• 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:
    This invention provides sulfonamide derivatives useful in the treatment of susceptible neoplasms in warm-blooded animals of formula (I): <CHEM> in which A is -O-, -@CH3, -CH2-, -CH2CH2-, or -CH2O-; D is -CH2- or -O-; R1 is hydrogen or halo, and R2 is halo or trifluoromethyl. E.g., N-([(4-chlorophenyl)amino]carbonyl)-2,3-dihydro-1H-indene-5-sulfonamide, m.p. 169-172 DEG C, is prepared by reacting 2,3-dihydro-5-indenylsulfonamide with 4-chlorophenylisocyanate.
    公开号:SU1545939A3
    申请号:SU4028196
    申请日:1986-09-22
    公开日:1990-02-23
    发明作者:Джеффри Хауберт Джеймс；Аустон Пур Джеральд；Джеффри Ридер Брент；Волтц Харпер Ричард；Ви-Пинг Тао Эдди；Абрахам Айкинс Джеймс
    申请人:Эли Лилли Энд Компани (Фирма)；
    IPC主号:
    专利说明:

    A755
    L
    6
    37.5 75.0
    150
    300 37.5 75
    150
    300 37.5 75.0
    30 67 91 99 A
    3} 37 58 24 36
    The results of two experiments, The percentage of life extension.
    Table
    Offerable in example 2
    4 5 6
    7 8
    300 150 300 150 300 150 300 150 300 150 300 150
    T a b l and c a 4
    0.30
    0.62
    0.06
    0.29
    ABOUT
    0.29
    0.03
    0.26
    ABOUT
    0.150, 51
    0.62
    权利要求:
    Claims (2)
    [1]
    1 1) 545939
    12 1
    Τ a b l c a 4
    CompoundDose mg / kg Toxicity Tumor size 6-mercaptopurine200 Toxic -100 0/10 0.74fifty 0/10 0.85
    Proposed by Example
    123The compound of formula I 22.51 1,05,0 Toxic _ 1G _ 0.220.70 following the example1 600,0 5/10 0.003 2 300,0 1/10 0.013 3 150.0 ' 0/10 0,089 4 75.0 0/10 0.333 5 37.5 0/10 0.702
    1 -R-- 3 1 4 150 69300 85600 100 M-5 37.5 5375.0 7Ά150 88300 96600 99 -Mod is on 37.5 4475.0 55150 '61300 80 X5563 * 37.5 0-3875 38-41150 50 - 54300 4 6 - 66 SZN 37.5 4975 901 50 96300 100 P388 12.5 10**25 8**fifty thirteen**100 19**200 51 ** B16-sc 37.5 thirteen75 thirteen150 3300 25
    * Results of two experiments. Life extension percentage.
    Table 3
    Compound-Dose mg / kg Toxicity The size tumors
    N-Me τμπ-; Ν-nitro urea (known)
    1 54 5 ‘) 39
    TO)
    Continuation tab. 1 17 I 1 6 15074 5 30097 7 15085300100 8 1503830049 10
    * Use orally in emulsor. Dosing begins one day after inoculation. Compounds are dosed once a day for 5-8 days, unless otherwise noted.
    table 2
    ------Connection example - -Tumorν ’ Dose, mg / kg, used orally in emulsor Inhibirova-% 1 2 3 4
    CA755 37.5 thirty 75.0 67 150 91 300 99 LL 37.5 4 75 3 e 150 37 300 58 06 37.5 24 75.0 36
    Continuation of the table. 2
    1Connectednationbyan example DoseTumor growth inhibition,% * mg / kg 1Ί 3 1 1503009199 fifty (twice a day) 65 75 (- -) 89 100 (’’ -) 93 150 (-) 100 200 (- ~) 99 300 (- ’’ -) 100 400 (- -) 100 2 1503003878 4 1503007194 5 1 5030071100
    [2]
    2 300 1/10 0.30150 0/9 0.62 4 300 0/10 0.06150 0/10 0.29 5 300 0/10 0150 0/10 0.29 6 300 0/10 0,03150 0/10 0.26 7 300 0/10 01 50 0/10 0.15 ' 8 300 0/10 0.51150 0/10 0.62
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    同族专利:
    公开号 | 公开日
    CN86106428A|1987-03-18|
    CY1659A|1993-05-14|
    EP0222475A1|1987-05-20|
    CN1013198B|1991-07-17|
    GR862353B|1987-01-19|
    IE59588B1|1994-03-09|
    HUT46657A|1988-11-28|
    PT83389A|1986-10-01|
    AU6294286A|1987-03-26|
    EP0222475B1|1989-11-29|
    HU200597B|1990-07-28|
    DK446986A|1987-03-24|
    UA5953A1|1994-12-29|
    PT83389B|1989-05-12|
    MX9203126A|1992-07-01|
    JPS6296459A|1987-05-02|
    KR880000204B1|1988-03-12|
    SG66892G|1992-09-04|
    JPH0662548B2|1994-08-17|
    DE3667168D1|1990-01-04|
    IE862503L|1987-03-23|
    HK88692A|1992-11-20|
    IL80032A|1992-07-15|
    KR870003086A|1987-04-15|
    AU587064B2|1989-08-03|
    DK160981C|1991-10-28|
    DK446986D0|1986-09-18|
    NZ217597A|1989-06-28|
    EG18046A|1991-08-30|
    DK160981B|1991-05-13|
    ES2001698A6|1988-06-01|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    DE1144259B|1956-05-29|1963-02-28|Hoechst Ag|Process for the preparation of sulfonylureas|
    US3097242A|1960-06-29|1963-07-09|Olin Mathieson|Hydrindene sulfonylureas|
    DE1159937B|1960-06-29|1963-12-27|Heyden Chem Fab|Process for the preparation of hydrindene sulfonylureas|
    DE1240866B|1961-06-29|1967-05-24|Heyden Chem Fab|Process for the preparation of indoline-6-sulfonylureas|
    US4634465A|1982-07-16|1987-01-06|Ciba-Geigy Corporation|Fused N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N'triazinylureas|
    IT1161220B|1983-04-21|1987-03-18|Montedison Spa|DIHYDRO-BENZOFURAN DERIVED FROM HERBICIDE ACTIVITIES|
    US4845128A|1984-06-27|1989-07-04|Eli Lilly And Company|Namino]carbonyl)benzene sulfonamides|US4845128A|1984-06-27|1989-07-04|Eli Lilly And Company|Namino]carbonyl)benzene sulfonamides|
    CA1331464C|1987-05-12|1994-08-16|Eli Lilly And Company|Anti-tumor method and compounds|
    HU202487B|1988-03-04|1991-03-28|Mta Koezponti Kemiai Kutato In|Process for producing n-sulfonylureas|
    US5216026A|1990-07-17|1993-06-01|Eli Lilly And Company|Antitumor compositions and methods of treatment|
    ZA915371B|1990-07-17|1993-03-31|Lilly Co Eli|Antitumor compositions and methods of treatment|
    US5262440A|1991-12-10|1993-11-16|Eli Lilly And Company|Antitumor compositions and methods of treatment|
    US5258406A|1991-12-20|1993-11-02|Eli Lilly And Company|Sulfonimidamides|
    US5234955A|1991-12-20|1993-08-10|Eli Lilly And Company|Antitumor compositions and methods of treatment|
    US5254582A|1992-02-05|1993-10-19|Eli Lilly And Company|Antitumor compositions and methods|
    US5169860A|1992-03-13|1992-12-08|Eli Lilly And Company|Antitumor compositions and methods of treatment|
    CA2110524A1|1992-12-10|1994-06-11|Gerald Burr Grindey|Antitumor compositions and methods of treatment|
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    EP0823401B1|1996-08-07|2003-10-29|Tomita Pharmaceutical Co., Ltd.|Granulate for treating waste water|
    AU709107B2|1996-08-22|1999-08-19|Dong Wha Pharmaceutical Industrial Co., Ltd.|Arylsulfonylimidazolone derivatives as an antitumor agent|
    ES2156550B1|1999-04-19|2002-02-01|Univ Navarra Publica|BENZO DERIVATIVESTHIOPHENOSULPHONAMIDE-1,1-DIOXIDE AND ITS USE AS ANTHINEOPLASTIC AGENTS.|
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    法律状态:
    2005-05-10| REG| Reference to a code of a succession state|Ref country code: RU Ref legal event code: MM4A Effective date: 20030923 |
    优先权:
    申请号 | 申请日 | 专利标题
    US77935485A| true| 1985-09-23|1985-09-23|
    US88867586A| true| 1986-07-24|1986-07-24|
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