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    Phenethanolamine derivatives
    4.
    发明授权
    Phenethanolamine derivatives 失效
    苯乙醇胺衍生物

    公开(公告)号：US5017619A

    公开(公告)日：1991-05-21

    申请号：US285269

    申请日：1988-12-16

    申请人： Leo Alig ,  Marcel Muller

    发明人： Leo Alig ,  Marcel Muller

    IPC分类号： A23K1/16 ,  A61K31/135 ,  A61K31/27 ,  C07C217/62

    CPC分类号： C07C217/62 ,  Y10S514/909 ,  Y10S514/91

    摘要： The invention is directed to phenethanolamine derivatives and their pharmaceutically compatible salts, having the formula ##STR1## wherein n is the number 1 or 2; L.sup.1 and L.sup.2 are hydrogen, C.sub.1-3 -(alkyl)carbonyl or C.sub.1-3 (alkoxy) carbonyl; T is hydrogen or methyl; X.sup.1 and X.sup.2 are phenyl or phenyl which is monosubstituted in the m-position by Br, Cl, F, CF.sub.3 and NO.sub.2 ; Y is --(CH.sub.2).sub.1-6 --O--G, --(CH.sub.2).sub.1-6 --CH.dbd.CH--C(O)--Z, --C(O)--Z or --CH(COOR").sub.2 ; G is C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl or --(CH.sub.2).sub.1-4 --Q; Q is phenoxy, phenyl, p-fluorophenyl or p-phenoxyphenyl; Z is a --OR or --N(R,R'); R and R' are hydrogen or C.sub.1-4 -alkyl or R and R' together with the N-atom to which they are attached form a 5- or 6-membered saturated ring which optionally contains an O-atom or an additional N-atom; and R" is C.sub.1-4 -alkyl.The compounds of the invention have catabolic activity and can be used for the treatment of obesity and of diabetes mellitus or of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals.

    摘要翻译： 本发明涉及具有下式的苯乙醇胺衍生物及其药学上相容的盐，其中n是数1或2; L 1和L 2是氢，C 1-3 - （烷基）羰基或C 1-3（烷氧基）羰基; T是氢或甲基; X 1和X 2是苯基或在m-位被Br，Cl，F，CF 3和NO 2单取代的苯基; Y是 - （CH 2）1-6 -O-G， - （CH 2）1-6 -CH = CH-C（O）-Z，-C（O）-Z或-CH（COOR“ G是C 1-4 - 烷基，C 1-4 - 烷氧基-C 1-4 - 烷基或 - （CH 2）1-4-Q; Q是苯氧基，苯基，对氟苯基或对苯氧基苯基; Z是-OR或-N（R，R'）; R和R'是氢或C 1-4 - 烷基或R和R'与它们所连接的N-原子一起形成5-或6-元饱和环，其任选地含有O-原子或另外的N- 原子; 和R“是C 1-4 - 烷基。 本发明的化合物具有分解代谢活性并且可用于治疗肥胖症和糖尿病或与增加的蛋白质分解有关的病症，或用作育肥动物的饲料添加剂。

    D-Homopregnanes
    5.
    发明授权
    D-Homopregnanes 失效

    公开(公告)号：US4285880A

    公开(公告)日：1981-08-25

    申请号：US82269

    申请日：1979-10-05

    申请人： Andor Furst ,  Peter Keller ,  Marcel Muller

    发明人： Andor Furst ,  Peter Keller ,  Marcel Muller

    IPC分类号： A61K31/20 ,  A61K31/575 ,  A61K31/585 ,  A61P7/10 ,  C07D307/94 ,  C07J63/00

    CPC分类号： C07J63/008 ,  Y10S514/869 ,  Y10S514/96 ,  Y10S514/962

    摘要： D-Homopregnanes of the formula ##STR1## wherein X is hydrogen, Y is hydroxy or X and Y taken together denote an oxygen to carbon bond; R.sup.6 is hydrogen, R.sup.7 is hydrogen, lower alkanoylthio or aroylthio, or R.sup.6 and R.sup.7 taken together denote a carbon to carbon bond and the dotted line in the 1,2-position of the A-ring together with the corresponding solid line denotes a single or double carbon to carbon bond or a pharmaceutically acceptable basic addition salt thereof when Y is hydroxy having diuretic activity are disclosed.

    摘要翻译： 其中X是氢，Y是羟基或X和Y一起表示氧碳键的式I- R6是氢，R7是氢，低级烷酰硫基或芳酰硫基，或R6和R7一起表示碳 - 碳键，A环的1,2位虚线与相应的实线一起表示单 或双碳 - 碳键或其药学上可接受的碱加成盐时，其中Y为具有利尿活性的羟基。

    D-homopregnanes
    8.
    发明授权
    D-homopregnanes 失效
    D-己内酯

    公开(公告)号：US4131655A

    公开(公告)日：1978-12-26

    申请号：US898070

    申请日：1978-04-20

    申请人： Leo Alig ,  Andor Furst ,  Marcel Muller ,  Ulrich Kerb ,  Rudolf Wiechert

    发明人： Leo Alig ,  Andor Furst ,  Marcel Muller ,  Ulrich Kerb ,  Rudolf Wiechert

    IPC分类号： A61K31/12 ,  A61K31/215 ,  A61K31/22 ,  A61K31/57 ,  A61P29/00 ,  C07J63/00 ,  C07F9/09 ,  C07C49/44

    CPC分类号： C07J63/008

    摘要： D-homopregnanes of the formula ##STR1## wherein R.sup.6 is hydrogen, chloro, fluoro or methyl; X is .beta.-hydroxymethylene or carbonyl; R.sup.17a is hydroxy, lower alkanoyloxy or aroyloxy; R.sup.21 is hydrogen, chloro, fluoro, hydroxy, lower alkanoyloxy, aroyloxy, sulfate or phosphate; and the dotted line in the 1,2-position of the A-ring denotes an additional carbon-carbon bondAnd pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them as the active ingredient are disclosed. The D-homopregnanes of the present invention exhibit hormonal activity and are useful for the treatment of inflammation.

    摘要翻译： 其中R6是氢，氯，氟或甲基的式XI的D-己内酯; X是β-羟基亚甲基或羰基; R17a是羟基，低级烷酰氧基或芳酰氧基; R21是氢，氯，氟，羟基，低级烷酰氧基，芳氧基，硫酸根或磷酸根; A环的1,2位的虚线表示另外的碳 - 碳键，并且其药学上可接受的盐，其制备方法和作为活性成分的药物组合物被公开。 本发明的D-己内酯具有激素活性，可用于治疗炎症。