|
    NO152605C|1985-10-23|
    ATA549278A|1982-08-15|
    GB2002764A|1979-02-28|
    ES472143A1|1979-03-16|
    DK351978A|1979-02-11|
    JPS5430177A|1979-03-06|
    PH19117A|1986-01-06|
    ZA784501B|1980-04-30|
    SU735168A3|1980-05-15|
    IT1107960B|1985-12-02|
    GR65024B|1980-06-16|
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    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    FR4267M|1963-12-19|
    GB1162287A|1967-11-07|1969-08-20|Union Pharma Scient Appl|New Salts of 2-Anilino-Nicotinic Acids|
    GB1264798A|1968-07-10|1972-02-23|
    ES416847A1|1973-07-12|1976-03-01|Hermes Sa Lab|2-Anilino-nicotinic acids - as analgesic antiinflammatory and antipyretic agents|DE3100516A1|1981-01-10|1982-08-12|C.H. Boehringer Sohn, 6507 Ingelheim|PYRIDYLAMINOBENZOESAEUR, THEIR PRODUCTION AND USE|
    FR2533567B1|1982-09-23|1985-01-18|Ki I Farmakologii|
    US4610991A|1983-04-18|1986-09-09|Sterling Drug Inc.|Antihypertensive pyridylaminobenzamide compounds|
    JPH0336835B2|1983-11-05|1991-06-03|Morishita Pharma|
    US4584379A|1985-01-22|1986-04-22|Merrell Dow Pharmaceuticals Inc.|Isoquinoline thromboxane synthetase inhibitors|
    EP0219308B1|1985-10-16|1991-10-23|Merck Frosst Canada Inc.|2-substituted quinolines|
    GB9615950D0|1996-07-30|1996-09-11|Univ Warwick|Variable reluctance machines|
    US6022884A|1997-11-07|2000-02-08|Amgen Inc.|Substituted pyridine compounds and methods of use|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    DE2735919A|DE2735919C2|1977-08-10|1977-08-10|
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