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1. 发明申请

US20050032756A1 Multistage preparation for contraception based on natural estrogens 审中-公开
标题翻译：基于天然雌激素的避孕多步骤准备
公开(公告)号：US20050032756A1
公开(公告)日：2005-02-10
申请号：US10891729
申请日：2004-07-15
申请人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Oster Wald
发明人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Oster Wald
IPC分类号： A61K31/57 , A61K31/56
CPC分类号： A61K31/57 , A61K2300/00
摘要： A multistage preparation for contraception based on a combination of natural estrogen and synthetic gestogen is described. The preferred preparation contains estradiol valerate as the natural estrogen and dienogest or drospirenone as the synthetic gestogen. In comparison to conventional multistage preparations the multistage preparation according to the invention has a higher contraceptive reliability over the entire cycle, improved cyclic bleeding behavior and minimizes or prevents side effects, such as breast tension, headaches, depressive moods and libido changes.
摘要翻译：描述了基于天然雌激素和合成gestogen的组合的用于避孕的多级制剂。优选的制剂包含戊酸雌二醇作为天然雌激素和依诺孕酮或屈螺酮作为合成孕酮。与常规多级制剂相比，根据本发明的多级制剂在整个循环中具有更高的避孕可靠性，改善的循环出血行为并且最小化或预防副作用，例如乳房张力，头痛，抑郁情绪和性欲改变。

2. 发明授权

US6133251A Combination compound for contraception based on natural estrogen 失效
标题翻译：基于天然雌激素的避孕组合化合物
公开(公告)号：US6133251A
公开(公告)日：2000-10-17
申请号：US738314
申请日：1996-10-25
申请人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Ostertag
发明人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Ostertag
IPC分类号： A61K31/565 , A61K31/57 , A61P15/00 , A61P15/18 , C07J1/00 , C07J7/00 , A61K31/56
CPC分类号： A61K31/57 , Y10S514/843
摘要： The combination preparation for contraception includes a first stage of 2 to 4 first stage daily dosage portions, a second stage of two groups of second stage daily dosage portions, a third stage of 2 to 4 third stage daily dosage portions and an additional stage of 2 to 4 additional stage daily dosage portions. The first stage daily dosage portion is an effective amount of natural estrogen, the second stage daily dosage portion is an effective amount of a combination of natural estrogen and natural or synthetic gestogen, the third stage daily dosage portion is another effective amount of natural estrogen and an additional stage daily dosage portion consists of a placebo. The first group of the second stage consists of 3 to 5 daily dosage portions and the second group, 13 to 17 daily dosage portions. More of the gestogen is included in the effective amount in the second group of the second stage than in the first group. The effective amount of the natural estrogen is constant in both the first and third stages, but smaller in the third stage than in the first stage.
摘要翻译：用于避孕的组合制剂包括第一阶段的2至4个第一阶段每日剂量部分，第二阶段的两组第二阶段日剂量部分，第三阶段的2至4个第三阶段每日剂量部分和另外的阶段2 至4个额外的阶段日剂量部分。第一阶段日剂量是天然雌激素的有效量，第二阶段日剂量是天然雌激素和天然或合成gestogen的组合的有效量，第三阶段日剂量是另一有效量的天然雌激素，额外的阶段每日剂量部分由安慰剂组成。第一组第一组由3〜5个日剂量组成，第二组为每日13〜17次。第二组的第二组中有更多的gestogen包含在第一组中。天然雌激素的有效量在第一和第三阶段都是恒定的，但在第三阶段中比在第一阶段更小。

3. 发明授权

US06884793B2 Combination preparation for contraception based on natural estrogens 失效
标题翻译：基于天然雌激素的避孕组合制剂
公开(公告)号：US06884793B2
公开(公告)日：2005-04-26
申请号：US09950915
申请日：2001-09-12
申请人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Ostertag
发明人： Michael Dittgen , Sabine Fricke , Herbert Hoffmann , Claudia Moore , Michael Oettel , Monika Ostertag
IPC分类号： A61K31/565 , A61K31/57 , A61P15/00 , A61P15/18 , C07J1/00 , C07J7/00 , A61K33/56
CPC分类号： A61K31/57 , Y10S514/843 , A61K31/565 , A61K2300/00
摘要： The combination preparation for contraception includes from 2 to 4 first stage daily dosage portions each including an effective amount of at least one natural estrogen as sole active ingredient, from 16 to 22 second stage daily dosage portions each including an effective amount of a combination of at least one natural estrogen and at least one natural or synthetic gestogen as active ingredient; from 2 to 4 third stage daily dosage portions each including an effective amount of at least one natural estrogen as sole active ingredient; and from 2 to 4 final stage daily dosage portions containing a pharmaceutically acceptable placebo. The estrogen may be estradiol, an estradiol compound that is metabolized to estradiol when taken into the body, a conjugated equine estrogen or a phytoestrogen. The natural or synthetic gestogen can be natural progesterone or a synthetic gestogens, such as medroxyprogesterone acetate.
摘要翻译：用于避孕的组合制剂包括2至4个第一阶段每日剂量部分，每个剂量部分包含有效量的至少一种天然雌激素作为唯一活性成分，16至22个第二阶段日剂量部分，每个包含有效量的组合至少一种天然雌激素和至少一种天然或合成的Gestogen作为活性成分; 2至4个第三阶段每日剂量部分，每个包含有效量的至少一种天然雌激素作为唯一活性成分; 和含有药学上可接受的安慰剂的2至4个最终阶段每日剂量部分。雌激素可以是雌二醇，当被摄入体内时被代谢为雌二醇的雌二醇化合物，共轭马雌激素或植物雌激素。天然或合成的gestogen可以是天然孕酮或合成的gestogens，如醋酸甲羟孕酮。

4. 发明授权

US5633242A Pharmaceuticals for contraception/hormone substitution containing a biogenous estrogen component 失效
标题翻译：含有生物雌激素成分的避孕药/激素替代药
公开(公告)号：US5633242A
公开(公告)日：1997-05-27
申请号：US511026
申请日：1995-08-03
申请人： Michael Oettel , Hermann Osterwald , Claudia Moore , Thomas Gr aser
发明人： Michael Oettel , Hermann Osterwald , Claudia Moore , Thomas Gr aser
IPC分类号： A61K31/565 , A61K31/57 , C07J1/00 , A61K31/56
CPC分类号： A61K31/565 , A61K31/57 , Y10S514/841 , Y10S514/843
摘要： This invention relates to a compound preparation for contraception and hormone replacement that consists of three steps totalling 28 daily doses. The pharmaceutical is characterized in thatstep 1 consists of 3 or 4 daily doses, each containing a preparation in which the active ingredient is at least one biogenous estrogen component,step 2 consists of 20 to 22 daily doses, each containing a preparation in which the active ingredients are at least one biogenous estrogen and one gestagen component from the group of C.sub.21 -gestagens including progesterone, as well as dienogest, desogestrel, 3-keto desogestrel, gestodene, levonorgestrel, norgestimate, norethisterone, norethisterone acetate and dydrogesterone, andstep 3 consists of 3 or 4 daily doses, each containing a preparation in which the active ingredient is at least one biogenous estrogen component.
摘要翻译：本发明涉及一种用于避孕和激素替代的化合物制剂，其由共计28日剂量的三个步骤组成。该药物的特征在于，步骤1由3或4个日剂量组成，每个剂量包含其中活性成分是至少一种生物雌激素组分的制剂，步骤2由20至22个日剂量组成，每个剂量包含其中活性成分是至少一种生物雌激素和一组孕激素组分，包括孕酮，以及依诺孕，去氧孕烯，3-酮去氧孕烯，孕二烯酮，左炔诺孕酮，诺孕酯，炔诺酮，醋酸炔诺酮和地屈孕酮，步骤3 由3或4个日剂量组成，每个剂量含有活性成分是至少一种生物雌激素成分的制剂。

5. 发明授权

US06670350B1 Method of administering dienogest in high dosages to reduce the body of the breast and pharmaceutical composition for same 失效
标题翻译：以高剂量给予丹那酸的方法，以减少乳房的身体和用于其的药物组合物
公开(公告)号：US06670350B1
公开(公告)日：2003-12-30
申请号：US09913554
申请日：2002-01-14
申请人： Michael Oettel , Claudia Moore , Adolf Eduard Schindler , Bernd Christensen
发明人： Michael Oettel , Claudia Moore , Adolf Eduard Schindler , Bernd Christensen
IPC分类号： A61K3156
CPC分类号： A61K31/57
摘要： A method of administering dienogest to a women in high dosages for reducing the body of the breast is described. The dosage should be at least ten times the effective dosage for inhibiting ovulation in the women. A pharmaceutical composition for use in the method is also described. Furthermore, retrogression of mastopathic changes in the body of the breast can be brought about. Dienogest is also outstandingly suitable for the prophylaxis of mastopathies. In high dosages, dienogest prevents the formation of mastopathic changes in the body of the breast.
摘要翻译：描述了向用于减少乳房身体的高剂量的妇女施用迪那霉素的方法。剂量应至少为有效剂量的十倍以抑制妇女排卵。还描述了用于该方法的药物组合物。此外，可以引起乳房身体的躯体变化的倒退。 Dienogest也非常适合预防性病理学。在高剂量下，抗抑郁药可以防止乳房体内的肌肉改变。

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