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1. 发明授权

US06288051B1 7 &agr;-(5-methylaminopentyl)-estratrienes, process for their production, pharmaceutical preparations that contain these 7 &agr;(5-methylaminopentyl)-estratrienes as well as their use for the production of pharmaceutical agents 失效
标题翻译： 7α-（5-甲基氨基戊基） - 雌三烯，其制备方法，含有这些7α（5-甲基氨基戊基） - 雌三醇的药物制剂及其制备药剂的用途
公开(公告)号：US06288051B1
公开(公告)日：2001-09-11
申请号：US09417765
申请日：1999-10-14
申请人： Dieter Bittler , Rolf Bohlmann , Nikolaus Heinrich , Jorg Kroll , Gerhard Sauer , Yukishige Nishino , Karsten Parczyk , Martin Schneider , Christa Hegelehartung , Rosemarie Lichtner
发明人： Dieter Bittler , Rolf Bohlmann , Nikolaus Heinrich , Jorg Kroll , Gerhard Sauer , Yukishige Nishino , Karsten Parczyk , Martin Schneider , Christa Hegelehartung , Rosemarie Lichtner
IPC分类号： A61K3156
CPC分类号： C07J1/0059 , C07J1/007 , C07J1/0074 , C07J17/00 , C07J31/006 , C07J41/0072 , C07J51/00
摘要： This invention describes the new 7&agr;-(5-methylaminopentyl)-estratrienes of general formula I in which R2 stands for a hydrogen or fluorine atom, R17 stands for a hydrogen atom, a methyl or ethinyl group, n stands for 2, 3 or 4, and x stands for 0, 1 or 2. The new compounds are strong, pure antiestrogens and can be used for the production of pharmaceutical agents for treatment of estrogen-dependent diseases, for example, breast cancer, endometrial carcinoma, prostatic hyperplasia, anovulatory infertility and melanoma.
摘要翻译：本发明描述了通式Iin的新的7α-（5-甲基氨基戊基） - 三亚甲基，其中R 2表示氢或氟原子，R 17表示氢原子，甲基或乙炔基，n表示2,3或4，x表示代表0，1或2.新化合物是强的纯粹的抗雌激素，可用于生产用于治疗雌激素依赖性疾病的药剂，例如乳腺癌，子宫内膜癌，前列腺增生，排卵不育和黑素瘤。

2. 发明授权

US5986115A 7.alpha.-(.xi.-aminoalkyl)-estratrienes, process for their production, pharmaceutical preparations which contain these 7.alpha.-(.xi.-aminoalkyl)-estratrienes as well as their use for the production of pharmaceutical agents 失效
标题翻译： 7α-（xi-氨基烷基） - 雌三烯，其制备方法，含有这些7α-（xi-氨基烷基） - 雌三烯的药物制剂及其用于生产药剂
公开(公告)号：US5986115A
公开(公告)日：1999-11-16
申请号：US239490
申请日：1999-01-28
申请人： Rolf Bohlmann , Dieter Bittler , Josef Heindl , Nikolaus Heinrich , Helmut Hofmeister , Hermann Kunzer , Gerhard Sauer , Christa Hegele-Hartung , Rosemarie Lichtner , Yukishige Nishino , Karsten Parczyk , Martin Schneider
发明人： Rolf Bohlmann , Dieter Bittler , Josef Heindl , Nikolaus Heinrich , Helmut Hofmeister , Hermann Kunzer , Gerhard Sauer , Christa Hegele-Hartung , Rosemarie Lichtner , Yukishige Nishino , Karsten Parczyk , Martin Schneider
IPC分类号： C07J41/00 , C07J43/00 , C07J53/00 , C07D315/00 , C07J1/00 , C07J13/00 , C07J31/00
CPC分类号： C07J53/002 , C07J41/0072 , C07J43/006 , C07J53/008
摘要： This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
摘要翻译：本发明描述了通式I的新的取代的7α-（xi-氨基烷基） - 三亚甲基，其中侧链SK是部分式的基团，以及它们与有机和无机酸的生理上相容的加成盐。新化合物代表具有非常强的抗雌激素作用的化合物。根据本发明的化合物一方面是纯抗雌激素，或者另一方面是具有雌激素部分作用的抗雌激素。基于这一作用范围，新化合物非常适合用于肿瘤治疗和激素替代治疗药物的生产。

3. 发明授权

US06271403B1 7&agr;-(xi-aminoalkyl)-estratrienes, process for their production, pharmaceutical preparations which contain these 7&agr;-(xi-aminoalkyl-estratrienes as well as their use for the production of pharmaceutical agents 失效
标题翻译： 7α-（xi-氨基烷基） - 三亚甲基，其制备方法，含有这些7α-（N-氨基烷基 - 雌三烯）及其用于生产药剂的用途的药物制剂
公开(公告)号：US06271403B1
公开(公告)日：2001-08-07
申请号：US09549724
申请日：2000-04-14
申请人： Rolf Bohlmann , Dieter Bittler , Josef Heindl , Nikolaus Heinrich , Helmut Hofmeister , Hermann Künzer , Gerhard Sauer , Christa Hegele-Hartung , Rosemarie Lichtner , Yukishige Nishino , Karsten Parczyk , Martin Schneider
发明人： Rolf Bohlmann , Dieter Bittler , Josef Heindl , Nikolaus Heinrich , Helmut Hofmeister , Hermann Künzer , Gerhard Sauer , Christa Hegele-Hartung , Rosemarie Lichtner , Yukishige Nishino , Karsten Parczyk , Martin Schneider
IPC分类号： C07J100
CPC分类号： C07J53/002 , C07J41/0072 , C07J43/006 , C07J53/008
摘要： This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I in which side chain SK is a radical of partial formula The new compounds represent compounds with very strong antiestrogenic action. The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
摘要翻译：本发明描述了通式Iin的新的取代的7α-（ε-氨基烷基） - 三亚甲基，其中链SK是部分式的基团。新化合物代表具有非常强的抗雌激素作用的化合物。根据本发明的化合物一方面，纯抗雌激素，或另一方面，具有雌激素部分作用的抗雌激素。基于这一作用范围，新化合物非常适合用于肿瘤治疗和激素替代治疗药物的生产。

4. 发明授权

US06780855B2 11&bgr;-HALOGEN-7&agr;-SUBSTITUTED ESTRATRIENES, PROCESS FOR THE PRODUCTION OF PHARMACEUTICAL PREPARATIONS THAT CONTAIN THESE 11&bgr;-HALOGEN-7&agr;-SUBSTITUTED ESTRATRIENES AS WELL AS THEIR USE FOR THE PRODUCTION OF PHARMACEUTICAL AGENTS 失效
标题翻译：用于生产药用制剂的方法，其用于生产药用制剂的制备方法，其包含这些11α-羟基-7α-取代的ESTRATRIENES，作为其用于生产药物代谢物
公开(公告)号：US06780855B2
公开(公告)日：2004-08-24
申请号：US09380413
申请日：1999-12-02
申请人： Rolf Bohlmann , Nikolaus Heinrich , Helmut Hofmeister , Jorg Kroll , Hermann Kunzer , Gerhard Sauer , Ludwig Zorn , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner , Yukishige Nishino , Karsten Parczyk , Martin Schneider
发明人： Rolf Bohlmann , Nikolaus Heinrich , Helmut Hofmeister , Jorg Kroll , Hermann Kunzer , Gerhard Sauer , Ludwig Zorn , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner , Yukishige Nishino , Karsten Parczyk , Martin Schneider
IPC分类号： C07J100
CPC分类号： C07J41/0094 , C07J31/006 , C07J41/0072 , C07J43/003
摘要： This invention describes the new 11&bgr;-halogen-7&agr;-substituted estratrienes of general formula I in which R11 is a fluorine or chlorine atom, and the other substituents have the meanings that are explained in more detail in the description. The compounds have antiestrogenic properties or tissue-selective estrogenic properties and are suitable for the production of pharmaceutical agents.
摘要翻译：本发明描述了通式Iin的新的11beta-卤素-7α-取代的雌三烯，其中R 11是氟或氯原子，其它取代基具有在本说明书中更详细解释的含义。化合物具有抗雌激素特性或组织选择性雌激素特性，并且适用于药剂的生产。

5. 发明授权

US5866560A 7.alpha.-(.xi.-aminoalkyl)-estratrienes, process for their production, pharmaceutical preparations which contain these 7.alpha.-(.xi.-aminoalkyl)-estratrienes as well as their use for the production of pharmaceutical agents 失效
标题翻译： 7α-（xi-氨基烷基） - 雌三烯，其制备方法，含有这些7α-（xi-氨基烷基） - 雌三烯的药物制剂及其用于生产药剂
公开(公告)号：US5866560A
公开(公告)日：1999-02-02
申请号：US915171
申请日：1997-08-20
申请人： Rolf Bohlmann , Dieter Bittler , Josef Heindl , Nikolaus Heinrich , Helmut Hofmeister , Hermann Kunzer , Gerhard Sauer , Christa Hegele-Hartung , Rosemarie Lichtner , Yukishige Nishino , Karsten Parczyk , Martin Schneider
发明人： Rolf Bohlmann , Dieter Bittler , Josef Heindl , Nikolaus Heinrich , Helmut Hofmeister , Hermann Kunzer , Gerhard Sauer , Christa Hegele-Hartung , Rosemarie Lichtner , Yukishige Nishino , Karsten Parczyk , Martin Schneider
IPC分类号： C07J41/00 , C07J43/00 , C07J53/00 , A61K31/56 , A61K31/58 , A61K45/00 , C07J1/00
CPC分类号： C07J53/002 , C07J41/0072 , C07J43/006 , C07J53/008
摘要： This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
摘要翻译：本发明描述了通式I的新的取代的7α-（xi-氨基烷基） - 三亚甲基（I），其中侧链SK是部分式“IMAGE”的基团，以及它们与有机物的生理上相容的加成盐和无机酸。新化合物代表具有非常强的抗雌激素作用的化合物。根据本发明的化合物一方面是纯抗雌激素，或者另一方面是具有雌激素部分作用的抗雌激素。基于这一作用范围，新化合物非常适合用于肿瘤治疗和激素替代治疗药物的生产。

6. 发明授权

US5807899A Triphenylethylenes, process for their production, pharmaceutical preparations that contain these triphenylethylenes as well as their use for the production of pharmaceutical agents 失效
标题翻译：三苯乙烯，其制备方法，含有这些三苯乙烯的药物制剂以及其用于生产药剂的用途
公开(公告)号：US5807899A
公开(公告)日：1998-09-15
申请号：US675906
申请日：1996-07-05
申请人： Rolf Bohlmann , Joseph Heindl , Hermann Kunzer , Yukishige Nishino , Karsten Parczyk , Martin Schneider
发明人： Rolf Bohlmann , Joseph Heindl , Hermann Kunzer , Yukishige Nishino , Karsten Parczyk , Martin Schneider
IPC分类号： C07C317/18 , C07C317/28 , C07C323/12 , C07C323/25 , C07C323/60 , C07D213/32 , C07D213/34 , A61K31/10 , C07C317/12 , C07C321/18 , C07C321/20
CPC分类号： C07C323/25 , C07C317/18 , C07C317/28 , C07C323/12 , C07C323/60 , C07D213/32 , C07D213/34
摘要： This invention describes the new triphenylethylenes of general formula I ##STR1## in which n means an integer from 1 to 10, R' means a sulfur-containing organic radical, R" means a hydrogen atom, an iodine atom or a hydroxy groups, E means a hydrogen atom, G means a hydrogen atom or E and G together mean a methylene bridge. The new compounds have strong antiestrogenic properties and are suitable for the production of pharmaceutical agents, for example for treating breast cancer.
摘要翻译：本发明描述了通式I（I）的新的三苯乙烯，其中n表示1至10的整数，R'表示含硫有机基团，R“表示氢原子，碘原子或羟基，E表示氢原子，G表示氢原子或E和G一起表示亚甲基桥。新化合物具有强的抗雌激素特性，适用于制药，例如用于治疗乳腺癌。

7. 发明授权

US6166075A Antiestrogens, process for their production and their pharmaceutical use 失效
标题翻译：抗雌激素，其生产过程及其药物用途
公开(公告)号：US6166075A
公开(公告)日：2000-12-26
申请号：US328451
申请日：1999-06-09
申请人： Ulrich Klar , Rolf Bohlmann , Karsten Parczyk , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner
发明人： Ulrich Klar , Rolf Bohlmann , Karsten Parczyk , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner
IPC分类号： C07D295/08 , A61K9/127 , A61K31/085 , A61K31/10 , A61K31/135 , A61K31/336 , A61K31/40 , A61K31/4465 , A61K31/45 , A61P5/32 , A61P35/00 , C07C43/23 , C07C217/14 , C07C275/08 , C07C317/18 , C07C323/12 , C07D303/16 , C07D303/22 , C07D303/26 , C07D303/34 , A61K31/22 , A61K31/045 , A61K31/075 , C07D303/00
CPC分类号： C07D303/22 , C07C43/23 , C07C217/14 , C07C317/18 , C07C323/12 , C07C2602/24
摘要： This invention relates to new antiestrogens of the general formula ##STR1## in which the substituents have the meanings that are explained in more detail in the description.The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens).Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.
摘要翻译：本发明涉及通式的新抗雌激素，其中取代基具有在说明书中更详细解释的含义。新化合物是a）纯抗雌激素或b）具有部分雌激素作用的抗雌激素（组织选择性雌激素）。基于这些性质，新化合物适用于生产药剂：a）例如用于治疗乳腺癌的情况; 在b）的情况下，例如用于激素替代疗法。

8. 发明授权

US06559181B1 Antiestrogens, process for their protection and their pharmaceutical use 失效
标题翻译：抗雌激素，其保护过程及其药物用途
公开(公告)号：US06559181B1
公开(公告)日：2003-05-06
申请号：US09706806
申请日：2000-11-07
申请人： Ulrich Klar , Rolf Bohlmann , Karsten Parczyk , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner
发明人： Ulrich Klar , Rolf Bohlmann , Karsten Parczyk , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner
IPC分类号： A61K3122
CPC分类号： C07D303/22 , C07C43/23 , C07C217/14 , C07C317/18 , C07C323/12 , C07C2602/24
摘要： This invention relates to new antiestrogens of the general formula in which the substituents have the meanings that are explained in more detail in the description. The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens). Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.
摘要翻译：本发明涉及一般形式的新抗雌激素，其取代基具有在本说明书中更详细解释的含义。新化合物是a）纯抗雌激素或b）具有部分雌激素作用的抗雌激素（组织选择性雌激素）。对于这些性质，新化合物适用于生产药剂：在a）的情况下，例如用于治疗乳腺癌; 在b）的情况下，例如用于激素替代疗法。

9. 发明授权

US07074829B2 Antiestrogens, process for their production and their pharmaceutical use 失效
公开(公告)号：US07074829B2
公开(公告)日：2006-07-11
申请号：US10369577
申请日：2003-02-21
申请人： Ulrich Klar , Rolf Bohlmann , Karsten Parczyk , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner
发明人： Ulrich Klar , Rolf Bohlmann , Karsten Parczyk , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner
IPC分类号： A01N37/02
CPC分类号： C07D303/22 , C07C43/23 , C07C217/14 , C07C317/18 , C07C323/12 , C07C2602/24
摘要： This invention relates to new antiestrogens of the general formula in which the substituents have the meanings that are explained in more detail in the description. The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens).Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.

10. 发明授权

US06767903B1 New7&agr;, 17&agr;-bis-alkylated testosterone derivatives and their use in long-term therapy of androgen-dependent diseases 失效
标题翻译： New7alpha，17α-双烷基化睾酮衍生物及其在长期治疗雄激素依赖性疾病中的应用
公开(公告)号：US06767903B1
公开(公告)日：2004-07-27
申请号：US09869000
申请日：2001-06-22
申请人： Arwed Cleve , Gerhard Sauer , Christoph Huwe , Karsten Parczyk , Jens Hoffmann , Martin Schneider
发明人： Arwed Cleve , Gerhard Sauer , Christoph Huwe , Karsten Parczyk , Jens Hoffmann , Martin Schneider
IPC分类号： A61K3159
CPC分类号： C07J1/00 , C07J5/00
摘要： The invention relates to new 7&agr;, 17&agr;, 17&bgr;-substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term antiandrogen therapy of prostate carcinoma. In the general formula (I) A is an unbranched C6-C13-alkylene group; B is an oxygen atom, —S(O)p— group, in which p is 0, 1 or 2, an iminocarbonyl group —C(O)N(Y)—, an imino group —N(Y)—, a carbonylimino group —N(Y)C(O)—, a sulfonylimino group —NN(Y)S(O)2—, where Y is a hydrogen atom or a C1-C8-alkyl group, a sulfonyloxy group —OS(O)2—, a dimethylsilyloxy group —O—Si(CH3)2— or a carbonylsulfanyl group —SC(O)— or a bond between A and C or, together with C, a bond between A and D; C is a bond between B and D or, together with B, a bond between A and D or an unbranched C1-C6-alkylene group, a phenylene group, a substituted phenylene group, a five-membered ring or six-membered ring heteroarylene group, a substituted five-membered ring or six-membered ring heteroarylene group or a five-membered ring or six-membered ring heteroarylene group fused with a phenyl ring; and D is a hydrogen atom, a C1-C4-alkyl group, a vinyl group, a C1-C4-alkoxy group, a C1-C4-alkoxycarbonyl group, a bis(C1-C4-alkoxycarbonyl)methyl group, an acetyl(C1-C4-alkoxybonyl)methyl group, a cyan group, a carboxy group, an azide group, a hydroxy group, a halogen atom or a rest of the formula CnFmHo, in which n is 1, 2, 3 or 4, m>1 and m+o=2n+1.
摘要翻译：本发明涉及通式（I）的新的7α，17α，17β-取代的睾酮衍生物及其作为用于长期治疗雄激素依赖性疾病的纯抗雄激素的用途，特别是用于前列腺癌的长期抗雄激素治疗。在通式（I）中，A是无支链的C 6 -C 13 - 亚烷基; B是氧原子，-S（O）对基，其中p是0,1或2，亚氨基羰基-C（O）N（Y） - ，亚氨基-N（Y） - ，羰基亚氨基-N（Y）C（O） - ，磺酰亚氨基-NN（Y）S（O）2 - ，其中Y是氢原子或C1-C8-烷基，磺酰氧基-OS（O ）2-，二甲基甲硅烷氧基-O-Si（CH 3）2 - 或羰基硫烷基-SSC（O） - 或A和C之间的键，或与C一起形成A和D之间的键; C是B和D之间的键，或者与B一起，A和D之间的键或无支链的C 1 -C 6 - 亚烷基，亚苯基，取代的亚苯基，五元环或六元环亚杂芳基取代的五元环或六元环亚杂芳基或与苯环稠合的五元环或六元环亚杂芳基; 和D是氢原子，C 1 -C 4烷基，乙烯基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 烷氧基羰基，双（C 1 -C 4 - 烷氧基羰基）甲基，乙酰基（ C 1 -C 4 - 烷氧基羰基）甲基，氰基，羧基，叠氮基，羟基，卤素原子或式C n F m H o的其余部分，其中n为1,2,3或4，m> 1和m + o = 2n + 1。

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