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    9-alpha-substituted estratrienes as selectively active estrogens
    1.
    发明申请
    9-alpha-substituted estratrienes as selectively active estrogens 失效
    9-α-取代的雌三醇作为选择性活性雌激素

    公开(公告)号：US20040087565A1

    公开(公告)日：2004-05-06

    申请号：US10458735

    申请日：2003-06-11

    Applicant: Schering AG

    Inventor： Dirk Kosemund ,  Gerd Mueller ,  Alexander Hillisch ,  Karl-Heinrich Fritzemeier ,  Peter Muhn

    IPC: A61K031/56 ,  C07J041/00

    CPC classification number: C07J41/00 ,  Y10S514/825 ,  Y10S514/843

    Abstract: This invention describes the new 9null-substituted estratrienes of general formula I 1 in which R3, R7, R7null, R13, R16 as well as R17 and R17null have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.

    Abstract translation: 本发明描述了通式I的新的9-取代的雌三烯，其中R 3，R 7，R 7'，R 13，R 16以及R 17和R 17， 17'具有在说明书中指出的含义，R 9表示具有2-6个碳原子的直链或支链，任选部分或完全卤化的烯基，乙炔基或丙-1-茚基 作为药物活性成分，其在体外具有比来自大鼠前列腺素的雌激素受体制剂更高的亲和力，而不是雌激素受体制剂从大鼠子宫和体内表现出优于子宫与子宫，其生产，其治疗用途相比的优先作用， 含有新化合物的药物分配形式。 本发明还描述了这些化合物用于治疗雌激素缺乏诱导的疾病和病症的用途。

    8Beta-substituted 11beta-aryl-estra-1,3,5,(10)-triene derivatives
    5.
    发明申请
    8Beta-substituted 11beta-aryl-estra-1,3,5,(10)-triene derivatives 审中-公开
    8Beta-取代的11ba-芳基 - 雌-1,3,5，（10） - 三烯衍生物

    公开(公告)号：US20030171345A1

    公开(公告)日：2003-09-11

    申请号：US10270077

    申请日：2002-10-15

    Applicant: Schering AG

    Inventor： Nico Brauer ,  Olaf Peters ,  Alexander Hillisch ,  Christa Hegele-Hartung ,  Peter Muhn

    IPC: C07J043/00 ,  A61K031/58 ,  A61K031/56 ,  C07J001/00

    CPC classification number: C07J1/00 ,  C07J43/00

    Abstract: This invention relates to 11null-(para-substituted)phenyl-estra-1,3,5(10)-trienes with a straight-chin or branched-chain, optionally partially or completely halogenated alkyl radical or alkenyl radical in each case with up to 5 carbon atoms, an ethinyl radical or prop-1-inyl radical in 8null-position. The new compounds can be used for contraception in men and women, without influencing other estrogen-sensitive organs, such as the uterus or the liver. They are also suitable for the treatment of benign or malignant proliferative diseases of the ovary, such as ovarian cancer and granulosa cell tumors.

    Abstract translation: 本发明涉及具有直链或支链，任选部分或完全卤代的烷基或烯基的11beta-（对位取代的）苯基 - 雌-1,3,5（10） - 三 至5个碳原子，乙炔基或丙-1-基在8beta位。 新化合物可用于男性和女性避孕，而不影响其他雌激素敏感性器官，如子宫或肝脏。 它们也适用于治疗卵巢良性或恶性增殖性疾病，如卵巢癌和颗粒细胞瘤。

    Antitumor wirksame 2-alkoxyestradiolsulfamate
    7.
    发明申请
    Antitumor wirksame 2-alkoxyestradiolsulfamate 失效
    抗肿瘤剂wirksame 2-烷氧基雌二甲酰氨基磺酸盐

    公开(公告)号：US20030100544A1

    公开(公告)日：2003-05-29

    申请号：US10217165

    申请日：2002-08-13

    Applicant: Schering AG

    Inventor： Ina Scherlitz-Hofmann ,  Jens Hoffmann ,  Alexander Hillisch ,  Eberhard Unger ,  Tobias Neumann ,  Sigfrid Schwarz ,  Olaf Peters ,  Thomas Michel

    IPC: A61K031/56

    CPC classification number: A61K31/565 ,  A61K31/56

    Abstract: The present invention relates to the use of 2-alkoxyestrogen sulfamates of general formula I 1 wherein R1 and R2 independently represent H, methyl, C1-C4 acyl, benzoyl R3 represents C1-C4 alkyl or a group of formula CnFmHo, wherein nnull1, 2, 3, 4, 5 or 6, m>1, and mnullonull2nnull1, R4 and R5 in each case represent H or, together, a methylene group or an additional double bond, R6 represents H. R7 represents OH, OC1-C4-alkyl, OC1-C11-acyl or OSO2NR1R2, the dashed lines in the B and C rings of the steroid skeleton additionally representing up to two double bonds, for the production of a medical drug for the treatment of tumor diseases which can be affected positively by inhibiting the tubulin polymerization. The inventive compounds are distinguished by the 2-alkoxy substitution in conjunction with the 17-hydroxy substitution. They have a special effect with regard to inhibiting tubulin polymerization and can be used, for example, for the treatment of prostate cancers.

    Abstract translation: 本发明涉及通式Ⅰ的2-烷氧基雌激素亚磺酸盐的用途，其中R 1和R 2独立地表示H，甲基，C 1 -C 4酰基，苯甲酰基，R 3表示C 1 -C 4烷基或式C n F m H 0基团，其中n = 2个，3个，4个，5个或6个，m> 1，m + o = 2n + 1，R4和R5各自表示H或者一起表示亚甲基或另外的双键，R6表示H. R7表示 OH，OC1-C4-烷基，OC1-C11-酰基或OSO2NR1R2，类固醇骨架的B和C环中的虚线另外代表多达两个双键，用于生产用于治疗肿瘤疾病的药物 这可以通过抑制微管蛋白聚合而受到积极的影响。 本发明化合物通过2-烷氧基取代与17-羟基取代相结合来区分。 它们在抑制微管蛋白聚合方面具有特殊的效果，并且可以用于例如前列腺癌的治疗。

    Substrate for PP2C
    9.
    发明申请
    Substrate for PP2C 失效
    PP2C基材

    公开(公告)号：US20030044875A1

    公开(公告)日：2003-03-06

    申请号：US10188374

    申请日：2002-07-03

    Applicant: Schering AG

    Inventor： Josef Krieglstein ,  Susanne Klumpp

    IPC: C12Q001/42

    CPC classification number: C07K14/4702 ,  C07K14/4703 ,  C07K14/4747 ,  C12N9/16

    Abstract: The invention relates to a combination of a protein phosphatase type 2C as an enzyme and a phospho-BAD as substrate. The protein BAD is dephosphorylated in position Ser155. Furthermore, the combination is used in an in vitro screening for ligands which modulate protein phosphatase type 2C, comprising the steps: incubating the protein phosphatase type 2C in combination with the substrate phospho-BAD and the ligand of the assay and detecting the decrease in phospho-BAD and/or the increase in phosphate and/or BAD. Therefore, new drugs for the treatment apoptosis may be found.

    Abstract translation: 本发明涉及作为酶的2C型蛋白磷酸酶与磷酸-BAD作为底物的组合。 蛋白质BAD在Ser155位置脱磷酸化。 此外，该组合用于体外筛选调节2C型蛋白磷酸酶的配体，包括以下步骤：将蛋白磷酸酶2C类型与底物磷酸-BAD和测定配体组合孵育，并检测磷酸化的降低 -BAD和/或磷酸盐和/或BAD的增加。 因此，可以发现用于治疗凋亡的新药物。

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