Unsaturated 2-oxa steroid derivatives and process for their preparation
    11.
    发明授权
    Unsaturated 2-oxa steroid derivatives and process for their preparation 失效
    不饱和的2-OXA甾体衍生物及其制备方法

    公开(公告)号:US3574688A

    公开(公告)日:1971-04-13

    申请号:US3574688D

    申请日:1968-05-14

    Applicant: ROUSSEL UCLAF

    Abstract: THIS INVENTION RELATES TO NOVEL UNSATURATED 2-OXA STEROID DERIVATIVES OF THE FORMULA

    6A-R,7-(X-O-)-2,4,6A,7,8,9,9A,9B,10,11-

    DECAHYDROCYCLOPENTA(5,6)NAPHTHO(1,2-C)PYRAN

    WHEREIN R IS ALKYL HAVING FROM 1 TO 6 CARBON ATOMS, X IS SELECTED FROM THE GROUP CONSISTING OF HYDROGN, ALKYL HAVING FROM 1 TO 5 CARBON ATOMS, ALKENYL HAVING FROM 3 TO 5 CARBON ATOMS, CYCLOALKYL HAVING FROM 5 TO 7 CARBON ATOMS, ARALKYL HAVING FROM 7 TO 11 CARBON ATOMS, ALKYLTHIOALKYL HAVING FROM 2 TO 5 CARBON ATOMS, ALKOXYALKYL HAVING FROM 2 TO 5 CARBON ATOMS, AND THE ACYL OF AN ORGANIC CARBOXYLIC ACID HAVING FROM 1 TO 18 CARBON ATOMS, AS WELL AS THE PROCESS OF PREPARING THE SAME. THESE COMPOUNDS HAVE AN ANABOLIC ACTION COUPLED WITH AN ANDROGENIC ACTION.

    Novel dibenzocycloheptenes
    14.
    发明授权
    Novel dibenzocycloheptenes 失效
    新型二苯并环庚烯

    公开(公告)号:US3892756A

    公开(公告)日:1975-07-01

    申请号:US32800673

    申请日:1973-01-30

    Applicant: ROUSSEL UCLAF

    CPC classification number: C07D451/02 C07F9/6561

    Abstract: Racemates and optically active isomers of a compound selected from the group consisting of a compound of the formula

    WHEREIN R is selected from the group consisting of hydrogen, lower alkyl optionally substituted with a member of the group consisting of hydroxy and halogen, lower alkenyl, lower alkynyl, -(CH2)n - COCH3 where n is 0 or 1,

    wherein X is selected from the group consisting of lower alkyl and optionally substituted phenyl, aralkyl of seven to eight carbon atoms, acyl of an organic carboxylic acid of one to six carbon atoms optionally substituted with

    where m is an integer from 0 to 6 and X1 is selected from the group consisting of hydrogen and lower alkyl,

    where p is an integer from 1 to 6 and X1 is as before and

    wherein X2 is lower alkyl and R1 and R2 are individually selected from the group consisting of hydrogen, halogen, lower alkyl, lower alkoxy, trifluoromethyl and dilower alkylamino and the non-toxic, pharmaceutically acceptable acid addition and quaternary ammonium salts thereof which have a stimulating effect on the central nervous system while possessing at the same time anticonvulsant activity and their preparation.

    Abstract translation: 选自下列化合物的化合物的外消旋物和旋光异构体:式WHEREIN R的化合物选自氢,任选被羟基和卤素的低级烷基取代的低级烷基,低级烯基,低级 炔基, - (CH 2)n -COCH 3,其中n是0或1,O并原-C-OX,其中X选自低级烷基和任选取代的苯基,7至8个碳原子的芳烷基,有机 任选被X1 - (CH2)mN ANGLE X1取代的1至6个碳原子的羧酸,其中m是0至6的整数,X 1选自氢和低级烷基,X 1 - (CH 2)p N ANGLE X1 其中p是1至6的整数,X 1如前所述,O& Y 2 -CH 2 -P 2 G 2,其中X 2是低级烷基,R 1和R 2分别选自氢,卤素,低级烷基,低级烷氧基 ,三氟甲基和二元烷基 否和其具有对中枢神经系统的刺激作用同时具有抗惊厥活性及其制备的无毒的药学上可接受的酸加成盐和季铵盐。

    Novel process for producing 10-hydrocarbon-19-nor-steroids
    15.
    发明授权
    Novel process for producing 10-hydrocarbon-19-nor-steroids 失效
    用于生产10-Hydrostar-19-NOR-STEROIDS的新工艺

    公开(公告)号:US3697511A

    公开(公告)日:1972-10-10

    申请号:US3697511D

    申请日:1970-10-20

    Applicant: ROUSSEL UCLAF

    CPC classification number: C07J5/00 C07J75/00

    Abstract: A novel process for introducing a 10-hydrocarbon group into a Delta 9(11)-19-nor-steroid by reacting a 13 Beta -lower alkylDelta 5(10),9(11)-19-nor steroid with a per carboxylic acid to form a mixture of the corresponding 5 Alpha ,10 Alpha - and 5 Beta ,10 Beta -epoxy steroids and reacting the latter with a hydrocarbon magnesium halide to form the corresponding 10hydrocarbon-13 Beta -lower alkyl-5-hydroxy- Delta 9(11)-19-norsteroid and to novel intermediates.

    Abstract translation: 通过使13β-低级烷基-DTATA 5(10),9(11)-19-或类固醇与一种或多种甾族化合物反应,将10-烃基引入到DELTA 9(11)-19-去 - 类固醇中的新方法 羧酸形成相应的5α,10α和5β,10β-环氧类固醇的混合物,并使其与烃卤化镁反应形成相应的10-烃-13β-低级烷基-5-羟基 - DELTA 9(11)-19-类固醇和新型中间体。

    7alpha-methyl-delta**4 9-gonadienes
    16.
    发明授权
    7alpha-methyl-delta**4 9-gonadienes 失效
    7ALPHA-METHYL-DELTA ** 4 9-GONADIENES

    公开(公告)号:US3637771A

    公开(公告)日:1972-01-25

    申请号:US3637771D

    申请日:1969-07-07

    Applicant: ROUSSEL UCLAF

    CPC classification number: C07J1/00 B65D5/72 C07J75/00

    Abstract: 7A-METHYL-13B-ALKYL-$4,9-GONADIENES OF THE FORMULA

    3-(O=),7-(H3C-),13-R,17-(X-O-),17-R1-GONA-4,9-DIENE

    WHEREIN R IS ALKYL OF 1 TO 4 CARBON ATOMS, R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND SATURATED AND UNSATURATED HYDROCARBON WHICH MAY BE SUBSTITUTED AND X IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ACYL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS, ACYL OF A SUBSTITUTED CARBONIC ACID OF 1 TO 18 CARBON ATOMS AND ALIPHATIC, 5 TO 6 MEMBER CYCLIC AND HETEROCYCLIC HYDROCARBONS WHICH MAY BE SUBSTITUTED AND TO NOVEL PROCESSES FOR THEIR PREPARATION. THE INVENTION ALSO RELATES TO NOVEL ANABOLIC AND/OR ANDROGENIC COMPOSITIONS HAVING REDUCED OR NO ESTROGENIC ACTIVITY.

    16 17-isoxazolino-delta-1 3 5(10)-gonatrienes
    17.
    发明授权
    16 17-isoxazolino-delta-1 3 5(10)-gonatrienes 失效
    16 17-ISOXAZOLINO-DELTA-1 3 5(10)-GONATRIENES

    公开(公告)号:US3629245A

    公开(公告)日:1971-12-21

    申请号:US3629245D

    申请日:1969-07-07

    Applicant: ROUSSEL UCLAF

    CPC classification number: C07J71/00 C07J75/00

    Abstract: 16A,17A-ISOXAZOLINE STEROIDS OF THE FORMULA

    2-R2,3-(R1-O-),13-Z,16,17-(-CH=N-O-),17-(R-O-)

    GONA-1,3,5(10)-TRIENE

    WHEREIN R AND R1 ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL OF 1 TO 7 CARBON ATOMS AND ACYL OF AN ORGANIC CARBOXYLIC ACIDS OF 1 TO 18 CARBON ATOMS, R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND HALOGEN AND Z IS ALKYL OF 1 TO 4 CARBON ATOMS AND THEIR PREPARATION AND NOVEL INTERMEDIATES. THE INVENTION ALSO INCLUDES HYPOCHOLESTEROLEMIC COMPOSITIONS HAVING NO SUBSTANTIAL ESTROGENIC ACTIVITY.

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