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1.发明授权17.alpha.-cyanomethylestra-4,9-dien derivatives and pharmaceutical compositions containing same 失效17α-氰基甲基雌-4,9-二烯衍生物和含有它们的药物组合物
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。
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2.发明授权Compound preparation for the treatment of hypogonadal men and men with hypophyseal diseases 失效复方制剂治疗性腺功能减退的男性和男性患有垂体病
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。
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3.发明申请公开(公告)号：US20070078091A1
公开(公告)日：2007-04-05
申请号：US11517301
申请日：2006-09-08
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。
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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
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。
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5.发明授权Methods and pharmaceutical compositions for reliable achievement of acceptable serum testosterone levels 有权可靠地达到可接受的血清睾酮水平的方法和药物组合物公开(公告)号：US07718640B2
公开(公告)日：2010-05-18
申请号：US10798780
申请日：2004-03-12
IPC分类号： A61K31/56
CPC分类号： A61K31/565 , A61K9/0019 , A61K31/56 , A61K31/568 , A61K31/57 , A61K47/14 , A61K47/44
摘要： The present invention relates to pharmaceutical compositions, formulated for injectable administration, which comprises a testosterone ester, in particularly testosterone undecanoate, in a vehicle comprising castor oil and a co-solvent. Upon injecting the compositions according to a particular administration scheme, reliable levels of testosterone in serum in the normal physiological range is achieved for a long period. This allows for the use of the compositions in hormone replacement therapy and male contraception without concomitant monitoring of testosterone levels in serum by a physician.
摘要翻译： 本发明涉及配制用于可注射给药的药物组合物，其包含睾酮酯，特别是十一酸睾酮，载体包含蓖麻油和共溶剂。 在根据特定给药方案注射组合物时，长时间内可获得在正常生理范围内血清中可靠水平的睾丸激素。 这允许在激素替代治疗和男性避孕中使用组合物，而无需伴随地监测医师对血清中的睾酮水平。
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6.发明授权Methods and pharmaceutical compositions for reliable achievement of acceptable serum testosterone levels 有权可靠地达到可接受的血清睾酮水平的方法和药物组合物公开(公告)号：US08338395B2
公开(公告)日：2012-12-25
申请号：US12391655
申请日：2009-02-24
IPC分类号： A61K31/56
CPC分类号： A61K31/565 , A61K9/0019 , A61K31/56 , A61K31/568 , A61K31/57 , A61K47/14 , A61K47/44
摘要： Described are methods for providing prolonged physiologically acceptable steady state serum testosterone levels in a patient deficient in endogenous testosterone levels, methods for male contraception and methods for treating a disease or symptom associated with deficient endogenous levels of testosterone in a man, by intramuscularly administering testosterone esters in a vehicle.
摘要翻译： 描述了在缺乏内源性睾丸激素水平的患者中提供延长的生理上可接受的稳态血清睾酮水平的方法，男性避孕方法和通过肌内施用睾酮酯治疗与男性睾酮缺乏的内源性水平相关的疾病或症状的方法 在一辆车上
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7.发明申请METHODS AND PHARMACEUTICAL COMPOSITIONS FOR RELIABLE ACHIEVEMENT OF ACCEPTABLE SERUM TESTOSTERONE LEVELS 有权方法和药物组合物可靠地实现可接受的血清TERMOSTERONE水平公开(公告)号：US20090156564A1
公开(公告)日：2009-06-18
申请号：US12391655
申请日：2009-02-24
IPC分类号： A61K31/56
CPC分类号： A61K31/565 , A61K9/0019 , A61K31/56 , A61K31/568 , A61K31/57 , A61K47/14 , A61K47/44
摘要： Described are methods for providing prolonged physiologically acceptable steady state serum testosterone levels in a patient deficient in endogenous testosterone levels, methods for male contraception and methods for treating a disease or symptom associated with deficient endogenous levels of testosterone in a man, by intramuscularly administering testosterone esters in a vehicle.
摘要翻译： 描述了在缺乏内源性睾丸激素水平的患者中提供延长的生理上可接受的稳态血清睾酮水平的方法，男性避孕方法和通过肌内施用睾酮酯治疗与男性睾酮缺乏的内源性水平相关的疾病或症状的方法 在一辆车上
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8.发明申请Methods and pharmaceutical compositions for reliable achievement of acceptable serum testosterone levels 有权可靠地达到可接受的血清睾酮水平的方法和药物组合物公开(公告)号：US20050032762A1
公开(公告)日：2005-02-10
申请号：US10798780
申请日：2004-03-12
IPC分类号： A61K9/00 , A61K31/56 , A61K31/565 , A61K31/568 , A61K31/57 , A61K36/47 , A61K47/14 , A61K47/44 , A61K35/78
CPC分类号： A61K31/565 , A61K9/0019 , A61K31/56 , A61K31/568 , A61K31/57 , A61K47/14 , A61K47/44
摘要： The present invention relates to pharmaceutical compositions, formulated for injectable administration, which comprises a testosterone ester, in particularly testosterone undecanoate, in a vehicle comprising castor oil and a co-solvent. Upon injecting the compositions according to a particular administration scheme, reliable levels of testosterone in serum in the normal physiological range is achieved for a long period. This allows for the use of the compositions in hormone replacement therapy and male contraception without concomitant monitoring of testosterone levels in serum by a physician.
摘要翻译： 本发明涉及配制用于可注射给药的药物组合物，其包含睾酮酯，特别是十一酸睾酮，载体包含蓖麻油和共溶剂。 在根据特定给药方案注射组合物时，长时间内可获得在正常生理范围内血清中可靠水平的睾丸激素。 这允许在激素替代治疗和男性避孕中使用组合物，而无需伴随地监测医师对血清中的睾酮水平。
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