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13 条记录 (耗时 0.011 秒)

    Novel pregnanoic acid derivatives
    1.
    发明授权
    Novel pregnanoic acid derivatives 失效
    新型孕酸衍生物

    公开(公告)号：US3906095A

    公开(公告)日：1975-09-16

    申请号：US45941274

    申请日：1974-04-09

    申请人： SCHERING AG

    发明人： LAURENT HENRY ,  WIECHERT RUDOLF ,  PREZEWOWSKY KLAUS ,  HOFMEISTER HELMUT ,  GERHARDS ERICH ,  KOLB KARL HEINZ ,  MENGEL KLAUS

    IPC分类号： A61K31/573 ,  A61K17/00

    CPC分类号： A61K31/573

    摘要： Pregnanoic acid derivatives of the formula

    WHEREIN 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, alkali metal or saturated or unsaturated hydrocarbon of 1-18 carbon atoms which is unsubstituted or substituted by hydroxy, halo, alkoxy, carboxy, carbalkoxy, amino, alkylamino, dialkylamino, nitro or sulfate, wherein alkyl in each instance contains 1-4 carbon atoms; and -A-B- is -CH CH-; -CCl CH- or, when at least one of X, Y and R1 is other than hydrogen, -CH2-CH2; possess pronounced topical anti-inflammatory activity.

    摘要翻译： 式WHEREIN X的孕酸衍生物是氢，卤素或甲基; Y是氢或卤素; Z是原子量不大于Y的羟基或卤素; R1是氢或甲基; R2是未取代或被羟基，卤素，烷氧基，羧基，烷氧基，氨基，烷基氨基，二烷基氨基，硝基或硫酸取代的1-18个碳原子的氢，碱金属或饱和或不饱和烃，其中烷基各自含有1个 -4个碳原子; 和-A-B-是-CH = CH-; -CCl = CH-或当X，Y和R 1中的至少一个不是氢时，-CH 2 -CH 2; 具有明显的局部抗炎活性。

    Novel 21,21-dichlorosteroids
    2.
    发明授权
    Novel 21,21-dichlorosteroids 失效
    二十一一二二氯二苯醚

    公开(公告)号：US3681405A

    公开(公告)日：1972-08-01

    申请号：US3681405D

    申请日：1970-07-22

    申请人： SCHERING AG

    发明人： LAURENT HENRY ,  KOLB KARL H ,  WIECHERT RUDOLF

    IPC分类号： C07J7/00 ,  A61K31/573 ,  C07J5/00 ,  C07C169/34

    CPC分类号： A61K31/573 ,  C07J5/00 ,  Y10S514/825 ,  Y10S514/826 ,  Y10S514/861 ,  Y10S514/863

    摘要： 21,21-Dichlorosteroids of the formula

    WHEREIN R1 is a hydrogen or chlorine atom; R2 is a hydrogen atom, a fluorine atom, or a methyl group; R3 is a hydrogen atom or a methyl group; R4 is a hydrogen atom or a free or esterified hydroxy group; and C1-C2 represents a single or double bond joining the carbon atoms at the 1- and 2-positions, have antiinflammatory activity.

    摘要翻译： 21,21-二氯类固醇，式WHEREIN R1是氢或氯原子; R2是氢原子，氟原子或甲基; R3是氢原子或甲基; R4是氢原子或游离或酯化的羟基; 且C1-C2表示在1位和2位连接碳原子的单键或双键，具有抗炎活性。

    11-halogen-substituted steroids
    3.
    发明授权
    11-halogen-substituted steroids 失效
    11-HALOGEN-替代的STEROIDS

    公开(公告)号：US3609171A

    公开(公告)日：1971-09-28

    申请号：US3609171D

    申请日：1968-08-15

    申请人： SCHERING AG

    发明人： LAURENT HENRY ,  KERB ULRICH ,  KOLB KARL HEINZ ,  WIECHERT RUDOLF ,  GERHARDS ERICH

    IPC分类号： A61K31/573 ,  C07J5/00 ,  C07J75/00 ,  C07C169/30

    CPC分类号： A61K31/573 ,  C07J5/00 ,  C07J75/00

    摘要： 11-halogen-substituted-steroids of the formula

    WHEREIN R is hydrogen or a cyl and X and Y are halogen, the molecular weight of Y being at least equal to that of X. The products of the invention are useful for pharmaceutical applications to reduce inflammations.

    摘要翻译： 作为活性成分含有式WHEREIN R的11-卤素取代的类固醇，至多15个碳原子的脂族酰基或至多总计15个碳原子并被氯取代的脂族酰基或羧酸的药物组合物 基团，硝基或硫酸根基团，并且其中X和Y是卤素，Y的分子量至少等于X的分子量。

    Novel 11-oxygenated pregneno (17,16{60 -D)-1,3-oxathiolanes and process for the preparation thereof
    6.
    发明授权
    Novel 11-oxygenated pregneno (17,16{60 -D)-1,3-oxathiolanes and process for the preparation thereof 失效
    新型11-氧合孕烯（17,16（60-D）-1,3-氧硫杂环戊烷）及其制备方法

    公开(公告)号：US3894004A

    公开(公告)日：1975-07-08

    申请号：US42660073

    申请日：1973-12-20

    申请人： SCHERING AG

    发明人： HOFMEISTER HELMUT ,  LAURENT HENRY ,  PREZEWOWSKY KLAUS ,  WIECHERT RUDOLF ,  MENGEL KLAUS ,  WENDT HANS

    IPC分类号： C07J7/00 ,  C07J13/00 ,  C07J31/00 ,  C07J41/00 ,  C07J71/00 ,  C07C173/00

    CPC分类号： C07J7/006 ,  C07J13/005 ,  C07J31/003 ,  C07J41/005 ,  C07J71/001 ,  C07J71/0089

    摘要： Topical anti-inflamatory 11-oxygenated pregneno(17,16 Alpha -d)1'', 3''-oxathiolanes of the formula I
    wherein R1 and R2, can be the same or different and are a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkyl containing hetero atoms, aryl, or heteroacyl; R1 and R2 together can be a (CH2)n bridge which can also contain hetero atoms, and wherein n has the values of 2-6; R3 represents a hydrogen or fluorine atom, or an alkyl; X is a hydrogen, fluorine, or chlorine atom; Y is an oxygen atom or the group

    WHEREIN R4 represents a hydrogen atom or an acyl; and C1 .... C2 represents a single or double bond between the C-1 and C-2 carbon atoms. This invention also comprises the process of producing the compounds by condensation of 16 Beta -hydroxy-17 Alpha mercaptopregnenes with carbonyl compounds under epimerization of the substituent at the C-16 carbon atom.

    摘要翻译： 式I的局部抗炎性11-氧化孕烯[17,16α-d] -1'，3'-氧硫杂环戊烷，其中R 1和R 2可以相同或不同，并且是氢原子，烷基，环烷基 ，含有杂原子，芳基或杂酰基的环烷基; R1和R2可以是也可以含有杂原子的（CH 2）n桥，其中n具有2-6的值; R3表示氢或氟原子，或烷基; X是氢，氟或氯原子; Y是氧原子或基团R 4代表氢原子或酰基; C 1 -C 2表示C 1和​​C 2的碳原子之间的单键或双键。 本发明还包括通过在C-16碳原子上的取代基的差向异构化下将16β-羟基-17α-己内酯与羰基化合物缩合制备化合物的方法。

    Method for the production of 21-fluoro-4 6-pregnadienes
    7.
    发明授权
    Method for the production of 21-fluoro-4 6-pregnadienes 失效
    用于生产21-氟-4-6-异丙苯的方法

    公开(公告)号：US3644441A

    公开(公告)日：1972-02-22

    申请号：US3644441D

    申请日：1969-11-17

    申请人： SCHERING AG

    发明人： WIECHERT RUDOLF ,  LAURENT HENRY

    IPC分类号： C07J53/00 ,  C07C167/28

    CPC分类号： C07J53/00

    摘要： 1. THE METHOD FOR THE PRODUCTION OF 21-FLUORO-DELTA4,6PREGNADIENES OF THE GENERAL FORMULA:

    1,2-(-CH2-),3,20-DI(O=),6-X,17-(R-O-),21-(F-)

    PREGNA-4,6-DIENE

    WHEREIN X IS SELECTED FROM THE GROUP CONSISTING OF FLOURINE AND CHLORINE AND R IS ACYL RADICAL OF A PHYSIOLOGICALLY TOLERABLE ALIPHATIC CARBOXYLIC ACID HAVING UP TO 16 CARBON ATOMS, COMPRISING: (A) REACTING AN ESTER OF A 21-FLUORO-6,7-OXIDO-1,2AMETHYLENE-DELTA4-PREGNENE - 17A - OL - 3,20 - DIONE IN AN ORGANIC ACID WITH HYDROCHLORIC ACID RMING THE 6 - CHLORO-DELTA6 GROUP AND OPENING THE 1,2METHYLENE LINKAGE FORMING THE 1-CHLORO-METHYL GROUP; (B) REMOVING THE RESULTANT WATER FORMED IN STEP (A) BY MEANS OF STRONG ACID, THEREBY CREATING A 6XDELTA6 CONFIGURATION AND FORMING A 4,6-DOUBLE BOND; (C) EFFECTING RECLOSURE OF THE 1,2A-MEHTYLENE RING OPENED IN STEPS (A) AND (B) BY THE ACTION OF A REAGENT SELECTED FROM THE GROUP CONSISTING OF AN ORGANIC BASE AND ALUMINUM OXIDE, TO FORM A 6-HALO-21-FLUORO1,2A-METHYLENE-DELTA4,6-PREGNADIENE - 17A-O1 - 3,20DIONE ESTER.

    N-substituted 4-aminosteroids
    8.
    发明授权
    N-substituted 4-aminosteroids 失效
    N-取代的4-氨基苯甲酸酯

    公开(公告)号：US3637668A

    公开(公告)日：1972-01-25

    申请号：US3637668D

    申请日：1969-02-27

    申请人： SCHERING AG

    发明人： LAURENT HENRY ,  STEINBECK HERMANN ,  WEICHERT RUDOLF

    IPC分类号： A61K31/57 ,  A61K31/573 ,  A61K31/58 ,  C07C173/00

    CPC分类号： A61K31/573 ,  A61K31/57 ,  A61K31/58

    摘要： 4-AMINOSTEROIDS OF THE PARTIAL FORMULA

    1-(R1-N(-R2)-),2-(O=)-2,3,3A,4-TETRAHYDROPENTALENE

    WHEREIN R1 AND R2 ARE ALKYL OR SUBSTITUTED ALKYL AND WHEREIN R1 AND R2 TOGETHER WITH THE NITROGEN WHICH IS ATTACHED IN THE 4-POSITION, MAY FORM AN ADDITIONAL RING AND WHEREIN SAID ADDITIONAL RING MAY INCLUDE A FURTHER HETERO ATOM OR A POSITIVE NITROGEN AND WHEREIN ST IS A STEROID MOLECULE RESIDUE. THE COMPOUNDS HAVE PARTICULAR USE AS PROGESTATIONAL AGENTS. THE COMPOUNDS OF THE ANDROSTANE SERIES HAVE ANDROGENOUS, ANABOLIC AND ANTIESTROGENIC PROPERTIES.

    Pregnanoic acid derivatives and process for the preparation thereof
    9.
    发明授权
    Pregnanoic acid derivatives and process for the preparation thereof 失效
    孕酸衍生物及其制备方法

    公开(公告)号：US3919421A

    公开(公告)日：1975-11-11

    申请号：US42670273

    申请日：1973-12-20

    申请人： SCHERING AG

    发明人： LAURENT HENRY ,  WIECHERT RUDOLF ,  HOFMEISTER HELMUT ,  MENGEL KLAUS ,  WENDT HANS ,  ANNEN KLAUS

    IPC分类号： C07J5/00 ,  C07J71/00 ,  C01B7/00

    CPC分类号： C07J5/0092 ,  C07J71/0031

    摘要： Pharmacologically active pregnanoic acid derivatives of the Formula I

    wherein -A-B- is -CH2-CH2-, -CH CH-, or -CCl CH-; X is a hydrogen atom, a halogen atom, or methyl; -Y-Z- is -CH-CH2-, C CH-, -CV-CHOU-, -CV-CO-, -CW-CHW''-, wherein U is a hydrogen atom or acyl, V is a hydrogen atom or a halogen atom, and W and W'' each are a halogen atom; R1 is alkyl; R2 is alkyl or aryl; or, R1 and R2 together represent a tetramethylene group or pentamethylene group; R3 is a hydrogen atom, an alkali metal atom, or a hydrocarbon. The invention also comprises the process of producing the compounds by various procedures.

    摘要翻译： 其中-A-B-是-CH 2 -CH 2 - ， - CH = CH-或-CCl = CH-的式I的药理学活性孕酸衍生物; X是氢原子，卤素原子或甲基; -YZ-是-CH-CH2-，-C = CH-，-CV-CHOU-，-CV-CO-，-CW-CHW'-，其中U是氢原子或酰基，V是氢原子或 卤素原子，W和W'各自为卤素原子; R1是烷基; R2是烷基或芳基; 或者R1和R2一起表示四亚甲基或五亚甲基; R3是氢原子，碱金属原子或烃。