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( 12 ) United States Patent US010426780B2 (12 ) United States Patent (10 ) Patent No. : US 10 ,426 , 780 B2 Underwood (45 ) Date of Patent : Oct . 1 , 2019 ( 54 ) ANTIVIRAL THERAPY 5 ,089 , 500 A 2 / 1992 Daluge 5 ,519 ,021 A 5 / 1996 Young et al. 5 ,641 , 889 A 6 / 1997 Daluge et al . (71 ) Applicant : VIIV HEALTHCARE COMPANY , 5 ,663 , 169 A 9 /1997 Young et al. Wilmington , DE (US ) 5 ,663 , 320 A 9 / 1997 Mansour et al. 5 ,693 ,787 A 12 / 1997 Mansour et al. (72 ) Inventor : Mark Richard Underwood , Research 5 ,696 ,254 A 12 / 1997 Mansour et al. Triangle Park , NC (US ) 5 , 808 , 147 A 9 / 1998 Daluge et al. 5 ,811 , 423 A 9 / 1998 Young et al . 5 , 840 , 990 A 11/ 1998 Daluge et al . ( 73 ) Assignee : ViiV Healthcare Company , 5 , 849 , 911 A 12 / 1998 Fassler et al. Wilmington , DE (US ) 5 , 905 , 082 A 5 / 1999 Roberts et al. 5 , 914 , 332 A 6 / 1999 Sham et al . ( * ) Notice : Subject to any disclaimer , the term of this 5 ,917 ,041 A 6 / 1999 Daluge et al. patent is extended or adjusted under 35 5 ,917 , 042 A 6 / 1999 Daluge et al . 5 ,919 ,941 A 7 / 1999 Daluge et al. U . S . C . 154 (b ) by 0 days. 5 , 922 ,695 A 7 / 1999 Arimilli et al. 5 , 935 , 94 A 8 / 1999 Munger et al . (21 ) Appl. No. : 15 / 366 , 442 5 ,977 ,089 A 11/ 1999 Arimilli et al . 6 ,043 ,230 A 3 / 2000 Arimilli et al . ( 22 ) Filed : Dec . 1 , 2016 6 ,051 , 709 A 4 / 2000 Goodyear et al. 6 ,069 , 249 A 5 / 2000 Arimilli et al. 6 , 087 , 383 A 7 / 2000 Singh et al. (65 ) Prior Publication Data 6 ,087 , 501 A 7 / 2000 Daluge et al . 6 ,281 , 367 B1 8 / 2001 Al - Farhan et al. US 2017 / 0079982 A1 Mar. 23 , 2017 6 , 294 , 540 B1 9 / 2001 Brodie et al. Related U . S . Application Data 6 ,329 ,522 B1 12 / 2001 Hill et al . 6 , 340 , 587 B1 1 /2002 Dawson et al. (63 ) Continuation of application No. 15 / 073, 728 , filed on 6 , 392 ,085 B2 5 / 2002 Daluge et al. Mar. 18 , 2016 , which is a continuation of application 6 ,436 , 989 B1 8 / 2002 Hale et al. 6 , 448, 403 B1 9 / 2002 Daluge et al . No . 14 /710 ,952 , filed on May 13 , 2015 , now 6 ,514 ,953 B1 2 / 2003 Armitage et al . abandoned , which is a continuation of application No . 6 ,544 , 961 B1 4 / 2003 St . Clair et al. 13 / 575, 380 , filed as application No . 6 , 552 , 193 B1 4 / 2003 Daluge et al. PCT /US2011 /022219 on Jan . 24, 2011 , now 6 ,555 ,133 B2 4 /2003 Makooi- Morehead et al. abandoned . ( Continued ) (60 ) Provisional application No . 61/ 298 , 589 , filed on Jan . 27, 2010 . FOREIGN PATENT DOCUMENTS (51 ) Int. CI. EP 0349242 1 / 1990 A61K 31/ 535 ( 2006 . 01 ) EP 0582455 2 / 1994 A61K 31 /51 ( 2006 .01 ) (Continued ) A61K 31/ 5365 ( 2006 .01 ) A61K 31 /675 ( 2006 .01 ) OTHER PUBLICATIONS A61K 45 / 06 ( 2006 .01 ) International Search Report and Written Opinion for Priority Appli A61K 31/ 4985 ( 2006 .01 ) cation No. PCT/ US2011 / 22219 . A61K 31 /52 ( 2006 . 01 ) European Search Report dated Aug . 14 , 2015 , for Co -related EP A61K 31 /536 ( 2006 . 01 ) Application No. 15164931. 6 . A61K 31 /513 ( 2006 .01 ) European Supplementary Search Report dated May 31, 2013 , for A61K 31 / 505 ( 2006 . 01 ) Co -related EP Application No. 11737484 . 3 . A61K 9 /00 ( 2006 . 01 ) Notice of Opposition by LaFrancol S . A . filed May 28 , 2013 , against (52 ) U . S . CI. Colombian Patent Application No. 12 - 125 -933 . CPC . .. A61K 31/ 5365 ( 2013 . 01 ) ; A61K 9 / 0014 GlaxoSmithKline Response to Notice of Opposition by LaFrancol ( 2013 .01 ) ; A61K 9 / 0019 ( 2013 .01 ) ; A61K S . A . filed May 28 , 2013 , against Colombian Patent Application No . 9 /0053 ( 2013 .01 ) ; A61K 31/ 4985 ( 2013 .01 ) ; 12 - 125 - 933 . A61K 31 /505 ( 2013 . 01 ) ; A61K 31/ 513 (Continued ) ( 2013 .01 ) ; A61K 31/ 52 (2013 .01 ) ; A61K 31/ 536 (2013 .01 ) ; A61K 31/ 675 ( 2013 .01 ) ; Primary Examiner — Shengjun Wang A61K 45 / 06 ( 2013 .01 ) (74 ) Attorney, Agent, or Firm — J. Scott Young ( 58 ) Field of Classification Search CPC .. .. .. .. .. .. .. A61K 31/ 5365 , A61K 31 /505 ABSTRACT USPC .. .. .. 514 / 230 . 2 , 275 ( 57 ) See application file for complete search history . The present invention relates to combinations of compounds comprising HIV integrase inhibitors and other therapeutic References Cited agents . Such combinations are useful in the inhibition of ( 56 ) HIV replication , the prevention and / or treatment of infection U . S . PATENT DOCUMENTS by HIV , and in the treatment of AIDS and / or ARC . 5 ,034 ,394 A 7 / 1991 Daluge 5 ,047 ,407 A 9 / 1991 Belleau et al 17 Claims, 2 Drawing Sheets US 10 ,Page426 ,2 780 B2 ( 56 ) References Cited No . 2080 - 2012 — In Spanish , no English Translation Available at This Time. U . S . PATENT DOCUMENTS GSK Response to Notice of Opposition by Industrial Association of 6 ,555 ,687 B1 4 / 2003 Daloge et al . Pharmaceutical Laboratories filed Sep . 24 , 2013 , against Chilean 6 ,639 , 071 B2 10 / 2003 Crocker et al . Application No . 8020 - 2012 - In Spanish , no English Translation 6 ,646 , 125 B1 11/ 2003 Jones et al. Available at This Time. 6 , 870 , 053 B23 / 2005 Daluge et al. Notice of Opposition dated Jan . 26 , 2016 , by Teva Pharmaceutical 6 ,939 , 964 B2 9 / 2005 Crocker et al . Industries against Co - related EP Application No . 11737484 . 3 , EP 7 , 109 , 228 B2 9 / 2006 Jones et al . Publication No. 2531027 . 7 , 119 , 202 B1 10 / 2006 Belleau et al. Notice of Opposition dated Feb . 4 , 2016 , by Ter Meer Steinmeister 7 , 534 , 809 B2 5 / 2009 Storer et al . 8 ,088 ,770 B2 1 /2012 Desai et al. & Partner Patentanwalte against Co - related EP Application No. 8 ,624 ,023 B2 1 / 2014 Yoshida 11737484 . 3 , EP Publication No . 2531027 . 9 , 242 , 986 B2 1 / 2016 Kawasuji Notice of Opposition dated Feb . 5 , 2016 , by LEK Pharmaceuticals 2005 /0171127 AL 8 / 2005 Currie et al. against Co -related EP Application No. 11737484 . 3 , EP Publication 2006 /0084627 AL 4 / 2006 Mardh No . 2531027 . 2006 /0246130 AL 11/ 2006 Dahl et al . Notice of Opposition dated Feb . 5 , 2016 , Annex 1 , by LEK 2007 /0124152 Al 5 / 2007 Johns et al. 2007 /0219243 A1 * 9 / 2007 Kearney . .. .. .. A61K 31/ 426 Pharmaceuticals against Co -related EP Application No . 11737484 . 514 /312 3 , EP Publication No . 2531027 . 2008 / 0039428 A1 2 / 2008 Allaway et al . Notice of Opposition dated Feb . 5 , 2016 , by Page White Farrer 2008 /0076738 A1 3 / 2008 Cai et al . Limited against Co - related EP Application No . 11737484 . 3 , EP 2008 / 0207620 Al 8 /2008 Desai et al. Publication No . 2531027 . 2008 / 0241289 Al 10 / 2008 Gant et al . Selleseth , et al ., Interactions of 1263W94 with Other Antiviral 2009 / 0012108 A1 * 1 / 2009 Guillemont . .. .. .. C07D 239 /48 Agents in Inhibition of Human Cytomegalovirus Replication , Anti 514 / 275 2009 /0075939 AL 3 / 2009 He et al. microbial Agents and Chemotherapy (2003 ) 47 ( 4 ) : 1468 -1471 . 2009 /0093454 Al 4 / 2009 Gudmundsson et al. Wenning , et al. , Lack of Significant Drug Interaction between 2009 /0181902 AL 7 / 2009 Desai et al . Raltegravir and Tenofovir , Antimicrobial Agents and Chemotherapy 2009 /0318421 Al 12 / 2009 Johns et al . ( 2008 ) 52 ( 9 ) : 3253 - 3258 . 2011/ 0076276 Al 3 / 2011 Guo et al . Notice of Publication of Eurasian Search Report with the Search Report - English Translations of both documents . FOREIGN PATENT DOCUMENTS Stellbrink , Hans - Jurgen , Novel compounds for the treatment of HIV EP 1 544 199 6 / 2005 type 1 infection , Antiviral Chemistry and Chemotherapy (2009 ) EP 1874117 2 / 2006 19 : 189 - 200 , pp . 189 -190 . JP 4295353 4 / 2009 Arribas , et al. , Once -daily S /GSK1349572 as part of combination WO 91/ 17159 11 / 1991 therapy in antiretroviral naive adults : rapid and potent antiviral WO 95 / 33464 12 / 1995 responses in the interim 16 -week analysis from Spring - 1 ( ING112276 ) , WO 96 / 30025 10 / 1996 XVIII International Aids Conference , Jul. 18 - 23 , 2010 , Vienna, WO 97 / 21685 6 / 1997 Austria , Abstract , www .aids2010 .org ( http : // pag . aids2010 .org WO 99 /48371 9 / 1999 Abstracts. aspx ? AID = 17600 . WO WO 2003 /016306 2 / 2003 Brown, et al. , Drug Interactions with New and Investigational WO WO 2004 /002433 1 / 2004 Antiretrovirals , Clinical Pharmacokinetics (2009 ) 48 ( 4 ) : 211 - 241. WO WO 2005 /021001 3 / 2005 WO 2005112930 12 / 2005 Chesney , Adherence to HAART Regimens, ( 2003 ) AIDS Patient WO WO 2006 /024668 3 / 2006 Care and STDS , 17 ( 4 ) . WO 2006 /096444 9 / 2006 Damond , et al. , Virological and immunological response to HAART WO 2006 / 116764 11 / 2006 regimen containing integrase inhibitor in HIV - 2 - infected patients , WO 2007 / 079260 7 / 2007 ( 2008 ) AIDS 22 ( 5 ) : 663- 668 , pp . 665 - 666 WO 2007082922 7 / 2007 De Clercq , Anti -HIV drugs : 25 compounds approved within 25 WO 2008 / 011117 1 /2008 years after the discovery of HV , International Journal of Antimi WO 2008 /042240 4 / 2008 crobial Agents , ( 2009 ) 33 :307 -320 . WO 2008 / 103949 8 / 2008 De Clercq , Perspectives of non - nucleoside reverse transcriptase WO 2008 / 1103899 8 / 2008 inhibitors (NNRTIs ) in the therapy of HIV - infection , ( 1999 ) II WO 2009 /005674 1 /2009 WO 2009 /005693 1 / 2009 Farmaco 54 :26 -45 . WO 2009 /007441 1 / 2009 Drug Data Report (2010 ) 32 ( 9 ) :893 - 895 . WO 2009 /008989 1 / 2009 EPZICOM® Prescribing Information . WO 2009 /058923 5 /2009 EPZICOM® Package Insert . WO 2009 / 059243 5 / 2009 Eron , et al ., Dolutegravir treatment response by baseline viral load WO 2009 /082810 7 / 2009 and NRTI backbone in treatment- naïve HIV - infected individuals, WO 2009 /082818 7 / 2009 Poster Abstract — P204 , Journal of the Int ' l AIDS Society (2012 ) WO 2009 /082819 7 / 2009 15 (Suppl 4 ) : 18264 .
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