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34 条记录 (耗时 0.035 秒)

    Pharmacologically active 3-substituted beta-carbolines
    1.
    发明授权
    Pharmacologically active 3-substituted beta-carbolines 失效

    公开(公告)号：US4435403A

    公开(公告)日：1984-03-06

    申请号：US331740

    申请日：1981-12-17

    申请人： Claus T. Braestrup ,  Jogen A. Christensen ,  Mogens Engelstoft ,  Gunter Neef ,  Ulrich Eder ,  Ralph Schmiechen ,  Andreas Huth ,  Dieter Rahtz ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Dieter Palenschat

    发明人： Claus T. Braestrup ,  Jogen A. Christensen ,  Mogens Engelstoft ,  Gunter Neef ,  Ulrich Eder ,  Ralph Schmiechen ,  Andreas Huth ,  Dieter Rahtz ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Dieter Palenschat

    IPC分类号： A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/675 ,  A61P25/00 ,  A61P25/20 ,  C07D209/08 ,  C07D209/20 ,  C07D471/04 ,  C07F9/6561 ,  C07D487/14

    CPC分类号： C07D471/04 ,  C07D209/08 ,  C07D209/20 ,  C07F9/6561

    摘要： 3-substituted beta-carbolines of the formula ##STR1## wherein R.sup.C is hydrogen, lower alkyl, alkoxyalkyl of up to 6 C-atoms, cycloalkyl of 3-6 C-atoms, aralkyl of up to 8 C-atoms, or (CH.sub.2).sub.n OR.sup.20wherein R.sup.20 is alkyl of up to 6 C-atoms, cycloalkyl of 3-6 C-atoms or aralkyl of up to 8 C-atoms and n is an integer of 1 to 3;Y is oxygen, two hydrogen atoms or NOR.sup.1,wherein R.sup.1 is hydrogen, lower alkyl, aryl or aralkyl of up to 6 C-atoms, COR.sup.2, wherein R.sup.2 is lower alkyl of up to 6 C-atoms,or Y is CHCOOR.sup.3, wherein R.sup.3 is hydrogen or lower alkylor Y is NNR.sup.4 R.sup.5,wherein R.sup.4 and R.sup.5 can be the same or different and each is hydrogen, lower alkyl, C.sub.6-10 -aryl, C.sub.7-10 -aralkyl or CONR.sup.6 R.sup.7,wherein R.sup.6 and R.sup.7 can be the same or different and each is hydrogen or lower alkyl or R.sup.4 and R.sup.5 together with the connecting N-atom, for a 5- or 6-membered heterocyclic ring which optionally may also contain an O-atom or up to 3 N-atoms and which optionally may be substituted by a lower alkyl group;Z is hydrogen, or alkoxy or aralkoxy each of up to 10 C-atoms and each optionally substituted by hydroxy, or Z is alkyl of up to 6 C-atoms, C.sub.6-10 -aryl or C.sub.7-10 -aralkyl each of which may optionally be substituted by a COOR.sup.8 -- or a CONR.sup.9 R.sup.10 group,wherein R.sup.8 is alkyl of up to 6 C-atoms, and R.sup.9 and R.sup.10 can be the same or different and each is hydrogen or alkyl of up to 6 C-atoms;or Z is NR.sup.9 R.sup.10, wherein R.sup.9 and R.sup.10 are as defined above;or Z is NR.sup.11 CHR.sup.12 R.sup.13,wherein R.sup.11 and R.sup.12 each is hydrogen or together form a N.dbd.C double bond,wherein R.sup.13 is C.sub.1-10 -alkyl or NR.sup.14 R.sup.15,wherein R.sup.14 and R.sup.15 are the same or different and each is hydrogen, OH or alkyl or alkoxy each of up to 6 C-atoms,or wherein R.sup.12 and R.sup.13 together are oxygen, in which case, R.sup.11 is hydrogen;or Z is COOR.sup.2 wherein R.sup.2 is as defined above;or Y and Z, together with the connecting C-atom, may form a 5- or 6-membered heterocyclic ring which contains an O-atom, adjoining O- and N-atoms or up to 4 N atoms and which optionally may be substituted by a lower alkyl group, hydroxy or oxo have valuable psychotropic properties which make them useful for example as tranquilizers.

    .beta.-carbolin-3-carboxylic acid derivatives useful for treating anxiety and related disorders
    4.
    发明授权
    .beta.-carbolin-3-carboxylic acid derivatives useful for treating anxiety and related disorders 失效
    可用于治疗焦虑和相关疾病的β-咔啉-3-羧酸衍生物

    公开(公告)号：US5010077A

    公开(公告)日：1991-04-23

    申请号：US188145

    申请日：1988-04-25

    申请人： Claus T. Braestrup ,  Mogens C. Nielsen ,  Joergen A. Christensen ,  Mogens Engelstoft ,  Henning Schou ,  Ulrich Eder ,  Gunter Neef ,  Andreas Huth ,  Dieter Rahtz ,  Ralph Schmiechen

    发明人： Claus T. Braestrup ,  Mogens C. Nielsen ,  Joergen A. Christensen ,  Mogens Engelstoft ,  Henning Schou ,  Ulrich Eder ,  Gunter Neef ,  Andreas Huth ,  Dieter Rahtz ,  Ralph Schmiechen

    IPC分类号： C07D471/04 ,  C07H13/10

    CPC分类号： C07D471/04 ,  C07H13/10

    摘要： 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.

    Process for the preparation of 13.beta.-alkyl-4-gonene-3,17-diones
    5.
    发明授权
    Process for the preparation of 13.beta.-alkyl-4-gonene-3,17-diones 失效
    制备13 {62-烷基-4-锑烯-3,17-二酮的方法

    公开(公告)号：US4024166A

    公开(公告)日：1977-05-17

    申请号：US621384

    申请日：1975-10-10

    申请人： Gerhard Sauer ,  Ulrich Eder ,  Gregor Haffer ,  Gunter Neef ,  Rudolf Wiechert

    发明人： Gerhard Sauer ,  Ulrich Eder ,  Gregor Haffer ,  Gunter Neef ,  Rudolf Wiechert

    IPC分类号： B01J23/00 ,  C07B61/00 ,  C07C317/14 ,  C07D317/26 ,  C07D317/72 ,  C07J1/00

    CPC分类号： C07C317/00 ,  C07D317/26 ,  C07D317/72 ,  C07J1/0059

    摘要： 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.

    摘要翻译： 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。

    Process for the preparation of 17.beta.-hydroxy-20-alkoxypregnane-21-oic acid derivatives
    7.
    发明授权
    Process for the preparation of 17.beta.-hydroxy-20-alkoxypregnane-21-oic acid derivatives 失效
    制备17 {62-羟基-20-烷氧基孕烷-21-酸酸衍生物的方法

    公开(公告)号：US4155923A

    公开(公告)日：1979-05-22

    申请号：US873444

    申请日：1978-01-30

    申请人： Gunter Neef ,  Gregor Haffer ,  Ulrich Eder ,  Gerhard Sauer ,  Rudolf Wiechert

    发明人： Gunter Neef ,  Gregor Haffer ,  Ulrich Eder ,  Gerhard Sauer ,  Rudolf Wiechert

    IPC分类号： C07J1/00 ,  C07J13/00 ,  C07J7/00

    CPC分类号： C07J13/005 ,  C07J1/0033 ,  C07J13/007

    摘要： A process for the preparation of 17.beta.-hydroxy-20-alkoxypregnane-21-oic acid derivatives of the formula ##STR1## WHEREIN R.sub.1 is methyl or ethyl;R.sub.2 is hydrogen or methyl, either being in the .alpha.-or .beta.-position;R.sub.3 is lower alkyl of 1-4 carbon atoms;R.sub.4 is alkyl of 1-8 carbon atoms or benzyl; andSt is the residue of a steroid ABC ring system;Comprises reacting (a) a 17-oxo compound of the formula ##STR2## WHEREIN R.sub.1 and R.sub.2 are as defined above andSt* is said steroid ABC ring system residue, St, in a form which is chemically compatible with said reaction;With (b) an enolate ion of an alkoxyacetic acid alkyl ester of the formula ##STR3## wherein R.sub.3 and R.sub.4 are as defined above.

    摘要翻译： 制备式Ia的17β-羟基-20-烷氧基孕烷-21-酸酸衍生物的方法，其中R1是甲基或乙基; R2是氢或甲基，或者是α位或β-位; R3是1-4个碳原子的低级烷基; R4是1-8个碳原子的烷基或苄基; St是类固醇ABC环系统的残基; 包含反应（A）制剂的17-OXO化合物，其中R1和R2如上所定义，St *是所述类固醇ABC环系统残基St，以与所述反应化学相容的形式; 具有（B）式（A）的化合物，其中R 3和R 4如上所定义的烷氧基酸酯。

    Process for the preparation of trans-deca hydronaphthalene derivatives
    8.
    发明授权
    Process for the preparation of trans-deca hydronaphthalene derivatives 失效
    反十氢化萘衍生物的制备方法

    公开(公告)号：US4077996A

    公开(公告)日：1978-03-07

    申请号：US676805

    申请日：1976-04-14

    申请人： Gerhard Sauer ,  Ulrich Eder ,  Gregor Haffer ,  Gunter Neef ,  Rudolf Wiechert

    发明人： Gerhard Sauer ,  Ulrich Eder ,  Gregor Haffer ,  Gunter Neef ,  Rudolf Wiechert

    IPC分类号： C07C69/013 ,  C07C45/00 ,  C07C49/385 ,  C07C49/517 ,  C07C49/753 ,  C07C67/00 ,  C07C69/66 ,  C07C253/00 ,  C07C255/31 ,  C07D317/50 ,  C07D317/72 ,  C07D321/00 ,  C07F7/18 ,  C07C120/00 ,  C07C121/46 ,  C07D319/02 ,  C07D319/04

    CPC分类号： C07F7/1856 ,  C07D317/50

    摘要： A process for the preparation of trans-decahydronaphthalene compounds of Formula I ##STR1## wherein X is lower alkyl, --(CH.sub.2).sub.3 --Z--R.sub.2, ##STR2## --(CH.sub.2).sub.3 COOR.sub.4, or --(CH.sub.2).sub.3 CN; Y and Z are ketalized carbonyl or free, esterified, or etherified hydroxymethylene;U is halogen;R.sub.1, r.sub.2, and R.sub.3 are lower alkyl; andR.sub.4 is alkyl;Wherein an octahydronaphthalene compound of Formula II ##STR3## is converted, in the presence of bases, by reaction of a trialkyl chlorosilane of the formula(R.sub.5).sub.3 Si--Clwherein the R.sub.5 each are lower alkyl group, to a hexahydronaphthalene compound of the formula ##STR4## The hexahydronaphthalene compound is hydrogenated, in an inert solvent with hydrogen in the presence of a platinum-, palladium-, or rhodium-containing hydrogenation catalyst, to an octahydronaphthalene compound of the formula ##STR5## and a vinyl ketone of the formulaXCOCH.dbd.CH.sub.2is added to the thus-obtained octahydronaphthalene compound in an inert solvent in the presence of a Lewis acid.

    摘要翻译： 制备式I的反十氢萘化合物的方法，其中X是低级烷基， - （CH 2）3 -Z-R 2， - （CH 2）3 COOR 4或 - （CH 2）3 C 3; Y和Z是缩酮化羰基或游离的，酯化的或醚化的羟基亚甲基; U是卤素; R1，R2和R3是低级烷基; 和R4是烷基; 在碱的存在下，通过式（R5）3Si-Cl的三烷基氯硅烷与各自为低级烷基的R 5反应得到式II的六氢萘化合物，其中式II的甲氧基二苯甲酮化合物转化为 式VI化合物在惰性溶剂中，在含有铂，钯或铑的氢化催化剂的存在下，用氢气将其氢化成式为“八氢”的八氢化合物和式 在路易斯酸存在下，在惰性溶剂中将式XCOCH = CH 2加入到如此获得的八氢萘化合物中。

    D-Homo-19-norsteroids
    9.
    发明授权
    D-Homo-19-norsteroids 失效
    D-Homo-19-诺贝星

    公开(公告)号：US4057561A

    公开(公告)日：1977-11-08

    申请号：US770433

    申请日：1977-02-22

    申请人： Andor Furst ,  Jurg Gutzwiller ,  Marcel Muller ,  Rudolf Wiechert ,  Ulrich Eder ,  Gunter Neef

    发明人： Andor Furst ,  Jurg Gutzwiller ,  Marcel Muller ,  Rudolf Wiechert ,  Ulrich Eder ,  Gunter Neef

    IPC分类号： C07J63/00 ,  C07C49/48 ,  C07C69/02 ,  C07D309/22

    CPC分类号： C07J63/008

    摘要： D-homosteroids of the formula ##STR1## WHEREIN R.sup.3.alpha. is hydrogen, R.sup.3.beta. is hydroxy, lower alkanoyloxy or aroyloxy and R.sup.3.alpha. and R.sup.3.beta. taken together are oxo; R.sup.17a.alpha. is hydrogen, lower alkyl, ethynyl, vinyl, allyl, methallyl, propadienyl, 1-propynyl, butadiynyl or chloroethynyl; R.sup.17a.beta. is hydrogen, alkanoyl, aroyl, lower alkyl, cycloalkyl-lower-alkyl, benzyl, furfuryl or tetrahydropyranyl; R.sup.18 is hydrogen or methyl and the dotted line in the C-ring denotes an additional carbon to carbon bond in the 11,12-position andProcesses for the preparation thereof are disclosed.The D-homosteroids of the present invention are useful as ovulation inhibitors and androgenic/anabolic agents.

    摘要翻译： 式中的β-均质甾族化合物，其中R3a是氢，R3β是羟基，低级烷酰氧基或芳酰氧基，R3a和R3β一起是氧代; R17a是氢，低级烷基，乙炔基，乙烯基，烯丙基，甲代烯丙基，丙炔基，1-丙炔基，丁二炔基或氯乙炔基; R17aβ是氢，烷酰基，芳酰基，低级烷基，环烷基 - 低级 - 烷基，苄基，糠基或四氢吡喃基; R18是氢或甲基，C环中的虚线表示11,12位中的另外的碳 - 碳键，并且其制备方法被公开。