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51. 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。

52. 发明授权

US06610736B1 16-Halogen-epothilone derivatives, method for producing them and their pharmaceutical use 失效
标题翻译： 16-卤素 - 埃坡霉素衍生物，其制备方法及其药物用途
公开(公告)号：US06610736B1
公开(公告)日：2003-08-26
申请号：US09913495
申请日：2001-12-07
申请人： Ulrich Klar , Werner Skuballa , Bernd Buchmann , Wolfgang Schwede , Michael Schirner
发明人： Ulrich Klar , Werner Skuballa , Bernd Buchmann , Wolfgang Schwede , Michael Schirner
IPC分类号： A61K31335
CPC分类号： C07D401/06 , C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07F7/1804 , Y02P20/55
摘要： The invention relates to novel epothilone derivatives of general formula (I), wherein R8 means a halogen atom, especially a fluorine or chlorine atom, and the remaining substituents have the meanings given in the description. The novel compounds are suitable for producing medicaments.
摘要翻译：本发明涉及通式（I）的新颖埃坡霉素衍生物，其中R8表示卤素原子，特别是氟或氯原子，其余取代基具有说明书中给出的含义。新型化合物适用于生产药物。

53. 发明授权

US6147065A 14-.alpha., 17-.alpha.-C.sub.2 bridged norprogesterone derivatives 失效
标题翻译： 14-α，17-α-C 2桥连的去甲孕酮衍生物
公开(公告)号：US6147065A
公开(公告)日：2000-11-14
申请号：US362214
申请日：1999-07-28
申请人： Klaus Schollkopf , Wolfgang Halfbrodt , Joachim Kuhnke , Wolfgang Schwede , Karl-Heinrich Fritzemeier , Rolf Krattenmacher , Hans-Peter Muhn
发明人： Klaus Schollkopf , Wolfgang Halfbrodt , Joachim Kuhnke , Wolfgang Schwede , Karl-Heinrich Fritzemeier , Rolf Krattenmacher , Hans-Peter Muhn
IPC分类号： A61K31/56 , A61K31/58 , A61P43/00 , C07J53/00 , C07J71/00
CPC分类号： C07J71/0005 , C07J53/00 , Y10S514/841 , Y10S514/843
摘要： Described are 14,17-C.sub.2 -bridged steroids of the formula (I) defined in the specification. The compounds are available, even after peroral administration, with high gestagenic action and are suitable for the production of pharmaceutical agents.
摘要翻译：描述了本说明书中定义的式（I）的14,17-C2桥连类固醇。甚至在口服给药后，化合物也具有高的孕激素作用，并且适用于生产药剂。

54. 发明授权

US5519027A D-homo-(16-ene)-11.beta.-aryl-4-estrenes, process for their production as well as their use as pharmaceutical agents 失效
标题翻译： D-均聚（16-烯）-11β-芳基-4-雌酮，其制备方法以及作为药剂的用途
公开(公告)号：US5519027A
公开(公告)日：1996-05-21
申请号：US78326
申请日：1994-02-25
申请人： Wolfgang Schwede , Eckhard Ottow , Arwed Cleve , Walter Elger , Krzysztof Chwalisz , Martin Schneider
发明人： Wolfgang Schwede , Eckhard Ottow , Arwed Cleve , Walter Elger , Krzysztof Chwalisz , Martin Schneider
IPC分类号： A61K31/57 , A61K31/58 , A61K31/585 , A61P5/38 , C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J21/00 , C07J41/00 , C07J63/00 , A61K31/565
CPC分类号： C07J63/008
摘要： New D-homo-(16-ene)-11.beta.-aryl-4-estrenes of general formula I ##STR1## as well as their pharmaceutically compatible addition salts with acids are described in whichX stands for an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 stands for an hydroxy group, a C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.10 acyloxy group,R.sup.11 stands for a fluorine, chlorine or bromine atom, and then R.sup.12 and R.sup.13 together mean an additional bond orR.sup.11 stands for a straight-chain or branched-chain C.sub.1 -C.sub.4 -alkyl radical or a hydrogen atom, and then R.sup.12 and R.sup.13 each mean a hydrogen atom or together mean an additional bond,and R.sup.3 and R.sup.4 have the usual meanings indicated in the description for competitive progesterone antagonists.The invention further relates to a process for the production of new compounds, pharmaceutical preparations containing these compounds, their use for the production of pharmaceutical agents as well as the new intermediate products necessary for the process.The new compounds have a strong affinity to the gestagen receptor and show strong antigestagen as well as antiglucocorticoid, antimineral corticoid and antiandrogenic properties.
摘要翻译： PCT No.PCT / EP91 / 02495 371日期1994年2月25日 102（e）1994年2月25日PCT PCT 1991年12月21日PCT公布。出版物WO92 / 11279 日期：1992年7月9日。通式I（I）的新型D-均 - （16-烯）-11β-芳基-4-雌酮及其与酸的药学上相容的加成盐描述于其中 X表示氧原子，羟基亚氨基> N不同OH或两个氢原子，R1表示氢原子或甲基，R2表示羟基，C1-C10烷氧基或C1-C10酰氧基，R11 代表氟，氯或溴原子，然后R 12和R 13一起表示另外的键或R 11表示直链或支链的C 1 -C 4烷基或氢原子，则R 12和R 13各自表示氢原子或一起表示另外的键，并且R3和R4具有在竞争性孕酮拮抗剂的描述中指出的通常含义。本发明还涉及生产新化合物的方法，含有这些化合物的药物制剂，其用于生产药物的用途以及该方法所需的新的中间产物。新化合物对孕激素受体具有强烈的亲和力，并显示出强的抗老化，以及抗糖皮质激素，抗癫痫皮质激素和抗雄激素的特性。

55. 发明授权

US09156877B2 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-benzylidene derivatives, methods for the production thereof and use thereof for treating diseases 有权
标题翻译： 17-羟基-17-五氟乙烯基-4,9（10） - 二 - 亚苄基衍生物，其制备方法和用于治疗疾病的用途
公开(公告)号：US09156877B2
公开(公告)日：2015-10-13
申请号：US13386031
申请日：2010-07-07
申请人： Ulrich Klar , Wolfgang Schwede , Carsten Möller , Andrea Rotgeri , Wilhelm Bone
发明人： Ulrich Klar , Wolfgang Schwede , Carsten Möller , Andrea Rotgeri , Wilhelm Bone
IPC分类号： A61K31/58 , A61K31/567 , C07J1/00 , C07J21/00 , C07J41/00 , C07J43/00
CPC分类号： C07J1/0033 , C07J1/0085 , C07J21/006 , C07J41/0094 , C07J43/003
摘要： The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-benzylidene derivatives of the formula I, in which Y and X are each as defined in the claims and the description, to a process for preparation thereof and to the use thereof as medicaments.
摘要翻译：本发明涉及式I的17-羟基-17-五氟乙基雌-4,9（10） - 二烯11-亚苄基衍生物，其中Y和X各自如权利要求书和描述中所定义，与制备方法以及作为药物的用途。

56. 发明授权

US09102701B2 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-diene-11-ethynylphenyl derivatives, methods for the production thereof and use thereof for treating diseases 有权
标题翻译： 17-羟基-17-五氟乙基 - 雌-4,9（10） - 二烯-11-乙炔基苯基衍生物，其制备方法和用于治疗疾病的用途
公开(公告)号：US09102701B2
公开(公告)日：2015-08-11
申请号：US13386420
申请日：2010-07-08
申请人： Ulrich Klar , Wolfgang Schwede , Carsten Möller , Andrea Rotgeri , Wilhelm Bone
发明人： Ulrich Klar , Wolfgang Schwede , Carsten Möller , Andrea Rotgeri , Wilhelm Bone
IPC分类号： A61K31/58 , A61K31/567 , C07J1/00 , C07J21/00 , C07J41/00 , C07J43/00
CPC分类号： C07J1/0081 , C07J1/0037 , C07J21/006 , C07J41/0083 , C07J41/0094 , C07J43/003
摘要： The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-ethynylphenyl derivatives of the formula I, in which R1 and X are each as defined in the claims and the description, and to a process for preparation thereof and to the use thereof as medicaments.
摘要翻译：本发明涉及式I的17-羟基-17-五氟乙基雌-4,9（10） - 二烯11-乙炔基苯基衍生物，其中R 1和X各自如权利要求和说明书所定义，其制备方法及其作为药物的用途。

57. 发明授权

US09096640B2 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-diene-11-methylene oxyalkylene aryl derivatives, process for preparation thereof, and use thereof for treatment of diseases 有权
标题翻译： 17-羟基-17-五氟乙基 - 雌-4,9（10） - 二烯-11-亚甲基氧亚烷基芳基衍生物，其制备方法及其用于治疗疾病的用途
公开(公告)号：US09096640B2
公开(公告)日：2015-08-04
申请号：US13384765
申请日：2010-07-07
申请人： Ulrich Klar , Wolfgang Schwede , Carsten Möller , Andrea Rotgeri , Wilhelm Bone
发明人： Ulrich Klar , Wolfgang Schwede , Carsten Möller , Andrea Rotgeri , Wilhelm Bone
IPC分类号： A61K31/567 , C07J1/00 , C07J7/00 , C07J41/00 , C07J43/00 , A61K31/573
CPC分类号： C07J1/0081 , A61K31/573 , C07J7/0085 , C07J41/0083 , C07J41/0094 , C07J43/003
摘要： The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene-11-methyleneoxyalkylenearyl derivative of the formula I with progesterone-antagonising action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.
摘要翻译：本发明涉及具有孕酮拮抗作用的式I的17-羟基-17-五氟乙基雌-4,9（10） - 二烯-11-亚甲基氧亚烷基壬基衍生物及其制备方法，用于治疗和/或预防的疾病和用于生产用于治疗和/或预防疾病，特别是子宫肌瘤（肌瘤，子宫平滑肌瘤），子宫内膜异位症，重度月经出血，脑膜瘤，激素依赖性乳腺癌和与更年期，或生育控制和紧急避孕。

58. 发明授权

US09085603B2 Progesterone receptor antagonists 有权
标题翻译：孕激素受体拮抗剂
公开(公告)号：US09085603B2
公开(公告)日：2015-07-21
申请号：US13577799
申请日：2011-02-08
申请人： Wolfgang Schwede , Ulrich Klar , Carsten Möller , Andrea Rotgeri , Wilhelm Bone , Christoph Huwe
发明人： Wolfgang Schwede , Ulrich Klar , Carsten Möller , Andrea Rotgeri , Wilhelm Bone , Christoph Huwe
IPC分类号： A61K31/58 , A61K31/567 , C07J1/00 , C07J43/00 , C07J41/00 , A61K31/573
CPC分类号： C07J43/003 , A61K31/573 , A61K31/58 , C07J41/0083
摘要： The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of the formula I with a progesterone antagonizing effect and processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and also their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular of uterus fibroids (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeding, meningiomas, hormone-dependent breast cancers and troubles associated with the menopause or for monitoring fertility and emergency contraception.
摘要翻译：本发明涉及具有孕酮拮抗作用的式I的17-羟基-17-五氟乙基 - 雌-4,9（10） - 二烯-11-芳基衍生物及其制备方法及其用于治疗和/或疾病的预防及其用于治疗和/或预防疾病，特别是子宫肌瘤（肌瘤，子宫平滑肌瘤），子宫内膜异位症，重度月经出血，脑膜瘤，激素依赖性乳腺癌和与更年期或监测生育和紧急避孕。

59. 发明申请

US20120232042A1 17-HYDROXY-17-PENTAFLUORETHYL-ESTRA-4,9(10)-DIEN-11-ACYLOXYALKYLENE PHENYL DERIVATIVES, METHODS FOR THE PRODUCTION THEREOF AND USE THEREOF FOR TREATING DISEASES 有权
标题翻译： 17-羟基-17-二芳基-ESTRA-4,9（10）-DIEN-11-氰基亚甲基苯衍生物，其生产方法及其用于治疗疾病
公开(公告)号：US20120232042A1
公开(公告)日：2012-09-13
申请号：US13384332
申请日：2010-07-07
申请人： Ulrich Klar , Wolfgang Schwede , Carsten Moller , Andrea Rotgeri , Ursula Krenz
发明人： Ulrich Klar , Wolfgang Schwede , Carsten Moller , Andrea Rotgeri , Ursula Krenz
IPC分类号： A61K31/57 , C07J43/00 , A61P15/18 , A61P15/00 , A61P35/00 , A61P15/08 , C07J7/00 , A61K31/58
CPC分类号： C07J1/0081 , A61K31/573 , A61K31/58 , C07J7/0085 , C07J41/0044 , C07J41/0083 , C07J43/003
摘要： The invention relates to 17-hydroxy-13-methyl-17-pentafluoroethyl-11-acyloxyalkylenephenyldodecahydrocyclopenta[a]phenanthren-3-one derivatives of the formula I with progesterone-antagonising action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.
摘要翻译：本发明涉及式I的17-羟基-13-甲基-17-五氟乙基-11-酰氧基亚烷基十一烷基十氢环戊并[a]菲-3-酮衍生物与孕酮拮抗作用及其制备方法，用于治疗和（或肌瘤，子宫平滑肌瘤），子宫内膜异位症，重度月经出血，脑膜瘤，荷尔蒙依赖性乳腺癌等的病症的治疗和/或预防用药物，以及与绝经相关的投诉，或生育控制和紧急避孕。

60. 发明授权

US07700621B2 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations 失效
公开(公告)号：US07700621B2
公开(公告)日：2010-04-20
申请号：US11214988
申请日：2005-08-31
申请人： Ulrich Klar , Wolfgang Schwede , Werner Skuballa , Bernd Buchmann , Jens Hoffmann , Rosemarie Lichtner
发明人： Ulrich Klar , Wolfgang Schwede , Werner Skuballa , Bernd Buchmann , Jens Hoffmann , Rosemarie Lichtner
IPC分类号： A01N43/42 , A01N43/78 , C07D417/00
CPC分类号： C07D493/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14
摘要： This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.

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