Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
2002-05-23
2010-06-08
Richter, Johann R (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S170000, C514S171000, C514S182000, C514S841000, C514S843000
Reexamination Certificate
active
07732430
ABSTRACT:
A method of contraception in mammalian females, which method comprises the oral administration of an estrogenic component and a progestogenic component to a female of childbearing capability in an amount effective to inhibit ovulation, wherein the estrogenic component is selected from the group consisting of substances represented by the following formula (1)in which R1, R2, R3, R4independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7is a hydroxyl group; and no more than 3 of R1, R2, R3, R4are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors. Another aspect of the invention concerns a pharmaceutical kit comprising oral dosage units that contain the aforementioned estrogenic component and/or a progestogenic component.
REFERENCES:
patent: 3440320 (1969-04-01), Sackler et al.
patent: 3797494 (1974-03-01), Zaffaroni
patent: 4460372 (1984-07-01), Campbell et al.
patent: 4573996 (1986-03-01), Kwiatek et al.
patent: 4624665 (1986-11-01), Nuwayser
patent: 4722941 (1988-02-01), Eckert et al.
patent: 4762717 (1988-08-01), Crowley, Jr.
patent: 4937238 (1990-06-01), Lemon
patent: 5063507 (1991-11-01), Lindsey et al.
patent: 5130137 (1992-07-01), Crowley, Jr.
patent: 5211952 (1993-05-01), Spicer et al.
patent: 5223261 (1993-06-01), Nelson et al.
patent: 5340584 (1994-08-01), Spicer et al.
patent: 5340585 (1994-08-01), Pike et al.
patent: 5340586 (1994-08-01), Pike et al.
patent: 5468736 (1995-11-01), Hodgen
patent: 5633242 (1997-05-01), Oettel et al.
patent: 5662927 (1997-09-01), Ehrlich et al.
patent: 5827843 (1998-10-01), Koninckx
patent: 6214815 (2001-04-01), Shangold et al.
patent: 6500814 (2002-12-01), Hesch
patent: 2002/0183299 (2002-12-01), Voskuhl
patent: 2336433 (1975-04-01), None
patent: 2336434 (1975-04-01), None
patent: 2426779 (1975-12-01), None
patent: 19917930 (2000-10-01), None
patent: 0402950 (1975-12-01), None
patent: 468690 (1991-07-01), None
patent: 1700602 (2001-05-01), None
patent: 9603929 (1966-02-01), None
patent: 9218107 (1992-10-01), None
patent: 9426207 (1994-11-01), None
patent: 9502408 (1995-01-01), None
patent: WO 95/17895 (1995-07-01), None
patent: 9603929 (1996-02-01), None
patent: 9858657 (1998-12-01), None
patent: 0062753 (2000-10-01), None
patent: WO 00/73416 (2000-12-01), None
patent: 0130357 (2001-05-01), None
patent: 0185154 (2001-11-01), None
U.S. Appl. No. 10/495,707, filed Nov. 2004, Coelingh Bennink et al.
Levine et al. (Am. J. Obstet. Gynecol. Mar. 15, 1984, p. 735-738).
Tseng et al. (Journal of Steroid Biochemistry, vol. 9, p. 1145-1128).
Holinka et al. (Biology of Reproduction, 1980, 22, p. 913-926).
Tulchinsky et al., Plasma Estetrol as an Index of Fetal Well-Being, J. Clin. Endocrinol. Metab., 40, 560-567, 1975.
Fishman, Fate of 15 α-Hydroxyestriol-'H in Adult Man, Fishman et al., J. Clin. Endocrinol. Metab., 31, 436-438, 1970.
Levine et al., Uterine Vascular Effects of Estetrol in Nonpregnant Ewes, Am J. Obstet. Gynecol., 148:73, 735-738, 1984.
Jozan et al., Different Effects of Oestradiol, Oestriol, Oestetrol and of Oestrone on Human Breast Cancer Cells (MCF-7) in Long Term Tissue Culture, Acta Endocrinologica, 98, 73-80, 1981.
Holinka et al., In vivo Effects of Estetrol on the Immature Rat Uterus, Biol. Reprod., 22, 913-926, 1980.
Holinka et al., Comparison of Effects of Estetrol and Tamoxifen with Those of Estriol and Estradiol on the Immature Rat Uterus, Biol. Reprod., 20, 242-246, 1979.
Martucci et al., Direction of Estradiol Metabolism as a Control of its Hormonal Action—Uterotrophic Activity of Estradiol Metabolites, Endocrin., 101, 1709-1715, 1977.
Tseng et al., Competition of Estetrol and Ethynylestradiol with Estradiol for Nuclear Binding in Human Endometrium, J. Steroid Biochem., 7, 817-822, 1976.
Martucci et al., Uterine Estrogen Receptor Binding of Catecholestrogens and of Estetrol (1,3,5(10)-Estratriene-3, 15α, 16α 17β-Tetrol), Steroids, 27, 325-333, 1976.
Allen et al., An Ovarian Hormone, JAMA, 81, 819-821, 1923.
Allen et al., The Induction of a Sexually Mature Condition in Immature Females by Injection of the Ovarian Follicular Hormone, Am. J. Physiol., 69, 577-588, 1924.
Jones et al., The Effects of Various Steroids on the Vaginal Histology in the Rat, Fertil. Steril., 24, 284-291, 1973.
Reel et al., Survey and Assessment of Mammalian Estrogen Biological Assays for Hazard Characterization, Fund. Applic. Toxicol., 34, 288-305, 1996.
Kuipers et al., Enterohepatic Circulation in the Rat, Gastroenterol., 88, 403-411, 1985.
Avvakumov et al., Steroid-binding Specificity of Human Sex Hormone-binding Globulin is Influenced by Occupancy of a Zinc-binding Site, J. Biol. Chem., 275, 25920-25925, 2000.
Schwartz, A Model for the Regulation of Ovulation in the Rat, Recent Prog. Horm. Res., 25, 1-55, 1969.
Beattie et al., The Differential Effects of Diestrous Progestogen Administration on Proestrous Gonadotrophin Levels, Endocrinol., 97, 885-890, 1975.
De Visser et al., Endocrinological Studies with (7α, 17 α)-17-Hydroxy-7-me norpregn-5(10)-en-20-yn-3-one (Org OD 14), Arzneim. Forsh., 34, 1010-1020, 1984.
Office Action mailed on May 22, 2009 in U.S. Appl. No. 10/478,264.
Office Action mailed on Mar. 17, 2008 in U.S. Appl. No. 10/478,357.
Office Action mailed on May 16, 2008 in U.S. Appl. No. 10/478,357.
Office Action mailed on Dec. 16, 2008 in U.S. Appl. No. 10/478,357.
Office Action mailed on May 28, 2009 in U.S. Appl. No. 10/478,357.
Office Action mailed on Jan. 24, 2007 in U.S. Appl. No. 10/495,707.
Office Action mailed on Dec. 28, 2007 in U.S. Appl. No. 10/495,707.
Office Action mailed on Aug. 19, 2008 in U.S. Appl. No. 10/495,707.
Office Action mailed on May 22, 2009 in U.S. Appl. No. 10/495,707.
Office Action mailed on Oct. 15, 2007 in U.S. Appl. No. 10/517,509.
Office Action mailed on Dec. 19, 2007 in U.S. Appl. No. 10/517,509.
Office Action mailed on Mar. 26, 2008 in U.S. Appl. No. 10/517,509.
Office Action mailed on Jan. 5, 2009 in U.S. Appl. No. 10/517,509.
Office Action mailed on Aug. 18, 2009 in U.S. Appl. No. 10/517,509.
Office Action mailed on Apr. 3, 2007 in U.S. Appl. No. 10/517,686.
Office Action mailed on Aug. 9, 2007 in U.S.Appl. No. 10/517,686.
Office Action mailed on Apr. 4, 2008 in U.S. Appl. No. 10/517,686.
Office Action mailed on May 29, 2009 in U.S. Appl. No. 10/517,686.
Office Action mailed on Apr. 23, 2007 in U.S. Appl. No. 10/521,040.
Office Action mailed on Aug. 17, 2007 in U.S. Appl. No. 10/521,040.
Office Action mailed on Apr. 2, 2008 in U.S. Appl. No. 10/521,040.
Office Action mailed on Jun. 1, 2009 in U.S. Appl. No. 10/521,040.
Visser et al., “In vitro effects of estetrol on receptor binding, drug targets and human liver cell metabolism,” CLIMACTERIC (2008) 11(1) Appx. II: 1-5.
Visser et al., “First human exposure to exogenous single-dose oral estetrol in early postmenopausal women,” CLIMACTERIC (2008) 11(1): 1-10.
Visser et al., “Clinical applications of estetrol,” J. Of Steroid Biochem and Molecular Biol. (2009) 114: 85-89.
Holinka et al., “Estetrol: A unique steroid in human pregnancy,” J. Of Steroid Biochem and Molecular Biol. (2009) 110: 138-143.
Coelingh Bennink et al., “Oral bioavailability and bone sparing effects of estetrol in an osteoporosis model,” CLIMACTERIC (2008) 11 (Supp 3): 1-13.
Albertazzi Paola et al., “The Effect of Tibolone Versus Continuous Combined Norethisterone Acetate and Oestradiol on Memory, Libido and Mood of Postmenopausal Women: A Pilot study”; Database Biosis ′Onlinel; Oct. 31, 2000; pp. 223-229; vol. 36, No. 3; Biosciences Information Service, Philadelphia, PA., U.S.
Hammond et al., A Versatile Method for the Determination of Serum Cortisol Binding Globulin and Sex Hormone Binding Globulin Binding Capacities, 1983, vol. 132, pp. 101-110.
Elger et al., Sulfamates of Various Estrogens are Prodrugs with Increased Systemic and
Bennink Herman Jan Tijmen Coelingh
Bunschoten Evert Johannes
Holinka Christian Franz
Chui Mei-Ping
Pantarhei Bioscience B.V.
Richter Johann R
The Webb Law Firm
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