Di-steroidal prodrugs of estradiol

Details Di-steroidal prodrugs of estradiol Di-steroidal prodrugs of estradiol

2006-06-27

2006-06-27

Qazi, Sabiha (Department: 1616)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

C514S169000, C514S170000, C552S201000, C552S203000, C552S205000, C552S502000, C552S540000, C552S541000

Reexamination Certificate

active

07067505

ABSTRACT:
The present invention is a di-steroidal prodrug of estradiol having the following formula:

REFERENCES:
patent: 3766223 (1973-10-01), Ercoli et al.
patent: 3828081 (1974-08-01), Ercoli et al.
patent: 3916002 (1975-10-01), Taubert et al.
patent: 3952030 (1976-04-01), Chambers et al.
patent: 4002747 (1977-01-01), van der Vies
patent: 4198405 (1980-04-01), Enomoto et al.
patent: 4310511 (1982-01-01), Holick
patent: 5117015 (1992-05-01), Yarino et al.
patent: 5610149 (1997-03-01), Burrows et al.
patent: 5888996 (1999-03-01), Farb
patent: 5955068 (1999-09-01), Gouin et al.
patent: 5989581 (1999-11-01), Groenewegen
patent: 6083941 (2000-07-01), Farb
patent: 6375930 (2002-04-01), Young et al.
patent: 6441206 (2002-08-01), Mikkonen et al.
patent: 2002/0131991 (2002-09-01), Milstein et al.
patent: 1 123 666 (1959-10-01), None
patent: 2 330 581 (1975-01-01), None
patent: 2 297 629 (1975-01-01), None
patent: 35-004967 (1960-05-01), None
patent: 7 308 083 (1974-12-01), None
patent: WO 98/52965 (1998-11-01), None
K. Parfitt, “Martindale—The Complete Drug Reference,” 32ed, 1999, Pharmaceutical Press, pp. 1455-1458.
K. Fotherby, “Intrasubject Variabiity in the Pharmacokinetics of Ethynyloestradiol,” Journal of Steroid Biochemistry and Molecular Biology, vol. 38, No. 6, 1991, pp. 733-736.
K. Fotherby, “Pharmacokinetics of Ethynyloestradiol in Humans,” Methods and Findings in Experimental Clinical Pharmacology, 1982, 4(2), pp. 133-141.
E. Diczfalusy, O. Ferno, H. Fex, and B. Hogberg, “Long-Acting p-Alkoxyhydrocinnamic Acid Esters of Steroid Hormones,” Acta Chemica Scandinavica, 1963, 17, pp. 2536-2547.
J. Fried and N.A. Abraham, “The Effect of Co-Solvents on Metal in Ammonia Reductions, The Formations of Dimeric Steroid Hormones,” Tetrahedron Letters, 1964, No. 28, pp. 1879-1885.
H. Kuhl and H. Taubert, “A New Class of Long-Acting Hormonal Steroid Preparation: Synthesis of Oligomeric Estradiol Derivatives,” Steroids, Jul. 1973, 22, pp. 73-87.
H. Kuhl and H. Taubert, “A New Class of Long-Acting Hormonal Steroid Prepartion: Synthesis of Dimeric Ethynodiol and Nortestosterone, or Dimeric and Trimeric Androgens and of Some Dimeric Combinations of Steroids,” Steroids, 1974, vol. 24, No. 5, pp. 613-626.
H. Kuhl, W. Auerhammer, and H. Taubert, “Oligomeric Oestradiol Esters: A New Class of Long-Acting Oestrogens,” Acta Endrocinologica, 1976, 83, pp. 439-448.
R. Vitali, S. Gladiali, G. Falconi, G. Celasco, M.A. Saccani, and R. Gardi, “Disteroidyl Ethers. 1. Synthesis and Oral Long-Lasting Uterotrophic Activity of 1,3,5(10)-Estratrien-17-yl Enol Ethers of 3-Keto Steroids,” Journal of Medicinal Chemistry, 1977, vol. 20, No. 3, pp. 359-364.
A. Ius, G. Meroni, and L. Ferrara, “Two Dimers, 4:4′ and 2:2′-Di[estradiol], Obtained by Chemical Oxidative Coupling of Estradiol,” Journal of Steroid Biochemistry, vol. 8, pp. 1259-1261.
D. Rabbouin, V. Perron, B. N'Zemba, R. Gaudreault, and G. Berube, “A Facile Synthesis of C2- Symmetric 17β-Estradiol Di3mers,” Bioorganic & Medicinal Chemistry Letters, 2003, 13, pp. 557-560.
Hu Zheng et al., Abstract of “Studies on polymer-supported drugs: synthesis of poly(ethylene glycol)-estrogen compounds,” Chemical Abstracts Service (XP002322263), and Yaoxue Xuebao (Database Accession No. 1988:423178), 1987, 22(8), 637-40.
Huai-De Shu et al., Abstract of “Structure-activity relationships of estradiol derivatives,” Chemical Abstracts of Service (XP002322264), and Yaoxue Xuebao (Database Accession No. 1979:604845), 1979, 14(6), 343-8.
W. Dirscherl, “Uber Kohlensaurederivate des Follikelhormons. 7. Mittellung uber Sexualhormone und verwandte Stoffe” Hoppe Seyler Zeitschrift Fur Physiol. Chemie, vol. 239, 1936, pp. 49-52. Translation included.

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