Benzopyran derivatives
    1.
    发明授权
    Benzopyran derivatives 失效
    BENZOPYRAN衍生物

    公开(公告)号:US3849447A

    公开(公告)日:1974-11-19

    申请号:US26121672

    申请日:1972-06-09

    申请人: SCHERING AG

    发明人: EDER U WIECHERT R

    摘要: 1. A BENZOPYRAN OF THE FORMULA

    2,3-(-CH2-CH2-C(-)(-R1)-C(-X)(-H(Y))-(CH2)N-B-A-),5-R2,

    5-(R3-O-)-5,6-DIHYDROPYRAN WHERE C(-) AND A ARE JOINED

    WHEREIN R1, R2 AND R3 EACH ARE LOWER ALKYL; N IS THE INTEGER 1 OR 2; A--B IS CH--CH2 OR C=CH; X IS OH, ALKOXY OF 1--10 CARBON ATOMS, ALKANOYLOXY OF 1-10 CARBON ATOMS OR BENZYLOXY AND Y IS H.

    Novel pregnanoic acid derivatives

    公开(公告)号:US3824260A

    公开(公告)日:1974-07-16

    申请号:US28471072

    申请日:1972-08-30

    申请人: SCHERING AG

    IPC分类号: C07D20060101 C07C169/36

    摘要: PREGNANOIC ACID DERIVATIVES OF THE FORMULA

    2-R1,3-(R2O-CO-CO-),3A-(H3C-),5-Z,5A-Y,6-(H3C-),6,7-(-A-B-

    CO-CH=),8-X-PERHYDRO-BENZ(E)INDENE

    WHEREIN X IS HYDROGEN,HALOGEN,ORMETHYL; Y IS HYDROGEN ORHALOGEN; Z IS HYDROXY OR HALOGEN HAVING AN ATOMIC WEIGHT NO GREATER THAN Y; R1 IS HYDROGEN OR METHYL; R2 IS HYDROGEN, ALKALI METAL OR SUBSTITUTED OR UNSUBSTITUTED HYDROCARBON OF 1-8 CARBON ATOMS WHICH IS UNSUBSTITUTED OR SUBSTITUTED BY HYDROXY, HALO, ALKOXY, CARBOXY, CARBALKOXY, AMINO, ALKYLAMINO, DIALKYLAMINO, NITRO OR SULFATO, WHEREIN ALKYL IN EACH INSTANCE CONTAINS 1-4 CARBON ATOMS; AND --A--B--IS--CH=CH--,--CCI=CH-- OR, WHEN AT LEAST ONE OF X, Y AND R1 IS OTHER THAN HYDROGEN, --CH2--CH2; PROCESS PRONOUNCED TOPICAL ANTI-INFLAMMATORY ACTIVITY.

    Dichloro-substituted estradiene
    4.
    发明授权
    Dichloro-substituted estradiene 失效
    DICHLORO取代的ESTRADIENE

    公开(公告)号:US3812166A

    公开(公告)日:1974-05-21

    申请号:US85348069

    申请日:1969-08-27

    申请人: SCHERING AG

    CPC分类号: C07J75/00

    摘要: A RACEMIC OR OPTICALLY ACTIVE, 4,6-DICHLORO-4,6-ESTRADIENE OF THE FORMULA

    4,6-DI(CL-),17-(R-O-),17-(CH*C-),18-CH3-ESTRA-4,6-DIEN-

    3-ONE

    WHEREIN R IS HYDROGEN, ALKYL, TETRADROPYRANYL OR AN ACID RESIDUE. TO FORM THE COMPOUNDS, THE 4-UNSUBSTITUTED 6-CHLOROESTRADIENE IS SUBJECTED TO THE ACTION OF AN AGENT FURNISHING POSITIVE AND NEGATIVE CHLORINE, THEREBY FORMING THE 6,6,7-TRICHLORO-SUBSTITUTED COMPOUND, FOLLOWED BY TREATMENT OF THE LATTER COMPOUND WITH A BASE. THE COMPOUNDS HAVE A VERY HIGH PROGESTERONE ACTIVITY.

    17-chloro steroids
    6.
    发明授权
    17-chloro steroids 失效
    17-CHLORO STEROIDS

    公开(公告)号:US3723484A

    公开(公告)日:1973-03-27

    申请号:US3723484D

    申请日:1971-09-15

    申请人: SCHERING AG

    摘要: 17-Chloro anti-inflammatory steroids of the formula

    WHEREIN X is H or Cl; Y is F or Cl; Z is OH, F or, when Y is Cl, Cl; and R is a free or esterified OH group, are produced by simultaneously reacting, in the presence of a sulfone, the corresponding 17-hydrogen compound or the corresponding Delta 9(11)-17-hydrogen compound with hydrogen fluoride and with an Nchloroacylamide or N-chloroacylimide.

    摘要翻译: 17-氯类抗炎类固醇,式为WHEREIN X为H或Cl; Y为F或Cl; Z是OH,F或当Y是Cl时,Cl; 并且R是游离的或酯化的OH基团,通过在砜的存在下,将相应的17-氢化合物或相应的DELTA 9(11)-17-氢化合物与氟化氢和N- 氯酰酰胺或N-氯酰酰亚胺。

    Novel pregnanoic acid derivatives
    7.
    发明授权
    Novel pregnanoic acid derivatives 失效
    新型孕激素衍生物

    公开(公告)号:US3833563A

    公开(公告)日:1974-09-03

    申请号:US29452772

    申请日:1972-10-03

    申请人: SCHERING AG

    CPC分类号: A61K31/573 C07J5/00

    摘要: CH=),8-X-PERHYDROBENZ(E)INDENE

    PREGNANOIC ACID DERIVATIVES OF THE FORMULA

    2-R1,3-(R3O-CO-CH(-OR2)-),3A,6-DI(H3C-),5-Z,6,7-(-B-A-CO-
    WHEREIN THE GROUP OR2 IS IN THE AF- OR BF-POSITION; X IS HYDROGEN, HALOGEN OR METHYL; Y IS HYDROGEN OR HALOGEN; Z IS HYDROXY OR HALOGEN HAVING AN ATOMIC WEIGHT NO GREATER THAN Y; R1 IS HYDROGEN OR METHYL; R2 IS HYDROGEN OR ACYL AND R3 IS HYDROGEN, ALKALI METAL OR SATURATED OR UNSATURATED UNSUBSTITUTED OR SUBSTITUTED HYDROCARBON OF 1-18 CARBON ATOMS, OR COLLECTIVELY R2 AND R3 ARE DIALKYLMETHYLENE OR CYCLOALKYLIDENE; AND AT LEAST ONE OF X, Y AND R1 ARE OTHER THAN HYDROGEN; AND -A-B- IS

    -CH2-CH2-, -CH=CH- OR -CCL=CH;

    POSSESS PRONOUNCED TOPICAL ANTI-INFLAMMATORY ACTIVITY AS WELL AS BEING INTERMEDIATES FOR THE PRODUCTION OF THE CORRESPONDING 20-KETO STEROIDS.

    Process for the preparation of pregnane derivatives
    9.
    发明授权
    Process for the preparation of pregnane derivatives 失效
    制备PREGNANE衍生物的方法

    公开(公告)号:US3741997A

    公开(公告)日:1973-06-26

    申请号:US3741997D

    申请日:1971-05-04

    申请人: SCHERING AG

    发明人: BERNDT H WIECHERT R

    CPC分类号: C07J75/00

    摘要: 17 Beta -Hydroxy-17 Alpha -ethynyl steroids are converted to 17-ethers and 17-esters of 17 Alpha -hydroxy-20-keto-pregnane steroids by forming a 17-sulfite ester of the 17 Beta -hydroxy group with thionyl chloride in the presence of base and then reacting the sulfite ester with an alcohol or carboxylic acid in the presence of an Hg salt.

    摘要翻译: 17β-羟基-17α-乙炔基类固醇通过将17β-羟基的17-亚硫酸酯与亚硫酰氯反应,转化成17α-羟基-20-酮 - 孕烷类固醇的17-醚和17-酯 碱的存在,然后在Hg ++存在下使亚硫酸酯与醇或羧酸反应。