公开(公告)号：US5614213A

公开(公告)日：1997-03-25

申请号：US295723

申请日：1994-08-31

申请人： Walter Elger ,  Birgitt Schneider ,  Michael Oettel ,  Michael Ernst ,  Doris Hubler ,  Michael Dittgen

发明人： Walter Elger ,  Birgitt Schneider ,  Michael Oettel ,  Michael Ernst ,  Doris Hubler ,  Michael Dittgen

IPC分类号： A61K9/06 ,  A61K9/70 ,  A61K31/565 ,  A61P3/02 ,  A61P19/10 ,  A61P43/00 ,  A61F13/00

CPC分类号： A61K9/7084 ,  A61K31/565 ,  Y10S514/969

摘要： The invention relates to the use of estriol as the sole active ingredient for the production of a transdermal medicament which continuously releases the active ingredient for the treatment of climacteric osteoporosis. It has been shown according to the invention that estriol, which has up until now been thought ineffective for the treatment of climacteric osteoporosis, develops strong anti-osteoporotic effectiveness upon continuous transdermal application.

摘要翻译： PCT No.PCT / EP93 / 00636 Sec。 371日期1994年8月31日 102（e）日期1994年8月31日PCT 1993年3月18日PCT公布。 出版物WO93 / 18774 日期1993年9月30日本发明涉及使用雌三醇作为唯一活性成分用于生产连续释放用于治疗更年期骨质疏松症的活性成分的透皮药物。 根据本发明已经显示，直至现在被认为对治疗更年期性骨质疏松症无效的雌三醇在连续经皮施用时发挥强烈的抗骨质疏松效果。

公开(公告)号：US20070078091A1

公开(公告)日：2007-04-05

申请号：US11517301

申请日：2006-09-08

申请人： Doris Hubler ,  Michael Oettel ,  Lothar Sobek ,  Walter Elger ,  Abdul-Abbas Al-Mudhaffar

发明人： Doris Hubler ,  Michael Oettel ,  Lothar Sobek ,  Walter Elger ,  Abdul-Abbas Al-Mudhaffar

IPC分类号： A61K38/09 ,  A61K31/57 ,  A61K31/56 ,  A61K31/519 ,  A61K31/517 ,  A61K31/4709 ,  A61K31/138

CPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/585 ,  A61K45/06 ,  A61K2300/00

摘要： This invention relates to pharmaceutical combinations for compensating for an absolute and relative testosterone deficiency in men with simultaneous prophylaxis for the development of a benign prostatic hyperplasia (BPH) or prostate cancer. The combinations according to the invention contain a natural or synthetic androgen in combination with a gestagen, an antigestagen, an antiestrogen, a GnRH analog, a testosterone-5α-reductase inhibitor, an α-andreno-receptor blocker or a phosphodiesterase inhibitor. In comparison to the combinations according to the invention, any active ingredient by itself cannot achieve the desired goal.

摘要翻译： 本发明涉及用于补偿男性绝对和相对睾酮缺乏的药物组合，同时预防良性前列腺增生（BPH）或前列腺癌的发展。 根据本发明的组合含有天然或合成的雄激素与孕激素，抗原成分，抗雌激素，GnRH类似物，睾酮-5α-还原酶抑制剂，α-肾上腺素受体阻断剂或磷酸二酯酶抑制剂的组合。 与根据本发明的组合相比，任何活性成分本身都不能实现期望的目标。

公开(公告)号：US20050131076A1

公开(公告)日：2005-06-16

申请号：US10923080

申请日：2004-08-23

申请人： Ralf Wyrwa ,  Sven Ring ,  Guenter Kaufmann ,  Walter Elger ,  Birgitt Schneider

发明人： Ralf Wyrwa ,  Sven Ring ,  Guenter Kaufmann ,  Walter Elger ,  Birgitt Schneider

IPC分类号： A61K31/12 ,  A61K31/56 ,  C07J63/00 ,  C07J75/00

CPC分类号： C07J63/00 ,  Y10S514/841

摘要： The invention relates to Δ15-D-homosteroids of general formula (I) process for their production and pharmaceutical compositions that contain these compounds. The compounds of general formula I according to the invention have androgenic activity.

摘要翻译： 本发明涉及其制备的通式（I）的三羟甲基-D-类固醇激素和含有这些化合物的药物组合物。 根据本发明的通式I化合物具有雄激素活性。

公开(公告)号：US07419972B2

公开(公告)日：2008-09-02

申请号：US11154947

申请日：2005-06-17

申请人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Wilko Regenhardt ,  Andrea Rosinus ,  Jerzy Adamski ,  Gabriele Moeller ,  Walter Elger ,  Birgitt Schneider ,  Ulrich Bothe

发明人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Wilko Regenhardt ,  Andrea Rosinus ,  Jerzy Adamski ,  Gabriele Moeller ,  Walter Elger ,  Birgitt Schneider ,  Ulrich Bothe

IPC分类号： A61K31/56 ,  A61K31/16 ,  C07J1/00 ,  C07J31/00

CPC分类号： C07J1/00

摘要： The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of formula I as well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for prophylaxis and/or therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17β-hydroxy steroid dehydrogenase type 1.

摘要翻译： 本发明涉及式I的新的2-取代的雌-1,3,5（10） - 三烯-17-酮及其药学上可接受的盐，其制备和用作预防和/或治疗药物的方法 雌激素依赖性疾病，可受1型17β-羟基类固醇脱氢酶抑制的影响。

公开(公告)号：US07199115B2

公开(公告)日：2007-04-03

申请号：US11104736

申请日：2005-04-13

申请人： Ulrich Bothe ,  Peter Droescher ,  Walter Elger ,  Gudrun Reddersen ,  Bernd Menzenbach ,  Hans-Udo Schweikert ,  Alexander Hillisch ,  Birgitt Schneider

发明人： Ulrich Bothe ,  Peter Droescher ,  Walter Elger ,  Gudrun Reddersen ,  Bernd Menzenbach ,  Hans-Udo Schweikert ,  Alexander Hillisch ,  Birgitt Schneider

IPC分类号： A61K31/56 ,  C07J3/00

CPC分类号： C07J3/00

摘要： New 17α-fluorosteroid compounds of formula (I) are disclosed: wherein R1 denotes H or methyl; R2 and R3 each denote H, Cl or methyl; and either a double bond or a single bond is present between C-6 and C-7 and also C-9 and C-10 of the steroid ring system respectively. These compounds have an activity profile with hybrid character so that they act as inhibitors for 5α-reductase and as high potency gestagens. Pharmaceutical compositions containing them are disclosed. They are suitable for treatment of conditions, which are caused by high levels of androgen in organs and tissues. These new compounds can be used in combination with other hormonal substances, such as estrogens, testosterone and other androgens, as contraceptives and for other applications.

摘要翻译： 公开了式（I）的新的17α-荧光素类化合物：

公开(公告)号：US20050277625A1

公开(公告)日：2005-12-15

申请号：US11134618

申请日：2005-05-23

申请人： Ralf Wyrwa ,  Sven Ring ,  Peter Droescher ,  Alexander Hillisch ,  Walter Elger ,  Birgitt Schneider ,  Gudrun Reddersen

发明人： Ralf Wyrwa ,  Sven Ring ,  Peter Droescher ,  Alexander Hillisch ,  Walter Elger ,  Birgitt Schneider ,  Gudrun Reddersen

IPC分类号： A61K31/56 ,  C07J1/00

CPC分类号： C07J1/00

摘要： This invention provides estriol and estetrol prodrugs of general formula (I), in which group Y is bonded to the steroid process for their production, pharmaceutical compositions that contain these compounds, as well as their use for the production of pharmaceutical agents with estrogenic action.

摘要翻译： 本发明提供了通式（I）的雌三醇和雌酮前体药物，其中Y基团与类固醇过程结合用于其生产，含有这些化合物的药物组合物以及其用于生产具有雌激素作用的药剂的用途。

公开(公告)号：US07732493B2

公开(公告)日：2010-06-08

申请号：US12192446

申请日：2008-08-15

申请人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Wilko Regenhardt ,  Gabriele Moeller ,  Dominga Deluca ,  Jerzy Adamski ,  Walter Elger ,  Birgitt Schneider

发明人： Alexander Hillisch ,  Olaf Peters ,  Christian Gege ,  Wilko Regenhardt ,  Gabriele Moeller ,  Dominga Deluca ,  Jerzy Adamski ,  Walter Elger ,  Birgitt Schneider

IPC分类号： A61K31/12 ,  A61K31/56 ,  C07J1/00 ,  C07C49/00

CPC分类号： C07J63/00

摘要： The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17β-hydroxy steroid dehydro-genase type 1.

摘要翻译： 本发明涉及通式I的新的2-取代的D-异 - 雌-1,3,5（10） - 三烯，其中R 2表示C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基或卤素 原子，R 13表示氢原子或甲基，R 17表示氢原子或氟原子，以及它们的药学上可接受的盐，它们的制备和用途，作为预防和治疗雌激素依赖性疾病的药物，其可受 抑制17＆bgr-羟基类固醇脱氢酶1型。

公开(公告)号：US20050026891A1

公开(公告)日：2005-02-03

申请号：US10631967

申请日：2003-08-01

申请人： Alexander Hillisch ,  Walter Elger ,  Gerd Schubert ,  Birgitt Schneider ,  Gudrun Reddersen

发明人： Alexander Hillisch ,  Walter Elger ,  Gerd Schubert ,  Birgitt Schneider ,  Gudrun Reddersen

IPC分类号： A61K31/56 ,  A61K31/565 ,  A61K31/566 ,  A61K45/06 ,  C07J1/00 ,  C07J41/00

CPC分类号： C07J41/0083 ,  A61K31/565 ,  A61K31/566 ,  A61K45/06 ,  C07J1/00 ,  Y10S514/814 ,  A61K2300/00

摘要： The invention relates to new compounds of general formula I, their production and pharmaceutical preparations that contain these compounds. The compounds according to the invention are preferably used for female birth control and for HRT.

摘要翻译： 本发明涉及通式Ⅰ的新化合物，它们的生产和含有这些化合物的药物制剂。 根据本发明的化合物优选用于女性避孕和HRT。

公开(公告)号：US06825182B2

公开(公告)日：2004-11-30

申请号：US10429247

申请日：2003-05-05

申请人： Sven Ring ,  Gerd Schubert ,  Ingo Tornus ,  Guenter Kaufmann ,  Walter Elger ,  Birgitt Schneider

发明人： Sven Ring ,  Gerd Schubert ,  Ingo Tornus ,  Guenter Kaufmann ,  Walter Elger ,  Birgitt Schneider

IPC分类号： A61K3156

CPC分类号： C07J41/00 ,  C07J75/00

摘要： Compounds of general formula I as well as their pharmaceutically compatible salts are described, in which R1 stands for hydrogen, C1- to C6-alkyl, COR4, COOR4, COSR4 or CONHR5, in which R4 is C1- to C6-alkyl or unsubstituted or substituted aryl and in which R5 is hydrogen, C1- to C6-alkyl or unsubstituted or substituted aryl, in which R2 also stands for hydrogen, C1- to C6-alkyl or C1- to C6-acyl, and R3 stands for a CnF2n+1 group, in which n=1, 2 or 3, or a CH2O(CH2)mCnF2n+1 group, in which m=0 or 1 and n=1, 2 or 3. In addition, a process for the production of the compounds with general formula I is indicated. The compounds can be used for the production of pharmaceutical agents.

公开(公告)号：US06534490B1

公开(公告)日：2003-03-18

申请号：US09720135

申请日：2000-12-21

申请人： Sven Ring ,  Sigfrid Schwarz ,  Walter Elger ,  Birgitt Schneider ,  Günter Kaufmann ,  Lothar Sobek

发明人： Sven Ring ,  Sigfrid Schwarz ,  Walter Elger ,  Birgitt Schneider ,  Günter Kaufmann ,  Lothar Sobek

IPC分类号： A61K3156

CPC分类号： C07J53/004

摘要： Described are new, unsaturated 14,15-cyclopropano-androstanes of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are characterized by hormonal (gestagenic and/or androgenic) activity and may be used for hormone replacement therapy.

摘要翻译： 描述了通式（I）的新的不饱和14,15-环丙烷 - 雄甾烷及其药学上可接受的盐，它们的制备方法和含有这些化合物的药物制剂。 化合物的特征在于激素（孕激素和/或雄激素）活性，可用于激素替代疗法。