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(12) United States Patent (10) Patent No.: US 9,561.238 B2 Coelingh Bennink Et Al

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(12) United States Patent (10) Patent No.: US 9,561.238 B2 Coelingh Bennink Et Al USOO956 1238B2 (12) United States Patent (10) Patent No.: US 9,561.238 B2 Coelingh Bennink et al. (45) Date of Patent: *Feb. 7, 2017 (54) PHARMACEUTICAL COMPOSITIONS 5,827,843. A 10, 1998 Koninckx et al. COMPRISING ESTETROL DERVATIVES (Continued) FOR USE IN CANCER THERAPY FOREIGN PATENT DOCUMENTS (71) Applicant: Donesta Bioscience B. V. Zeist (NL) DE 23 36 434 A1 4, 1975 (72) Inventors: Herman Jan Tijmen Coelingh DE 24, 26 779 A1 12/1975 Bennink, Zeist (NL); Evert Johannes (Continued) Bunschoten, Heesch (NL) OTHER PUBLICATIONS (73) Assignee: Donesta Bioscience B.V., Zeist (NL) al-AZZawi, F. Estrogen and Colon Cancer: Current Issues, Climac (*) Notice: Subject to any disclaimer, the term of this teric May 2002, PubMed, retrieved from the Internet: <URL:http:// patent is extended or adjusted under 35 www.ncbi.nlm.nih.gov/pubmed/11974.557, 1 page. Albertazzi Paola et al., “The Effect of Tibolone Versus Continuous U.S.C. 154(b) by 0 days. Combined Norethisterone Acetate and Oestradiol on Memory, This patent is Subject to a terminal dis Libido and Mood of Postmenopausal Women: A Pilot study”. Database Biosis 'Online; Oct. 31, 2000; pp. 223-229; vol. 36, No. claimer. 3: Biosciences Information Service, Philadelphia, PA., U.S. Ali-AZZawi, et al. “Estrogen and colon cancer: current issues'. (21) Appl. No.: 14/621,267 CLIMACTERIC, 2002, vol. 5, pp. 3-14. Allen et al. An Ovarian Hormone Preliminary Report on Its (22) Filed: Feb. 12, 2015 Localization, Extraction and Partial Purification and Action in Test Animals, Jour. A.M.A., Sep. 8, 1923, pp. 819-821, vol. 81, No. 10. (65) Prior Publication Data (Continued) US 2015/O150887 A1 Jun. 4, 2015 Primary Examiner — John Pak Assistant Examiner — Andriae M Holt Related U.S. Application Data (74) Attorney, Agent, or Firm — Foley & Lardner LLP: Sunit Talapatra (63) Continuation of application No. 10/532,320, filed as application No. PCT/NL03/00718 on Oct. 23, 2003, (57) ABSTRACT now Pat. No. 8,987,240. The present invention relates to a method of treating or preventing estrogen-suppressed tumors in a mammal, said (30) Foreign Application Priority Data method comprising the administration of a therapeutically effective amount of an estrogenic component to said mam Oct. 23, 2002 (EP) ..................................... O2O79414 mal, wherein the estrogenic component is selected from the group consisting of (51) Int. Cl. substances represented by the following formula A6 IK3I/S65 (2006.01) A6 IK 45/06 (2006.01) (52) U.S. Cl. OH CPC ............. A61 K3I/565 (2013.01); A61K 45/06 OH (2013.01) (58) Field of Classification Search CPC .............................. A61K 3 1/565; A61K 45/06 See application file for complete search history. OH (56) References Cited U.S. PATENT DOCUMENTS 3,440,320 A 4, 1969 Sackler et al. 3,797.494. A 3, 1974 Zaffaroni 4,460.372 A 7/1984 Campbell et al. 4,573.996 A 3, 1986 Kwiatek et al. in which formula R. R. R. R. independently are a hydro 4,624,665 A 11/1986 Nuwayser 4,722,941 A 2f1988 Eckert et al. gen atom, a hydroxyl group or an alkoxy group with 1-5 4,762,717 A 8/1988 Crowley, Jr. carbon atoms; precursors capable of liberating a Substance 4.937,238 A 6, 1990 Lemon according to the aforementioned formula when used in the 5,063,507 A 11/1991 Lindsey et al. present method; and mixtures of one or more of the afore 5,130,137 A 7/1992 Crowley, Jr. mentioned substances and/or precursors. 5,211,952 A 5/1993 Spicer et al. 5,223,261 A 6, 1993 Nelson et al. The estrogenic component according to the invention is 5,340,584 A 8/1994 Spicer et al. particularly useful in the treatment or prevention of colorec 5,340,585 A 8, 1994 Pike et al. tal and prostate cancer and, unlike commonly used estro 5,340,586 A 8, 1994 Pike et al. gens, does not simultaneously enhance the risk of estrogen 5,468,736 A 11/1995 Hodgen stimulated cancers such as breast cancer. 5,633,242 A 5, 1997 Oettel et al. 5,662.927 A 9, 1997 Ehrlich et al. 16 Claims, 1 Drawing Sheet US 9,561.238 B2 Page 2 (56) References Cited <URL: www.emedicinehealth.com/script/main/art. asp?articlekey=58782&pf=3&page=2 10 pages. U.S. PATENT DOCUMENTS Corbishley et al., Androgen Receptor in Human Normal and Malig nant Pancreas and Cell Lines, XP-009025474, Abstracts of the First 6,214,815 B1 4/2001 Shangold et al. 6,291,456 B1 9, 2001 Stein et al. International Conference of Anticancer Research, Oct. 26-30, 1985, 6,500,814 B1 12/2002 Hesch p. 603. 8,048,869 B2 11/2011 Bunschoten et al. Cushing et al., 1998, Obstet. Gynecol., vol. 91, pp. 35-39. 2002fOO13304 A1 1/2002 Wilson et al. Cushing et al., Risk of Endometrial Cancer in Relation to Use of 2002.0156059 A1 10, 2002 Elliesen Low-Dose, Unopposed Estrogens, Estrogen and Endometrial Can 2002fO183299 A1 12/2002 Voskuhl cer, Jan. 1998, pp. 35-39, vol. 91, No. 1. 2003,0008012 A1 1/2003 Pena et al. De Visser et al., Endocrinological Studies with (7a, 17 a)-17 2003/0203933 A1 10/2003 Lee et al. Hydroxy-7-me norgregn-5(10-en-20-yn-3-one (Org OD 14), 2004/O192598 A1 9/2004 Kragie 2006, O247221 A1 11/2006 Coelingh Bennink et al. Arzneim. Forsh., vol. 34, pp. 1010-1020, (1984). Definition of Prevent, online. Merriam-Webster Online Diction ary, 2006, retrieved on Aug. 18, 2009). Retrieved from the Internet: FOREIGN PATENT DOCUMENTS <URL:http://web.archive.org/web/20060518124943/http://mer EP O 402 950 A 12/1990 riam-Webster.com/dictionary prevent>, 1 page. EP O 468 690 A1 1, 1992 Elger et al., Sulfamates of Various Estrogens are Prodrugs with EP 1 112 O114 A2 8, 2001 Increased Systemic and Reduced Hepatic Estrogenicity at Oral WO WO-92, 18107 A1 10, 1992 Application, J. Steroid Biochem, Molec. Biol. 1995, vol. 55, No. WO WO-93,09771 5, 1993 WO WO-94,262O7 11, 1994 3/4, pp. 395-403. WO WO-95.02408 A1 1, 1995 Erdbruegger et al., Drug Discovery Today: Disease Mechanisms WO WO-95, 17895 7, 1995 (2004), vol. 1, pp. 73-81. WO WO-96,03929 A1 2, 1996 Estrogens in the Treatment of Advanced Prostate Cancer, online). WO WO-98.58657 A1 12, 1998 Phoenix 5, CIHF, 1995, retrieved on Mar. 13, 2011. Retrieved WO WO-00,73416 A1 12/2000 from the Internet: <URL:http://www.phoenix5.org/Infolink/ad WO WO-01/30357 A 5, 2001 vancedestrogen.html>, 2 pages. WO WO-01 32683 A1 5, 2001 WO WO-01f85154 A2 11/2001 Fishman et al., “Fate of 15 a-Hydroxyestriol-3H in Adult Man”. J. WO WO-O2,30355 A2 4/2002 Clin. Endocrinol. Metab., (1970), vol. 31, pp. 436-438. WO WO-O2/O94275 A1 11, 2002 Fogary, Jr., “Postmaturity”. J. Am. Osteopath. Assoc., (Jan. 1976), WO WO-02/094276 A1 11, 2002 vol. 75, No. 5, pp. 512-517. WO WO-O2/O94277 A1 11, 2002 Gorwill et al., “Unconjugated Serum Oestriol Levels in Mother and WO WO-02/094278 A1 11, 2002 Baby with Meconium Staining of the Amniotic Fluid'. Br. J. Obstet. WO WO-O2/O94279 A1 11, 2002 WO WO-02/094281 A1 11, 2002 Gynaecol. (Aug. 1978), vol. 85, No. 8, pp. 602-604. WO WO-02/094289 A1 11, 2002 Hammond et al., A Versatile Method for the Determination of Serum Cortisol Binding Globulin and Sex Hormone Binding Globulin Binding Capacities, Clinica Chimica Acta, 1983, vol. 132, pp. OTHER PUBLICATIONS 101-110. Allen et al., The Induction of a Sexually Mature Condition in Heining, et al. “Clinical management of breast cancer in males: a Immature Females by Injection of the Ovarian Follicular Hormone, report of four cases”, European Journal of Obstetrics & Gynecology Washington University School of Medicine, Saint Louis, The and Reproductive Biology, 2002, vol. 102, pp. 67-73. Department of Anatomy, University of Missouri, and the Labora Holinka et al., “Estetrol: A unique steroid in human pregnancy,” J. tories of Biological Chemistry, Saint Louis University School of of Steroid Biochem and Molecular Biol. (2009) 110: 138-143. Medicine, May 16, 1924, pp. 577-587. Holinka et al., Biology of Reproduction, 1980, vol. 22, pp. 913-926. Alvarado-Pisani et al., Thyroid Hormone Receptors in Human Holinka et al., In vivo Effects of Esterol on the Immature Rat Breast Cancer: Effect of the Thyroxine Administration and Interre Uterus, Biology of Reproduction, 1979, pp. 242-246, vol. 20. lation with Sex Hormone Axis, XP-009025474, Abstracts of the Holinka et al., Comparison of Effects of Esterol and Tamoxifen with First International Conference of Anticancer Research, Oct. 26-30, Those of Estriol and Estradiol on the Immature Rat Uterus, Biology 1985, p. 603. of Reproduction, 1980, pp. 913-926, vol. 22. Avvakumov et al., Steroid-binding Specificity of Human Sex Hor Jannson et al., “Estrogen Induces a Potent Suppression of Experi mone-binding Globulin is Influenced by Occupancy of a Zinc mental Autoimmune Encephalomyelitis and Collagen-Induced binding Site. The Journal of Biological Chemistry, 2000, vol. 275, Arthritis in Mice'. Journal of Neuroimmunology, Elsevier Science No. 34, pp. 25920-29525. Publishers BV XX, 1994, vol. 53, No. 2, pp. 203-207. Beattie et al., “The Differential Effects of Diestrous Progestogen Jones, M.S. et al., The Effects of Various Steroids on the Vaginal Administration on Proestrous Gonadotrophin Levels, Endocrinol”. Histology in the Rat, Fertility and Sterility, Apr.
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