Progesterone receptor modulator

Selective progesterone receptor modulators (SPRMs, mesoprogestins) are progesterone receptor (PR) ligands... 

The precursor 3 served as a starting material for a series of trisubstituted thiophenes in a study towards progesterone receptor modulators, giving for example the product 4 upon reaction with an appropriate bromoketone. The fact that rather complex thiophene derivatives could be prepared in a straightforward manner compensates for the low overall yields <06JHC1391>. 

Chwalisz K, Garg R, Brenner RM, Schubert G, Eiger W (2002) Selective progesterone receptor modulators (SPRMs) a novel therapeutic concept in endometriosis. Ann NY Acad Sci 955 373-388... 

Olive DL (2002) Role of progesterone antagonists and new selective progesterone receptor modulators in reproductive health. Obstet Gynecol Surv 57 S55-63... 

Spitz IM (2003) Progesterone antagonists and progesterone receptor modulators an overview. Steroids 68 981-993... 

Winneker RC, Fensome A, Wrobel JE, Zhang Z, Zhang P. Nonsteroidal progesterone receptor modulators structure activity relationships. Semin. Reprod. Med. 2005 23 46-57. 

Schubert, G. and Chwalisz, K. (2003) Asoprisnil (J867) a selective progesterone receptor modulator for gynecological therapy. Steroids, 68, 1019-1032. 

Progesterone Receptor Overview of Modern Steroidal Progestins and Developments in the Field of Nonsteroidal Selective Progesterone Receptor Modulators... 

Winneker, R.C., Fensome, A., Wrobel, J.E., Zhang, Z. and Zhang, P. (2005) Nonsteroidal progesterone receptor modulators structure-activity relationships. Seminars in Reproductive Medicine, 23, 46-57. 

Klijn, J.G., Setyono Han, B. and Foekens, J.A. (2000) Progesterone antagonists and progesterone receptor modulators in the treatment of breast cancer. Steroids, 65, 825-830. 

DeManno, D., Eiger, W., Garg, R., Lee, R., Schneider, B., Hess-Stumpp, H., Schubert, G. and Chwalisz, K. (2003) Asoprisnil (J867) a selective progesterone receptor modulator for gynecological therapy. Steroids, 68, 1019-1032. 

Chwalisz, K., Perez, M.C., Demanno, D., Winkel, C., Schubert, G. and Eiger, W. (2005) Selective progesterone receptor modulator development and use in the treatment of leiomyomata and endometriosis. Endocrine Reviews, 26, 423 138. 

Chwalisz, K., Brenner, R.M., Fuhrmann, U.U., Hess Stumpp, H. and Eiger, W. (2000) Antiproliferative effects of progesterone antagonists and progesterone receptor modulators on the endometrium. Steroids, 65, 741-751. 

Chwalisz, K., Eiger, W., Stickler,T., Mattia-Goldberg, C. and Larsen, L. (2005) The effects of one-month administration of asoprisnil (J867), a selective progesterone receptor modulator, in normal women. Human Reproduction, 20, 1090-1099. 

Creinin, M.D., Schlaff, W., Archer, D.F., Wan, L., Frezieres, R., Thomas, M., Rosenberg, M. and Higgins, J. (2006) Progesterone receptor modulator for emergency contraception a randomized controlled trial. Obstetrics and Gynecology, 108, 1089-1097. 

Chwalisz, K., Mattia-Goldberg, K., Lee, M., Eiger, W. and Edmonds, A. (2004) Treatment of endometriosis with the novel selective progesterone receptor modulator (SPRM) asoprisnil. Fertility and Sterility, 82, S83. 

Horne, F.M. and Blithe, D.L. (2007) Progesterone receptor modulators and the endometrium changes and consequences. Human Reproduction Update, 13, 567-580. 

Williams, A.R., Critchley, H.O., Osei, J., Ingamells, S., Cameron, I.T., Han, C. and Chwalisz, K. (2007) The effects of the selective progesterone receptor modulator asoprisnil on the morphology of uterine tissues after 3 months treatment in patients with symptomatic uterine leiomyomata. Human Reproduction, 22, 1696-1704. 

Klaus Schollkopf and Norbert Schmees give an overview of the biology of the progesterone receptor and of the development of research in the field of steroidal progestins and recent trends in discovery of nonsteroidal selective progesterone receptor modulators. 

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