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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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3.发明授权2-substituted D-homo-estra-1,3,5(10)-trienes as inhibitors of 17β-hydroxy steroid dehydrogenase type 1 失效2-取代的D-异孕烯-1,3,5（10） - 三烯作为17型和β-羟基类固醇脱氢酶1型的抑制剂公开(公告)号：US07732493B2
公开(公告)日：2010-06-08
申请号：US12192446
申请日：2008-08-15
申请人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
发明人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
CPC分类号： C07J63/00
摘要： The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17β-hydroxy steroid dehydro-genase type 1.
摘要翻译： 本发明涉及通式I的新的2-取代的D-异 - 雌-1,3,5（10） - 三烯，其中R 2表示C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基或卤素 原子，R 13表示氢原子或甲基，R 17表示氢原子或氟原子，以及它们的药学上可接受的盐，它们的制备和用途，作为预防和治疗雌激素依赖性疾病的药物，其可受 抑制17＆bgr-羟基类固醇脱氢酶1型。
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4.发明申请NEW 2-SUBSTITUTED D-HOMO-ESTRA-1,3,5(10)-TRIENES AS INHIBITORS OF 17BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 失效新的2-取代的D-HOMO-ESTRA-1,3,5（10） - 作为17BA-羟基甾体脱氢酶1型的抑制剂公开(公告)号：US20080306164A1
公开(公告)日：2008-12-11
申请号：US12192446
申请日：2008-08-15
申请人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
发明人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
IPC分类号： C07J63/00 , A61K31/122
CPC分类号： C07J63/00
摘要： The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17β-hydroxy steroid dehydro-genase type 1.
摘要翻译： 本发明涉及通式I的新的2-取代的D-异 - 雌-1,3,5（10） - 三烯，其中R 2表示C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基或卤素 原子，R 13表示氢原子或甲基，R 17表示氢原子或氟原子，以及它们的药学上可接受的盐，它们的制备和用途，作为预防和治疗雌激素依赖性疾病的药物，其可受 抑制17β-羟基类固醇脱氢基因型1型。
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5.发明授权2-substituted D-homo-estra-1,3,5(10)-trienes as inhibitors of 17β-hydroxy steroid dehydrogenase type 1 失效2-取代的D-均一雌-1,3,5（10）三烯作为17β-羟基类固醇脱氢酶1型的抑制剂公开(公告)号：US07435757B2
公开(公告)日：2008-10-14
申请号：US11171476
申请日：2005-07-01
申请人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
发明人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
CPC分类号： C07J63/00
摘要： The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17β-hydroxy steroid dehydro-genase type 1.
摘要翻译： 本发明涉及通式I的新的2-取代的D-异 - 雌-1,3,5（10） - 三烯，其中R 2是指C 1〜 -C 8 - 烷基，C 1 -C 8 - 烷氧基或卤素原子，R 13 >表示氢原子或甲基，R 17表示氢原子或氟原子，以及它们的药学上可接受的盐，它们作为用于预防和治疗雌激素依赖性药物的制备和用途 可能受到抑制17β-羟基类固醇脱氢基因型1的影响的疾病。
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6.发明申请New 2-substituted D-homo-estra-1,3,5(10)-trienes as inhibitors of 17beta-hydroxy steroid dehydrogenase type 1 失效新的2-取代的D-同 - 雌-1,3,5（10） - 三烯作为17β-羟基类固醇脱氢酶1型的抑制剂公开(公告)号：US20060052461A1
公开(公告)日：2006-03-09
申请号：US11171476
申请日：2005-07-01
申请人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
发明人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
CPC分类号： C07J63/00
摘要： The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17β-hydroxy steroid dehydro-genase type 1.
摘要翻译： 本发明涉及通式I的新的2-取代的D-异 - 雌-1,3,5（10） - 三烯
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7.发明授权2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17β-hydroxy steroid dehydrogenase type 1 失效2-取代的雌-1,3,5（10） - 三烯-17-酮作为17β-羟基类固醇脱氢酶1型的抑制剂公开(公告)号：US07419972B2
公开(公告)日：2008-09-02
申请号：US11154947
申请日：2005-06-17
申请人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Andrea Rosinus , Jerzy Adamski , Gabriele Moeller , Walter Elger , Birgitt Schneider , Ulrich Bothe
发明人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Andrea Rosinus , Jerzy Adamski , Gabriele Moeller , Walter Elger , Birgitt Schneider , Ulrich Bothe
CPC分类号： C07J1/00
摘要： The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of formula I as well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for prophylaxis and/or therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17β-hydroxy steroid dehydrogenase type 1.
摘要翻译： 本发明涉及式I的新的2-取代的雌-1,3,5（10） - 三烯-17-酮及其药学上可接受的盐，其制备和用作预防和/或治疗药物的方法 雌激素依赖性疾病，可受1型17β-羟基类固醇脱氢酶抑制的影响。
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公开(公告)号：US20060009434A1
公开(公告)日：2006-01-12
申请号：US11154947
申请日：2005-06-17
申请人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Andrea Rosinus , Jerzy Adamski , Gabriele Moeller
发明人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Andrea Rosinus , Jerzy Adamski , Gabriele Moeller
CPC分类号： C07J1/00
摘要： The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of general formula I in which R2 means a saturated or unsaturated C1-C8-alkyl group, a C1-C5-alkyloxy group, an aralkyl radical or alkylaryl radical, a radical —O—CnFmHo, whereby n=1, 2, 3, 4, 5 or 6, m≧1 and m+o=2n+1, or a group CH2XY, in which X stands for an oxygen atom and Y stands for an alkyl radical with 1 to 4 carbon atoms, as well as a halogen atom or a nitrile group, R13 means a hydrogen atom or a methyl group, R16 means a hydrogen atom or a fluorine atom, Z means an oxygen atom or a sulfur atom, R3 and R5, in each case independently of one another, mean an α- or β-position hydrogen atom, R4 and R6, in each case independently of one another, mean an α- or β-position hydrogen atom, a C1-C5-alkyl group, a C1-C5-alkyloxy group, a C1-C5-acyl group or a hydroxy group or an aralkyl radical or alkylaryl radical, R3 and R4 together mean an oxygen atom, R5 and R6 together mean an oxygen atom, R7 and R8 in each case mean a hydrogen atom or together a CH2 group, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17β-hydroxy steroid dehydrogenase type 1.
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