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A61k 47/32 (2013.01) US0092.594.17B2 (12) United States Patent (10) Patent No.: US 9.259,417 B2 Soll et al. (45) Date of Patent: Feb. 16, 2016 (54) PARASITICIDAL ORAL VETERINARY USPC .......................................................... 514/378 COMPOSITIONS COMPRISING See application file for complete search history. SYSTEMICALLY-ACTING ACTIVE AGENTS, METHODS AND USES THEREOF (56) References Cited (71) Applicant: MERIAL INC., Duluth, GA (US) U.S. PATENT DOCUMENTS 3,887.964 A 6, 1975 Richards (72) Inventors: Mark David Soll, Alpharetta, GA (US); 4,284,652 A 8, 1981 Christensen Diane Larsen, Buford, GA (US); Susan 4,327,076 A 4/1982 Puglia et al. Mancini Cady, Yardley, PA (US); Peter 4,393,085 A 7/1983 Spradlin et al. Cheifetz, East Windsor, NJ (US); is: A 2. 3. SE, Izabela Galeska, Newtown, PA (US) 4,997,671- - - A 3/1991 SpanierO C. a. 5,236,730 A 8, 1993 Yamada et al. (73) Assignee: MERLAL, INC., Duluth, GA (US) 5,262,167 A 1 1/1993 Vegesna et al. 5,380,535 A 1/1995 Geyer et al. (*) Notice: Subject to any disclaimer, the term of this 5.439,924 A 8, 1995 Miller patent is extended or adjusted under 35 5,578.336 A 1 1/1996 Monte U.S.C. 154(b) by O. davs. 5,605,889 A 2f1997 Curatolo et al. (b) by yS 5,637,313 A 6, 1997 Chau 5,753,255 A 5/1998 Chaukin et al. (21) Appl. No.: 14/627,499 5,824,336 A 10/1998 Janset al. (22) Filed: Feb. 20, 2015 5,827,5655:3. A 10,36 1998 Axelrodin Set al. (65) Prior Publication Data (Continued) US 2015/O164864 A1 Jun. 18, 2015 FOREIGN PATENT DOCUMENTS Related U.S. Application Data AU 2008320992 6, 2010 (63) Continuation of application No. 13/754.969, filed on AU 2010206029 8, 2010 Jan. 31, 2013. (Continued) (60) Provisional application No. 61/595,463, filed on Feb. OTHER PUBLICATIONS 6, 2012. Glossary of medical education terms, Institute of International Medi cal Education. http://www.iime.org/glossary.htm Accessed in Mar. (51) Int. Cl. 2013. A6 IK3I/42 (2006.01) Halos etal. Flea control failure? Mvthsyth and realities. Trends Parasitol A6 IK3I/94 (2006.01) 30:228-233, May 2014. A6 IK9/00 (2006.01) EMEA Report. Committee for Veterinary Medicinal Products: Poly ethylene Glycol Stearates and Polyethylene Glycol 15 Hydroxystear gll, %4. 3:08: ate, Summary Report. EMEAfMRL/392/98-FINAL Rev.1, Jun. 2003. A6 IK3I/4985 (2006.01) Starch 1500 Partially pregelatinized maize starch technical informa A6 IK3I/7048 (2006.01) tion brochure; Colorcon company, 1999. A6 IK3I/365 (2006.01) A6 IK3I/27 (2006.01) (Continued) A6 IK3I/437 (2006.01) Primary Examiner — Mark Shibuya A6 IK 47/10 (2006.01) Assistant Examiner — Yih-Horng Shiao A6 IK 47/12 (2006.01) (74) Attorney, Agent, or Firm — Judy Jarecki-Black; John A6 IK 47/4 (2006.01) Ezcurra; Merial, Inc. A6 IK 47/32 (2006.01) (57) ABSTRACT A6 IK 47/4447/36 (2006.01)2006.O1 This invention relates to veterinary compositions for treating ( .01) and/or preventing fleas or ticks infection or infestation in an (52) U.S. Cl. animal comprising an isoxazoline active agent of Formula CPC ............... A6 IK3I/42 (2013.01); A61 K9/0056 (II): (2013.01); A61 K9/0068 (2013.01); A61 K 31/194 (2013.01); A61 K3I/27 (2013.01); A6 IK3I/365 (2013.01); A61 K3I/437 (II) (2013.01); A61K 31/4985 (2013.01); A61K O-N O 31/7048 (2013.01); A61K 45/06 (2013.01); FC \ A61K47/14A61K47/10 (2013.01); A61K 47/3247/12 (2013.01); C O HN NH A61K47/36 (2013.01); A61K 47/44 (2013.01); O C07D 261/04 (2013.01) C CH (58) Field of Classification Search CPC ... A61K 31/42: A61 K9/0056; A61K 31/194; or a pharmaceutically acceptable salt thereof, and a pharma A61K31/7048. A61K47/44. A61K47/36. ceutically acceptable carrier. A61K 47/14: A61K 47/10; A61K 2300/00 24 Claims, 3 Drawing Sheets US 9,259,417 B2 Page 2 (56) References Cited WO 2008. 144275 11, 2008 WO WO2008, 148027 A1 12/2008 U.S. PATENT DOCUMENTS WO WO2008,154528 A1 12/2008 WO WO2009/002809 A1 12/2008 6,060,078 A 5, 2000 Lee WO 2010/OO3923 1, 2010 6,086,940 A 7/2000 Axelrod WO 2010/056999 5, 2010 6,093.427 A 7/2000 Axelrod WO 2010/07907 7 T 2010 6,093441. A 7/2000 Axelrod WO 2010/084067 T 2010 6,110,521 A 8/2000 Axelrod WO 2011,067272 6, 2011 6,159,516 A 12/2000 Axelrod et al. WO 2011 O92287 8, 2011 6,270,790 B1 8/2001 Robinson et al. WO 2011 104087 9, 2011 6,387.381 B2 5/2002 Christensen WO 2011/154433 12/2011 6,500.463 B1 12/2002 van Lengerich WO 2011/154434 12/2011 7,348,027 B2 3/2008 Rose et al. WO 2011/154494 12/2011 7,662.972 B2 2/2010 Mita et al. WO 2011/157733 12/2011 7,947,715 B2 5, 2011 Mita et al. WO WO2011, 149749 A1 12/2011 7,951,828 B1 5/2011 Mita et al. WO 2012/OO7426 1, 2012 7.955,632 B2 6/2011 Paulsen et al. 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OTHER PUBLICATIONS 38 1993 A. 58: his “Understanding and optimizing the dual excipient functionality of 2003,7958OOO 1/2003 Chen sodium lauryl sulfate in tablet formulation of poorly water soluble 2004/0037869 A1 2/2004 Cleverly et al. drug: wetting and lubrication.” Aljaberi et al., Pharmaceutical Devel 2004.0043925 A1 3, 2004 Kolbe et al. opment and Technology, 2013; 18(2): 490-503. 2004/0234579 A1 11, 2004 Finke “Parasites of domestic owned cats in Europe: co-infestations and risk 2005/0O3.2718 A1 2/2005 Burke et al. factors.” Beugnet et al., Parasites & Vectors, 2014, 7:291. 2005/0226908 A1* 10, 2005 Huron et al. .................. 424/442 "Pharmacokinetics of fluralaner in dogs following a single oral or 2006/014 1009 A1 6/2006 Cady et al. intravenous administration.” Kilp et al., Parasites & Vectors, 2014, 2006/0222684 A1 10, 2006 ISele 7:85. 2009,028O159 A1 11, 2009 Paulsen et al. 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A. 1933; Rial “Onset of activity of fluralaner (BRAVECTOTM) against 2012, 0035122 A1 2/2012 Vaillancourt et al. Stephalides felis on dogs.” Taenzler et al., Parasites & Vectors, 5858. A. 33. St.it al. U.S. Freedom of Information Summary for NADA 141-426 BRAVECTO, May 15, 2014. 2015,0057239 A1 2/2015 Freehaufetal. “Comparative efficacy of two oral treatments for dogs containing either afoxolaner or fluralaner against Rhipicephalus Sanguineus FOREIGN PATENT DOCUMENTS sensulato and Dermacentor reticulatus.” Beugnet et al., Veterinary Parasitology, 209 (2015), 142-145. EP O273OO1 6, 1988 “Comparative speed of efficacy against Ctenocephalides felis of two EP 492235 7, 1992 oral treatments for dogs containing either afoxolaner or fluralaner.” EP O75443 3, 1993 Beugnet et al., Veterinary Parasitology, 207 (2015), 297-301. EP 1023841 8, 2000 “Safety of fluralaner, a novel systemic antiparasitic drug, in EP 1247456 10, 2002 MDR1(--) Collies after oral administration.” Walther et al., Para GB 2300 103 10, 1996 sites & Vectors, 2014, 7:86. NZ 286545 11, 1998 “Safety of the concurrent treatment of dogs with BravectoM NZ 568.394 6, 2010 (fluralaner) and ScaliborTM protectorband (deltamethrin).” Walther et WO 99.48372 9, 1999 al., Parasites & Vectors, 2014, 7:105. W. 85.835 383 “Safety of concurrent treatment of dogs with fluralaner (BravectoM) WO O3/030653 4/2003 and milbemycin Oxime praziquantel.” Walther et al., Parasites & WO WO2005/O137142005/O13714 A1 2, 2005 E.e effect of foodE. on the pharmacokinetics of oral fluralaner in WO 2005/O16356 3, 2005 dogs.” Walther et al., Parasites & Vectors, 2014, 7:84. WO WO2005/062782 A1 7/2005 “The speed of kill of fluralaner (BravectoM) against Ixodes ricinus WO 2005/099.453 10/2005 tickson dogs.” Wengenmayer et al., Parasites & Vectors, 2014, 7:525. WO WO2005/0996.92 A1 10, 2005 Fluralaner, al novel isoxazoline, prevents flea (Ctenocephalides WO 2007/07O606 6, 2007 felis) reproduction in vitro and in a simulated home environment.” WO 2007/075459 7/2007 Williams et al., Parasites & Vectors, 2014, 7:275. WO 2007/079162 7/2007 “Safety of fluralaner chewable tablets (Bravecto"), a novel systemic WO 2007/123855 11, 2007 antiparasitic drug, in dogs after oral administration.” Walther et al. WO 2008/030469 3, 2008 Parasites & Vectors, 2014, 7:87.
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