Non-steroidal progesterone receptor modulators

被引:0
|
作者
Zhang, PW
Fensome, A
Wrobel, J
Winneker, R
Zhang, ZM
机构
[1] Wyeth Ayerst Res, Chem & Screening Sci, Collegeville, PA 19426 USA
[2] Wyeth Ayerst Res, Womens Hlth Res Inst, Collegeville, PA 19426 USA
关键词
contraception; endometriosis; hormone therapy; progesterone receptor (PR); PR agonists; PR antagonists; uterine fibroids;
D O I
10.1517/eotp.13.12.1839.22905
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Progesterone (P-4) plays an essential role in female reproduction and progesterone receptor (PR) agonists have been used in female contraceptives and in postmenopausal hormone therapy. Recent studies in women and non-human primates show that PR antagonists may also have potential as contraceptive agents and for the treatment of various gynaecological and obstetric diseases, including fibroids, endometriosis and, possibly, hormone-dependent cancers. Clinically available PR agonists and antagonists are steroidal compounds and often cause various side effects due to their functional interaction with other steroid receptors. Recently, numerous receptor-selective nonsteroidal PR agonists and antagonists have emerged. This patent review will focus on the latest developments in these areas (since 2000).
引用
收藏
页码:1839 / 1847
页数:9
相关论文
共 50 条
  • [1] Non-steroidal steroid receptor modulators
    Buijsman, RC
    Hermkens, PHH
    van Rijn, RD
    Stock, HT
    Teerhuis, NM
    [J]. CURRENT MEDICINAL CHEMISTRY, 2005, 12 (09) : 1017 - 1075
  • [2] Non-steroidal steroid receptor modulators
    Hermekns, PHH
    Kamp, S
    Lusher, S
    Veeneman, GH
    [J]. IDRUGS, 2006, 9 (07) : 488 - 494
  • [3] 5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators
    Kern, Jeffrey C.
    Terefenko, Eugene
    Trybulski, Eugene
    Berrodin, Thomas J.
    Cohen, Jeffrey
    Winneker, Richard C.
    Yudt, Matthew R.
    Zhang, Zhiming
    Zhu, Yuan
    Zhang, Puwen
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (23) : 6666 - 6669
  • [4] Non-steroidal progesterone receptor specific ligands
    Allan, GF
    Sui, Z
    [J]. MINI-REVIEWS IN MEDICINAL CHEMISTRY, 2005, 5 (08) : 701 - 708
  • [5] MEDI 18-Next-generation contraceptives: The discovery of non-steroidal progesterone receptor modulators
    Fensome, Andrew
    Adams, Andrea
    Adams, William
    Bender, Reinhold
    Berrodin, Thomas
    Chopra, Rajiv
    Cohen, Jeff
    Collins, Mark A.
    Deng, Lin
    Fletcher, Horace, III
    Gallucci, Phyllis
    Hudak, Valerie
    Huselton, Christine
    Lockhead, Susan
    Malakianl, Karl
    Marella, Michael
    Melenski, Edward
    McComas, Casey C.
    Mugford, Cheryl
    Norlund, Layne
    Olland, Andrea
    Ruble, David
    Russo, Louise
    Slayden, Ov
    Svenson, Kristine
    Terefenko, Eugene A.
    Unwalla, Raymond
    Wang, Jianyao
    Wilhelm, James
    Wolfrom, Scott
    Yates, David
    Yudt, Matthew
    Zhang, Zhiming
    Zhang, Puwen
    Winneker, Richard C.
    Wrobel, Jay
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2007, 234
  • [6] Novel class of non-steroidal progesterone receptor antagonists
    Zhi, L
    Marschke, KB
    [J]. EXPERT OPINION ON THERAPEUTIC PATENTS, 1999, 9 (06) : 695 - 700
  • [7] Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators
    Ray, Nicholas C.
    Clark, Robin D.
    Clark, David E.
    Williams, Karen
    Hickin, H. G.
    Crackett, Peter H.
    Dyke, Hazel J.
    Lockey, Peter M.
    Wong, Melanie
    Devos, Rene
    White, Anne
    Belanoff, Joseph K.
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (17) : 4901 - 4905
  • [8] Dissociated non-steroidal glucocorticoid receptor modulators:: an update on new compounds
    Schacke, Heike
    Berger, Markus
    Hansson, Thomas G.
    McKerrecher, Darren
    Rehwinkel, Hartmut
    [J]. EXPERT OPINION ON THERAPEUTIC PATENTS, 2008, 18 (03) : 339 - 352
  • [9] SARM harm: Are non-steroidal selective adrenergic receptor modulators as safe as they claim?
    Flores, J.
    Chitturi, S.
    Walker, S.
    [J]. JOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY, 2019, 34 : 99 - 100
  • [10] The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation
    Edman, Karl
    Ahlgren, Ragnhild
    Bengtsson, Malena
    Bladh, Hakan
    Backstrom, Stefan
    Dahmen, Jan
    Henriksson, Krister
    Hillertz, Per
    Hulikal, Vijakumar
    Jerre, Anders
    Kinchin, Liz
    Kase, Charlotte
    Lepisto, Matti
    Mile, Irene
    Nilsson, Stinabritt
    Smailagic, Amir
    Taylor, John
    Tjornebo, Ann
    Wissler, Lisa
    Hansson, Thomas
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2014, 24 (11) : 2571 - 2577