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United States Patent (10) Patent No.: US 8,399.440 B2 Fogler Et Al

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United States Patent (10) Patent No.: US 8,399.440 B2 Fogler Et Al USOO839944OB2 (12) United States Patent (10) Patent No.: US 8,399.440 B2 Fogler et al. (45) Date of Patent: Mar. 19, 2013 (54) DISEASE MODIFYING ANTI-ARTHRITIC 4,172,132 A 10/1979 Draper et al. ACTIVITY OF 2-METHOXYESTRADIOL 4.212,864 A 7/1980 Tax 4,307,086 A 12, 1981 Tax (75) Inventors: WilliamO O E. Fogler, Rockville, MD (US); 4,522,7584,444,767 A 4,6, 19851984 WETorelli et al. Stacy M.Plum, Arlington, VA (US); 4.552,758. A 1 1/1985 Murphy et al. Carolyn F. Sidor, Chapel Hill, NC (US) (Continued) (73) Assignee: EntreMed, Inc., Rockville, MD (US) FOREIGN PATENT DOCUMENTS (*) Notice: Subject to any disclaimer, the term of this RE E. 1943: patent is extended or adjusted under 35 U.S.C. 154(b) by 905 days. (Continued) (21) Appl. No.: 11/726,361 OTHER PUBLICATIONS (22) Filed: Mare 20,a? V.9 2007 Tishler et al., Ann Rheumat Dis, 1992:51(12): 1330-1331.* (Continued) (65) Prior Publication Data US 2007/0231.410A1 Oct. 4, 2007 Primary Examiner — San-Ming Hui (74) Attorney, Agent, or Firm — Suzannah K. Sundby, Esq.; Related U.S. Application Data Smith, Gambrell & Russell, LLP (60) Eyal application No. 60/784,206, filed on Mar. (57) ABSTRACT s The present invention relates a composition for treating rheu (51) Int. Cl. matic diseases. The compositionp comprisesp a compoundp hav A6 IK3I/56 (2006.01) ing the formula A 6LX3L/2197 (2006.01) (52) U.S. Cl. ...................... 514/171; 514/182: 514/252.1 OH (58) Field of Classification Search .................. 514/182, 514/252.02,252.029, 252.1, 171 See application file for complete search history. Ra (56) References Cited U.S. PATENT DOCUMENTS HO 2,584.271 A 2f1952 Huffman 2,846,453 A 8, 1958 Hoehn 3,117,140 A 1/1964 Heeker wherein R is selected from —OCH —OCHCH, —CH, 3,166.577 A 1/1965 Ringold et al. —CHCH, CCCH, -CHCH-CH, or CH, CHCH: 3.410,879 A 11, 1968 Smith et al. and one or more anti-rheumatic agents. 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