2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C514S182000, C514S614000, C514S625000, C514S626000, C552S525000, C552S536000

Reexamination Certificate

active

07419972

ABSTRACT:
The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of formula Ias well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for prophylaxis and/or therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17β-hydroxy steroid dehydrogenase type 1.

REFERENCES:
patent: 3562260 (1971-02-01), De Ruggieri et al.
patent: 6127401 (2000-10-01), Singh et al.
patent: 6747018 (2004-06-01), Tanabe et al.
patent: 6933386 (2005-08-01), Bhide et al.
patent: 2003/0073674 (2003-04-01), Slaga et al.
patent: 2004/0009959 (2004-01-01), Potter et al.
patent: 857 081 (1960-12-01), None
patent: WO 99/46279 (1999-09-01), None
patent: WO 00/07576 (2000-02-01), None
patent: WO 01/70093 (2001-09-01), None
patent: WO 02/15910 (2002-02-01), None
patent: WO 02/15910 (2002-02-01), None
patent: WO 02/15910 (2002-02-01), None
patent: WO 02/32409 (2002-04-01), None
patent: WO 02/36605 (2002-05-01), None
patent: WO 02/36605 (2002-05-01), None
patent: WO 02/062347 (2002-08-01), None
patent: WO 02/100877 (2002-12-01), None
patent: WO 2004/101595 (2004-11-01), None
patent: WO 2004/101595 (2004-11-01), None
patent: WO 2005/089256 (2005-09-01), None
Page et al., “Efficient regioselective A-ring functionalization of oestrogens.”, Tetrahedron, vol. 46(6), pp. 2059-2068, 1990.
Kaneko et al., “The synthesis of 2- and 4-alkoxymethylestrogens”, Chem. Pharm. Bull., vol. 12(2), pp. 196-203, 1964.
Seimbille et al., “Synthesis of 2,16alpha- and 4,16alpha-difluoroestradiols and their 11beta-methoxy derivatives as potential estrogen receptor-binding radiopharmaceuticals”. J. Chem. Soc., Perkin Trans. 1, pp. 657-663, 2002.
Berg et al., “Synthesis of immunogenic C-6 derivatives of 2-methoxyestrone and 2-methoxy-17beta-estradiol and characterization of the corresponding antiserums”. Hoppe-Seyler's Zeitschrift fuer Physiologische Chemie, vol. 363(7), 1982, Abstract only.
Yoshizawa et al., “Clinical analysis on steroids. XVIII. Preparation of 6,17-dioxo-catechol estrogen and its related compounds.” Yakugaku Zasshi, vol. 101(3), 1981, Abstract only.
Database CA ′Online! Chemical Abstracts Service, Columbus, Ohio, US; Patton, Tad et al: “Estrogens V. The Relation of Estrogenic Activity and Molecular Structure” XP002353442 & Archives of Biochemistry and Biophysics, 101, 181-5 Coden: ABB1A4; ISSN: 0003-9861, 1963.
Database CA ′Online! Chemical Abstracts Service, Columbus, Ohio, US; Jefferson, A. et al: “Abnormal Claisen Rearrangement of 3,3-Dimethylallyl Estrone Ether” XP002353443, Database Accession No. 1969:68602 & Journal of the Chemical Society Sectioni C: Organic, (2), 243-5 Coden: JS00AX; ISSN: 0022-4952, 1969.
Cushman, Mark et al: “The Effect of Exchanging Various Substituents at the 2-Position of 2-Methoxyestradiol on Cytotoxicity in Human Cancer Cell Cultures and Inhibition of Tubulin Polymerization”, Journal of Medicinal Chemistry, Bd. 45, Nr. 21, Oct. 10, 2002, pp. 4748-4754, XP002368004; ISSN: 0022-2623.
Omar A-Mohsen M et al: “Synthesis, Estrogen Receptor Binding Affinity and Biological Evaluation of Some 2-Substituted Estrone Derivates” Farmaco (Rome) Bd. 52, Nr. 4, 1997, pp. 219-225; XP002368005; ISSN: 0014-827X.
Database CA ′Online! Chemical Abstracts Service, Columbus, Ohio, US; Kaneko Hidehiko et al: “Synthesis of 2-and 4-alkoxymethylestrogens” XP002368010; Database Acession No. 1964:91085 & Chemical & Pharmaceutical Bulletin 12(2), 196-203 Coden: CPBTAL; ISSN: 0009-2363, 1964.
Database CA′Online! Chemical Abstracts Service, Columbus Ohio, US; Yan Jiaming et al: “Mass Spectrometric Study on Estrogen Derivatives” XP002368011; Database Accession No. 1994:192069 & Sichuan Daxue Xuebao, Ziran Kexueban, 30(1) 88-97 Coden: Scthao; ISSN: 0490-6756, 1993.
Wood et al: “Inhibition of Superoxide Dismutase by 2-Methoxyoestradiol Analogues and Oestrogen Derivatives: Structure-Activity Relationships” Anti-Cancer Drug Design, Baskingstoke, GB, Bd. 16, Nr. 4/5, 2001 pp. 209-215; XP008055013; ISSN; 0266-9536.
Y. Seimbille et al: “Synthesis of 2,16.-Alpha.-and 4.16.Alpha.-Dilfuoroestradiols and Their 11.Beta.-Methoxy Derivatives as Potential Estrogen Receptor Binidng Radiopharmaceuticals” Journal of the Chemical Society, Perkin Transactions 1., 2002, pp. 657-663; XP002368006.
Ali et al: “Synthesis of A-Ring Fluorinated Derivatives of (17.Alpha,20E/Z)-1251! Iodovinylestradiols: Effect on Receptor Binding and Receptor-Mediated Target Tissue Uptake” Journal of Medicinal Chemistry, 36(21), 3061-72 Coden: JMCMAR; ISSN: 0022-2623, 1993, XP002368007.
Page et al: “Efficient Regioselective A-Ring Functionalization of Oestrogens” Tetrahedron, Elsevier Science Publishers, Amsterdam, NL, Bd 46, Nr. 6, 1990, pp. 2059-2068, XP000867284; ISSN: 0040-4020.
Zhang Bolton: “Synthesis of the Equine Estrogen Metabolites 2-Hydroxyequilin and 2-Hydroxyequilenin” Chemical Research in Toxicology, American Chemical Society, Washington, DC, US, Bd. 12, Nr. 2, Jan. 1999, pp. 200-203, XP002955800; ISSN: 0893-228X.
Hasrat Ali et al: “Synthesis and Receptor Binding Affinity of 7Alpha-and 17 Alpha-Substituted 2-and 4-Chloroestradiol Derivatives” Journal of the Chemical Society, Perkin Transactions 1, Chemical Society, Letchworth, GB, Nr. 10, 1991, pp. 2485-2491, XP009043140; ISSN: 0300-922X.
Numazawa et al: “Structure-Activity Relationships of 2-, 4-, or 6-Substituted Estrogens as Aromatase Inhibitors” Journal of Steroid Biochemistry and Molcular Biology, Elsevier Science Ltd., Oxford, GB, Bd. 96, Nr. 1 Jun. 2005, pp. 51-58, XP005003329; ISSN: 0960-0760.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3987033

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.