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1. 发明授权

US09206219B2 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl derivatives, methods for the production thereof and the 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-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：US09206219B2
公开(公告)日：2015-12-08
申请号：US13386421
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： A61K31/57 , C07J7/00 , C07J1/00 , C07J21/00 , C07J41/00 , C07J43/00
CPC分类号： C07J1/0081 , C07J21/006 , C07J41/0044 , C07J41/0094 , C07J43/003
摘要： The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-aryl derivatives of the formula I with progesterone-antagonizing 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-芳基衍生物及其制备方法，用于治疗和/或预防疾病及其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。

2. 发明授权

US08278469B2 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives, method of production thereof and use thereof for the treatment of diseases 有权
标题翻译： 17-羟基-17-五氟乙基 - 雌-4,9（10） - 二-11-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：US08278469B2
公开(公告)日：2012-10-02
申请号：US13324912
申请日：2011-12-13
申请人： Wolfgang Schwede , Ulrich Klar , Carsten Moller , Andrea Rotgeri , Wilhelm Bone
发明人： Wolfgang Schwede , Ulrich Klar , Carsten Moller , Andrea Rotgeri , Wilhelm Bone
IPC分类号： C07J1/00 , A61K31/56
CPC分类号： A61K31/567 , A61K31/573 , C07J31/006 , C07J41/0083
摘要： The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of Formula I with progesterone antagonizing action and method of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of fibroids of the uterus (myomas, uterine leiomyoma), 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-17-五氟乙基 - 雌-4,9（10） - 二烯-11-芳基衍生物与孕酮拮抗作用及其制备方法，其用途用于治疗和/或预防疾病及其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相关疾病的药物的用途与更年期或生育控制和紧急避孕。

3. 发明授权

US07741333B2 Quinazoline derivatives, their preparation, their use, and medicaments comprising them 失效
标题翻译：喹唑啉衍生物，它们的制备方法，用途和包含它们的药物
公开(公告)号：US07741333B2
公开(公告)日：2010-06-22
申请号：US11766232
申请日：2007-06-21
申请人： Olaf Prien , Knut Eis , Wolfgang Schwede , Judith Guenther , Dieter Zopf , Dominic E. A. Brittain
发明人： Olaf Prien , Knut Eis , Wolfgang Schwede , Judith Guenther , Dieter Zopf , Dominic E. A. Brittain
IPC分类号： A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D513/04 , C07D239/70 , C07D487/04 , C07D491/04 , C07D495/04
摘要： The present invention relates to a quinazoline derivative having the general formula (A): in which R1, R2, X, Y and Z are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).
摘要翻译：本发明涉及具有通式（A）的喹唑啉衍生物：其中R1，R2，X，Y和Z在说明书和权利要求中表示，通式（A）的化合物用于各种病症的治疗，以及通式（A）的化合物的制备。

4. 发明申请

US20090030010A1 3-Amino-pyrazolo[3,4b]pyridines as inhibitors of protein tyrosine kinases, their production and use as pharmaceutical agents 失效
标题翻译： 3-氨基 - 吡唑并[3,4b]吡啶作为蛋白酪氨酸激酶的抑制剂，其生产和用作药剂
公开(公告)号：US20090030010A1
公开(公告)日：2009-01-29
申请号：US11302307
申请日：2005-12-14
申请人： Wolfgang Schwede , Hermann Kuenzer , Antonius Ter Laak , Benjamin Bader , Roman Hillig , Ursula Moenning , Arndt Schmitz , Dieter Zopf
发明人： Wolfgang Schwede , Hermann Kuenzer , Antonius Ter Laak , Benjamin Bader , Roman Hillig , Ursula Moenning , Arndt Schmitz , Dieter Zopf
IPC分类号： A61K31/496 , C07D471/04 , C07D213/78 , A61K31/437
CPC分类号： C07D471/04 , C07D213/85
摘要： This invention relates to compounds of general formula I in which R1 and R2 are described in this application, the use of the compounds of general formula I as inhibitors of protein tyrosine kinases for treatment of various diseases as well as the compounds of general formulas II and III as intermediate compounds for the production of compounds of general formula I, whereby X, R1a and R2a have the meaning that is described in general formulas II and III.
摘要翻译：本发明涉及通式Ⅰ化合物，其中本申请中描述了R1和R2，通式I化合物用作蛋白酪氨酸激酶抑制剂用于治疗各种疾病以及通式II和 III为制备通式I化合物的中间体化合物，其中X，R 1a和R 2a具有通式II和III所述的含义。

5. 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。

6. 发明申请

US20060252782A1 Sulfoximine-macrocycle compounds and salts thereof, pharmaceutical compositions comprising said compounds, methods of preparing same and uses of same 审中-公开
标题翻译：磺酰亚胺 - 大环化合物及其盐，包含所述化合物的药物组合物，其制备方法及其用途
公开(公告)号：US20060252782A1
公开(公告)日：2006-11-09
申请号：US11399619
申请日：2006-04-07
申请人： Ulrich Luecking , Georg Kettschau , Hans Briem , Wolfgang Schwede , Martina Schaefer , Karl-Heinz Thierauch , Manfred Husemann
发明人： Ulrich Luecking , Georg Kettschau , Hans Briem , Wolfgang Schwede , Martina Schaefer , Karl-Heinz Thierauch , Manfred Husemann
IPC分类号： A61K31/519 , C07D487/14
CPC分类号： C07D209/48 , C07D239/42 , C07D513/08
摘要： The invention relates to macrocyctic sulfoximines of the general Formula I: wherein A, X, Y, R1, R2 and R3 have the meaning as given in the specification and the claims, and to salts thereof; to pharmaceutical compositions comprising the macrocyclic sulfoximines, and to a method of preparing the macrocyclic sulfoximines, as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with angiopoietin and therefore influence Tie2 signalling.
摘要翻译：本发明涉及通式I的大环氰基亚砜：其中A，X，Y，R 1，R 2和R 3具有在说明书和权利要求书中给出的含义及其盐; 涉及包含大环亚磺酰亚胺的药物组合物，以及制备大环亚砜亚胺的方法及其制备用于治疗失调血管生长疾病的药物组合物或伴有血管生长失调的疾病的用途，其中该化合物有效地干扰血管生成素，因此影响Tie2信号。

7. 发明授权

US06930102B2 16-halogen-epothilone derivatives, process for their production, 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：US06930102B2
公开(公告)日：2005-08-16
申请号：US10364337
申请日：2003-02-12
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： A61K31/336 , A61K31/427 , A61K31/4427 , A61P35/00 , C07D401/06 , C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07F7/18 , A61K31/395 , C07D269/00
CPC分类号： C07D401/06 , C07D405/06 , C07D417/06 , C07D493/04 , C07D493/08 , C07F7/1804 , Y02P20/55
摘要： A compund of formula I, an epothilone derivative, its method of preparation, and use as a pharmaceutical agent in treating malignant tumors
摘要翻译：式I化合物，埃坡霉素衍生物，其制备方法和用作治疗恶性肿瘤的药物的组合物

8. 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。

9. 发明授权

US5703066A Progestationally active 19,11-bridged 4-estrenes 失效
标题翻译：推荐活跃的19,11桥接4-雌激素
公开(公告)号：US5703066A
公开(公告)日：1997-12-30
申请号：US484318
申请日：1995-06-07
申请人： Eckhard Ottow , Wolfgang Schwede , Wolfgang Halfbrodt , Karl-Heinrich Fritzemeier , Rolf Krattenmacher
发明人： Eckhard Ottow , Wolfgang Schwede , Wolfgang Halfbrodt , Karl-Heinrich Fritzemeier , Rolf Krattenmacher
IPC分类号： A61K31/56 , A61K31/569 , A61K31/57 , A61K31/58 , A61K31/585 , A61P5/34 , A61P13/02 , A61P15/00 , A61P15/18 , C07J53/00 , C07J75/00
CPC分类号： C07J53/002
摘要： In this invention, the new etheno- and ethano-19,11-bridged 4-estrenes of general formula I ##STR1## are described, in which W, R.sup.1, R.sup.2, R.sup.6a, R.sup.6b, R.sup.7, R.sup.14, R.sup.15, R.sup.16, R.sup.11, R.sup.11' and R.sup.19 have the meaning indicated in the description, as well as a process for their production. The new compounds have strong progestational activity and are suitable for the production of pharmaceutical agents.
摘要翻译：在本发明中，描述了通式I（I）的新的乙烯 - 和乙酰基-19,11-桥接的4-雌酮，其中W，R 1，R 2，R 6a，R 6b，R 7，R 14，R 15， R16，R11，R11'和R19具有说明书中指出的含义，以及其制备方法。新化合物具有强烈的促孕活性，适用于制药。

10. 发明授权

US5426102A 14.beta.-H-, 14-and 15-En-11.beta.-aryl-4-oestrenes 失效
标题翻译： 14β-H，14和15-En-11β-芳基-4-盎司
公开(公告)号：US5426102A
公开(公告)日：1995-06-20
申请号：US81269
申请日：1993-06-22
申请人： Wolfgang Schwede , Eckhard Ottow , Gunter Neef , Arwed Cleve , Krzysztof Chwalisz , Horst Michna
发明人： Wolfgang Schwede , Eckhard Ottow , Gunter Neef , Arwed Cleve , Krzysztof Chwalisz , Horst Michna
IPC分类号： A61K31/57 , A61K31/58 , A61K31/585 , A61P5/38 , C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J17/00 , C07J21/00 , C07J33/00 , C07J41/00 , C07J43/00
CPC分类号： C07J1/0092 , C07J1/0088 , C07J1/0096 , C07J17/00 , C07J33/002 , C07J41/0094 , C07J43/003 , C07J9/00
摘要： Novel compounds of the general formula I ##STR1## and the pharmacologically tolerable addition salts thereof with acids are described, in which eitherIa) R.sup.11 represents a hydrogen atom in the .beta.-configuration and each of R.sup.12 and R.sup.13 represents a hydrogen atom, orIb) R.sup.11 represents a hydrogen atom in the .beta.-configuration and R.sup.12 and R.sup.13 together represent a second bond, orIc) R.sup.11 and R.sup.12 together represent a second bond and R.sup.13 represents a hydrogen atom, orId) R.sup.11 represents a hydrogen atom in the .alpha.-configuration and R.sup.12 and R.sup.13 together represent a second bond,and in Ia), Ib), Ic) or Id)X represents an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 represents a hydrogen atom or a methyl group,R.sup.2 represents a hydroxy group, a C.sub.1 -C.sub.10 -alkoxy group or a C.sub.1 -C.sub.10 -acyloxy group, andR.sup.3 and R.sup.4 have the meanings customary for competitive progesterone antagonists specified in the description.The invention relates also to processes for the preparation of the novel compounds, to pharmaceutical compositions containing those compounds, to their use for the manufacture of medicaments, and to the novel intermediates required for the process.The novel compounds have a strong affinity for the gestagen receptor and exhibit pronounced antigestagenic and also antiglucocorticoid, antimineralocorticoid and antiandrogenic properties.
摘要翻译： PCT No.PCT / EP91 / 02494 371日期：1993年6月22日 102（e）日期1993年11月1日PCT 1991年12月21日PCT PCT。出版物WO92 / 11278 描述了通式I的新型化合物（Ⅰ）及其与酸的药理学上可以忍受的加成盐，其中Ia）R11表示β-构型中的氢原子， R 12和R 13表示氢原子，或Ib）R 11表示β构型中的氢原子，R 12和R 13一起表示第二键，或者Ic）R 11和R 12一起表示第二键，R 13表示氢原子，或 Id）R11表示α-构型中的氢原子，R 12和R 13一起表示第二键，并且在Ia），Ib），Ic）或Id）中X表示氧原子，羟基亚氨基> N不同OH或两个氢原子，R 1表示氢原子或甲基，R 2表示羟基，C 1 -C 10 - 烷氧基或C 1 -C 10 - 酰氧基，R 3和R 4具有常规用于在描述。本发明还涉及制备新化合物的方法，含有这些化合物的药物组合物，其用于制备药物的方法以及该方法所需的新型中间体。新化合物对于孕激素受体具有强烈的亲和力，并且具有显着的抗原成分和抗糖皮质激素，抗皮质激素和抗雄激素的特性。

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