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    THERAPEUTICALLY ACTIVE 17-NITROGEN SUBSTITUTED ESTRATRIENTHIAZOLE DERIVATIVES AS INHIBITORS OF 17.BETA.-HYDROXYSTEROID DEHYDROGENASE
    2.
    发明申请
    THERAPEUTICALLY ACTIVE 17-NITROGEN SUBSTITUTED ESTRATRIENTHIAZOLE DERIVATIVES AS INHIBITORS OF 17.BETA.-HYDROXYSTEROID DEHYDROGENASE 审中-公开
    作为17.BETA.-羟基脱氢酶脱氢酶的抑制剂的治疗性活性的17-硝基取代的咪唑并噻吩衍生物

    公开(公告)号：WO2014207310A1

    公开(公告)日：2014-12-31

    申请号：PCT/FI2014/050518

    申请日：2014-06-25

    Applicant: FORENDO PHARMA LTD

    Inventor： ELORANTA, Maire ,  HIRVELÄ, Leena ,  KANGAS, Lauri ,  KOSKIMIES, Pasi ,  LAMMINTAUSTA, Risto ,  UNKILA, Mikko

    IPC: C07J43/00 ,  C07J71/00 ,  A61K31/58 ,  A61P5/32

    CPC classification number: C07J43/003 ,  A61K31/58 ,  C07J71/0052 ,  C07J71/0068

    Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R2to R7are as defined in the claims. The invention further relates to their use as inhibitors of 17β-HSD and in treatment or prevention of steroid hormone de- pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17β-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the afore- mentioned compounds or pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐，其中R 2至R 7如权利要求中所定义。 本发明进一步涉及它们作为17β-抑制剂-HSD的抑制剂的用途，以及用于治疗或预防类固醇激素依赖性疾病或病症，例如类固醇激素依赖性疾病或需要抑制17β-HSD1酶和/或 需要降低内源性雌二醇浓度。 本发明还涉及上述化合物的制备和药物组合物，其包含一种或多种上述化合物或其药学上可接受的盐作为活性成分。

    PROCESS FOR THE PURIFICATION OF SAPONINS
    7.
    发明申请
    PROCESS FOR THE PURIFICATION OF SAPONINS 审中-公开
    SAPONINS的净化方法

    公开(公告)号：WO2014016374A1

    公开(公告)日：2014-01-30

    申请号：PCT/EP2013/065708

    申请日：2013-07-25

    Applicant: GLAXOSMITHKLINE BIOLOGICALS S.A.

    Inventor： DIAZ GARCIA, Juan Jose ,  HOLZER, Margit Theresia

    IPC: C07H1/08 ,  C07H15/256

    CPC classification number: C07J71/0052 ,  A61K2236/00 ,  C07H1/08 ,  C07H15/256

    Abstract: The present invention provides methods for purifying at least one saponin in a solution comprising the steps of: (a) providing at least one saponin in a first solvent comprising a solubilizing component; (b) replacing at least a portion of the solubilizing component with an exchange solvent, thereby producing a replaced solvent; and (c) removing the replaced solvent, to produce a dried saponin product comprising at least one saponin.

    Abstract translation: 本发明提供了用于纯化溶液中至少一种皂苷的方法，包括以下步骤：（a）在包含增溶组分的第一溶剂中提供至少一种皂苷; （b）用交换溶剂代替溶解成分的至少一部分，由此制造更换的溶剂; 和（c）除去置换的溶剂，以产生包含至少一种皂苷的干燥皂苷产品。

    17β-HSD1 AND STS INHIBITORS
    8.
    发明申请
    17β-HSD1 AND STS INHIBITORS 审中-公开
    17β-HSD1和STS抑制剂

    公开(公告)号：WO2006125800A1

    公开(公告)日：2006-11-30

    申请号：PCT/EP2006/062587

    申请日：2006-05-24

    Applicant: SOLVAY PHARMACEUTICALS GMBH

    Inventor： MESSINGER, Josef ,  THOLE, Heinrich-Hubert ,  HUSEN, Bettina ,  KOSKIMIES, Pasi ,  PIRKKALA, Lila ,  WESKE, Michael

    IPC: C07J41/00 ,  C07J71/00 ,  C07J43/00 ,  A61K31/565 ,  A61K31/58 ,  A61P5/32

    CPC classification number: C07J71/0052 ,  C07J41/0072 ,  C07J43/003 ,  C07J71/0068

    Abstract: The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration.

    Abstract translation: 本发明涉及代表17β-羟类固醇脱氢酶I型（17β-HSD1）的选择性抑制剂的新型取代的类固醇衍生物，此外，其可以代表类固醇硫酸酯酶及其盐的药物制剂 含有这些化合物和制备这些化合物的方法。 此外，本发明涉及所述新型取代的类固醇衍生物的治疗用途，特别是其用于治疗或预防类固醇激素依赖性疾病或病症，例如类固醇激素依赖性疾病或需要抑制I型17β-羟类固醇脱氢酶的病症或 /或类固醇硫酸酶和/或需要降低内源性17β-雌二醇浓度。

    11'beta'-SUBSTITUTED PROGESTERONE ANALOGS
    9.
    发明申请
    11'beta'-SUBSTITUTED PROGESTERONE ANALOGS 审中-公开
    11 beta - 发酵的孕激素类似物

    公开(公告)号：WO1989012448A1

    公开(公告)日：1989-12-28

    申请号：PCT/US1989002706

    申请日：1989-06-23

    Applicant: RESEARCH TRIANGLE INSTITUTE

    Inventor： RESEARCH TRIANGLE INSTITUTE ,  COOK, C., Edgar ,  WANI, Mansukh, C. ,  LEE, Yue-Wei ,  REEL, Jerry, R. ,  RECTOR, Douglas

    IPC: A61K31/56

    CPC classification number: C07J41/0083 ,  C07J7/002 ,  C07J7/0045 ,  C07J13/005 ,  C07J53/004 ,  C07J71/0052

    Abstract: An 11 beta -aryl-19-norprogesterone steroid of formula (I): wherein (i) R is H, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, OH, OC(O)CH3, or OC(O)R , wherein R is C2-8 alkyl, C2-8 alkenyl, C2-8 alkynyl or aryl, R2 is H, R is H, C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl, R is H, CH3, F or Cl, R is H, (CH3)2N, CH3O, CH3CO, CH3S, CH3SO, CH3SO2, and X is O or NOCH3; or (ii) R and R taken together are a carbon-carbon bond and R , R , R and X are as defined above; or (iii) R and R taken together are -CH2- or -N=N-CH2-, R is H and R , R and X are as defined above; or (iv) R and R taken together are =CH2 and R , R , R and X are as defined above.

    Abstract translation: 式（I）的11β-芳基-19-去甲孕酮类固醇：其中（i）R 1是H，C 1-4烷基，C 2-4烯基，C 2-4炔基，OH，OC（O）CH 3， 或OC（O）R 5，其中R 5是C 2-8烷基，C 2-8烯基，C 2-8炔基或芳基，R 2是H，R 3是H，C 1-4烷基，C 2 -4-烯基或C 2-4炔基，R 4是H，CH 3，F或Cl，R 6是H，（CH 3）2 N，CH 3 O，CH 3 CO，CH 3 S，CH 3 SO，CH 3 SO 2，X是O或NOCH 3 ; 或（ii）R 1和R 2一起是碳 - 碳键，R 3，R 4，R 6和X如上所定义; 或（iii）R 1和R 3一起是-CH 2 - 或-N = N-CH 2 - ，R 2是H且R 4，R 6和X如上所定义 ; 或（iv）R 2和R 3一起为= CH 2且R 1，R 4，R 6和X如上所定义。

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