Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
2011-01-18
2011-01-18
Hui, San-ming (Department: 1628)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S182000
Reexamination Certificate
active
07871995
ABSTRACT:
A method of contraception in mammalian females, which method comprises the parenteral or rectal 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 drug delivery system for parenteral or rectal administration that contains the aforementioned estrogenic component and a progestogenic component, said drug delivery system being selected from the group consisting of suppositories, systems for intravaginal delivery, inhalers, nasal sprays and transdermal delivery systems.
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 (1992-01-01), None
patent: 1700602 (2001-05-01), None
patent: 9218107 (1992-10-01), None
patent: 9426207 (1994-11-01), None
patent: 9502408 (1995-01-01), None
patent: 9517895 (1995-07-01), None
patent: 9603929 (1996-02-01), None
patent: 9858657 (1998-12-01), None
patent: 0062753 (2000-10-01), None
patent: 0073416 (2000-12-01), None
patent: 0130357 (2001-05-01), None
patent: 0185154 (2001-11-01), None
Katzung, Basic and Clinical Pharmacology, 6th ed., 1995, pp. 608-624.
Tseng et al., “Heterogeneity of Saturable Estradiol Binding Sites in Nuclei of Human Endometrium. Estetrol Studies”, (1978), vol. 9, pp. 1145-1148.
Fishman et al., “Fate of 15 α-Hydroxyestriol-3H in Adult Man”, J. Clin. Endocrinol. Metab., (1970), vol. 31, pp. 436-438.
Levine et al., “Uterine vascular effects of estetrol in nonpregnant ewes”, Am. J. Obstet. Gynecol., (1984), [148], vol. 73, pp. 735-738.
Martucci et al., “Direction of Estradiol Metabolish as a Control of its Hormonal Action—Uterotrophic Activity of Estradiol Metabolites”, Endocrin., (1977), vol. 101, pp. 1709-1715.
Martucci et al., “Uterine Estrogen Receptor Binding of Catecholestrogens and of Estetrol (1,3,5(10)-Estratriene-3, 15a, 16a, 17 β-Tetrol)”, Steroids, (1976), vol. 27, pp. 325-333.
Seeger et al., “The inhibitory effect of endogenous estrogen metabolies on copper-mediated in vitro oxidation of LDL”, Int. Journal of Clinical Pharmacology and Therapeutics, (1998), vol. 36, No. 7, pp. 383-385.
Tseng et al., “Competition of Estetrol and Ethynylestradiol with Estradiol for Nuclear Binding in Human Endometrium”, Journal of Steroid Biochemistry, (1976), vol. 7, pp. 817-822.
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.
Allen et al., An Ovarian Hormone: Preliminary Report on Its Localization, Extraction and Partial Purification, and Action in Test Animals, JAMA, Sep. 8, 1923, vol. 81, pp. 819-821.
Allen et al., The Induction of a Sexually Mature Condition in Immature Females by Injection of the Ovarian Follicular Hormone, Am. J. Physiol., 1924, vol. 69, pp. 577-588.
Jones et al., The Effects of Various Steroids on the Vaginal Histology in the Rat, Fertility and Sterility, Apr. 1973, vol. 24, No. 4, pp. 284-291.
Tulchinsky et al., Plasma Esterol as an Index of Fetal Well-Being, J. Clin. Endrocrinol. Metab., 1975, vol. 40. pp. 560-567.
Jozan et al., Different Effects of Oestradiol, Oestriol, Oestrol and of Oestrone on Human Breast Cancer Cells (MCF-7) in Long Term Tissue Culture, Acta Endocrinologica, 1981, vol. 98, pp. 73-80.
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 Reduced Hepatic Estrogenicity at Oral Application, J. Steroid Biochem. Molec. Biol., 1995, vol. 55, No. 3 / 4, pp. 395-403.
Murphy et al., Endometrial Effects of Long-Term Low-Dose Administration of RU486, Fertility and Sterility, Apr. 1995, vol. 63, No. 4, pp. 761-766.
Reel et al., Survey and Assessment of Mammalian Estrogen Biological Assays for Hazard Characterization, Fundamental and Applied Toxicology, 1996, vol. 34, pp. 288-305.
Beral et al., Use of HRT and the Subsequent Risk of Cancer, Journal of Epidemiology and Biostatistics, 1999, vol. 4, No. 3, pp. 191-215.
Tavani et al., The Adverse Effects of Hormone Replacement Therapy, Drugs & Aging, May 1999, vol. 14, No. 5, pp. 347-357.
Pike et al., Progestins and Menopause: Epidemiological Studies of Risks of Endometrial and Breast Cancer, Steroids, 2000, vol. 65, pp. 359-664.
Avvakumov et al., Steroid-binding Specificity of Human Sex Hormon-binding Globulin Is Influenced by Occupancy of a Zinc-binding Site, The Journal of Biological Chemistry, Aug. 25, 2000, vol. 275, No. 34, pp. 25920-25925.
Holinka et al., “In Vivo Effects of Esterol on the Immature Rat Uterus”, Biology of Reproduction, Society for the Reproduction Society for the Study of Reproduction, Champaign, IL, US, Mar. 1979, vol. 20, No. 2, pp. 242-246.
Holinka, et al., “Comparison of Effects of Esterol and Tamoxifen with Those of Estriol and Estradiol on the Immature Rat Uterus”, Biology of Reproduction, Society for the Reproduction Society for the Study of Reproduction, Champaign, IL, US, 1980, vol. 22, No. 4, pp. 913-926.
Jansson et al., “Estrogen Induces a Potent Suppression of Experimental Autoimmune Encephalomyelitis and Collagen-Induced Arthritis in Mice”, Journal of Neuroimmunology, Elsevier Science Publishers BV XX, 1994, vol. 53, No. 2, pp. 203-207.
Erdbruegger et al., Drug Discovery Today: Disease Mechanisms (2004), vol. 1
Bennink Herman Jan Tijmen Coelingh
Bunschoten Evert Johannes
Holinka Christian Franz
Hui San-ming
Pantarhei Bioscience B.V.
The Webb Law Firm
LandOfFree
Drug delivery system comprising a tetrahydroxylated estrogen... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Drug delivery system comprising a tetrahydroxylated estrogen..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Drug delivery system comprising a tetrahydroxylated estrogen... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2678331