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    • 1. 发明授权
    • 8.alpha.-Substituted ergoline-I derivatives
    • 8α-取代的麦角灵-I衍生物
    • US4348392A
    • 1982-09-07
    • US189295
    • 1980-09-22
    • Theodor FehrPaul StadlerPeter Stutz
    • Theodor FehrPaul StadlerPeter Stutz
    • C07D457/02C07D457/04C07D457/12A61K31/48
    • C07D457/04C07D457/02C07D457/12
    • This invention provides new compounds of formula I, ##STR1## wherein X is hydrogen, chlorine or bromine,R.sub.1 is methyl or ethyl, andR.sub.2 is CH.sub.2 --CN, or a group NR.sub.3 R.sub.4, whereinR.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms, andR.sub.4 is SO.sub.2 R.sub.5, wherein R.sub.5 is alkyl of 1 to 4 carbon atoms, mono- to tri-halogenalkyl of 1 to 4 carbon atoms, phenyl, pyridyl, phenyl monosubstituted by halogen or alkoxy of 1 to 4 carbon atoms, or a group NR.sub.6 R.sub.7, wherein each ofR.sub.6 and R.sub.7 is independently hydrogen or alkyl of 1 to 4 carbon atoms, orR.sub.6 and R.sub.7 together are one of the groups (CH.sub.2).sub.n or (CH.sub.2).sub.2 --A--(CH.sub.2).sub.2, whereinn is a number from 3 to 7, andA is oxygen, sulphur or nitrogen substituted by alkyl of 1 to 4 carbon atoms or phenyl,useful as prolactin secretion agents and antiparkinson agents.
    • 本发明提供了新的式I化合物,其中X是氢,氯或溴,R1是甲基或乙基,R2是CH2-CN,或NR3R4基团,其中R3是氢或1-4个碳原子的烷基 碳原子,R 4为SO 2 R 5,其中R 5为1至4个碳原子的烷基,1至4个碳原子的一至三卤代烷基,苯基,吡啶基,被卤素或1-4个碳原子的烷氧基取代的苯基,或 基团NR 6 R 7,其中R 6和R 7各自独立地为氢或1至4个碳原子的烷基,或者R 6和R 7一起为(CH 2)n或(CH 2)2 -A-(CH 2)2基团之一,其中 n为3至7的数,A为氧,硫或被1至4个碳原子的烷基取代的氮或苯基,可用作催乳激素分泌剂和抗帕金森药剂。
    • 2. 发明授权
    • Sulfonamido and sulfamoylamino-ergoline-I derivatives
    • 磺酰胺氨基和氨磺酰氨基 - 麦角林-I衍生物
    • US4348391A
    • 1982-09-07
    • US189068
    • 1980-09-22
    • Peter StutzTheodor FehrPaul Stadler
    • Peter StutzTheodor FehrPaul Stadler
    • C07D457/02A61K31/48A61K31/535A61P25/00A61P25/24A61P25/26C07D457/04C07D457/06C07D457/12
    • C07D457/04C07D457/06C07D457/12
    • The present invention provides compounds of formula I, ##STR1## wherein X is hydrogen, chlorine or bromine,R.sub.1 is methyl or ethyl,R.sub.2 is alkyl of 1 to 4 carbon atoms or allyl,R.sub.3 is CH.sub.2 CN or a group --NR.sub.4 R.sub.5, wherein R.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms, and R.sub.5 is alkanoyl of 1 to 5 carbon atoms, alkoxycarbonyl of 2 to 5 carbon atoms in the aggregate thereof, or mono-, di- or tri-haloalkoxycarbonyl of 3 to 5 carbon atoms, wherein the alkoxy group is substituted by halogen other than in the .alpha. position to the oxygen atom, or R.sub.5 is SO.sub.2 R.sub.6, wherein R.sub.6 is alkyl of 1 to 4 carbon atoms, mono-, di- or tri-haloalkyl of 1 to 4 carbon atoms, phenyl, phenyl mono-substituted by halogen or alkoxy of 1 to 4 carbon atoms, or pyridyl, or R.sub.6 is a group NR.sub.7 R.sub.8, wherein R.sub.7 and R.sub.8 are, independently, hydrogen or alkyl of 1 to 4 carbon atoms, or R.sub.7 and R.sub.8 together form --[CH.sub.2 ].sub.n -- or --[CH.sub.2 ].sub.2 --A--[CH.sub.2 ].sub.2 --, wherein n is a whole number from 3 to 7, and A is oxygen, sulphur, or nitrogen substituted by alkyl of 1 to 4 carbon atoms or phenylwhich are useful as prolactin inhibitors, anti-parkinson agents, and anti-depressants.
    • 本发明提供式I化合物,其中X是氢,氯或溴,R1是甲基或乙基,R2是1-4个碳原子的烷基或烯丙基,R3是CH2CN或基团-NR4R5,其中 R4是氢或1〜4个碳原子的烷基,R5是1〜5个碳原子的烷酰基,2〜5个碳原子的烷氧基羰基,3〜5个碳原子的一,二 - 或三 - 卤代烷氧基羰基 原子,其中烷氧基被除了在氧原子的α位置以外的卤素取代,或R 5是SO 2 R 6,其中R 6是1至4个碳原子的烷基,1至4的一,二或三卤代烷基 碳原子,苯基,被卤素或1-4个碳原子的烷氧基取代的苯基,或吡啶基,或R6是NR7R8基团,其中R7和R8独立地是氢或1-4个碳原子的烷基或R7 和R8一起形成 - [CH 2] n - 或 - [CH 2] 2 -A- [CH 2] 2 - ,其中n是3至7的整数,A是氧,硫或被烷基取代的氮 1个1-4个碳原子的苯基或可用作催乳激素抑制剂的苯基,抗帕金森试剂和抗抑郁剂。