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1. 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。

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

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。

4. 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。

5. 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。

6. 发明授权

US06790842B1 11&bgr; LONG-CHAIN SUBSTITUTED ESTRATRIENES, METHOD FOR THEIR PRODUCTION, PHARMACEUTICAL PREPARATIONS CONTAINING SAID 11&bgr; LONG-CHAIN SUBSTITUTED ESTATRIENES, AND THEIR USE FOR PRODUCING MEDICAMENTS 失效
标题翻译： 11β长链取代的ESTRATRIENES，其生产方法，含有11β长链取代的ESTATRIRIES的药物制剂及其用于生产药物的用途
公开(公告)号：US06790842B1
公开(公告)日：2004-09-14
申请号：US10018429
申请日：2002-05-07
申请人： Rolf Bohlmann , Nikolaus Heinrich , Jorg Kroll , Gerhard Sauer , Karl-Heinrich Fritzemeier , Christa Hegele-Hartung , Jens Hoffmann , Rosemarie Lichtner , Ludwig Zorn
发明人： Rolf Bohlmann , Nikolaus Heinrich , Jorg Kroll , Gerhard Sauer , Karl-Heinrich Fritzemeier , Christa Hegele-Hartung , Jens Hoffmann , Rosemarie Lichtner , Ludwig Zorn
IPC分类号： A61K3158
CPC分类号： C07J1/00
摘要： This invention describes a 11&bgr;-long-chain-substituted estratriene of general formula (I), in which R11 is a long-chain radical that has a nitrogen atom and optionally a sulfur atom, which in addition can be functionalized in the terminal position with a perfluoroalkyl group or an optionally substituted arly radical. The compound can have antiestrogenic or tissue-selective estrogenic properties and be suitable for the production of pharmaceutical agents.
摘要翻译：本发明描述了通式（I）的11b-长链取代的雌三烯，其中R 11是具有氮原子和任选的硫原子的长链基团，其还可以在具有全氟烷基或任选取代的芳基的末端位置。该化合物可以具有抗雌激素或组织选择性雌激素特性，并且适用于生产药剂。

7. 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。

8. 发明授权

US06958327B1 18 Norsteroids as selectively active estrogens 失效
标题翻译： 18只小鼠作为选择性活性雌激素
公开(公告)号：US06958327B1
公开(公告)日：2005-10-25
申请号：US10111933
申请日：2000-11-02
申请人： Alexander Hillisch , Werner Boidol , Wolfgang Schwede , Peter Esperling , Gerhard Sauer , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier
发明人： Alexander Hillisch , Werner Boidol , Wolfgang Schwede , Peter Esperling , Gerhard Sauer , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J1/00
摘要： The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R1, R2, R3, R6, R7, R8, R9, R11, R11′, R14, R15, R15′, R16, R17 and R17′ have the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention. The invention also relates to utilization of steroids based on the gonatriene molecular skeleton in order to treat estrogen deficiency-induced diseases and disorders, in addition to the use of said gonatriene structural component in the total structure of compounds which dissociate to produce enhanced estrogen activity in bone as compared to the uterus
摘要翻译：本发明涉及通式（I）的新颖的18-降胆固醇（高三烯），其中R 1，R 2，R 3，R 3， R 6，R 7，R 8，R 9，R 11，R 11，R 11， R 11，R 14，R 15，R 15'，R 16， R 17和R 17'具有说明书中引用的含义，以及所述化合物作为药物活性成分的用途。所述化合物在体外对大鼠前列腺的雌激素受体制剂和大鼠子宫的雌激素受体制剂中表现出高亲和力。与刺激5HT2a受体和转运蛋白分子表达相关的子宫和/或显着活性相比，所述化合物在骨骼上表现出体内优先活性。本发明还涉及所述化合物的生产，本发明新化合物中所含化合物的治疗用途和盖仑型形式。本发明还涉及除了在分解以产生增强的雌激素活性的化合物的总体结构中使用所述三氢结构组分之外，还可以利用基于分子量分子骨架的类固醇来治疗雌激素缺乏诱导的疾病和病症骨与子宫相比

9. 发明申请

US20050282791A1 18-nor steroids as selectively active estrogens 审中-公开
标题翻译： 18-或类固醇作为选择性活性雌激素
公开(公告)号：US20050282791A1
公开(公告)日：2005-12-22
申请号：US11184784
申请日：2005-07-20
申请人： Alexander Hillisch , Werner Boidol , Wolfgang Schwede , Peter Esperling , Gerhard Sauer , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier
发明人： Alexander Hillisch , Werner Boidol , Wolfgang Schwede , Peter Esperling , Gerhard Sauer , Christa Hegele-Hartung , Uwe Kollenkirchen , Karl-Heinrich Fritzemeier
IPC分类号： A61K31/56 , A61K31/58
CPC分类号： C07J1/0051
摘要： This invention describes the new 18-nor steroids (gonatrienes) of general formula (I), in which R1, R2, R3, R6, R7, R8, R9, R11, R11′, R14, R15, R15, R16, R17 and R17′ have the meanings that are indicated in the description, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo a preferential action on bone in comparison to the uterus, and/or pronounced action relative to the stimulation of the expression of 5HT2a-receptors and transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention further describes the use of steroids, on which the gonatriene skeleton is based, for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of the gonatriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bone in comparison to the uterus.
摘要翻译：本发明描述了通式（I）的新的18-或类固醇（高碳二烯），其中R 1，R 2，R 3，R 3， R 6，R 7，R 8，R 9，R 11，，R 11，R 14，R 15，R 15，R 16， R 17和R 17具有在说明书中指出的含义，作为具有体外对大鼠前列腺的雌激素受体制剂具有更高亲和力的药物活性成分而不是雌激素受体制剂的大鼠子宫和体内与子宫相比优于骨骼的优势，和/或相对于刺激5HT2a受体和转运蛋白表达的显着作用，其生产，其治疗用途和药物分配包含新化合物的形式。本发明进一步描述了用于治疗雌激素缺乏诱导的疾病和病症以及在有兴趣解离的化合物的总体结构中使用三烯结构部分的用途，与子宫相比，它们对骨骼的雌激素作用。

10. 发明授权

US4591585A 1-alkyl-androsta-1,4-diene-3,17-diones their production and pharmaceutical preparations containing same 失效
标题翻译： 1-烷基 - 雄甾-1,4-二烯-3,17-将其制备和含有它们的药物制剂分离
公开(公告)号：US4591585A
公开(公告)日：1986-05-27
申请号：US621769
申请日：1984-06-18
申请人： Ulrich Kerb , Gerhard Sauer , Rudolf Wiechert , David Henderson , Yukishige Nishino , Sybille Beier
发明人： Ulrich Kerb , Gerhard Sauer , Rudolf Wiechert , David Henderson , Yukishige Nishino , Sybille Beier
IPC分类号： A61K31/565 , A61P13/02 , A61P15/00 , A61P35/00 , C07J1/00 , A61K31/56
CPC分类号： C07J1/0011
摘要： 1-Alkyl androsta-1,4-diene-3,17-diones of the formula ##STR1## wherein R.sub.1 is a methyl, ethyl, hydroxymethyl, C.sub.1 -C.sub.3 -alkoxymethyl, or C.sub.1 -C.sub.4 -alkanoyloxymethyl group, R.sub.6 is a hydrogen atom or a methyl group, and R.sub.7 is a hydrogen atom or a methyl group in the 7.alpha.- or 7.beta.-position, are useful for fertility control and for the treatment of estrogen-triggered diseases.
摘要翻译：其中R 1是甲基，乙基，羟甲基，C 1 -C 3 - 烷氧基甲基或C 1 -C 4 - 烷酰氧基甲基，R 6是氢原子的1-烷基雄甾-1,4-二烯-3,17-二酮原子或甲基，R7是7α-或7β-位中的氢原子或甲基，可用于生育调控和用于治疗雌激素引发的疾病。

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