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1. 发明授权

US06596713B1 Steroid esters and amides, process for their production and their pharmaceutical use 失效
标题翻译：类固醇酯和酰胺，其生产过程及其药物用途
公开(公告)号：US06596713B1
公开(公告)日：2003-07-22
申请号：US08914176
申请日：1997-08-19
申请人： Ulrich Klar , Arwed Cleve , Guenter Neef , Eckhard Ottow , Klaus Stoekemann , Karl-Heinrich Fritzemeier
发明人： Ulrich Klar , Arwed Cleve , Guenter Neef , Eckhard Ottow , Klaus Stoekemann , Karl-Heinrich Fritzemeier
IPC分类号： A61K3156
CPC分类号： C07J53/00 , C07J41/0083 , C07J41/0094 , C07J53/002
摘要： New steroids and amides of formula I are described, in which the variables are defined by the description. Relative to the basic hydroxy compounds (“initial compounds”), the new compounds are distinguished by a considerably improved solubility and partially also by increased biological action and selectivity. The new compounds are suitable for the production of pharmaceutical agents.
摘要翻译：描述了新的类固醇和酰胺，其中变量由描述定义。相对于碱性羟基化合物（“初始化合物”），新化合物通过显着改善的溶解度和部分地通过增加的生物作用和选择性来区分。新化合物适用于制药。

2. 发明授权

US6096732A Steroid esters, process for their production and their pharmaceutical use 失效
标题翻译：类固醇酯，其生产过程及其药物用途
公开(公告)号：US6096732A
公开(公告)日：2000-08-01
申请号：US986592
申请日：1997-12-08
申请人： Ulrich Klar , Arwed Cleve , Wolfgang Schwede , Gunter Neef , Eckhard Ottow , Kristof Chwalisz , Martin Schneider
发明人： Ulrich Klar , Arwed Cleve , Wolfgang Schwede , Gunter Neef , Eckhard Ottow , Kristof Chwalisz , Martin Schneider
IPC分类号： A61K31/565 , A61P35/00 , C07J53/00 , A61K31/56
CPC分类号： C07J53/002 , Y10S514/843
摘要： Steroid esters of formula I ##STR1## are described, wherein m, n and x are as defined by the specification. The compounds are distinguished from the basic hydroxy compounds by considerably improved solubility as well by increased biological activity and selectivity.The compounds are suitable for the production of pharmaceutical agents.
摘要翻译：描述式I的类固醇酯，其中m，n和x如本说明书所定义。通过显着改善溶解度以及增加的生物活性和选择性，化合物与碱性羟基化合物的区别。该化合物适用于生产药剂。

3. 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。

4. 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。

5. 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.

6. 发明授权

US06806263B2 Antigestagenically active steroids with a fluorinated 17-alpha-alkyl chain 失效
标题翻译：具有氟化17-α-烷基链的抗发生活性类固醇
公开(公告)号：US06806263B2
公开(公告)日：2004-10-19
申请号：US10304742
申请日：2002-11-27
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K3156
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： 17&agr;-fluoroalkyl steroids of formula I as well as their physiologically compatible salts with acids and for —CO2R9 radicals with R9 meaning hydrogen, as well their physiologically compatible salts with bases, have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：具有式I的17α-氟烷基类固醇以及其与酸的生理上相容的盐以及具有R 9意义氢的-CO 2 R 9基团以及它们与碱的生理上相容的盐具有非常强的抗前体作用，并且适用于生产药物制剂。

7. 发明授权

US06503895B2 Antigestagenically active steroids with a fluorinated 17&agr;-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US06503895B2
公开(公告)日：2003-01-07
申请号：US09978689
申请日：2001-10-18
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K3156
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17&agr;fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with bases. The new compounds have an extraordinary strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了通式Ⅰ的新型17-氟烷基类固醇，以及它们与碱的生理上相容的盐。新化合物具有特别强的抗前列腺素作用，适用于制备药物制剂。

8. 发明授权

US07148213B2 Antigestagenically active steroids with a fluorinated 17α-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US07148213B2
公开(公告)日：2006-12-12
申请号：US10948652
申请日：2004-09-24
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K31/56
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17α-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with bases. The new compounds have an extraordinary strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了通式I的新的17α-氟烷基类固醇以及它们与碱的生理上相容的盐。新化合物具有非常强的抗前体作用，适用于制备药物制剂。

9. 发明授权

US06316432B1 Antigestagenically active steroids with a flourinated 17 &agr;-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US06316432B1
公开(公告)日：2001-11-13
申请号：US09516359
申请日：2000-03-01
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K3156
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17&agr;-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with acids, and for —CO2R9 radicals with R9 meaning hydrogen as well as their physiologically compatible salts with bases. The new compounds have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了具有通式Ⅰ的新的17α-氟烷基类固醇以及它们与酸的生理上相容的盐，对于含有R9的-CO 2 R 9基团以及它们与碱的生理上相容的盐。新化合物具有非常强的抗前体作用适用于药物制剂的生产。

10. 发明申请

US20050080060A1 Antigestagenically active steroids with a fluorinated 17alpha-alkyl chain 失效
标题翻译：具有氟化17α-烷基链的抗发生活性类固醇
公开(公告)号：US20050080060A1
公开(公告)日：2005-04-14
申请号：US10948652
申请日：2004-09-24
申请人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
发明人： Wolfgang Schwede , Arwed Cleve , Ulrich Klar , Gunter Neef , Kristof Chwalisz , Martin Schneider , Ulrike Fuhrmann , Holger Heb-Stumpp
IPC分类号： A61K31/56 , A61P5/36 , C07J1/00 , C07J41/00 , C07J43/00 , C07J53/00
CPC分类号： C07J1/0033 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002
摘要： This invention describes the new 17α-fluoroalkyl steroids of general formula I in which R1 stands for a methyl or ethyl group, R2 stands for a radical of formula CnFmHo, whereby n is 2, 3, 4, 5 or 6, m>1 and m+o=2n+1, R3 stands for a free, etherified or esterified hydroxy group, R4 and R5 each stand for a hydrogen atom, or together for an additional bond or a methylene group, St stands for a steroidal ABC-ring system of partial formula A, B or C in which R6 means a hydrogen atom, a straight-chain C1-C4 alkyl group or branched C3-C4 alkyl group or a halogen atom, R7 means a hydrogen atom, a straight-chain C1-C4 alkyl group or a branched C3-C4 alkyl group, or if St stands for a steroidal ABC-ring system A or B, in addition R6 and R7 together can mean an additional bond, X means an oxygen atom, a hydroxyimino grouping ═N—OH or two hydrogen atoms, R8 means a radical Y or an aryl radical that is optionally substituted in several places with a group Y, whereby Y is a hydrogen atom, a halogen atom, an —OH, —NO2, —N3, —CN, —NR9aR9b, —NHSO2R9, —CO2R9, C1-C10 alkoxy, C1-C10 alkanoyloxy, benzoyloxy, C1-C10 alkanoyl, C1-C10 hydroxyalkyl or benzoyl group, and R9a and R9b are the same or different and in the same way as R9 represent a hydrogen atom or a C1-C10 alkyl group, and for —NR9aR9b radicals, as well as their physiologically compatible salts with acids and for —CO2R9 radicals with R9 meaning hydrogen, as well as their physiologically compatible salts with bases. The new compounds have an extraordinarily strong antigestagenic action and are suitable for the production of pharmaceutical preparations.
摘要翻译：本发明描述了通式I的新型17α-氟烷基类固醇，其中R 1代表甲基或乙基，R 2代表式C n F m H o基团，其中n为2,3,4,5或 6，m> 1和m + o = 2n + 1，R 3表示游离的醚化或酯化的羟基，R 4和R 5各自代表氢原子，或一起代表另外的键或亚甲基，St代表部分式A，B或C的甾族ABC-环体系，其中R 6表示氢原子，直链C 1 -C 4烷基或支链C 3 -C 4烷基或卤素原子，R 7表示氢原子，直链C 1 -C 4烷基或支链C 3 -C 4烷基，或者如果St代表甾族ABC环系统A或B，另外R R 6和R 7一起可以表示另外的键，X表示氧原子，羟基亚氨基= N-OH或两个氢原子，R 8表示任意取代的基团Y或芳基几个地方有一个Y组，Y是一个氢原子，卤素原子，-OH，-NO 2，-N 3，-CN，-NR 9a R 9b，-NHSO 2 R 9，-CO 2 R 9，C 1 -C 10烷氧基，C 1 -C 10 烷酰氧基，苯甲酰氧基，C 1 -C 10烷酰基，C 1 -C 10羟烷基或苯甲酰基，R 9a和R 9b相同或不同，并且R 9表示氢原子或C1- C10烷基，对于-NR 9a R 9b基团，以及它们与酸的生理上相容的盐以及具有R 9表示氢的-CO 2 R 9基团，以及它们与基地新化合物具有非常强的抗前体作用，适用于制备药物制剂。

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