Pyridine-ethanolamine derivatives
    14.
    发明授权
    Pyridine-ethanolamine derivatives 失效
    吡啶 - 乙醇胺衍生物

    公开(公告)号:US4800206A

    公开(公告)日:1989-01-24

    申请号:US57150

    申请日:1987-06-03

    摘要: Pyridine-ethanolamines of the formula ##STR1## wherein n, X, Y, R.sup.1, R.sup.2 and R.sup.3 have the significances given in the description, their corresponding enantiomers, diastereomers, and racemates as well as the pysiologically compatible salts thereof are describe. The compounds of formula I 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. The compounds of formula I can be prepared by alkylating the primary or secondary amines corresponding to the secondary or tertiary amines of formula I.

    摘要翻译: 其中n,X,Y,R 1,R 2和R 3具有说明书中给出的含义,其相应的对映异构体,非对映异构体和外消旋物以及其生理相容的盐的吡啶 - 乙醇胺。 式I化合物具有分解代谢活性,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,或作为育肥动物的饲料添加剂。 式I化合物可以通过将对应于式I的仲胺或叔胺的伯胺或仲胺烷基化来制备。

    D-Homopregnanes
    15.
    发明授权

    公开(公告)号:US4202841A

    公开(公告)日:1980-05-13

    申请号:US973336

    申请日:1978-12-26

    摘要: D-Homopregnanes of the formula ##STR1## wherein the dotted line in the 1,2-position together with the corresponding solid line denotes a single or double carbon-carbon bond; R.sup.6 is hydrogen, fluoro, chloro or methyl; R.sup.9 is hydrogen, fluoro, chloro or bromo; R.sup.11 is hydroxyl, acyloxy, fluoro or chloro; and R.sup.17a is hydroxyl or acyloxy with the proviso that when R.sup.9 is fluoro, chloro or bromo and R.sup.11 is fluoro or chloro, the atomic number of R.sup.11 is less than or equal to that of R.sup.9 ; and with the further proviso that when R.sup.6 is hydrogen, and R.sup.11 and R.sup.17a are hydroxy or when R.sup.6 is fluoro, R.sup.11 and R.sup.17a are hydroxyl and the dotted line in the 1,2-position together with the corresponding solid line denotes a single carbon-carbon bond, R.sup.9 is fluoro, chloro or bromo and processes for the preparation thereof are disclosed.

    摘要翻译: 式Ⅰ的D-homopregnanes其中1,2位虚线连同相应实线表示单碳双键; R6是氢,氟,氯或甲基; R9是氢,氟,氯或溴; R11是羟基,酰氧基,氟或氯; 并且R 17a是羟基或酰氧基,条件是当R 9是氟时,氯或溴,R 11是氟或氯,R 11的原子数小于或等于R 9的原子数; 并且进一步的条件是当R6为氢时,R11和R17a为羟基或当R6为氟时,R11和R17a为羟基,1,2-位与虚线相应的实线表示单个碳 - 碳键,R9是氟,氯或溴,并且其制备方法被公开。

    Phenethanolamine derivatives
    17.
    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

    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
    19.
    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

    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。