Title:
Ｎ置換アゼチジン誘導体
Document Type and Number:
Japanese Patent JP5886873
Kind Code:
B2
Abstract:
The present invention relates to novel N-substituted azetidine derivativesto pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium cancer, ovarian cancer, endometriosis, osteoporosis, prostate cancer, benign prostatic hypertrophy, and breast cancer, in particular ER-positive breast cancer, more in particular ER-positive, hormone treatment-resistant breast cancer. Said N-substituted azetidine derivatives have estrogen receptor alpha (ERα) antagonistic and—in certain embodiments—selective estrogen receptor downregulating (SERD) activity in ER-positive breast cancer cells.
Inventors:
Fredricks Antonius, Daisics
Scottish The Ames, Lusher
Stock, Hermann Teges
Benemann, Gerrit Hermann
Scottish The Ames, Lusher
Stock, Hermann Teges
Benemann, Gerrit Hermann
Application Number:
JP2013545218A
Publication Date:
March 16, 2016
Filing Date:
December 16, 2011
Export Citation:
Assignee:
Merck Sharp End Dome Bf
International Classes:
C07D409/12; A61K31/397; A61K31/41; A61K31/42; A61K31/425; A61K31/4439; A61K31/568; A61P13/08; A61P15/00; A61P19/00; A61P35/00; A61P43/00; C07D205/04; C07D405/12; C07D409/14; C07D413/12; C07D413/14; C07D417/12; C07D417/14; C07J43/00
Domestic Patent References:
| JP2005517731A | ||||
| JP2005506337A |
Foreign References:
| EP1577288A1 | ||||
| WO2009067600A1 | ||||
| US3983245 |
Attorney, Agent or Firm:
Yoshikazu Iwase
Makoto Ono
Kenkyo Kanayama
Mitsuaki Tsubokura
Kazuki Shigemori
Kenji Ando
Yasufumi Shiroyama
Makoto Ono
Kenkyo Kanayama
Mitsuaki Tsubokura
Kazuki Shigemori
Kenji Ando
Yasufumi Shiroyama