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公开(公告)号：US20110021480A1
公开(公告)日：2011-01-27
申请号：US12892351
申请日：2010-09-28
申请人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
发明人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
IPC分类号： A61K31/58 , C07J41/00 , C07D295/185 , C07D277/46 , C07D317/58 , C07D213/40 , C07D209/14 , A61K31/566 , A61K31/565 , A61P35/00 , A61P15/00 , A61P13/00 , A61P17/08 , A61P17/10 , A61P3/10 , A61P19/02 , A61P21/04 , A61P25/28 , A61P11/06 , A61P17/02
CPC分类号： C07J43/00
摘要： Substituted steroid compounds which represent selective inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17β-estradiol concentration.
摘要翻译： 代表17＆bgr-羟基类固醇脱氢酶I型选择性抑制剂（17＆bgr-HSD1）的替代类固醇化合物，另外还可以代表类固醇硫酸酯酶的抑制剂，其盐，含有这些化合物的药物制剂及其制备方法 的这些化合物。 还公开了使用这种取代的类固醇化合物的治疗方法，特别是在治疗，抑制，预防或预防类固醇激素依赖性疾病或病症例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶I 和/或类固醇硫酸酯酶和/或需要降低内源性17β-雌二醇浓度。
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公开(公告)号：US20060281710A1
公开(公告)日：2006-12-14
申请号：US11441200
申请日：2006-05-26
申请人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
发明人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
IPC分类号： A61K31/675 , A61K31/58 , C07J43/00
CPC分类号： C07J43/00
摘要： The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration.
摘要翻译： 本发明涉及代表17β-羟基类固醇脱氢酶I型（17β-HSD1）的选择性抑制剂的新型取代的类固醇衍生物，此外，其可以代表类固醇硫酸酯酶及其盐的抑制剂与药物制剂 含有这些化合物和制备这些化合物的方法。 此外，本发明涉及所述新型取代的类固醇衍生物的治疗用途，特别是其用于治疗，抑制，预防或预防类固醇激素依赖性疾病或病症（例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇的病症） 脱氢酶I和/或类固醇硫酸酶和/或需要降低内源性17β-雌二醇浓度。
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公开(公告)号：US08030298B2
公开(公告)日：2011-10-04
申请号：US11441200
申请日：2006-05-26
申请人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
发明人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
IPC分类号： A61K31/565 , A61K31/58 , C07J1/00 , C07J53/00 , C07J71/00
CPC分类号： C07J43/00
摘要： The present invention relates to novel substituted steroid derivatives which represent selective inhibitors of the 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration.
摘要翻译： 本发明涉及代表17β-羟基类固醇脱氢酶I型（17＆amp; -HSD1）的选择性抑制剂的新型取代的类固醇衍生物，此外，其可以代表类固醇硫酸酯酶的抑制剂及其盐，至 含有这些化合物的药物制剂和这些化合物的制备方法。 此外，本发明涉及所述新型取代的类固醇衍生物的治疗用途，特别是其用于治疗，抑制，预防或预防类固醇激素依赖性疾病或病症（例如类固醇激素依赖性疾病或需要抑制17＆ I类和/或类固醇硫酸酶的羟基类固醇脱氢酶和/或需要降低内源性17β-雌二醇浓度。
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公开(公告)号：US08435973B2
公开(公告)日：2013-05-07
申请号：US12892351
申请日：2010-09-28
申请人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
发明人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Michael Weske , Pasi Koskimies , Lila Pirkkala
IPC分类号： A61K31/566 , A61K31/58 , C07J1/00 , C07J17/00 , C07J43/00
CPC分类号： C07J43/00
摘要： Substituted steroid compounds which represent selective inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17β-estradiol concentration.
摘要翻译： 代表17β-羟基类固醇脱氢酶I型（17β-HSD1）的选择性抑制剂的替代类固醇化合物，另外可以代表类固醇硫酸酯酶的抑制剂，其盐，含有这些化合物的药物制剂及其制备方法 化合物。 还公开了使用这种取代的类固醇化合物的治疗方法，特别是在治疗，抑制，预防或预防类固醇激素依赖性疾病或病症例如类固醇激素依赖性疾病或需要抑制I型17β-羟类固醇脱氢酶的病症和 /或类固醇硫酸酯酶和/或需要降低内源性17β-雌二醇浓度。
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公开(公告)号：US07524853B2
公开(公告)日：2009-04-28
申请号：US11011744
申请日：2004-12-15
申请人： Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Taneli Pentikaeinen , Tommi Nyroenen , Tiina Annamaria Salminen , Mark Stuart Johnson , Pekka Lehtovuori , Pauli Saarenketo , Bartholomeus Johannes Van Steen , Heinrich-Hubert Thole , Mikko Unkila , Josef Messinger , Johanna Kiviniemi , Lila Pirkkala , Bettina Husen
发明人： Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Taneli Pentikaeinen , Tommi Nyroenen , Tiina Annamaria Salminen , Mark Stuart Johnson , Pekka Lehtovuori , Pauli Saarenketo , Bartholomeus Johannes Van Steen , Heinrich-Hubert Thole , Mikko Unkila , Josef Messinger , Johanna Kiviniemi , Lila Pirkkala , Bettina Husen
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D495/04 , A61K31/519
摘要： Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17β-hydroxysteroid dehydrogenase enzymes.
摘要翻译： 噻吩并嘧啶酮化合物及其在治疗中的用途，特别是用于治疗和/或预防类固醇激素依赖性疾病或病症，例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶的病症。
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公开(公告)号：US20050176742A1
公开(公告)日：2005-08-11
申请号：US11011744
申请日：2004-12-15
申请人： Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Pentikaeinen , Tommi Nyroenen , Tiina Salminen , Mark Johnson , Pekka Lehtovuori , Pauli Saarenketo , Bartholomeus Van Steen , Heinrich-Hubert Thole , Mikko Unkila , Josef Messinger , Johanna Kiviniemi , Lila Pirkkala , Bettina Husen
发明人： Leena Hirvelae , Nina Johansson , Pasi Koskimies , Olli Pentikaeinen , Tommi Nyroenen , Tiina Salminen , Mark Johnson , Pekka Lehtovuori , Pauli Saarenketo , Bartholomeus Van Steen , Heinrich-Hubert Thole , Mikko Unkila , Josef Messinger , Johanna Kiviniemi , Lila Pirkkala , Bettina Husen
IPC分类号： A61K31/519 , C07D495/04 , C07D498/02
CPC分类号： C07D495/04 , A61K31/519
摘要： Thiophenepyrimidinone compounds and their use in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring inhibition of 17β-hydroxysteroid dehydrogenase enzymes.
摘要翻译： 噻吩并嘧啶酮化合物及其在治疗中的用途，特别是用于治疗和/或预防类固醇激素依赖性疾病或病症，例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶的病症。
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公开(公告)号：US20050192263A1
公开(公告)日：2005-09-01
申请号：US10983887
申请日：2004-11-09
申请人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Bartholomeus Van Steen , Gyula Schneider , Johannes Bernardus Hulshof , Pasi Koskimies , Nina Johansson , Jerzy Adamski
发明人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Bartholomeus Van Steen , Gyula Schneider , Johannes Bernardus Hulshof , Pasi Koskimies , Nina Johansson , Jerzy Adamski
CPC分类号： C07J1/0059 , C07J21/008 , C07J41/0044 , C07J43/003
摘要： 3,15-substituted estrone compounds which act as inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, particularly in the treatment or inhibition of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration, as well as the general use of selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment or inhibition of benign gynecological disorders, particularly endometriosis.
摘要翻译： 作为17β-羟类固醇脱氢酶I型（17β-HSD1）的抑制剂的3,15-取代的雌酮化合物，其盐，含有这些化合物的药物制剂，制备这些化合物的方法，以及这些化合物的治疗用途，特别是在治疗 或抑制类固醇激素依赖性疾病或病症，例如需要抑制17β-羟类固醇脱氢酶I型酶和/或需要降低内源性17β-雌二醇浓度的类固醇激素依赖性疾病或病症，以及一般使用 具有额外的选择性17β-羟类固醇脱氢酶1型抑制剂，其除了雌激素受体之外还没有纯化的拮抗性结合亲和力，用于治疗或抑制良性妇科疾病，特别是子宫内膜异位症。
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公开(公告)号：US08088758B2
公开(公告)日：2012-01-03
申请号：US10983887
申请日：2004-11-09
申请人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Bartholomeus Johannes Van Steen , Gyula Schneider , Johannes Bernardus Everardus Hulshof , Pasi Koskimies , Nina Johansson , Jerzy Adamski
发明人： Josef Messinger , Heinrich-Hubert Thole , Bettina Husen , Bartholomeus Johannes Van Steen , Gyula Schneider , Johannes Bernardus Everardus Hulshof , Pasi Koskimies , Nina Johansson , Jerzy Adamski
CPC分类号： C07J1/0059 , C07J21/008 , C07J41/0044 , C07J43/003
摘要： 3,15-substituted estrone compounds which act as inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, particularly in the treatment or inhibition of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17β-estradiol concentration, as well as the general use of selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment or inhibition of benign gynecological disorders, particularly endometriosis.
摘要翻译： 3,15-取代的雌酮化合物，其作为17β-羟基类固醇脱氢酶I（17＆amp; -HSD1）的抑制剂，其盐，含有这些化合物的药物制剂，制备这些化合物的方法，以及这些化合物的治疗用途，特别是 类固醇激素依赖性疾病或病症的治疗或抑制，例如类固醇激素依赖性疾病或需要抑制17β-羟基类固醇脱氢酶I型酶和/或需要降低内源性17β-雌二醇浓度的病症，以及 一般使用选择性17＆bgr-羟基类固醇脱氢酶1型抑制剂，其除了具有雌激素受体以外还没有纯化的拮抗性结合亲和力，用于治疗或抑制良性妇科疾病，特别是子宫内膜异位症。
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9.发明申请公开(公告)号：US20080255075A1
公开(公告)日：2008-10-16
申请号：US11947025
申请日：2007-11-29
申请人： Josef MESSINGER , Uwe Schoen , Heinrich-Hubert Thole , Bettina Husen , Pasi Koskimies , Mikko Unkila
发明人： Josef MESSINGER , Uwe Schoen , Heinrich-Hubert Thole , Bettina Husen , Pasi Koskimies , Mikko Unkila
CPC分类号： C07J43/00
摘要： Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17β-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.
摘要翻译： 可用于治疗，特别是治疗或抑制需要抑制17β-羟类固醇脱氢酶（17β-HSD）1型，2型和/或3型酶的类固醇激素依赖性病症的式（I）化合物的取代雌三烯化合物， 以及它们的盐，含有这些化合物的药物组合物和制备这些化合物的方法。
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公开(公告)号：US20080146531A1
公开(公告)日：2008-06-19
申请号：US11856768
申请日：2007-09-18
申请人： Josef Messinger , Uwe Schoen , Heinrich-Hubert Thole , Bettina Husen , Pasi Koskimies , Lila KALLIO nee Pirkkala
发明人： Josef Messinger , Uwe Schoen , Heinrich-Hubert Thole , Bettina Husen , Pasi Koskimies , Lila KALLIO nee Pirkkala
CPC分类号： C07J43/00 , Y10S514/825 , Y10S514/826 , Y10S514/863 , Y10S514/866 , Y10S514/903
摘要： Estratrien-triazoles corresponding to formula (I) (shown below) which are useful in therapy, especially for the treatment and/or prevention or inhibition of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17β-HSD) such as 17β-HSD type 1, type 2 or type 3 enzyme.
摘要翻译： 对应于式（I）（如下所示）的依那他三唑可用于治疗，特别是用于治疗和/或预防或抑制类固醇激素依赖性病症，优选需要抑制17β的类固醇激素依赖性疾病或病症 - 类固醇脱氢酶（17β-HSD），如17β-HSD 1型，2型或3型酶。
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