会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 4. 发明授权
    • .beta.-carbolin-3-carboxylic acid derivatives useful for treating
anxiety and related disorders
    • 可用于治疗焦虑和相关疾病的β-咔啉-3-羧酸衍生物
    • US5010077A
    • 1991-04-23
    • US188145
    • 1988-04-25
    • Claus T. BraestrupMogens C. NielsenJoergen A. ChristensenMogens EngelstoftHenning SchouUlrich EderGunter NeefAndreas HuthDieter RahtzRalph Schmiechen
    • Claus T. BraestrupMogens C. NielsenJoergen A. ChristensenMogens EngelstoftHenning SchouUlrich EderGunter NeefAndreas HuthDieter RahtzRalph Schmiechen
    • C07D471/04C07H13/10
    • C07D471/04C07H13/10
    • A .beta.-carbolin-3-carboxylic acid derivative of the formula ##STR1## wherein: X is oxygen, sulphur or NR.sup.10, wherein R.sup.10 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkenyl, C.sub.3-7 -cycloalkyl or C.sub.3-7 -cycloalkenyl;R.sup.3 is (a) C.sub.1-10 -alkoxy, C.sub.1-10 -alkenyloxy, C.sub.6-10 -aryloxy, C.sub.7-11 -aralkoxy or C.sub.8-12 -aralkenyloxy, each optionally substituted with one or more hydroxy groups, halogen atoms, CF.sub.3 groups, C.sub.1-10 -alkoxy groups or C.sub.2-4 -alkenyloxy groups or each optionally substituted with an amino, di-C.sub.1-6 -alkylamino, C.sub.1-10 -alkoxycarbonyl or C.sub.1-10 -alkenyloxycarbonyl group; or (b) NR.sup.11 R.sup.12, wherein R.sup.11 and R.sup.12 are the same or different and each is (i) hydrogen, (ii) hydroxy, (iii) C.sub.1-10 -alkyl, (iv) C.sub.2-10 -alkenyl, (v) C.sub.6-10 -aryl, (vi) C.sub.7-11 -aralkyl, (vii) C.sub.8-12 -aralkenyl, (viii) C.sub.3-7 -cycloalkyl, or (ix) C.sub.3-7 -cycloalkenyl, each of groups (iii)-(ix) optionally substituted with hydroxy, carboxamido, carboxy, C.sub.1-10 -alkoxycarbonyl or C.sub.1-10 -alkenyloxycarbonyl; or (x) amino optionally substituted with C.sub.1-10 -alkyl, C.sub.2-10 -alkenyl, C.sub.6-10 -aryl, C.sub.7-11 -aralkyl, C.sub.8-12 -aralkenyl, C.sub.3-7 -cycloalkyl or C.sub.3-7 -cycloalkenyl; or wherein R.sup.11 and R.sup.12 together with the connecting nitrogen atom form a 5-, 6- or 7-membered heterocyclic ring, which may also contain one additional N or one O atom, and which may be optionally substituted with the same groups of substituents listed for groups (iii)-(ix) above, with the proviso that R.sup.11 and R.sup.12 cannot both be hydroxy; or wherein X and R.sup.3 together represent a single nitrogen atom;R.sup.4 is hydrogen, C.sub.1-10 -alkyl, C.sub.2-10 -alkenyl, C.sub.3-7 -cycloalkyl, C.sub.3-7 -cycloalkenyl, C.sub.7-10 -aralkyl, C.sub.8-10 -aralkenyl, phenyl, C.sub.7-10 -alkoxyphenyl or C.sub.8-10 -alkenyloxyphenyl;R.sup.A is F, Cl, Br, I, NO.sub.2, NR.sup.13 R.sup.14, NHCOR.sup.13, CN, COOR.sup.13, OR.sup.13, SCH.sub.3 or SO.sub.2 NR.sup.11 R.sup.12, wherein R.sup.13 and R.sup.14 each is hydrogen or C.sub.1-6 -alkyl optionally substituted with hydroxy or halogen; and wherein R.sup.11 and R.sup.12 are as defined above, and wherein there may be 1-4 identical or different R.sup.A 's; andR.sup.9 is hydrogen, C.sub.1-8 -alkyl, C.sub.1-8 -alkenyl, C.sub.1-8 -alkoxycarbonyl, C.sub.1-8 -alkenyloxycarbonyl, or C.sub.1-8 -alkenyloxy;with the proviso that R.sup.11 and R.sup.12 are not both hydrogen, when X is oxygen and when R.sup.4, R.sup.A and R.sup.9 each is hydrogen; that one of R.sup.11 and R.sup.12 is not hydrogen when the other is amino and when X is oxygen and R.sup.4, R.sup.A and R.sup.9 each are hydrogen; and that R.sup.4, R.sup.A and R.sup.9 each is not hydrogen when X is oxygen and R.sup.3 is OCH.sub.3.have valuable pharmacological properties.
    • 8. 发明授权
    • Process for the preparation of 13.beta.-alkyl-4-gonene-3,17-diones
    • 制备13 {62-烷基-4-锑烯-3,17-二酮的方法
    • US4024166A
    • 1977-05-17
    • US621384
    • 1975-10-10
    • Gerhard SauerUlrich EderGregor HafferGunter NeefRudolf Wiechert
    • Gerhard SauerUlrich EderGregor HafferGunter NeefRudolf Wiechert
    • B01J23/00C07B61/00C07C317/14C07D317/26C07D317/72C07J1/00
    • C07C317/00C07D317/26C07D317/72C07J1/0059
    • Novel process for the preparation of 13.beta.-alkyl-4-gonene-3,17-diones of the formula ##STR1## wherein R.sub.1 is methyl or ethyl, consists of REACTING A 7A.beta.-ALKYL,5,6,7,7A-TETRAHYDROINDANE-1,5-DIONE WITH FORMALDEHYDE AND AN ARYLSULFINIC ACID OR AN ADDUCT OF FORMALDEHYDE AND ARYLSULFINIC ACID TO PRODUCE A TETRAHYDROINDANE DERIVATIVE;Hydrogenating the tetrahydroindane derivative with hydrogen in the presence of a palladium-, platinum-, or rhodium-containing hydrogenation catalyst to produce a perhydroindane derivative;Condensing the perhydroindane derivative in the presence of a proton-accepting agent with a 7,7-alkylenedioxy-3-oxooctanoic acid ester;Treating the product obtained with a strong aqueous base and then heating the product in an inert solvent to produce a 4,5-secosteroid;Hydrogenating the 4,5-secosteroid in the presence of a palladium-, platinum-, rhodium-, or nickel-containing hydrogenation catalyst; andHydrolyzing and cyclizing the hydrogenated 4,5-secosteroid by treatment with a strong acid.
    • 用于制备式“IMAGE”的13β-烷基-4-单宁-3,17-二酮的新方法,其中R 1是甲基或乙基,由反应A7Aβ-烷基,5,6,7,7a- 四氢呋喃-1,5-二酮与甲醛和氨基磺酸或甲醛和芳香酸的添加以生产四氢衍生物衍生物; 在含有氢氧化钯,或含氢氧化铑的氢化催化剂存在下氢化四氢呋喃衍生物生成四氢呋喃衍生物; 在具有7,7-亚甲基氧化亚硝酸酯酸酯的接受原料的情况下,冷凝该衍生物衍生物; 处理用强碱性基质获得的产品,然后加入产品中的产品用于生产4,5代谢物; 在含有钯,铑,铑,或含镍的氢化催化剂存在下氢化4,5-二氧化硫; 并通过用强酸处理氢化和循环氢化的4,5代谢物。