公开(公告)号：EP2456783A2

公开(公告)日：2012-05-30

申请号：EP10732868.4

申请日：2010-07-08

申请人： Bayer Pharma Aktiengesellschaft

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

IPC分类号： C07J7/00

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-pentafluorethyl-estra-4,9(10)-dien-11-ethyinylphenyl derivatives of formula (I), wherein R
1 and X are defined as in the claims and in the description, to a method for the production thereof and to the use thereof as medicaments.

公开(公告)号：EP2456782A2

公开(公告)日：2012-05-30

申请号：EP10731477.5

申请日：2010-07-07

申请人： Bayer Pharma Aktiengesellschaft

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

IPC分类号： C07J7/00

CPC分类号： C07J1/0033 ,  C07J1/0085 ,  C07J21/006 ,  C07J41/0094 ,  C07J43/003

摘要： The invention relates to 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-ethyinylphenyl derivatives of formula (I), wherein Y and X are defined as in the claims and in the description, to a method for the production thereof and to the use thereof as medicaments.

公开(公告)号：EP3384914A1

公开(公告)日：2018-10-10

申请号：EP18164909.6

申请日：2018-03-29

申请人： Bayer Pharma Aktiengesellschaft

发明人： SCHULTZE-MOSGAU, Marcus-Hillert ,  CHANG, Xinying ,  SEITZ, Christian ,  MÖLLER, Carsten

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 and gynaecological diseases in particular Endometriosis or Uterine Fibroids (UF), as a sole agent or in combination with other active ingredients wherein circulating endogenous estradiol 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：EP2432798A2

公开(公告)日：2012-03-28

申请号：EP10735198.3

申请日：2010-07-07

申请人： Bayer Pharma Aktiengesellschaft

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

IPC分类号： C07J31/00 ,  C07J41/00 ,  A61K31/567 ,  A61P5/36

CPC分类号： A61K31/567 ,  A61K31/573 ,  C07J31/006 ,  C07J41/0083

摘要： The invention relates to 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl derivatives of formula (I) exhibiting progesterone-antagonistic effects and to methods for the production thereof, to the use thereof for the treatment and/or prophylaxis of diseases and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases, in particular uterine fibroids (myomas, uterine leiomyomas), endometriosis, menorrhagia, meningiomas, hormone-dependent mammary carcinomas and menopause-associated troubles, or for fertility control and emergency contraception.

公开(公告)号：EP2456780A2

公开(公告)日：2012-05-30

申请号：EP10730103.8

申请日：2010-07-08

申请人： Bayer Pharma Aktiengesellschaft

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

IPC分类号： C07J7/00

CPC分类号： C07J1/0081 ,  C07J21/006 ,  C07J41/0044 ,  C07J41/0094 ,  C07J43/003

摘要： The invention relates to 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl derivatives of formula (I) exhibiting progesterone-antagonistic effects and to methods for the production thereof, to the use thereof for the treatment and/or prophylaxis of diseases and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases, in particular uterine fibroids (myomas, uterine leiomyomas), endometriosis, menorrhagia, meningiomas, hormone-dependent mammary carcinomas and menopause-associated troubles, or for fertility control and emergency contraception.

摘要翻译： 本发明涉及17-羟基-17- pentafluoroethylestra -4,9（10）二烯类式I与孕酮拮抗作用，并为制备方法及其11 - 芳基衍生物，及其用于治疗和/或预防 疾病和涉及其用于生产药物用于治疗和/或预防疾病，爱的尤其是子宫的肌瘤（肌瘤，子宫平滑肌瘤），子宫内膜异位，月经出血，脑膜瘤，与相关联的激素依赖性乳腺癌和投诉 绝经，或生育控制和紧急避孕。

公开(公告)号：EP2456781A2

公开(公告)日：2012-05-30

申请号：EP10730384.4

申请日：2010-07-07

申请人： Bayer Pharma Aktiengesellschaft

发明人： KLAR, Ulrich ,  SCHWEDE, Wolfgang ,  MÖLLER, Carsten ,  ROTGERI, Andrea ,  KRENZ, Ursula

IPC分类号： C07J7/00

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-pentafluorethyl-11-acyloxyalkylenephenyl-dodecahydro-cyclopenta[a]phenanthrene-3-on derivatives of formula (I) exhibiting progesterone-antagonistic effects and to methods for the production thereof, to the use thereof for the treatment and/or prophylaxis of diseases and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases, in particular uterine fibroids (myomas, uterine leiomyomas), endometriosis, menorrhagia, meningiomas, hormone-dependent mammary carcinomas and menopause-associated troubles, or for fertility control and emergency contraception.

公开(公告)号：EP2456779A2

公开(公告)日：2012-05-30

申请号：EP10739294.6

申请日：2010-07-07

申请人： Bayer Pharma Aktiengesellschaft

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

IPC分类号： C07J1/00

CPC分类号： C07J1/0081 ,  A61K31/573 ,  C07J7/0085 ,  C07J41/0083 ,  C07J41/0094 ,  C07J43/003

摘要： The invention relates to a 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11methylene oxyalkylene aryl derivative of formula (I) exhibiting progesterone-antagonistic effects and to methods for the production thereof, to the use thereof for the treatment and/or prophylaxis of diseases and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases, in particular uterine fibroids (myomas, uterine leiomyomas), endometriosis, menorrhagia, meningiomas, hormone-dependent mammary carcinomas and menopause-associated troubles, or for fertility control and emergency contraception.