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：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：US5855905A

公开(公告)日：1999-01-05

申请号：US841719

申请日：1997-04-30

申请人： Michael Oettel ,  Siegfried Golbs ,  Michael Dittgen ,  Carsten Timpe ,  Thomas Graser ,  Doris Hubler

发明人： Michael Oettel ,  Siegfried Golbs ,  Michael Dittgen ,  Carsten Timpe ,  Thomas Graser ,  Doris Hubler

IPC分类号： A61K31/565

CPC分类号： A61K31/565

摘要： A compound preparation for the treatment of hypogonadal men and men with hypophyseal diseases. This invention relates to compound preparations containing biogenous or synthetic androgens and biogenous or synthetic estrogens that are used for the treatment of imbalances of the testosterone metabolism in old age, of hypogonadal men, and of men with hypophyseal diseases. These compound preparations are present in various galenic formulations such as ointments, gels, sprays, TTS systems, tablets, lozenges, capsules, and suppositories. These preparations are used to treat the fluctuations of the testosterone metabolism occurring in old age and with certain diseases such as hypophyseal diseases (adenoma), hypogonadism and/or metabolic syndrome, to maintain the balance between androgens and estrogens found in young and healthy men in ill and/or elderly men as well. The preparations for treating these imbalances are suitable for oral, parenteral, percutaneous, sublingual or rectal administration depending on their galenic form. Thus, unphysiological changes in steroid-converting enzymes such as aromatases and reductases are avoided, which considerably improves the outcome of the therapy.

摘要翻译： 用于治疗性腺功能减退的男性和男性的复方制剂。 本发明涉及包含生物或合成雄激素和生物或合成雌激素的化合物制剂，其用于治疗老年睾酮代谢失调，性腺机能不良男性和具有垂体浸润性疾病的男性的不平衡。 这些复合制剂存在于各种盖仑制剂如软膏，凝胶剂，喷雾剂，TTS系统，片剂，锭剂，胶囊和栓剂中。 这些制剂用于治疗老年发生的睾酮代谢的波动，以及诸如垂体疾病（腺瘤），性腺机能减退和/或代谢综合征等某些疾病，以维持年轻和健康男性发现的雄激素和雌激素之间的平衡 生病和/或老年男子。 用于治疗这些不平衡的制剂适用于口服，肠胃外，经皮，舌下或直肠给药，取决于其盖仑形式。 因此，避免类固醇转化酶如芳香酶和还原酶的非生理变化，这显着改善了治疗的结果。

公开(公告)号：US5866559A

公开(公告)日：1999-02-02

申请号：US771805

申请日：1996-12-20

申请人： Gerhard Teichmuller ,  Gerd Muller ,  Sigfrid Schwarz ,  Bernd Undeutsch ,  Harry Henkel ,  Ronald Gebuhr ,  Gunter Kaufmann ,  Doris Hubler ,  Michael Oettel

发明人： Gerhard Teichmuller ,  Gerd Muller ,  Sigfrid Schwarz ,  Bernd Undeutsch ,  Harry Henkel ,  Ronald Gebuhr ,  Gunter Kaufmann ,  Doris Hubler ,  Michael Oettel

IPC分类号： A61K31/565 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07J41/00 ,  C07J75/00 ,  A61K31/57 ,  C07J7/00

CPC分类号： C07J41/0016 ,  C07J41/0094

摘要： The 17.alpha.-cyanomethylestra-4,9-diene derivative compounds are of formula I: ##STR1## wherein R.sub.1 is an alkyl group having from 1 to 2 carbon atoms; R.sub.2 is an alkyl group with 1 to 10 carbon atoms, an acyl group with 1 to 10 carbon atoms or a trialkylsilyl group; and R.sub.3 is an oxygen atom or a R--O--N group, wherein R is a hydrogen atom, an acyl group with 1 to 10 carbon atoms, an alkyl group with 1 to 10 carbon atoms, a sulfamoyl group, an alkylsilyl group or a trialkylsilyl group. These compounds, particularly in combination with at least one suitable estrogen, are suitable for treatment of endometrioses or gestagen-dependent tumors and for hormonal contraception and climacteric hormone replacement therapy (HRT). Processes for making the new steroids are described as well as methods of making the pharmaceutical compositions containing them.

摘要翻译： 17α-氰基甲基雌甾-4,9-二烯衍生物化合物具有式I：其中R 1是具有1至2个碳原子的烷基; R2是碳原子数为1〜10的烷基，碳原子数1〜10的酰基或三烷基甲硅烷基; R3为氧原子或R-O-N基，其中R为氢原子，具有1-10个碳原子的酰基，具有1-10个碳原子的烷基，氨磺酰基，烷基甲硅烷基或三烷基甲硅烷基。 这些化合物，特别是与至少一种合适的雌激素组合，适用于治疗子宫内膜异位症或孕激素依赖性肿瘤以及激素避孕和更年期激素替代疗法（HRT）。 描述了制备新类固醇的方法以及制备含有它们的药物组合物的方法。

公开(公告)号：US5693628A

公开(公告)日：1997-12-02

申请号：US309175

申请日：1994-09-20

申请人： Gerd Schubert ,  Gunther Kaufmann ,  Lothar Sobeck ,  Michael Oettel ,  Walter Elger ,  Anatoli Kurischko

发明人： Gerd Schubert ,  Gunther Kaufmann ,  Lothar Sobeck ,  Michael Oettel ,  Walter Elger ,  Anatoli Kurischko

IPC分类号： A61K31/56 ,  A61K31/565 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  C07J41/00 ,  C07J75/00 ,  C07J1/00

CPC分类号： C07J41/0094 ,  C07J41/0083

摘要： This invention relates to new 11-benzaldoxime-estra-diene derivatives of the general formula I ##STR1## and their pharmaceutically acceptable salts, a method for their production, and pharmaceuticals containing such compounds. The compounds described show strong antigestagenic effects combined with reduced glucocorticoid activity.

摘要翻译： 本发明涉及通式I（I）的新的11-苯甲醛肟 - 雌二烯衍生物及其药学上可接受的盐，其制备方法和含有这些化合物的药物。 所描述的化合物显示出强的抗前体效应以及糖皮质激素活性降低。

公开(公告)号：US07053077B1

公开(公告)日：2006-05-30

申请号：US09744574

申请日：1999-05-13

申请人： Walter Elger ,  Pekka Lähteenmäki ,  Matti Lehtinen ,  Gudrun Reddersen ,  Holger Zimmermann ,  Michael Oettel ,  Sigfrid Schwarz

发明人： Walter Elger ,  Pekka Lähteenmäki ,  Matti Lehtinen ,  Gudrun Reddersen ,  Holger Zimmermann ,  Michael Oettel ,  Sigfrid Schwarz

IPC分类号： A61K31/56

CPC分类号： A61K31/566 ,  A61K31/565 ,  A61K31/57 ,  Y10S514/874 ,  A61K2300/00

摘要： The invention relates to the use of biogenic estrogen sulfamates for the oral discontinuous application for hormone replacement therapy (HRT). The discontinuous administration takes place in intervals ranging from 2 to 40 days. The invention also provides the additional application of gestagens, preferably continuously in the form of an implant or in the form of an intrauterine releasing system (IUD). Estrone sulfamate, estradiol sulfamate or an N-acyl sulfamate of estrone, estradiol or estriol having up to 7 C-atoms in the acyl chain, or a combination comprised of two or more of said active ingredients are used as biogenic estrogen sulfamates.

摘要翻译： 本发明涉及用于激素替代治疗（HRT）的口服不连续应用的生物源性雌激素氨基磺酸盐的用途。 不连续给药时间间隔为2至40天。 本发明还提供了孕妇的额外应用，优选连续地以植入物的形式或以子宫内释放系统（IUD）的形式。 氨基磺酸氨基磺酸酯，氨基磺酸雌二醇酯或酰基链中具有至多7个C原子的雌酮，雌二醇或雌三醇的N-酰基氨基磺酸酯或由两种或更多种所述活性成分组成的组合物用作生物来源的雌激素亚磺酸盐。

公开(公告)号：US5576310A

公开(公告)日：1996-11-19

申请号：US309270

申请日：1994-09-20

申请人： Gerd Schubert ,  G unther Kaufmann ,  Lothar Sobeck ,  Michael Oettel ,  Walter Elger ,  Anatoli Kurischko

发明人： Gerd Schubert ,  G unther Kaufmann ,  Lothar Sobeck ,  Michael Oettel ,  Walter Elger ,  Anatoli Kurischko

IPC分类号： C07J41/00 ,  A61K31/56

CPC分类号： C07J41/0083

摘要： This invention relates to new 11-benzaldoxime-estra-diene derivatives of the general formula I ##STR1## wherein Z is --CO--CH.sub.3, --CO--O--C.sub.2 H.sub.5, --CO--NH-phenyl, --CO--NH--C.sub.2 H.sub.5, --CO--C.sub.2 H.sub.5, --CH.sub.3, or --CO-phenyland their pharmaceutically acceptable salts, a method for their production, and pharmaceuticals containing such compounds. The compounds of the general formula I are produced by esterifying or etherizing a compound of the general formula II ##STR2## The compounds described show strong antigestagenic effects combined with reduced glucocorticoid activity.

摘要翻译： 本发明涉及通式Ⅰ的新的11-苯甲醛肟 - 雌二烯衍生物，其中Z是-CO-CH 3，-CO-O-C 2 H 5，-CO-N-苯基，-CO-NH- C 2 H 5，-CO-C 2 H 5，-CH 3或-CO-苯基及其药学上可接受的盐，其制备方法和含有这些化合物的药物。 通式I的化合物是通过酯化或醚化通式Ⅱ化合物来制备的。所述化合物显示出强的抗前体效应以及降低的糖皮质激素活性。

公开(公告)号：US06225299B1

公开(公告)日：2001-05-01

申请号：US09219660

申请日：1998-12-23

申请人： Siegfried Golbs ,  Michael Oettel ,  Michael Dittgen ,  Thomas Graser ,  Christoph Luderschmidt

发明人： Siegfried Golbs ,  Michael Oettel ,  Michael Dittgen ,  Thomas Graser ,  Christoph Luderschmidt

IPC分类号： A61K3156

CPC分类号： A61K31/56 ,  A61K8/63 ,  A61Q7/00 ,  Y10S514/859 ,  Y10S514/864

摘要： The pharmaceutical composition, especially for treating skin with seborrhea, Acne vulgaris and androgonically conditioned alopecia, contains a hormonal agent including the gestogen, dienogest, or a combination of dienogest and an estrogen, as active ingredient. Methods for treatment of this type of skin condition include topical application of the composition including the dienogest which results in an outstanding sebosuppression, a drastic reduction of androstandiol glucuronide and a moderate competitive blockage of androgen receptor sites. Galenic formulations are described which limit and/or prevent the permeation of the active ingredient through the skin. The pharmaceutical preparation including the dienogest and conventional dermatologically acceptable carrier and auxiliary substances in the described galenic formulation advantageously provides a drastic reduction in androstandiol glucuronide and moderate androgen receptor blockage without passing through the skin barrier so that systemic effects including side reactions are substantially prevented.

摘要翻译： 药物组合物，特别是用于治疗皮脂溢，皮肤寻常痤疮和阴道调理性脱发的皮肤，含有激素剂，包括睾酮，依那诺或二烯酸和雌激素的组合作为活性成分。 用于治疗这种类型皮肤病症的方法包括局部应用组合物，其包括引起明显的抑制作用的替奈格明，葡萄糖醛酸葡萄糖醛酸葡聚糖和葡萄糖醛酸葡聚糖的剧烈降低以及雄激素受体位点的适度竞争性阻断。 描述了限制和/或防止活性成分渗透皮肤的Galenic制剂。 在所述盖仑制剂中包含地那烯酸和常规皮肤病学可接受的载体和辅助物质的药物制剂有利地提供了葡萄糖醛酸葡萄糖醛酸葡萄糖苷和中和雄激素受体阻断物的急剧降低，而不会通过皮肤屏障，从而基本上防止包括副反应的全身效应。

公开(公告)号：US5910493A

公开(公告)日：1999-06-08

申请号：US714463

申请日：1996-09-16

申请人： Siegfried Golbs ,  Michael Oettel ,  Michael Dittgen ,  Thomas Graser ,  Christoph Luderschmidt

发明人： Siegfried Golbs ,  Michael Oettel ,  Michael Dittgen ,  Thomas Graser ,  Christoph Luderschmidt

IPC分类号： A61K8/63 ,  A61Q5/00 ,  A61Q7/00 ,  A61Q19/00 ,  A61K31/56

CPC分类号： A61K31/567 ,  A61K8/63 ,  A61Q19/00 ,  A61Q5/00 ,  A61Q7/00 ,  Y10S514/859 ,  Y10S514/864

摘要： The pharmaceutical composition, especially for treating skin with seborrhea, Acne vulgaris and androgonically conditioned alopecia, contains a hormonal agent including the gestogen, dienogest, or a combination of dienogest and an estrogen, as active ingredient. Methods for treatment of this type of skin condition include topical application of the composition including the dienogest which results in an outstanding sebosuppression, a drastic reduction of androstandiol glucuronide and a moderate competitive blockage of androgen receptor sites. Galenic formulations are described which limit and/or prevent the permeation of the active ingredient through the skin. The pharmaceutical preparation including the dienogest and conventional dermatologically acceptable carrier and auxiliary substances in the described galenic formulation advantageously provides a drastic reduction in androstandiol glucuronide and moderate androgen receptor blockage without passing through the skin barrier so that systemic effects including side reactions are substantially prevented.

摘要翻译： 药物组合物，特别是用于治疗皮脂溢，皮肤寻常痤疮和阴道调理性脱发的皮肤，含有激素剂，包括睾酮，依那诺或二烯酸和雌激素的组合作为活性成分。 用于治疗这种类型皮肤病症的方法包括局部应用组合物，其包括引起明显的抑制作用的替奈格明，葡萄糖醛酸葡萄糖醛酸葡聚糖和葡萄糖醛酸葡聚糖的剧烈降低以及雄激素受体位点的适度竞争性阻断。 描述了限制和/或防止活性成分渗透皮肤的Galenic制剂。 在所述盖仑制剂中包含地那烯酸和常规皮肤病学可接受的载体和辅助物质的药物制剂有利地提供了葡萄糖醛酸葡萄糖醛酸葡萄糖苷和中和雄激素受体阻断物的急剧降低，而不会通过皮肤屏障，从而基本上防止包括副反应的全身效应。

公开(公告)号：US20060142257A1

公开(公告)日：2006-06-29

申请号：US11356012

申请日：2006-02-17

申请人： Eberhard Nieschlag ,  Axel Kamischke ,  Michael Oettel ,  Alexander Ruebig ,  Ekkerhard Schillinger ,  Ursula-Friederike Habenicht

发明人： Eberhard Nieschlag ,  Axel Kamischke ,  Michael Oettel ,  Alexander Ruebig ,  Ekkerhard Schillinger ,  Ursula-Friederike Habenicht

IPC分类号： A61K31/56

CPC分类号： A61K31/56

摘要： A formulation for male contraception comprising a progestin possessing both estrogenic and androgenic properties is remarkably effective for spermatogenesis suppression in males. The progestin Norethisterone (NET), particularly its derivatives Norethisterone acetate and Norethisterone enanthate in sufficient doses induce oligozoospermia or azoospermia in males. Formulations further comprising an androgen, such as a testosterone derivative such as a testosterone ester, particularly testosterone undecanoate, are especially effective male contraceptive formulations.