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1. 发明公开

EP2383279A1 Process for the preparation of estetrol 审中-公开
标题翻译： HerstellungsverfahrenfürEsterol
公开(公告)号：EP2383279A1
公开(公告)日：2011-11-02
申请号：EP11174509.7
申请日：2011-07-19
申请人： Pantarhei Bioscience B.V.
发明人： Platteeuw, Johannes Jan , Coelingh Bennink, Herman Jan Tijmen , Damen, Franciscus Wilhelmus Petrus , Van Vliet, Michiel Christian Alexander
IPC分类号： C07J75/00
CPC分类号： C07J1/007 , C07J1/0059 , C07J13/005 , C07J75/00 , Y02P20/55
摘要： The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3,15α,16α,17β-tetraol (estetrol), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, wherein A is a protecting group and B is ―Si(R 2 ) 3 .
The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10),15-tetraen-17-one, wherein A is a protecting group, via said silyl enol ether derivative.
摘要翻译：本发明涉及通过甲硅烷基烯醇醚衍生物17-B-oxy制备雌-1,3,5（10） - 三烯-3,15±，16±，17-四醇（雌酮）的方法 -3-A-氧 - 雌-1,3,5（10），16-四烯，其中A为保护基，B为€（Si（R 2）3）。本发明还涉及通过所述甲硅烷基烯醇醚衍生物合成其中A为保护基的3-A-氧 - 雌-1,3,5（10），15-四烯-17-酮的方法。

2. 发明公开

EP1462057A1 Sampler for taking samples from a body cavity, such as cervical samples 审中-公开
标题翻译： wer Zervixzellen的Gerätzur Entnahme von Gewebeproben aus einerKörperhöhle
公开(公告)号：EP1462057A1
公开(公告)日：2004-09-29
申请号：EP03075850.2
申请日：2003-03-24
申请人： Pantarhei Bioscience B.V.
发明人： Wiegerinck, Martinus Antonius Hermanus Maria , Coelingh Bennink, Herman Jan Tijmen , Boerrigter, Petrus Johannes
IPC分类号： A61B10/00
CPC分类号： A61B10/0291 , A61B10/0096 , A61B10/0283 , A61B2010/0074
摘要： Sampler (11) for independent taking of samples from a body cavity, such as cervical samples. Optimum accessibility of the cervix is achieved through the fact that the sampler comprises a rigid plastic tube (14) which is rounded at the front side. As a result, during its introduction by the user, the sampler can accurately be moved to the cervix. Moreover, the sampler is surrounded by the vagina and it is possible to prevent leakage of flushing liquid (15), and consequently it is possible to make do with a relatively small quantity of flushing liquid (15) while at the same time producing a sample with a high concentration of cervical cells. In this way, it is possible to reach the sampling location in a simple and more accurate way which does not damage tissue. As a result of the tube simultaneously being designed as a cylinder for a plunger (12), it is possible, firstly, to flush the desired location with a solution using a cylinder-plunger assembly obtained in this way and, secondly, to take the sample by drawing the plunger (12) back.
摘要翻译：采样器（11）用于独立取样体腔，如宫颈样品。子宫颈的最佳可达性是通过采样器包括在前侧为圆形的刚性塑料管（14）的事实来实现的。因此，在用户引入期间，采样器可以准确地移动到子宫颈。此外，取样器被阴道包围，并且可以防止冲洗液（15）的泄漏，因此可以用相对少量的冲洗液（15）进行制造，同时制造样品具有高浓度的宫颈细胞。以这种方式，可以以不损伤组织的简单且更准确的方式到达采样位置。由于管同时被设计为用于柱塞（12）的气缸，因此首先可以使用以这种方式获得的气缸 - 柱塞组件用溶液冲洗所需位置，其次，取通过将柱塞（12）拉回来来抽样。

3. 发明公开

EP1700602A1 Pharmaceutical composition for use in hormone replacement therapy 审中-公开
标题翻译： Pharmaceutishe Zusammensetzungfürdie Hormonersatztherapie
公开(公告)号：EP1700602A1
公开(公告)日：2006-09-13
申请号：EP06114704.7
申请日：2002-05-17
申请人： Pantarhei Bioscience B.V.
发明人： Holinka, Christian Franz , Coelingh Bennink, Herman Jan Tijmen , Bunschoten, Evert Johannes
IPC分类号： A61K31/565 , A61P5/30
CPC分类号： A61K9/0034 , A61K31/00 , A61K31/56 , A61K31/565 , A61K45/06 , A61K2300/00
摘要： One aspect of the invention is concerned with the use of an estrogenic component selected from the group consisting of:
substances represented by the following formula

in which formula R 1 , R 2 , R 3 , R 4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R 5 , R 6 , R 7 is a hydroxyl group; and no more than 3 of R 1 , R 2 , R 3 , R 4 are hydrogen atoms; derivatives of these substances wherein the hydrogen atom of at least one of the hydroxyl groups in said formula has been substituted by an acyl radical of a hydrocarbon carboxylic, sulfonic or sulfamic acid of 1-25 carbon atoms, tetrahydrofuranyl, tetrahydropyranal, or a straight or branched chain glycosidic residue containing 1-20 glycosidic units per residue; and mixtures thereof; in the preparation of a composition for use in a method of hormone replacement therapy, which method comprises non-orally administering to a person in need of such a therapy an effective amount of the estrogenic component without adjunctive progestogen or anti-progestogen treatment, said composition containing no progestogen or anti-progestin.
Another aspect of the invention relates to a drug delivery system for enteral or parenteral administration that contains at least 1 µg of the aforementioned estrogenic component and no progestogen or anti-progestin.
摘要翻译：本发明的一个方面涉及使用选自下列物质的雌激素成分：下式表示的物质，其中式R 1，R 2，R 3，R 4独立地为氢原子，羟基或具有1-5个碳原子的烷氧基; R 5，R 6，R 7各自为羟基; R 1，R 2，R 3，R 4为不大于3的氢原子; 这些物质的衍生物，其中所述式中至少一个羟基的氢原子被1-25个碳原子的烃羧酸，磺酸或氨基磺酸的酰基取代，四氢呋喃基，四氢吡喃或直链或每个残基含有1-20个糖苷单元的支链糖苷残基; 及其混合物; 在制备用于激素替代疗法的组合物中，该方法包括非需要这种治疗的人口服给予有效量的无辅助性孕激素或抗孕激素治疗的雌激素成分，所述组合物不含孕激素或抗孕激素。本发明的另一方面涉及用于肠内或肠胃外给药的药物递送系统，其包含至少1μg的上述雌激素成分，而不含孕激素或抗孕激素。

4. 发明公开

EP1287817A1 Method of treating uterine leiomyomas and intravaginal drug delivery vehicle for use in such method 审中-公开
标题翻译： Verfahren und intravaginales Arzneiverabreichungsvorrichtung zur Behandlung von uterinem Myom
公开(公告)号：EP1287817A1
公开(公告)日：2003-03-05
申请号：EP01203305.6
申请日：2001-08-31
申请人： Pantarhei Bioscience B.V.
发明人： Coelingh Bennink, Herman Jan Tijmen , Thijssen, Joseph Helenus Hubert
IPC分类号： A61K9/00 , A61K45/00 , A61K45/06 , A61P15/00
CPC分类号： A61K45/06 , A61K9/0034 , A61K31/00 , A61K31/56 , A61K31/565 , A61K2300/00
摘要： The present invention relates to a method of treating uterine leiomyomas (fibroids or myomas) in mammal females. More particularly the present invention relates to such a method comprising intravaginal administration of a drug delivery vehicle to a female mammal suffering from uterine leiomyomas, said drug delivery vehicle containing an estrogen activity suppressant selected from the group consisting of aromatase inhibitors, anti-estrogens and mixtures thereof, wherein the method provides the estrogen activity suppressant in a therapeutically effective dosage to inhibit the growth and/or to achieve atrophy of the myomas. The intravaginal administration of estrogen activity suppressant, in comparison to other routes of administration, achieves the desired clinical effect at lower dosage levels and/or without seriously affecting overall estrogen blood serum levels.
Another aspect of the invention is concerned with a drug delivery vehicle for intravaginal use, which drug delivery vehicle comprises at least 10 µg of an aromatase inhibitor and/or at least 10 µg of an anti-estrogen and pharmaceutically acceptable excipient.
摘要翻译：本发明涉及一种治疗哺乳动物雌性子宫平滑肌瘤（肌瘤或肌瘤）的方法。更具体地说，本发明涉及这样一种方法，其包括向患有子宫平滑肌瘤的女性哺乳动物施用药物递送载体的所述方法，所述药物递送载体含有选自以下的雌激素活性抑制剂：芳香酶抑制剂，抗雌激素和混合物其中所述方法提供治疗有效剂量的雌激素活性抑制剂以抑制生长和/或实现肌瘤的萎缩。与其他给药途径相比，雌激素活性抑制剂的阴道内施用在较低剂量水平下和/或不严重影响总体雌激素血清水平达到期望的临床效果。本发明的另一方面涉及用于阴道内使用的药物递送载体，该药物递送载体包含至少10μg的芳香酶抑制剂和/或至少10μg的抗雌激素和药学上可接受的赋形剂。

5. 发明授权

EP1462107B1 Method of female contraception and kit for use in such method 有权
标题翻译：女性避孕和药物制剂，其适用于这样的方法
公开(公告)号：EP1462107B1
公开(公告)日：2008-09-24
申请号：EP03075905.4
申请日：2003-03-28
申请人： Pantarhei Bioscience B.V.
发明人： Coelingh Bennink, Herman Jan Tijmen , Visser, Monique
IPC分类号： A61K31/565 , A61K31/57 , A61P15/18
CPC分类号： A61K31/565 , A61K31/57 , A61K2300/00

6. 发明公开

EP1260225A1 A pharmaceutical composition for use in hormone replacement therapy 审中-公开
标题翻译： Pharmazeutische Zusammensetzungfürdie Hormonersatztherapie
公开(公告)号：EP1260225A1
公开(公告)日：2002-11-27
申请号：EP01201896.6
申请日：2001-05-18
申请人： Pantarhei Bioscience B.V.
发明人： Holinka, Christian Franz , Coelingh Bennink, Herman Jan Tijmen
IPC分类号： A61K31/565 , A61P5/30
CPC分类号： A61K9/0034 , A61K31/00 , A61K31/56 , A61K31/565 , A61K45/06 , A61K2300/00
摘要： The present invention is concerned with a pharmaceutical composition for use in a method of hormone replacement. More particularly, the present invention relates to a pharmaceutical composition for use in a method of hormone replacement therapy, which method comprises administering to a person in need of such a therapy an effective amount of an active component selected from the group consisting of:

substances represented by the following formula
in which formula R 1 , R 2 , R 3 , R 4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; R 5 , R 6 , R 7 independently are a hydrogen atom or a hydroxyl group; no more than 3 of R 1 , R 2 , R 3 , R 4 , R 5 , R 6, R 7 are hydrogen atoms and at least 2 of R 5 , R 6, R 7 are a hydroxyl group;
precursors capable of liberating a substance according to the aforementioned formula when used in the present method, and mixtures thereof;
said composition containing virtually no progestogen or anti-progestin.
An example of a known substance which may suitably be used in the method of the invention is 1,3,5 (10)-estatrien-3, 15α,16α,17β-tetrol (estetrol).
摘要翻译：本发明涉及用于激素替代方法的药物组合物。更具体地说，本发明涉及一种用于激素替代疗法的药物组合物，该方法包括对需要这种治疗的人施用有效量的活性成分，所述活性成分选自：代表的物质其中式R1，R2，R3，R4独立地为氢原子，羟基或具有1-5个碳原子的烷氧基; R5，R6，R7独立地为氢原子或羟基; 不超过3个R 1，R 2，R 3，R 4，R 5，R 6，R 7为氢原子，R 5，R 6，R 7中至少2个为羟基; 当用于本发明方法时能够释放根据上述式的物质的前体及其混合物; 所述组合物几乎不含孕激素或抗孕激素。可适用于本发明方法的已知物质的实例是1,3,5（10） - 雌三烯-3,15α，16α，17β-四烯醇（雌酮）。

7. 发明公开

EP1468690A1 Use of estrogens for the treatment of infertility in male mammals 有权
标题翻译： Verwendung von Estrogenen zur Behandlung vonMännerunfruchtbarkeit
公开(公告)号：EP1468690A1
公开(公告)日：2004-10-20
申请号：EP03075894.0
申请日：2003-03-27
申请人： Pantarhei Bioscience B.V.
发明人： Maas, Jacob Jan , Coelingh Bennink, Herman Jan Tijmen , Nieschlag, Eberhard
IPC分类号： A61K31/565 , A61K38/11 , A61P15/08
CPC分类号： A61K31/565 , A61K38/11 , A61K2300/00
摘要： The present invention relates to a method of improving the fertility of a male mammal. More particularly, the present invention relates to a method of improving the fertility of a male mammal, said method comprising administering to said male mammal estrogen or a combination of estrogen and oxytocin agonist in an amount effective to increase the reproductive quality of the male's semen. Generally accepted parameters that are indicative of the reproductive quality of semen include total sperm count, sperm concentration, ejaculate volume, sperm motility and sperm morphology.
Another aspect of the invention relates to an intranasal drug delivery system comprising an intranasal drug delivery device and a drug delivery composition for intranasal delivery, said composition containing at least 3 µg/ml estrogen, at least 3 µg/ml oxytocin agonist and pharmaceutically acceptable excipient.
摘要翻译：本发明涉及一种改善男性哺乳动物生育能力的方法。更具体地说，本发明涉及一种改善男性哺乳动物生育能力的方法，所述方法包括以有效提高男性精液生殖质量的量向所述雄性哺乳动物施用雌激素或雌激素和催产素激动剂的组合。表明精液生殖质量的普遍接受的参数包括精子总数，精子浓度，射精体积，精子活力和精子形态。本发明的另一方面涉及鼻内药物递送系统，其包含鼻内药物递送装置和用于鼻内递送的药物递送组合物，所述组合物含有至少3μg/ ml雌激素，至少3μg/ ml 催产素激动剂和药学上可接受的赋形剂。

8. 发明授权

EP1293210B1 Means and method for hormonal contraception 有权
标题翻译：筹备激素避孕
公开(公告)号：EP1293210B1
公开(公告)日：2003-11-19
申请号：EP01201945.1
申请日：2001-05-23
申请人： Pantarhei Bioscience B.V.
发明人： Van Beek, Agatha Antonia Magdalena , Coelingh Bennink, Herman Jan Tijmen
IPC分类号： A61K31/57 , A61P15/18
CPC分类号： A61K31/56 , A61K31/565

9. 发明授权

EP1468690B1 Use of estrogens for the treatment of infertility in male mammals 有权
标题翻译：使用雌激素对男性不育症的治疗
公开(公告)号：EP1468690B1
公开(公告)日：2008-10-08
申请号：EP03075894.0
申请日：2003-03-27
申请人： Pantarhei Bioscience B.V.
发明人： Maas, Jacob Jan , Coelingh Bennink, Herman Jan Tijmen , Nieschlag, Eberhard
IPC分类号： A61K31/565 , A61K38/11 , A61P15/08
CPC分类号： A61K31/565 , A61K38/11 , A61K2300/00

10. 发明公开

EP1862182A2 Method of controlled ovarian hyperstimulation and pharmaceutical kit for use in such method 审中-公开
标题翻译：用于该方法中的控制的卵巢过度刺激和药物试剂盒的使用方法
公开(公告)号：EP1862182A2
公开(公告)日：2007-12-05
申请号：EP07116815.7
申请日：2002-12-20
申请人： Pantarhei Bioscience B.V.
发明人： Coelingh Bennink, Herman Jan Tijmen , Bunschoten, Evert Johannes
IPC分类号： A61K45/06 , A61K38/24
CPC分类号： A61K38/24 , A61K45/06 , A61K2300/00
摘要： One aspect of the present invention relates to a method of controlled ovarian hyperstimulation in a mammalian female, said method comprising administration to said female of a substance having follicle stimulating hormone activity (FSH substance) in an amount effective to stimulate follicular development and of anti-P in an effective amount to prevent a premature endogenous LH-surge, followed by the administration of a meiosis and luteinisation inducing substance (ML substance) in an amount effective to stimulate resumption of meiosis and luteinisation, and of a progestogen and/or a precursor thereof in an amount effective to prevent or suppress symptoms of progesterone antagonism and/or deficiency, wherein the progestogen and/or the precursor thereof is administered within 24 hours of the first administration of the ML substance.
Another aspect of the present invention relates to a pharmaceutical kit for use in a method of controlled ovarian hyperstimulation in mammalian females, said kit comprising a parenteral dosage unit containing a FSH substance, a parenteral or oral dosage unit containing an anti-P and a parenteral or oral dosage unit containing a progestogen and/or a precursor thereof.
摘要翻译：本发明的一个方面涉及控制卵巢过度刺激的雌性哺乳动物的方法，所述方法包括给药于具有毛囊在有效量一刺激素活性（FSH物质）的物质的所述阴刺激卵泡发育和抗 p在以有效量以防止过早的内源性LH峰，接着在有效刺激恢复减数分裂和黄体化的量的减数分裂和黄体化诱导物质（ML物质）的施用，和一种孕激素和/或前体的其以有效地防止或抑制孕酮拮抗作用和/或不足的症状的量，worin孕激素和/或其前体在24小时的ML物质在第一次施用的内施用。本发明的另一个方面涉及药物试剂盒，用于在雌性哺乳动物控制性超排卵的方法中使用，所述试剂盒包括肠胃外剂量单位含有一个FSH物质，肠胃外或口服剂量单位含有抗P和肠胃外的或口服剂量单位含孕激素和/或它们的前体。

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