US007 1991.51B2 (12) United States Patent (10) Patent No.: US 7,199,151 B2 Shashoua et al. (45) Date of Patent: *Apr. 3, 2007 (54) DHA-PHARMACEUTICAL AGENT 4,692,441 A 9, 1987 Alexander et al. CONUGATES OF TAXANES 4,704,393 A 11/1987 Wakabayashi et al. 4,729,989 A 3, 1988 Alexander (75) Inventors: Victor E. Shashoua, Brookline, MA 4,788,063 A 11/1988 Fisher et al. (US); Charles E. Swindell, Merion, PA is: A RE s al (US); Nigel L. Webb, Bryn Mawr, PA 4s68161. A 9, 1989 Roberts (US); Matthews O. Bradley, 4.902,505 A 2/1990 Pardridge et al. Laytonsville, MD (US) 4,933,324. A 6/1990 Shashoua 4,939,174 A 7, 1990 Shashoua (73) Assignee: Luitpold Pharmaceuticals, Inc., 4,943,579 A 7, 1990 Vishnuvajala et al. Shirley, NY (US) 4,968,672 A 1 1/1990 Jacobson et al. 5,059,699 A 10/1991 Kingston et al. (*) Notice: Subject to any disclaimer, the term of this 5,068,224. A 11/1991 Fryklund et al. patent is extended or adjusted under 35 5, 112,596 A 5/1992 Malfroy-Camine U.S.C. 154(b) by 81 days. 5, 112,863 A 5/1992 Hashimoto et al. 5,116,624 A 5/1992 Horrobin et al. This patent is Subject to a terminal dis- 5, 120,760 A 6/1992 Horrobin claimer. 5,141,958 A 8, 1992 Crozier-Willi et al. 5,169,762 A 12/1992 Grey et al. (21) Appl. No.: 10/618,884 5,169,764 A 12/1992 Shooter et al. 5,194,654 A 3, 1993 Hostetler et al. (22) Filed: Jul. 14, 2003 5,214,062 A 5/1993 Mark et al. 5,216,023 A 6/1993 Literati-Nagy et al. (65) Prior Publication Data 5,216,142 A 6/1993 Horribin et al. 5,223,263. A 6/1993 Hostetler et al. US 2004/O180949 A1 Sep. 16, 2004 5,246,726 A 9, 1993 Horribin et al. 5,250,722 A 10, 1993 Bombardelli et al. Related U.S. Application Data 5,276,020 A 1/1994 Horribin et al. (63) Continuation of application No. 09/846,838, filed on 5,278.324 A 1/1994 Kingston et al. 5,284,876 A 2, 1994 Shashoua et al. May 1, 2001, now Pat. No. 6,602,902, which is a 5,308,832 A 5/1994 Garleb et al. continuation of application No. 09/135,291, filed on 5.314.991 A 5/1994 Oka et all Aug. 17, 1998, now abandoned, which is a continu- 5,336,684 A 8/1994 Murray et al ation of application No. 08/651.312, filed on May 22, 5,352.596 A 10, 1994 Cheung et al. 1996, now Pat. No. 5,795,909. 5,356,928 A 10/1994 Murray et al. 5,362,831 A 11/1994 Mongelli et al. (51) Int. Cl. A 6LX 3/59 (2006.01) A 6LX 3/592 (2006.01) (Continued) A6 IK 9/42 (2006.01) FOREIGN PATENT DOCUMENTS A6 IK 47/48 (2006.01) A61 K 47/00 (2006.01) AU T46472 6, 1999 (52) U.S. Cl. ...................... 514/449; 514/560; 514/558: 514/552; 514/549; 514/943 (Continued) (58) Field of Classification Search ................ 514/449, OTHER PUBLICATIONS 514/560, 558,552,549; 549/510 See application file for complete search history. 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