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(12) United States Patent (10) Patent No.: US 7.803,838 B2 Davis Et Al

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(12) United States Patent (10) Patent No.: US 7.803,838 B2 Davis Et Al USOO7803838B2 (12) United States Patent (10) Patent No.: US 7.803,838 B2 Davis et al. (45) Date of Patent: Sep. 28, 2010 (54) COMPOSITIONS COMPRISING NEBIVOLOL 2002fO169134 A1 11/2002 Davis 2002/0177586 A1 11/2002 Egan et al. (75) Inventors: Eric Davis, Morgantown, WV (US); 2002/0183305 A1 12/2002 Davis et al. John O'Donnell, Morgantown, WV 2002/0183317 A1 12/2002 Wagle et al. (US); Peter Bottini, Morgantown, WV 2002/0183365 A1 12/2002 Wagle et al. (US) 2002/0192203 A1 12, 2002 Cho 2003, OOO4194 A1 1, 2003 Gall (73) Assignee: Forest Laboratories Holdings Limited 2003, OO13699 A1 1/2003 Davis et al. (BM) 2003/0027820 A1 2, 2003 Gall (*) Notice: Subject to any disclaimer, the term of this 2003.0053981 A1 3/2003 Davis et al. patent is extended or adjusted under 35 2003, OO60489 A1 3/2003 Buckingham U.S.C. 154(b) by 455 days. 2003, OO69221 A1 4/2003 Kosoglou et al. 2003/0078190 A1* 4/2003 Weinberg ...................... 514f1 (21) Appl. No.: 11/141,235 2003/0078517 A1 4/2003 Kensey 2003/01 19428 A1 6/2003 Davis et al. (22) Filed: May 31, 2005 2003/01 19757 A1 6/2003 Davis 2003/01 19796 A1 6/2003 Strony (65) Prior Publication Data 2003.01.19808 A1 6/2003 LeBeaut et al. US 2005/027281.0 A1 Dec. 8, 2005 2003.01.19809 A1 6/2003 Davis 2003,0162824 A1 8, 2003 Krul Related U.S. Application Data 2003/0175344 A1 9, 2003 Waldet al. (60) Provisional application No. 60/577,423, filed on Jun. 2003/0176426 A1 9/2003 Wagle et al. 4, 2004. 2003/0225146 Al 12/2003 Wagle et al. 2004.0005306 A1 1/2004 Loscalzo et al. (51) Int. Cl. 2004/0023967 A1 2/2004 Cohn et al. A6 IK3I/352 (2006.01) 2004.0054177 A1 3/2004 Otake et al. C07D 3II/04 (2006.01) 2004/0063646 A1 4/2004 Fujikura et al. (52) U.S. Cl. ............................ 514/456; 514/1: 514/451 (58) Field of Classification Search ..................... 514/1, 514/183, 451, 456 See application file for complete search history. (Continued) FOREIGN PATENT DOCUMENTS (56) References Cited EP 1 400 529 3, 2004 U.S. PATENT DOCUMENTS 5,874,461 A 2/1999 De Chaffoy de Courcelles et al. 5,922,341 A 7, 1999 Smith et al. 6,075,046 A 6/2000 De Chaffoy de Courcelles et al. (Continued) 6,465,463 B1 10/2002 Cohn et al. OTHER PUBLICATIONS 6,495,154 B1 12/2002 Tam et al. 6,541479 B1 4/2003 Mehanna et al. Neutel J., “Clinical Studies of CS-866, the Newest Angiotensin II 6,545,040 B1 4/2003 Xhonneux et al. Receptor Antagonist.” American Journal of Cardiology 2001: 6,595,926 B1 7/2003 Laragh 87(suppl):37c-43c.* 6,596,744 B2 7/2003 Wagle et al. 6,596,745 B2 7, 2003 Gall 6,632,180 B1 10/2003 Laragh (Continued) 6,635,273 B1 10/2003 Loscalzo et al. Primary Examiner Frederick Krass 6,770,663 B2 8/2004 Wagle et al. Assistant Examiner Walter E Webb 6,784, 177 B2 8, 2004 Cohn et al. (74) Attorney, Agent, or Firm—Charles Ryan, J.D.; Michael 6,869,966 B2 3/2005 Sato et al. 6,946,141 B2 9, 2005 Tam et al. Cirado, J.D. 6,951,860 B2 10/2005 Mehanna et al. 7,030,106 B2 4, 2006 Cho (57) ABSTRACT 7,056,906 B2 6/2006 Strony 2001/0008896 A1 7/2001 Smith et al. 2001/0044584 A1 1 1/2001 Kensey Nebivolol has been shown to be beneficial in the treatment of 2002fOO32149 A1 3/2002 Kensey cardiovascular diseases such hypertension, congestive heart 2002fOO61835 A1 5/2002 Kensey failure, arterial stiffness and endothelial dysfunction. The 2002.0068729 A1 6/2002 Egan et al. present invention features a pharmaceutical composition 2002/0107245 A1 8/2002 Wagle et al. comprising nebivolol and at least one other active agent, 2002fO115655 A1 8/2002 Mehanna et al. wherein the at least one other active agent is a cardiovascular 2002/O123485 A1 9, 2002 Alexander et al. agent. 2002fO147.184 A1 10/2002 Kosoglou et al. 2002fO151536 A1 10, 2002 Davis et al. 2002fO161016 A1 10, 2002 Tam et al. 12 Claims, 4 Drawing Sheets US 7,803.838 B2 Page 2 U.S. PATENT DOCUMENTS WO WO O2/41883 5, 2002 WO WO O2/43806 6, 2002 2004f0071766 A1 4/2004 Loscalzo et al. WO WO O2/O53161 T 2002 2004f0071777 A1 4/2004 Trespidietal. WO WO O2/O58685 8, 2002 2004/0097482 A1 5, 2004 Davis et al. WO WO O2/O58731 8, 2002 2004/OO97495 A1 5/2004 Wagle et al. WO WO O2/O58733 8, 2002 2004/010.5850 A1 6/2004 Loscalzo et al. WO WOO2O58731 8, 2002 2004.01098.94 A1 6, 2004 Shefer et al. 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Kolck, et al., “Pharmacological basis of antihypertension drug EP 1405,859 4/2004 therapy”, vol. 93, No. 20, pp. 847-856, May 12, 2004. EP 1541 175 6, 2005 "Rationale for Fixed-Dose Combinations in the Treatment of Hyper EP 1544208 6, 2005 tension”. Drugs, 2002, D.A. Sica, vol. 62 (3), pp. 443-462. EP 1548 024 6, 2005 “Hypertension Primer, Third Edition” Izzo and Black, 2003 pp. 408 EP 1550 668 7/2005 429 (Chapter C138). EP 1553 091 7/2005 Kamali. F., at al. A pharmacokinetic and pharmocodynamic interac EP 1637 539 3, 2006 tion study between nebivolol . ; 1977 Blackwell Science Ltd Br/ WO WO 97.49394 12/1997 Clin Pharmacol; 43; pp. 201-204. WO WOOO.38653 T 2000 Nebivolol; Drugs of the Future, vol. 14; No. 10; 1989: pp.957-959. WO WOO1? 12584 2, 2001 Lu, H.R., et al.; Effects of B-adrenoceptor antagoinists on cardiac WO WOO1f17528 3, 2001 function in ischemic-reperfused . ; European Journal of Pharma WO WOO1/35961 5, 2001 cology, 184 (1990) 65-74. 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