• 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:
    An ergoline derivative of formula I: wherein R₁ represents a hydrogen atom or a methyl group; R₂ represents a hydrogen or halogen atom, a methyl, cyano or phenyl group or an alkylthio group having from 1 to 4 carbon atoms; R₃ represents a hydrocarbon group having from 1 to 4 carbon atoms; R₄ represents a hydrogen atom, a phenyl group or a hydrocarbon group having from1 to 4 carbon atoms; either (a) each of R₆ and R₇ represents a hydrogen atom or, taken together, R₆ and R₇ represent a valence bond and R₈ represents a hydrogen atom or a methoxy group, or (b) R₆ represents a hydrogen atom and R₇ and R₈ taken together represent a valence bond; W represents an oxygen atom or an imino group; A represents a group of the formula CHR₅, CH=CR₅ or CH₂CHR₅ wherein R₅ represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms; X represents an oxygen or sulphur atom or an imino group; and n is 0, 1 or 2; or a pharmaceutically acceptable salt of such ergoline derivative; is an antihypertensive agent.
    公开号:SU1634137A3
    申请号:SU884355906
    申请日:1988-06-20
    公开日:1991-03-07
    发明作者:Мантегани Серджио；Бромбилла Энцо；Темперилли Альдемио；Руггиери Даниэла；Сальвати Патрициа
    申请人:Фармиталиа Карло Эрба С.Р.Л. (Фирма)；
    IPC主号:
    专利说明:

    Table 1
    Way
    o Connection




    1- Ј (6-Methyl-D 9,10-ergolen8L-yl) methyl -2,4- (1H, ZN) -dihydropyrimidinedione
    1- Ј (6-Methyl-y-9,10-ergolen8-yl) metshG -2, A- (1H, 3N) -dihydropyrimidinedione-N-tb-oxide
    1 (6 Methyl-D-9,10-ergolsl-8ft-yl) methyl -2,4-imidazolin-dione
    1 - (6-Methyl-D, -9,10-ergolen-8Y-yl) methyl -2,4-imidazolidinedione-N-6-oxide
    Edouf, mg / kg p „s, (through the mouth)
    0.046
    0.050
    0.190
    0.198
    权利要求:
    Claims (1)
    [1]
    Claim
    A method of obtaining ergoline derivatives of the general formula where Rή is C ^ -C ^ -alkyl;
    A is a group —CH ^ CH — or —CHn = 0.1 or 2, characterized in that N-oxidation of the compound of the general formula is carried out wherein R 4 and A have the indicated meanings using organic peracid in a mixture of tetrahydrofuran and dimethylformamide at room temperature temperature for 2 hours 0
    Table 1
    Way o Compound Vdu about > mg / kg r.s. (through the mouth) Famous 1 ”£ (6-Methyl-D ~ 9,10-ergolen- (EP 0126968) ββ-yl) methyl] -2,4- (1Η, 3H) -di- 0,046 hydropyrimidinedione Proposed 1- ^ (b-Methyl-D-9,10-ergolen- as in example 1 8 $ -yl) methyl-2,4- (1Η, 3H) -dihydropyrimidinedione-N-tb-oxide 0,050 Famous(EP 0126968) 1 - [(6-Methyl-D-9,10-ergolsi-8] ¾-yl) methyl] -2,4-imidazolin- 0.190 DION Available 1- £ (6-Methyl-A-9,10-ergolen- as in example 2 8β-yl) methyl] -2,4-imidazole-dindione — Ν — 6-oxide 0.198
    I
    T l b l i c a 1
    Compound Dose, mg / kg p.o. Smell of average blood pressure, no mercury, ea time "· 1 15 min 130 days | 1 h | 2 h 3 h 4 h 5 h 6 h | 8 h 1 ! 2h Famous her 9 e ♦ * (EP 0126968) Suggested 0.125 176.7 -22.9 -34.5 -33.9 -37.5-12.2 ** -21.0 -32.2 -35.5 -34.5 -42.7 -28.9 -25.5 -10.5 -7.3 -6.7 as in example 1 0.5 173.1 -45.1 -55.1 -58.5 -54.3 -44.3 -35.3 -27 Known (EP 0126968) 0.25 186.1 -26.8 -31, * -29.6 -37.5 -35.7 -31.4 -15.7 -14.6 ** “2.5 ** -4.5 ** -9,*"* Proposed in Example 2 1 179.1 -23.1 -27.5 -35.9 -3 *, 1 -35.0 -38.4 -36.5 -34.1 “27.8 -22.3 -14.2
    * Average blood pressure before thymya (before treatment), 1 Minor
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    同族专利:
    公开号 | 公开日
    EP0296830B1|1993-02-03|
    KR890000478A|1989-03-14|
    NZ225099A|1990-09-26|
    PT87790B|1992-10-30|
    IL86795D0|1988-11-30|
    IL86795A|1991-11-21|
    PT87790A|1988-07-01|
    US4859678A|1989-08-22|
    DK341988A|1988-12-25|
    HU197743B|1989-05-29|
    FI882978A|1988-12-25|
    IE63372B1|1995-04-19|
    AU1818688A|1989-01-05|
    GB8714767D0|1987-07-29|
    KR960015965B1|1996-11-25|
    HUT46913A|1988-12-28|
    EP0296830A3|1989-12-06|
    IE881862L|1988-12-24|
    EP0296830A2|1988-12-28|
    DE3878052T2|1993-05-19|
    DK341988D0|1988-06-22|
    FI88301B|1993-01-15|
    JPS6422875A|1989-01-25|
    DE3878052D1|1993-03-18|
    ES2053736T3|1994-08-01|
    AU609144B2|1991-04-26|
    FI88301C|1993-04-26|
    FI882978A0|1988-06-22|
    ZA884451B|1989-05-30|
    AT85336T|1993-02-15|
    CA1293247C|1991-12-17|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    GB2120242A|1982-04-30|1983-11-30|Erba Farmitalia|Ergoline derivatives|
    DE3323119A1|1982-09-03|1984-03-08|Farmitalia Carlo Erba S.p.A., 20159 Milano|7-Cyano-ergolines|
    PH21123A|1983-04-28|1987-07-27|Erba Farmitalia|Ergoline derivatives|
    GB2173189B|1985-02-21|1988-04-27|Maruko Pharmaceutical Co|Ergoline derivatives and salts thereof and pharmaceutical compositions thereof|
    DE3700825A1|1986-01-24|1987-07-30|Sandoz Ag|8 alpha -Acylaminoergolines, their preparation and use|
    NL8700046A|1986-01-24|1987-08-17|Sandoz Ag|8 ALFA-ACYLAMINOERGOLINES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM.|
    GB8617907D0|1986-07-22|1986-08-28|Erba Farmitalia|Tetracyclic indole derivatives|DK0628042T3|1992-12-24|2001-11-12|Pharmacia & Upjohn Spa|Serotoninergic ergoline derivatives|
    GB9407637D0|1994-04-18|1994-06-08|Erba Carlo Spa|Serotoninergic abeo-ergoline derivatives|
    GB9603226D0|1996-02-15|1996-04-17|Pharmacia Spa|Heterocyclyl-ergoline derivatives|
    US6060483A|1996-06-27|2000-05-09|Pharmacia & Upjohn S.P.A.|Antineurodegenerative ergoline derivatives|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    GB878714767A|GB8714767D0|1987-06-24|1987-06-24|Egoline derivatives|
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