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18 条记录 (耗时 0.02 秒)

    9,10-Seco-steroid preparation
    1.
    发明授权
    9,10-Seco-steroid preparation 失效
    9,10-类固醇制剂

    公开(公告)号：US4045490A

    公开(公告)日：1977-08-30

    申请号：US651764

    申请日：1976-01-23

    申请人： Jean-Marie Cassal ,  Andor Furst ,  Werner Meier

    发明人： Jean-Marie Cassal ,  Andor Furst ,  Werner Meier

    IPC分类号： C07C401/00 ,  C07C49/76 ,  C07C49/82 ,  C07C49/84

    CPC分类号： C07C201/12 ,  C07C49/753 ,  C07C2102/24

    摘要： A process for the preparation of 9,10-seco-steroids of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently are hydrogen, amino, OR.sup.5, OCOR.sup.6 or NHCOR.sup.5 wherein R.sup.5 is hydrogen or lower alkyl and R.sup.6 is lower alkyl or phenyl; R.sup.3 is lower alkyl; R.sup.4 is oxo, ##STR2## wherein R.sup.13 is lower alkyl, lower alkoxy - lower alkylene, tetrahydropyranyl or tetrahydrofuryl, R.sup.14 is lower alkyl or aryl and R.sup.15 and R.sup.16 are lower alkyl or taken together form lower alkylene or arylene, and n is 1 or 2 is disclosed. The 9,10-seco-steroids of this invention are useful intermediates for the preparation of steroids.

    摘要翻译： 其中R1和R2独立地是氢，氨基，OR5，OCOR6或NHCOR5，其中R5是氢或低级烷基，R6是低级烷基或苯基; R3是低级烷基; R4是氧代，其中R13是低级烷基，低级烷氧基 - 低级亚烷基，四氢吡喃基或四氢呋喃基，R14是低级烷基或芳基，R15和R16是低级烷基或一起形成低级亚烷基或亚芳基，n是1或 2。 本发明的9,10-秒类固醇是制备类固醇的有用中间体。

    9,10-Seco-steroids
    2.
    发明授权
    9,10-Seco-steroids 失效
    9,10-类固醇

    公开(公告)号：US4064173A

    公开(公告)日：1977-12-20

    申请号：US651763

    申请日：1976-01-23

    申请人： Jean-Marie Cassal ,  Andor Furst ,  Werner Meier

    发明人： Jean-Marie Cassal ,  Andor Furst ,  Werner Meier

    IPC分类号： C07C401/00 ,  C07C49/27

    CPC分类号： C07C205/45 ,  C07C2102/24

    摘要： A process for the preparation of 9,10-seco-steroids of the formula ##STR1## WHEREIN R.sup.1 and R.sup.2 independently are hydrogen, amino, OR.sup.5, OCOR.sup.6 or NHCOR.sup.5 wherein R.sup.5 is hydrogen or lower alkyl and R.sup.6 is lower alkyl or phenyl; R.sup.3 is lower alkyl; R.sup.4 is oxo, ##STR2## wherein R.sup.13 is lower alkyl, lower alkoxy -- lower alkylene, tetrahydropyranyl or tetrahydrofuryl, R.sup.14 is lower alkyl or aryl and R.sup.15 and R.sup.16 are lower alkyl or taken together form lower alkylene or arylene, and n is 1 or 2 is disclosed. The 9,10-seco-steroids of this invention are useful intermediates for the preparation of steroids.

    摘要翻译： 其中R 1和R 2独立地为氢，氨基，OR 5，OCOR 6或NHCOR 5，其中R 5为氢或低级烷基且R 6为低级烷基或苯基; R3是低级烷基; R4是氧代，其中R13是低级烷基，低级烷氧基 - 低级亚烷基，四氢吡喃基或四氢呋喃基，R14是低级烷基或芳基，R15和R16是低级烷基或一起形成低级亚烷基或亚芳基，n是1或 2。 本发明的9,10-秒类固醇是制备类固醇的有用中间体。

    Phenyl-pyridinium salts and use thereof in inhibiting intestinal resorption
    6.
    发明授权
    Phenyl-pyridinium salts and use thereof in inhibiting intestinal resorption 失效
    苯基吡啶鎓盐及其在抑制肠吸收中的应用

    公开(公告)号：US4675328A

    公开(公告)日：1987-06-23

    申请号：US819187

    申请日：1986-01-15

    申请人： Jean-Marie Cassal ,  Albrecht Edenhofer ,  Henri Ramuz

    发明人： Jean-Marie Cassal ,  Albrecht Edenhofer ,  Henri Ramuz

    IPC分类号： A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/4425 ,  A61P1/00 ,  A61P3/04 ,  A61P3/06 ,  A61P9/10 ,  C07C49/84 ,  C07D211/72 ,  C07D213/04 ,  C07D213/20 ,  C07D233/60 ,  C07D239/26 ,  C07D277/22 ,  C07D303/22 ,  C07D303/34 ,  C07D303/36 ,  C07D317/22 ,  C07D211/84 ,  C07D213/69 ,  C07D213/78

    CPC分类号： C07D213/20 ,  C07C205/45 ,  C07C49/84 ,  C07D303/22 ,  C07D303/34 ,  C07D303/36 ,  C07D317/22

    摘要： Polycyclic salts of the formulaA-XN+CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O):Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar-C.sub.1-4 -alkyl, ArO or ArC(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.5,with the proviso that the N-atom in the 3-position of an imidazolium group XN.sup.+ is substituted by Ar,Ar-C.sub.1-4 -alkyl or C.sub.1-4 -alkyl,R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 individually are H, halogen, CF.sub.3, NO.sub.2, CN, C.sub.1-4 - -(alkyl, alkoxy, alkylthio or alkylsulphonyl), SO.sub.2 N(R,Q), C(O)N(Q.sup.4,Q.sup.5), C(O)Q.sup.4, C(O)OQ.sup.4 or OC(O)Q.sup.4,R, Q, Q.sup.1, Q.sup.2 and Q.sup.3 individually are H orC.sub.1-4 -alkyl, andQ.sup.4 and Q.sup.5 individually are C.sub.1-4 -alkyl inhibit the intestinal resorption of cholesterol and of bile salts in the enterohepatic circulation. These salts containing a quaternary N-atom can be manufactured starting from corresponding amines.

    摘要翻译： 式A-XN + CH2-（Y）n-（CH2）p-（Z）q-L-（T）r-MⅠ的多环盐，其中A-是强有机或无机酸的阴离子; XN +是被R1，R2和R3取代的吡啶鎓，嘧啶鎓，噻唑鎓或咪唑鎓; n，q和r分别为整数1或0，p为1至15的整数; Y是CH 2，C（H，OH）或C（O）：Z是O，S，CH 2，C（O），NQ 1，SO 2，C（O）O，OC（O） Q1）或N（Q1）C（O）; L是被R4取代的对亚苯基; 并且M是被R 5和R 6取代的苯基，T具有以上给出的含义之一，对于Z或是C（CH 3）2，C 2 H 4，C（Q 2）= C（Q 3），C 3 D C，CH 2 C（O） C（O）CH 2，CH 2 O或OCH 2，R 1是Ar，Ar-C 1-4 - 烷基，ArO或ArC（O）基团，Ar是被R 7，R 8和R 9取代的苯基; R 2和R 3分别是H，C 1-4 - 烷基，C 1-4 - 烷氧基或C 6 H 5，条件是咪唑鎓基团XN +的3-位上的N-原子被Ar取代，Ar-C 1-4 - 烷基或C 1-4 - 烷基，R 4，R 5，R 6，R 7，R 8和R 9分别是H，卤素，CF 3，NO 2，CN，C 1-4 - （烷基，烷氧基，烷硫基或烷基磺酰基），SO 2 N（R， Q），C（O）N（Q4，Q5），C（O）Q4，C（O）OQ4或OC（O）Q4，R，Q，Q1，Q2和Q3分别为H或C1-4烷基 ，Q4和Q5分别为C1-4烷基，抑制肠肝循环中胆固醇和胆汁盐的肠道吸收。 这些含有季氮原子的盐可以从相应的胺开始制备。

    Phenylsulfonylamide pyrimidine
    9.
    发明授权
    Phenylsulfonylamide pyrimidine 失效

    公开(公告)号：US5420129A

    公开(公告)日：1995-05-30

    申请号：US164167

    申请日：1993-12-08

    申请人： Volker Breu ,  Kaspar Burri ,  Jean-Marie Cassal ,  Martine Clozel ,  Georges Hirth ,  Bernd-Michael Loffler ,  Marcel Muller ,  Werner Neidhart ,  Henri Ramuz

    发明人： Volker Breu ,  Kaspar Burri ,  Jean-Marie Cassal ,  Martine Clozel ,  Georges Hirth ,  Bernd-Michael Loffler ,  Marcel Muller ,  Werner Neidhart ,  Henri Ramuz

    IPC分类号： A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/5377 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D239/52 ,  C07D239/56 ,  C07D239/69 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  A61K31/50

    CPC分类号： C07D239/47 ,  C07D239/48 ,  C07D239/52 ,  C07D239/56 ,  C07D239/69 ,  C07D401/12 ,  C07D405/12

    摘要： The invention is concerned with novel sulphonamides and their use as medicaments. In particular, the invention is concerned with compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, lower-alkyl, lower-alkoxy, lower-alkylthio, halogen or trifluoromethyl;R.sup.2 is hydrogen, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or --OCH.sub.2 COOR.sup.9 ;R.sup.3 is hydrogen, lower-alkyl, halogen, lower-alkylthio, trifluoromethyl, lower-alkoxy or trifluoromethoxy;R.sup.2 and R.sup.3 together are butadienyl, methylenedioxy, ethylenedioxy or isopropylidenedioxy;R.sup.4 is hydrogen, lower-alkyl, trifluoromethyl, lower-alkoxy, lower-alkylthio, hydroxy-lower-alkyl, hydroxy-lower-alkoxy, hydroxy-lower-alkoxy-lower-alkyl, hydroxy-lower-alkoxy-lower-alkoxy, alkoxy-lower-alkyl, alkoxy-lower-alkyloxy, lower-alkylsulfinyl, lower-alkylsulfonyl, 2-methoxy-3-hydroxypropoxy, 2-hydroxy-3-phenylpropyl, amino-lower-alkyl, lower-alkylamino-lower-alkyl, di-lower-alkylamino-lower-alkyl, amino, lower-alkylamino, di-lower-alkylamino, arylamino, aryl, arylthio, aryloxy, aryl-lower-alkyl, heterocyclyl, heterocyclo-lower-alkyl, heterocyclylamino, heterocyclylthio, heterocyclyloxy, --CHO, --CH.sub.2 OH or --CH.sub.2 Cl;R.sup.5 to R.sup.8 are independently hydrogen, halogen, trifluoromethyl, lower-alkoxy, lower-alkylthio or cyano;R.sup.6 and R.sup.5 or R.sup.7 together are butadienyl, methylene-dioxy, ethylenedioxy or isopropylidenedioxy;X is --O-- or --S--;Y is --CHO, C.sub.1-4 -alkyl, --(CH.sub.2).sub.1-4 --Z--R.sup.9, --(CH.sub.2).sub.1-4 --OC(O)(CH.sub.2).sub.1-4 CH.sub.3, --(CH.sub.2).sub.1-4 OC(O)Het, --(CH.sub.2).sub.1-4 NHC(O)R.sup.10, --(CH.sub.2).sub.1-4 OCH.sub.2 CH(OH)CH.sub.2 OH and cyclic ketals thereof, --(CH.sub.2).sub.1-4 NR.sup.9 CH.sub.2 CH(OH)CH.sub.2 OH, --(CH.sub.2).sub.1-4 OCH.sub.2 CH.sub.2 SCH.sub.3, --(CH.sub.2).sub.1-4 OCH.sub.2 CH.sub.2 S(O)CH.sub.3, --(CH.sub.2).sub.1-4 O(CH.sub.2).sub.1-4 --Z H, --(CH.sub.2).sub.1-4 O(CH.sub.2).sub.1-4 OC(O)R.sup.10, --(CH.sub.2).sub.1-4 NR.sup.9 (CH.sub.2).sub.1-4 Z H, --(CH.sub.2).sub.1-4 O(CH.sub.2).sub.1-4 OC(O)Het, --(CH.sub.2).sub.0-3 CH(OH)R.sup.10, --(CH.sub.2).sub.0-3 CH(OH)(CH.sub.2).sub.1-4 Z H, --(CH.sub.2).sub.0-3 CH(OH)CH.sub.2 SCH.sub.3, --(CH.sub.2).sub.0-3 CH(OH)CH.sub. 2 S(O)CH.sub.3, --(CH.sub.2).sub.0-3 CH(OH)OCH.sub.2 CH.sub.2 OH, --(CH.sub.2).sub.0-3 C(O)(CH.sub.2).sub.1-4 CH.sub.3, --(CH.sub.2).sub.0-3 C(O)(CH.sub.2).sub.1-4 Z R.sup.11, --(CH.sub.2).sub.0-3 C(O)CH.sub.2 Hal, --(CH.sub.2).sub.1-4 Hal, --(CH.sub.2).sub.1-4 CN, --(CH.sub.2).sub.0-3 C(O)OR.sup.9, --OR.sup.12 or --SR.sup.12 ;R.sup.9 is hydrogen or C.sub.1-4 -alkyl;R.sup.10 is C.sub.1-4 -alkyl;R.sup.11 is hydrogen, C.sub.1-4 -alkanoyl or heterocyclylcarbonyl;R.sup.12 is C.sub.1-4 -alkyl or --(CH.sub.2).sub.0-4 -aryl;Z is --O--, --S-- or --NR.sup.9 --;Het is a heterocyclic residue;Hal is halogen; andn is 0 or 1; and salts thereof.