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1.发明公开MESOPROGESTINS FOR THE TREATMENT AND PREVENTION OF BENIGN HORMONE DEPENDENT GYNECOLOGICAL DISORDERS 有权Mesoprogestins用于治疗和预防激素依赖性良性妇科疾患
公开(公告)号：EP1229906A2
公开(公告)日：2002-08-14
申请号：EP00957914.5
申请日：2000-08-31
发明人： CHWALISZ, Kristof , ELGER, Walter , SCHUBERT, Gerd
IPC分类号： A61K31/00 , A61K31/567 , A61K31/4365 , A61K38/08 , A61K38/09 , A61K38/14 , A61P15/00
摘要： This present invention disclosed the use of mesoprogestins, a new class of progesterone receptor modulators (PRMs), for the treatment and prevention of benign hormone dependent gynecological disorders: a) for the treatment of gynecological disorder such as endometriosis, uterine fibroids, postoperative peritoneal adhesions, dysfunctional bleeding (metrorrhagia, menorrhagia) and dysmenorrhea; b) for the prevention of gynecological disorders such as postoperative, peritoneal adhesions, dysfunctional uterine bleeding (metrorrhagia, menorrhagia) and dysmenorrhea; and c) a method of treatment and prevention of the above mentioned disorders in a female, preferably in a human female, in need of treatment or prevention of one or more of these disorders, with an effective amount of a mesoprogestin. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. The daily dose of mesoprogestin is 0.5 to 100 mg, preferably 5.0 to 50 mg and most preferably 10 to 25 mg. J867, J912, J956 and J1042 are the mesoprogestins preferred according to the invention.
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2.发明授权14,15-CYCLOPROPANOSTEROIDE DER 19-NORANDROSTAN-REIHE, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE 有权14,15-CYCLOPROPANOSTEROIDE 19 norandrostane系列，方法产生它们和药物制剂
公开(公告)号：EP1090029B1
公开(公告)日：2002-03-20
申请号：EP99938196.5
申请日：1999-06-18
发明人： SCHWARZ, Sigfrid , SCHUBERT, Gerd , RING, Sven , ELGER, Walter , SCHNEIDER, Birgitt , KAUFMANN, Günter , SOBEK, Lothar
IPC分类号： C07J53/00 , A61K31/565 , A61K31/58
CPC分类号： C07J53/004
摘要： Disclosed are novel 14,15-cyclopropanosteroids of the 19-norandostane series, having general formula (I) and the pharmaceutically acceptable salts thereof. The invention also relates to a method for the production thereof and to pharmaceutical preparations containing said compounds. The compounds are characterised by hormonal (gestagenic and/or androgenic) activity.
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3.发明公开14,15-CYCLOPROPANOSTEROIDE DER 19-NORANDROSTAN-REIHE, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE PRÄPARATE 有权14,15-CYCLOPROPANOSTEROIDE 19 norandrostane系列，方法产生它们和药物制剂
公开(公告)号：EP1090029A1
公开(公告)日：2001-04-11
申请号：EP99938196.5
申请日：1999-06-18
发明人： SCHWARZ, Sigfrid , SCHUBERT, Gerd , RING, Sven , ELGER, Walter , SCHNEIDER, Birgitt , KAUFMANN, Günter , SOBEK, Lothar
IPC分类号： C07J53/00 , A61K31/565 , A61K31/58
CPC分类号： C07J53/004
摘要： Disclosed are novel 14,15-cyclopropanosteroids of the 19-norandostane series, having general formula (I) and the pharmaceutically acceptable salts thereof. The invention also relates to a method for the production thereof and to pharmaceutical preparations containing said compounds. The compounds are characterised by hormonal (gestagenic and/or androgenic) activity.
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4.发明公开11-BETA-PHENYLESTRADIEN-DERIVATE MIT FLUORALKYLGRUPPEN IN DER AROMATISCHEN SEITENKETTE, DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN 审中-公开WITH IN氟烷含有芳香族侧链11-β-PHENYLESTRADIEN衍生物，含有其制备和CONNECTIONS药物组合物
公开(公告)号：EP1237903A1
公开(公告)日：2002-09-11
申请号：EP00988736.5
申请日：2000-11-21
申请人： JENAPHARM GmbH
发明人： TORNUS, Ingo , SCHUBERT, Gerd , KAUFMANN, Günter
IPC分类号： C07J41/00 , C07J1/00 , A61K31/565
CPC分类号： C07J1/0081 , C07J41/0083
摘要： The invention relates to novel 11-β-phenylestradiene derivatives with fluoroalkyl groups in the aromatic side chain, of general formula (I), to a method for producing them and to pharmaceutical preparations containing these compounds. The inventive compounds are suitable for treating diseases that are stimulated by cortisol or corticoids, for reducing the secreted cortisol, for stimulating lactation, for treating dysmenorrhea and myomas, for treating Cushing's disease and for cervical maturation, for improving cognitive performance, for treating endometriosis or for hormone replacement therapy (HRT).
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5.发明公开S-SUBSTITUIERTE 11BETA-BENZALDOXIM-ESTRA-4,9-DIEN-KOHLENSÄURETHIOLESTER, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENE PHARMAZEUTISCHE ZUBEREITUNGEN 有权S-取代11β-benzaldoximoestra -4,9-二烯KOHLENSÄURETHIOLESTER，为他们制造方法及其所包含药物制剂
公开(公告)号：EP1060187A1
公开(公告)日：2000-12-20
申请号：EP99915475.0
申请日：1999-02-10
IPC分类号： C07J41/00 , A61K31/565 , C07J43/00
CPC分类号： C07J41/0083 , C07J43/006
摘要： The invention relates to S-substituted 11β-benzaldoxime-estra-4,9-diene-carbonic acid thiolesters of general formula (I) and the pharmaceutically acceptable salts thereof. The invention additionally relates to a method for the production of said compounds and to the pharmaceutical preparations containing these compounds. The compounds are bonded on the progesterone receptor and comprise a distinctly reduced antiglucocorticoidal effect.
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