公开(公告)号：EP2520301B2

公开(公告)日：2021-03-03

申请号：EP10837927.2

申请日：2010-12-14

发明人： ÁNGELES URIBE, Juan ,  SAVOIR VILBOEUF, John Claude

IPC分类号： A61K9/14 ,  A61K31/565 ,  A61K31/57 ,  A61K9/10 ,  A61P5/34 ,  A61K45/06 ,  A61P5/30

公开(公告)号：EP3384913A1

公开(公告)日：2018-10-10

申请号：EP17164666.4

申请日：2017-04-03

申请人： Bayer Pharma Aktiengesellschaft

发明人： Schultze-Mosgau, Marcus-Hillert

IPC分类号： A61K31/57 ,  A61K38/09 ,  A61K31/505 ,  A61P5/34 ,  A61P15/00 ,  A61P15/12

CPC分类号： A61K31/57 ,  A61K31/505 ,  A61K38/09 ,  A61P5/34 ,  A61P15/00 ,  A61P15/12 ,  A61K2300/00

摘要： The present invention is related to Selective Progesterone Receptor Modulators (SPRM) as described and defined herein, and covers the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of sexual hormone dependent diseases in particular Endometriosis or Uterine Fibroids (UF), as a sole agent or in combination with other active ingredients wherein circulating endogenous estrogen concentration of treated women is maintained to a level in a range of 40 pg/mL to 85 pg/mL.

公开(公告)号：EP3263112A1

公开(公告)日：2018-01-03

申请号：EP17184128.1

申请日：2007-10-24

申请人： Repros Therapeutics Inc.

发明人： PODOLSKI, Joseph S.

IPC分类号： A61K31/56 ,  A61K31/573 ,  A61K45/06 ,  A61K31/57 ,  A61K31/567 ,  A61P5/34 ,  A61P5/36 ,  A61K31/575 ,  A61K9/00

摘要： The subject matter of the instant invention is pertinent to the field of hormone therapy. More specifically, the subject matter of the instant invention concerns methods of treating estrogen-dependent conditions such as endometrial hyperplasia and endometrial cancer in a female undergoing estrogen and/or selective estrogen receptor modulator (SERM) therapy. The instant invention is also relevant to the suppression of endometrial proliferation. The instant invention is also relevant to the treatment of pain associated with endometriosis. The compositions for practicing the methods, comprising progesterone antagonists are also disclosed. Embodiments of the instant invention also disclose methods for identifying new selective progesterone receptor modulators for practicing disclosed methods of treatment.

摘要翻译： 本发明的主题与激素治疗领域有关。 更具体地说，本发明的主题涉及在接受雌激素和/或选择性雌激素受体调节剂（SERM）治疗的女性中治疗雌激素依赖性病症如子宫内膜增生和子宫内膜癌的方法。 本发明也与抑制子宫内膜增殖有关。 本发明还涉及治疗与子宫内膜异位症相关的疼痛。 还公开了用于实践该方法的组合物，其包含孕酮拮抗剂。 本发明的实施方案还公开了鉴定新的选择性黄体酮受体调节剂用于实践所公开的治疗方法的方法。

公开(公告)号：EP3019172A4

公开(公告)日：2017-03-29

申请号：EP14822946

申请日：2014-07-11

申请人： EVESTRA INC

发明人： NICKISCH KLAUS ,  SANTHAMMA BINDU ,  AHMED GULZAR ,  MEECE FREDERICK ,  ELGER WALTER ,  WYRWA RALF ,  NAIR HAREESH

IPC分类号： C07J41/00 ,  A61K31/56 ,  A61K31/568 ,  A61P5/26 ,  A61P5/30 ,  A61P5/34 ,  C07J43/00 ,  C07J51/00

CPC分类号： C07J43/003 ,  C07J41/0072 ,  C07J41/0088 ,  C07J51/00

摘要： Various prodrug compounds having the general structure: Active agent-(acid)-(linker)-SO2NR1R2 are described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.

摘要翻译： 具有一般结构的各种前药化合物在此描述为活性剂 - （酸） - （接头）-SO2NR1R2。 具有这种一般结构的化合物显示出比未修饰的母体分子更具口服活性。

公开(公告)号：EP2925369A1

公开(公告)日：2015-10-07

申请号：EP13811121.6

申请日：2013-11-22

申请人： Altergon S.A.

发明人： BERNAREGGI, Alberto ,  PUPPINI, Nadia ,  NENCIONI, Alessandro

IPC分类号： A61K47/48 ,  A61K9/08 ,  A61K31/568 ,  A61K31/57 ,  A61P15/08 ,  A61P5/34

CPC分类号： A61K47/48969 ,  A61K31/568 ,  A61K31/57 ,  A61K47/6951 ,  B82Y5/00

摘要： The present invention concerns the preparation and the therapeutic use of aqueous solutions of Progesterone or Testosterone, complexed with hydroxypropyl-3-cyclodextrin (HP&bgr;CD) that are suitable for oral administration. The solutions are characterised by a specific molar ratio between HP&bgr;CD and the hormones such as to ensure high hormone plasma levels, following oral administration, thanks to the optimisation of their solubility, permeability, metabolic stability and ultimately, bio availability. The formulation object of the present patent makes it possible to achieve effective plasma concentrations following oral administration of lower doses of hormone with respect to oral formulations currently on the market (e.g. Prometrium, Andriol) to the advantage of greater safety and compliance of the patients.

公开(公告)号：EP2534167B1

公开(公告)日：2014-11-19

申请号：EP11704431.3

申请日：2011-02-08

申请人： Bayer Intellectual Property GmbH

发明人： SCHWEDE, Wolfgang ,  KLAR, Ulrich ,  MÖLLER, Carsten ,  ROTGERI, Andrea ,  BONE, Wilhelm ,  HUWE, Christoph

IPC分类号： C07J41/00 ,  C07J43/00 ,  A61P5/34 ,  A61K31/567

CPC分类号： C07J43/003 ,  A61K31/57 ,  A61K31/58 ,  C07J41/0083

公开(公告)号：EP2520301A4

公开(公告)日：2013-10-23

申请号：EP10837927

申请日：2010-12-14

申请人： TECHSPHERE S A DE CV

发明人： ANGELES URIBE JUAN ,  SAVOIR VILBOEUF JOHN CLAUDE

IPC分类号： A61K31/565 ,  A61K9/16 ,  A61K31/57 ,  A61K45/06 ,  A61P5/30 ,  A61P5/34

CPC分类号： A61K45/06 ,  A61K9/0019 ,  A61K9/10 ,  A61K9/14 ,  A61K9/145 ,  A61K31/565 ,  A61K31/57 ,  A61K2300/00

公开(公告)号：EP2534167A2

公开(公告)日：2012-12-19

申请号：EP11704431.3

申请日：2011-02-08

申请人： Bayer Intellectual Property GmbH

发明人： SCHWEDE, Wolfgang ,  KLAR, Ulrich ,  MÖLLER, Carsten ,  ROTGERI, Andrea ,  BONE, Wilhelm ,  HUWE, Christoph

IPC分类号： C07J41/00 ,  C07J43/00 ,  A61P5/34 ,  A61K31/567

CPC分类号： C07J43/003 ,  A61K31/57 ,  A61K31/58 ,  C07J41/0083

摘要： The invention relates to 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-diene-11-aryl derivatives of formula (I) having an antagonist effect on progesterone, and to a method for the production thereof, to the use thereof for treating and/or preventing illnesses, and to the use thereof for producing medications for treating and/or preventing illnesses, in particular uterine fibroids (myoma, uterine leiomyoma), endometriosis, severe menstrual bleeding, meningioma, hormone-related mamma carcinomas, and disorders associated with menopause, or for fertility control and emergency contraception.

摘要翻译： 本发明涉及对孕酮具有拮抗作用的式（I）的17-羟基-17-五氟乙基 - 雌甾-4,9（10） - 二烯-11-芳基衍生物及其制备方法，涉及 其用于治疗和/或预防疾病，以及其用于生产用于治疗和/或预防疾病的药物，特别是子宫肌瘤（肌瘤，子宫平滑肌瘤），子宫内膜异位症，严重月经出血，脑膜瘤，与激素相关的乳房癌 ，以及与绝经，或生育控制和紧急避孕有关的疾病。

公开(公告)号：EP2170925B1

公开(公告)日：2012-10-24

申请号：EP08758990.9

申请日：2008-06-04

申请人： Bayer Intellectual Property GmbH

发明人： KUHNKE, Joachim ,  HUEBNER, Jan ,  BOHLMANN, Rolf ,  FRENZEL, Thomas ,  KLAR, Ulrich ,  MENGES, Frederik ,  RING, SVEN ,  BORDEN, Steffen ,  MUHN, Hans-Peter ,  PRELLE, Katja

IPC分类号： C07J53/00 ,  C07J41/00 ,  A61K31/56 ,  A61P5/34

CPC分类号： C07J53/008 ,  C07J41/0094 ,  C07J53/007

公开(公告)号：EP2038294B1

公开(公告)日：2010-12-08

申请号：EP07765033.1

申请日：2007-06-29

申请人： Bayer Schering Pharma Aktiengesellschaft

发明人： BOHLMANN, Rolf ,  KUHNKE, Joachim ,  HÜBNER, Jan ,  GALLUS, Norbert ,  MENGES, Frederik ,  BORDEN, Steffen ,  MUHN,Hans-Peter ,  PRELLE, Katja

IPC分类号： C07J53/00 ,  A61K31/58 ,  A61P5/42 ,  A61P5/34

CPC分类号： C07J53/008

摘要： The invention relates to novel 18-methyl-19-nor-androst-4-en-17,17- spiroether of general formula (I), where Z = O, two H, =NOR or =NNHSO2R, R = H, or straight or branched chain C1-4 or C3-4alkyl, R4 = H, halogen, or CF3 and R6 and/or R7 are α- or ß-positioned and R6 and R7 independently = H or straight or branched chain C1-4 or C3-4alkyl or a straight or branched chain C2-4 or C3-4alkylene or a saturated C3-5 cycloalkyl, or together form a methylene group or a double bond. The novel compounds have gestagenic and antimineralcorticoid action.