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    8.BETA.-HYDROCARBYL-SUBSTITUIERTE ESTRATRIENE ALS SELEKTIV WIRKSAME ESTROGENE
    3.
    发明公开
    8.BETA.-HYDROCARBYL-SUBSTITUIERTE ESTRATRIENE ALS SELEKTIV WIRKSAME ESTROGENE 有权
    8.BETA.烃基取代雌三烯作为选择性雌激素有效

    公开(公告)号：EP1272504A1

    公开(公告)日：2003-01-08

    申请号：EP01931609.0

    申请日：2001-04-12

    Applicant: Schering Aktiengesellschaft

    Inventor： PETERS, Olaf ,  HILLISCH, Alexander ,  THIEME, Ina ,  ELGER, Walter ,  HEGELE-HARTUNG, Christa ,  KOLLENKIRCHEN, Uwe ,  FRITZEMEIER, Karl-Heinrich ,  PATCHEV, Vladimir

    IPC: C07J1/00 ,  A61K31/565 ,  C07J41/00 ,  A61P5/30

    CPC classification number: C07J1/007 ,  C07J1/0059 ,  C07J1/0062 ,  C07J1/0074 ,  C07J41/0072

    Abstract: The invention relates to novel 8ß-substituted estratrienes of the general formula (I), wherein R?2, R3, R6, R6', R7, R7', R9, R11, R11', R12, R14, R15, R15', R16, R16', R17 and R17'¿ are defined as in the description and R8 represents a straight- or branched-chained, optionally partially or completely halogenated alkyl or alkenyl group with up to 5 carbon atoms, an ethinyl or prop-1-inyl group. The inventive estratrienes are used as pharmaceutically active substances that have in vitro a higher affinity to estrogen receptor preparations of rat prostate than to estrogen receptor preparations of rat uterus and which in vivo preferably have a preferential effect on bone material as compared to uterus and/or a pronounced effect with respect to the stimulation of the expression of 5HT2a receptor and transporter. The invention further relates to the production of these novel compounds, to their use in therapy and to the pharmaceutical forms of administration that contain said novel compounds. The invention further describes the use of said compounds for treating estrogen-deficiency related diseases and conditions and to the use of an 8ß-substituted estratriene structural part in the overall structures of compounds that are characterized by a dissociation in favor of their estrogen effect on the bone as compared to the uterus.

    14,16$g(b)-ETHANO-15$g(b),16?1 -CYCLO-14$g(b)-ESTRA-1,3,5(10)-TRIENE
    4.
    发明公开
    14,16$g(b)-ETHANO-15$g(b),16?1 -CYCLO-14$g(b)-ESTRA-1,3,5(10)-TRIENE 失效
    （b）-ETHANO-15 $ g（b），16±1 -CYCLO-14 $ g（b）-ESTRA-1,3,5（10） - 三烯

    公开(公告)号：EP0639201A1

    公开(公告)日：1995-02-22

    申请号：EP92902943.0

    申请日：1992-01-24

    Applicant: SCHERING AKTIENGESELLSCHAFT

    Inventor： BULL, James, R. ,  ELGER, Walter ,  CHWALISZ, Krzysztof ,  FRITZEMEIER, Karl-Heinrich

    IPC: A61K31 ,  A61P3 ,  A61P43 ,  C07J53

    CPC classification number: C07J53/008 ,  C07J53/002

    Abstract: Described are 14,16β-ethano-15β-161 -cyclo-14β-estra-1,3,5(10)-trienes of the general formula (I), in which R1 is a hydrogen atom, a C¿1?-C9 alkyl residue or a C1-C9 acyl residue; R?2¿ is a hydrogen atom, a C¿1?-C9 alkyl residue, a C2-C9 alkenyl residue or a C2-C9 alkinyl residue; and R?3¿ is a hydroxy group or a C¿1?-C9 acyloxy residue. Also described is a method of preparing these compounds. The new compounds have high (peroral) activity and are suitable for the preparation of drugs.

    Abstract translation: 描述了通式（I）的14,16β-乙内酰-15β-161-环-14β-雌-1,3,5（10） - 三烯，其中R 1是氢原子，C 1〜 C9烷基残基或C1-C9酰基残基; R 2是氢原子，C 1 -C 9烷基残基，C 2 -C 9链烯基残基或C 2 -C 9炔基残基; R 3是羟基或C 1 -C 9酰氧基残基。 还描述了制备这些化合物的方法。 这些新化合物具有很高的（口服）活性，适用于制备药物。

    NEUE 9-HALOGEN-PROSTAGLANDINE
    5.
    发明授权
    NEUE 9-HALOGEN-PROSTAGLANDINE 失效

    公开(公告)号：EP0213129B1

    公开(公告)日：1992-11-11

    申请号：EP85901971.3

    申请日：1985-04-12

    Applicant: SCHERING AKTIENGESELLSCHAFT

    Inventor： RADÜCHEL, Bernd ,  SKUBALLA, Werner ,  VORBRÜGGEN, Helmut ,  LOGE, Olaf ,  ELGER, Walter

    IPC: C07C405/00 ,  A61K31/557

    CPC classification number: C07C405/0016 ,  C07C405/00 ,  C07C405/0033 ,  C07C405/0041

    Abstract: 9-halogen-prostane having the formula (I) wherein Hal represents a chlorine or fluorine atom in position alpha or beta; R1 represents the rest CH2OH or the formula (A) with R2 representing a hydrogen atom, an alkyl, cycloalkyl, aryl or heterocyclic rest or R1 represents the rest of formula (B) with R3 representing an acid rest or the rest R2; A is a group -CH2-CH2-, -CH=CH- trans or -C=C-; W is free or functionally transformed hydroxy methylene group or a free or functionally transformed group having the formula (C), the group OH susceptible of being in position alpha or beta; D and E represent together a direct bound or D represents a straight branched or cyclic chain alkylene group with 1 to 10 atoms of carbon, substituted optionally by fluorine atoms, and E represents oxygen or sulfur, a direction bound, a bound -C=C- or a group -CR6=CR7, R6 and R7 being different and representing hydrogen, chlorine or alkyl with 1 to 4 atoms of carbon; R4 is a free or functionally modified hydroxy group; R5 is a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl, an optionally substituted aryl or a heterocyclic group; as well as, if R2 represents a hydrogen atom, the salts thereof with physiologically acceptable bases, the preparation process thereof and the pharmaceutical utilization thereof.

    Abstract translation: 具有式（I）的9-卤素 - 前列腺素，其中Hal代表α或β位的氯或氟原子; R 1代表剩余的CH 2 OH或式（A），其中R 2代表氢原子，烷基，环烷基，芳基或杂环基，或者R 1代表式（B）的其余部分，其中R 3代表酸残基或剩余的R 2; A是基团-CH 2 -CH 2 - ， - CH = CH-反式或-C≡C-; W为游离或功能性转化的羟基亚甲基或具有式（C）的游离或功能转化的基团，所述基团OH易位于α位或β位; D和E一起表示直接结合或D表示具有1至10个碳原子且任选被氟原子取代的直链支链或环状链亚烷基，并且E表示氧或硫，方向结合，结合的-C = C - 或基团-CR 6 = CR 7，R 6和R 7不同且代表氢，氯或具有1至4个碳原子的烷基; R4是游离的或功能性修饰的羟基; R5是氢原子，烷基，卤素取代的烷基，环烷基，任选取代的芳基或杂环基团; 以及如果R2代表氢原子，则其与生理上可接受的碱形成的盐，其制备方法和其药物利用。

    NEUE 9-HALOGEN-PROSTAGLANDINE
    6.
    发明公开
    NEUE 9-HALOGEN-PROSTAGLANDINE 失效
    NEW 9卤素前列腺素。

    公开(公告)号：EP0213129A1

    公开(公告)日：1987-03-11

    申请号：EP85901971.0

    申请日：1985-04-12

    Applicant: SCHERING AKTIENGESELLSCHAFT

    Inventor： RADÜCHEL, Bernd ,  SKUBALLA, Werner ,  VORBRÜGGEN, Helmut ,  LOGE, Olaf ,  ELGER, Walter

    IPC: C07C ,  A61K31 ,  C07C67 ,  C07C401 ,  C07C405 ,  C07D521

    CPC classification number: C07C405/0016 ,  C07C405/00 ,  C07C405/0033 ,  C07C405/0041

    Abstract: Dérivés de 9-halogène-prostane de formule (I) où Hal représente un atome de chlore ou de fluor en position alpha ou beta; R1 représente le résidu CH2OH ou formule (A) avec R2 représentant un atome d'hydrogène, un résidu alkyle, cycloalkyle, aryle ou hétérocyclique ou R1 représente le résidu formule (B) avec R3 représentant un résidu acide ou le résidu R2; A représente un groupe -CH2-CH2-, -CH=CH- trans ou -C=C-; W représente un groupe hydroxyméthylène libre ou fonctionnellement transformé ou un groupe formule (C) libre ou fonctionnellement transformé, le groupe OH pouvant se trouver en alpha ou en beta; D et E représentent ensemble une liaison directe ou D représente un groupe alcène à chaîne droite, ramifiée ou cyclique avec de 1 à 10 atomes de C, substitué le cas échéant par des atomes de fluor, et E représente un oxygène ou un soufre, une liaison directe, une liaison -C=C- ou un groupe -CR6=CR7, R6 et R7 étant différents et représentant un hydrogène, un chlore ou un alkyle avec de 1 à 4 C; R4 représente un groupe hydroxy libre ou fonctionnellement modifié; R5 représente un atome d'hydrogène, un groupe alkyle, alkyle halogène-substitué, cycloalkyle, aryle le cas échéant substitué ou hétérocyclique; ainsi que, si R2 représente un atome d'hydrogène, leurs sels avec des bases physiologiquement acceptables, leur procédé de préparation et leur utilisation pharmaceutique.

    COMBINATION OF DROSPIRENONE AND AN ESTROGEN SULPHAMATE FOR HRT
    9.
    发明公开
    COMBINATION OF DROSPIRENONE AND AN ESTROGEN SULPHAMATE FOR HRT 审中-公开
    屈螺酮和ESTROGENSULPHAMATE衍生物作为激素替代疗法组合

    公开(公告)号：EP1406634A1

    公开(公告)日：2004-04-14

    申请号：EP02755534.1

    申请日：2002-07-12

    Applicant: SCHERING AKTIENGESELLSCHAFT

    Inventor： SCHUERMANN, Rolf ,  ELGER, Walter

    IPC: A61K31/565 ,  A61K31/58

    CPC classification number: A61K31/565 ,  A61K31/58 ,  A61K2300/00

    Abstract: A pharmaceutical dosage unit comprising drospirenone and an estrogen sulphamate, such as an estradiol sulphamate or an estriol sulphamate for use in hormone replacement therapy is disclosed. This, combination therapy may comprise continuous or discontinuous administration of drospirenone and/or the estrogen sulphamate, such as weekly administration of both agents or weekly administration of the estrogen sulphamate and daily administration of the drospirenone.

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