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1.发明授权PHARMAZEUTISCHE ZUSAMMENSETZUNGEN MIT ESTRA-1,3,5(10)-TRIEN-DERIVATEN 失效WITH雌-1,3,5（10） - 三烯衍生物的药物组合物
公开(公告)号：EP0775156B1
公开(公告)日：2003-09-03
申请号：EP95925680.1
申请日：1995-07-03
发明人： SIEMANN, Hans-Joachim , ELGER, Walter , SCHWARZ, Sigfrid , REDDERSEN, Gudrun , SCHNEIDER, Birgitt
CPC分类号： C07J53/004 , A61K31/565 , A61K31/58 , C07J41/0072 , C07J43/003 , Y10S514/841 , Y10S514/842 , Y10S514/843 , Y10S514/874
摘要： The invention concerns pharmaceutical compositions containing as the active substance estra-1,3,5(10)-triene derivatives with an R-SO2-O- group on the 3 C-atom, R being an R1R2N- group in which R?1 and R2¿, independently of each other, are a hydrogen atom, an alkyl group with 1 to 5 C-atoms or, together with the N-atom, a polymethyleneimino group with 4 to 6 C-atoms or a morpholino group. The compounds described are suitable for use in hormonal contraception and in climacteric hormone-replacement therapy (HRT), as well as in the treatment of gynaecological and andrological conditions. The compounds described thus only have a low hepatic oestrogenicity.
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2.发明公开NICHTESTROGENE DERIVATE DES ESTRADIOLS MIT ANTIOXIDATIVER AKTIVITÄT 失效雌二醇的雌激素NICHTESTROGENE衍生物具有抗氧化活性
公开(公告)号：EP0986573A1
公开(公告)日：2000-03-22
申请号：EP98934761.2
申请日：1998-05-20
发明人： DROESCHER, Peter , MENZENBACH, Bernd , RÖMER, Wolfgang , SCHNEIDER, Brigitt , ELGER, Walter , KAUFMANN, Günter
CPC分类号： C07J41/0072 , C07J1/0062 , C07J1/007 , C07J1/0085 , C07J1/0088 , C07J31/006
摘要： New non-estrogenic estradiol derivatives with an antioxidant effect are disclosed. These estradiol derivatives, which have no estrogenic effect but a high antioxidant effect, are potentially useful as non-estrogenic antioxidants, in particular for postmenopausal women and for men. Moreover, the disclosed compounds are potential aromatase and sulfatase inhibitors.
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3.发明授权SULFAMAT-DERIVATE VON 1,3,5(10)-ESTRATRIEN-DERIVATEN, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN 失效作者-1,3,5（10） - 雌三烯衍生物，METHOD FOR PRODUCING他们和氨基磺酸酯衍生物的药物COMPOSITIONS CONTAINING
公开(公告)号：EP0862577B1
公开(公告)日：1999-04-14
申请号：EP96945140.0
申请日：1996-09-19
发明人： SCHWARZ, Sigfrid , ELGER, Walter , REDDERSEN, Gudrun , SCHNEIDER, Birgitt , THIEME, Ina , RICHTER, Margit
IPC分类号： C07J41/00 , A61K31/565
CPC分类号： C07J41/0072
摘要： The invention relates to novel sulphamate derivatives of 1,3,5(10)-estratriene derivatives of general formula (I) in which the 3-sulphamate group is acylated, sulphonated or amido-sulphonated. Also disclosed are methods of producing these compounds and pharmaceutical compounds containing them. The claimed compounds have estrogen-like properties.
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4.发明公开SULFAMAT-DERIVATE VON 1,3,5(10)-ESTRATRIEN-DERIVATEN, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN 失效作者-1,3,5（10） - 雌三烯衍生物，METHOD FOR PRODUCING他们和氨基磺酸酯衍生物的药物COMPOSITIONS CONTAINING
公开(公告)号：EP0862577A2
公开(公告)日：1998-09-09
申请号：EP96945140.0
申请日：1996-09-19
申请人： JENAPHARM GmbH
发明人： SCHWARZ, Sigfrid , ELGER, Walter , REDDERSEN, Gudrun , SCHNEIDER, Birgitt , THIEME, Ina , RICHTER, Margit
CPC分类号： C07J41/0072
摘要： The invention relates to novel sulphamate derivatives of 1,3,5(10)-estratriene derivatives of general formula (I) in which the 3-sulphamate group is acylated, sulphonated or amido-sulphonated. Also disclosed are methods of producing these compounds and pharmaceutical compounds containing them. The claimed compounds have estrogen-like properties.
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5.发明授权
公开(公告)号：EP1084569B1
公开(公告)日：2003-03-05
申请号：EP99938132.0
申请日：1999-06-07
CPC分类号： A61K31/565 , A61K31/57 , A61K31/585 , A61K45/06 , A61K2300/00
摘要： The invention relates to pharmaceutical combinations for compensating for an absolute and relative testosterone deficiency in men while simultaneously preventing the development of benign prostatic hypertrophy (BPH) or of prostatic cancer. The inventive combinations contain a natural or synthetic androgen combined with a gestagen, an antigestagen, an antiestrogen, a GnRH analog, a testosterone-5α-reductase inhibitor, an α-adrenergic blocking agent or a phosphodiesterase inhibitor. Compared to the inventive combinations, each active ingredient cannot carry out the desired objective alone.
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6.发明授权NICHTESTROGENE DERIVATE DES ESTRADIOLS MIT ANTIOXIDATIVER AKTIVITÄT 失效雌二醇的雌激素NICHTESTROGENE衍生物具有抗氧化活性
公开(公告)号：EP0986573B1
公开(公告)日：2002-10-09
申请号：EP98934761.2
申请日：1998-05-20
发明人： DROESCHER, Peter , MENZENBACH, Bernd , RÖMER, Wolfgang , SCHNEIDER, Brigitt , ELGER, Walter , KAUFMANN, Günter
CPC分类号： C07J41/0072 , C07J1/0062 , C07J1/007 , C07J1/0085 , C07J1/0088 , C07J31/006
摘要： New non-estrogenic estradiol derivatives with an antioxidant effect are disclosed. These estradiol derivatives, which have no estrogenic effect but a high antioxidant effect, are potentially useful as non-estrogenic antioxidants, in particular for postmenopausal women and for men. Moreover, the disclosed compounds are potential aromatase and sulfatase inhibitors.
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7.发明公开14,15-CYCLOPROPANOSTEROIDE DER 19-NORANDROSTAN-REIHE, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN 有权14,15-CYCLOPROPANOSTEROIDE DER 19-NORANDROSTAN-REIHE，VERFAHREN ZU IHRER HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZUUTISCHE ZUSAMMENSETZUNGEN
公开(公告)号：EP1242445A1
公开(公告)日：2002-09-25
申请号：EP00988735.7
申请日：2000-11-21
发明人： RING, Sven , ELGER, Walter , KAUFMANN, Günter
IPC分类号： C07J53/00 , A61K31/567 , A61P35/00
CPC分类号： C07J53/004
摘要： The invention relates to novel 14,15-cyclopropanosteroids of the 19-norandrostane series having the general formula (I), preparation thereof and pharmaceutical compositions containing said compounds. Compounds of the formula (I) have an interesting androgen/gestagen mixture profile. The activity of the androgens or the gestagens can predominate, depending on the respective substitution.
摘要翻译： 本发明涉及具有通式（I）的19-去甲基雄甾烷系列的新型14,15-环丙烷类固醇，其制备和含有该化合物的药物组合物。 式（I）化合物具有令人感兴趣的雄激素/孕激素混合物特征。 取决于各自的取代，雄激素或孕激素的活性可占主导地位。
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8.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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公开(公告)号：EP1056769B1
公开(公告)日：2002-06-19
申请号：EP98965592.3
申请日：1998-11-30
IPC分类号： C07J53/00 , A61K31/565
CPC分类号： C07J53/004
摘要： The invention relates to novel 15-methyl-cyclopropanosteroids of general formula (I), wherein R1 represents a hydrogen atom, an alkyl group, an acyl group, or a sulfamoyl group, R2 and R3 represent independently from each other a hydrogen atom or a halogen atom, R4 represents an oxo group or a hydrogen atom and a hydroxy group, and the 14,15-methylene group has either an alpha or beta configuration, wherein the 15-methyl group is in beta position when the 14,15-methylene group is arranged in alpha position and vice-versa. The invention also relates to 15 methyl-pentasteroids which are suitable as parent compounds in the production of the inventive 15-methyl-cyclopropanosteroids. The invention further relates to a method for the production of the inventive 15-methyl-cyclopropanosteroids and 15-methylpentaensteroids.
摘要翻译： 本发明涉及新颖的通式（I），其中R1表示氢原子，烷基，酰基，或氨磺酰基，R2和R3彼此氢原子或独立地表示15甲基cyclopropanosteroids 卤原子，R 4表示氧代基团或氢原子和羟基，以及14,15-亚甲基组具有α或β构型，其中15-甲基是在β位当14,15-亚甲基 组排列在alpha位置，反之亦然。 本发明还涉及在制备本发明的15-甲基 - 环丙烷类固醇时适合作为母体化合物的15种甲基 - 五溴甾体。 本发明进一步涉及用于生产本发明的15-甲基 - 环丙烷类固醇和15-甲基戊五萜类的方法。
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10.发明公开NEUE C13-SUBSTITUIERTE ESTRA-1,3,5(10)-TRIEN-3-YL-SULFAMATE, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN ZUR HEMMUNG VON ÖSTRON SULFATASE 审中-公开NEW C13-取代雌-1,3,5（10） - 三烯-3-基 - 氨基磺酸酯，用于生产它们，药物组合物，雌甾酮硫酸来抑制
公开(公告)号：EP1212346A1
公开(公告)日：2002-06-12
申请号：EP00967631.3
申请日：2000-08-28
申请人： JENAPHARM GmbH
发明人： SCHWARZ, Sigfrid , KOSEMUND, Dirk , MÜLLER, Gerd , RICHTER, Margit , PETERS, Olaf , SCHERLITZ-HOFMANN, Ina , MICHEL, Thomas , ELGER, Walter , REDDERSEN, Gudrun , SCHNEIDER, Birgitt
IPC分类号： C07J41/00 , A61K31/565 , A61P5/32
CPC分类号： C07J41/0072
摘要： The invention relates to novel C13-substituted estra-1,3,5(10)-triene-3-yl-sulfamates of the general formula (I), in which R1 represents the acyl radical, oxycarbonyl radical, aminocarbonyl radical, sulfonyl radical or aminosulfonyl radical and R15 stands for C2-C5 alkyl, C2-C5 alkenyl or C2-C5-alkinyl. The invention also relates to a method for producing these compounds and to pharmaceutical compositions which contain said compounds. The inventive compounds of the general formula (I) inhibit the activity of steroid sulfatases (EC 3.1.6.2) and do not exhibit any oestrogenic action.
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