专利号:US-7667056-B2 优先权日:2002-08-02 标 题 :Process and new intermediates for the preparation of steroids with a progestogen activity 发明人:GRISENTI PARIDE; PECORA FABIO; VERZA ELISA; LEONI MASSIMO; BOSSI LAURA 权利人:POLI IND CHIMICA SPA 摘要:The present invention relates to a new process of synthesis and to some new intermediates for the preparation of steroids with progestogen activity, more particularly, for the preparation of Desogestrel of formula (I). Said process is characterized by the regioselective reduction of the compound of formula (II) to give the intermediate of formula (III).
专利号:US-6225298-B1 优先权日:1994-11-22 标 题 :Compositions and methods for contraception and for treatment of benign gynecological disorders 发明人:SPICER DARCY V; PIKE MALCOLM CECIL; DANIELS JOHN R 权利人:BALANCE PHARMACEUTICALS INC 摘要:Compositions and methods for use in preventing conception or treating benign gynecological disorders, wherein an effective amount of an antiprogestational agent [e.g., progesterone (progestin, progestogen, gestagen) antagonist or progesterone synthesis inhibitor] administered over a first period of time is combined with an effective amount of a progestogen for a second period of time. The antiprogestational agent is selected from single agents or mixtures thereof. The progestogen is selected from single agents or mixtures of natural or synthetic progestogens. The formulations are effective as contraceptive agents and for treatment of benign gynecological disorders including uterine fibroids, premenstrual syndrome, dysfunctional uterine bleeding, polycystic ovarian syndrome and endometriosis.
专利号:US-2008234340-A1 优先权日:2007-03-09 标 题:Synthesis and characterization of polymorph form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-YL)thiazol-4-YL)benzonitrile 发明人:MIRMEHRABI MAHMOUD; NIU YUPING; TADAYON ABDOLSAMAD; DESHMUKH SUBODH; KU MANNCHING SHERRY 权利人:WYETH CORP 摘要:A polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form II are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. n Further provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.
专利号:US-2008249148-A1 优先权日:2007-03-09 标题:Synthesis and characterization of polymorph form III 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile 发明人:MIRMEHRABI MAHMOUD; TADAYON ABDOLSAMAD; DESHMUKH SUBODH 权利人:WYETH CORP 摘要:A polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form III are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. n Also provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.
专利号:EP-1586579-B1 优先权日:2004-03-08 标 题:Process for the preparation of delta(15-16)-17-ketosteroids and use thereof in the synthesis of pharmacologically active compounds 发明人:GRISENTI PARIDE; REZA HELAI SHARZAD; PENGO DANIELE 权利人:EUTICALS SPA
专利号:US-2001016578-A1 优先权日:1997-06-18 标 题 :Compositions and methods for contraception and for treatment of benign gynecological disorders 发明人:SPICER DARCY V; PIKE MALCOLM CECIL; DANIELS JOHN R 权利人:BALANCE PHARMACEUTICALS INC 摘要:Compositions and methods for use in preventing conception or treating benign gynecological disorders, wherein an effective amount of an antiprogestational agent [e.g., progesterone (progestin, progestogen, gestagen) antagonist or progesterone synthesis inhibitor] administered over a first period of time is combined with an effective amount of a progestogen for a second period of time. The antiprogestational agent is selected from single agents or mixtures thereof. The progestogen is selected from single agents or mixtures of natural or synthetic progestogens. The formulations are effective as contraceptive agents and for treatment of benign gynecological disorders including uterine fibroids, premenstrual syndrome, dysfunctional uterine bleeding, polycystic ovarian syndrome and endometriosis.
1: Waellnitz K, Duijkers I, Klipping C, Rautenberg T, Rohde B, Zurth C. A two-centre, open-label, randomised study of ovulation inhibition with three transdermal contraceptive patches, each containing different amounts of ethinyl estradiol and gestodene in healthy, young women. J Obstet Gynaecol. 2016 Jan;36(1):106-13. doi: 10.3109/01443615.2015.1041882. Epub 2015 Sep 30. doi: 10.1007/s13318-014-0215-8. Epub 2014 Jul 6. doi: 10.5414/CP202085. doi: 10.1016/j.contraception.2014.04.018. Epub 2014 May 20. doi: 10.1016/j.contraception.2013.12.003. Epub 2013 Dec 19. Review. Chinese. doi: 10.2217/whe.13.71. doi: 10.1016/j.jchromb.2013.12.003. Epub 2013 Dec 8. doi: 10.1007/s40268-013-0028-2. 10: Jaithitivit L, Jaisamrarn U, Taneepanichskul S. Cycle control, safety and acceptability of a new oral contraceptive containing ethinylestradiol 15 micrograms and gestodene 60 micrograms. J Med Assoc Thai. 2012 May;95(5):630-5. doi: 10.1016/j.contraception.2009.12.014. Epub 2010 Jan 27. doi: 10.1002/bmc.1265. Chinese. doi: 10.1007/s00404-008-0907-x. Epub 2009 Jan 6. doi: 10.1016/j.ijpharm.2009.05.017. Epub 2009 May 20. Epub 2007 Feb 20. Bulgarian.
合成参考文献
参考文献:10.3109/13625187.2011.591217 摘要:Rebelo AC, Tamburús N, Salviati M, Celante V, Takahashi A, de Sá MF, Catai A, Silva E. Influence of third-generation oral contraceptives on the complexity analysis and symbolic dynamics of heart rate variability. The European Journal of Contraception & Reproductive Health Care. 2011 Jul 20;16(4):289–97. doi: 10.3109/13625187.2011.591217.