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( 12 ) United States Patent US010392434B2 (12 ) United States Patent (10 ) Patent No. : US 10 , 392 ,434 B2 Bigal et al. (45 ) Date of Patent: Aug . 27 , 2019 ( 54 ) TREATING REFRACTORY MIGRAINE 5 ,851 , 556 A 12 / 1998 Breton et al. 5 , 932 ,215 A 8 / 1999 De Lacharriere et al. 5 , 935 , 586 A 8 / 1999 De Lacharriere et al . ( 71 ) Applicant: Teva Pharmaceuticals International 5 , 938 , 586 A 8 / 1999 De Lacharriere et al. GmbH , Jona (CH ) 6 , 168 , 809 B1 1 /2001 De Lacharriere et al. 6 , 180 ,370 B1 1 /2001 Queen et al. (72 ) Inventors : Marcelo Bigal, Doylestown , PA (US ) ; 6 ,313 ,097 B1 11 / 2001 Eberlein et al. Ernesto Aycardi, Andover, MA (US ) 6 , 344 , 438 B1 2 /2002 De Lacharriere et al. 6 , 344 ,449 B1 2 / 2002 Rudolf et al. 6 , 509 ,014 B1 1 / 2003 De Lacharriere et al. ( 73 ) Assignee : Teva Pharmaceuticals International 6 , 521 ,609 B1 2 / 2003 Doods et al . GmbH , Jona ( CH ) 6 ,552 ,043 B1 4 / 2003 Patchett et al. 6 ,586 ,458 B1 7 / 2003 Plachetka ( * ) Notice : Subject to any disclaimer , the term of this 6 ,737 ,056 B1 5 / 2004 Presta patent is extended or adjusted under 35 6 , 767 ,056 B2 5 /2004 Presta 7 , 109 , 214 B2 9 / 2006 Zimmer et al . U . S . C . 154 (b ) by 0 days . 7 , 384 . 930 B2 6 / 2008 Chaturvedula et al. 7 ,479 , 488 B2 1 / 2009 Mueller et al. ( 21) Appl. No .: 15 /712 ,444 7 ,772 ,224 B2 8 / 2010 Paone et al . 8 , 007 , 794 B2 8 / 2011 Zeller et al. 8 , 168 , 592 B2 5 / 2012 Gegg , Jr. et al . ( 22) Filed : Sep . 22 , 2017 8 , 293 , 239 B2 10 / 2012 Poulsen et al. 8 , 298 , 536 B2 10 /2012 Poulsen et al. (65 ) Prior Publication Data 8 ,586 ,045 B2 11 / 2013 Zeller et al . US 2018 /0127490 A1 May 10 , 2018 8 , 597 ,649 B2 12 /2013 Zeller et al . 8 ,623 ,366 B2 1 /2014 Pios et al . 8 ,669 , 368 B2 3 / 2014 Leahy et al . Related U . S . Application Data 8 ,734 , 802 B1 5 / 2014 Zeller et al . 9 , 115 , 194 B2 8 / 2015 Zeller et al . (60 ) Provisional application No. 62/ 399, 180 , filed on Sep . 9 , 266 , 951 B2 2 /2016 Zeller et al. 23 , 2016 , provisional application No . 62 / 558 , 557 , 9 , 328 , 167 B2 5 /2016 Poulsen et al . 9 , 328 , 168 B2 5 /2016 Zeller et al. filed on Sep . 14 , 2017 . 9 , 340 ,614 B2 5 / 2016 Zeller et al. 9 , 346 ,881 B2 5 /2016 Zeller et al . (51 ) Int . CI. 9 , 365 ,648 B1 6 / 2016 Zeller et al . A61K 9 / 00 ( 2006 .01 ) 9 , 505 , 838 B2 11 /2016 Allan et al. A61K 39 / 00 ( 2006 . 01 ) A61K 45 / 06 ( 2006 .01 ) (Continued ) A61P 25 / 06 ( 2006 . 01 ) FOREIGN PATENT DOCUMENTS CO7K 16 / 18 ( 2006 .01 ) A61K 39 /395 ( 2006 . 01) CA 2563687 11 / 2005 U . S . CI. CN 1308676 8 / 2001 CPC .. .. COZK 16 / 18 ( 2013 . 01 ) ; A61K 9 / 0019 (Continued ) ( 2013 .01 ) ; A61K 39 / 3955 ( 2013 .01 ) ; A61K 45 / 06 ( 2013 .01 ) ; A61P 25 / 06 (2018 .01 ) ; A61K OTHER PUBLICATIONS 2039 / 505 ( 2013 .01 ) ; A61K 2039 / 54 ( 2013 .01 ) ; A61K 2039 /545 (2013 . 01) ; COZK 2317 / 21 Chen “ Enhancement and destruction of antibody function by somatic (2013 .01 ) ; COZK 2317 / 24 (2013 .01 ) ; COOK mutation : unequal occurrence is controlled by V gene combinatorial 2317 / 33 (2013 .01 ) ; CO7K 2317 /34 (2013 .01 ) ; associations ” EMBO Journal vol . 14 No . 1 2 pp . 2784 - 2794 ( Year : CO7K 2317 /55 (2013 .01 ) ; CO7K 2317/ 56 1995 ) . * (2013 .01 ) ; C07K 2317 /565 ( 2013 . 01 ) ; CO7K (Continued ) 2317 /76 (2013 .01 ) ; CO7K 2317 /92 (2013 . 01 ) ; CO7K 2317 / 94 (2013 .01 ) Primary Examiner — Adam Weidner (58 ) Field of Classification Search None ( 74 ) Attorney, Agent, or Firm — Fish & Richardson P . C . See application file for complete search history . ( 57 ) ABSTRACT ( 56 ) References Cited Disclosed herein are methods of treating or reducing inci U . S . PATENT DOCUMENTS dence of migraine and / or at least one secondary symptom associated with refractory migraine in a subject having 4 ,816 , 567 A 3 / 1989 Cabilly et al. refractory migraine comprising administering to the subject 5 , 116 , 964 A 5 / 1992 Capon et al. 5 , 500 , 362 A 3 / 1996 Robinson et al. a monoclonal antibody that modulates the CGRP pathway . 5 , 545 , 806 A 8 / 1996 Longberg et al . Compositions for use in the disclosed methods are also 5 , 545 , 807 A 8 / 1996 Surani et al. provided . Antagonist antibody G1 and antibodies derived 5 , 569 , 825 A 10 / 1996 Longberg et al. from G1 directed to CGRP are also described . 5 ,625 , 126 A 4 / 1997 Longberg et al . 5 ,633 , 425 A 5 / 1997 Longberg et al . 5 ,661 , 016 A 8 / 1997 Longberg et al. 5 , 750 , 373 A 5 / 1998 Garrard et al. 13 Claims, 8 Drawing Sheets 5 , 821 , 337 A 10 / 1998 Carter et al . Specification includes a Sequence Listing . US 10 ,392 ,434 B2 Page 2 (56 ) References Cited WO WO 1998 /008630 3 / 1998 WO WO 1998 / 009630 3 / 1998 U . S . PATENT DOCUMENTS WO WO 1998 /011128 3 / 1998 WO WO 1998 /056779 12 / 1998 9 , 884 ,907 B2 2 / 2018 Zeller et al . WO WO 1999 /058572 11 / 1999 9 , 884 , 908 B2 2 / 2018 Zeller et al . WO WO 2000 /018764 4 / 2000 9 , 890 , 210 B2 2 / 2018 Zeller et al . Wo WO 2001 /027160 4 / 2001 9 , 890 ,211 B2 2 / 2018 Zeller et al . wo WO 2003 / 027252 4 / 2003 9 ,896 ,502 B2 2 / 2018 Bigal et al. wo WO 2003/ 093472 11 / 2003 2001/ 0036946 A1 11/ 2001 Rudulf et al . WO WO 2003 / 104236 12 / 2003 2002 /0162125 Al 10 / 2002 Salmon et al. WO WO 2004 / 003019 1 / 2004 2002 /0164707 AL 11/ 2002 Adamou et al . WO WO 2004 /014351 2 / 2004 2003 / 0069231 A1 4 / 2003 Rudolf et al . WO WO 2004 /050683 6 / 2004 2003 /0194404 Al 10 / 2003 Greenfeder et al. WO WO 2004 /082602 9 / 2004 2004 /0110170 A1 6 / 2004 Pisegna et al . WO WO 2004 / 082605 9 / 2004 2005 / 0234054 Al 10 / 2005 Mueller et al. WO WO 2004 /082678 9 / 2004 2006 / 0183700 A18 / 2006 Vater et al. WO WO 2004 /083187 9 / 2004 2009 / 0220489 A1 * 9 / 2009 Zeller . .. CO7K 16 / 26 WO WO 2004 /087649 10 / 2004 424 / 130 . 1 WO WO 2004 / 091514 10 / 2004 2010 / 0172895 A17 / 2010 Boone et al. WO WO 2004 / 092166 10 / 2004 2011/ 0054150 AL 3 / 2011 Poulsen et al. Wo WO 2004 /092168 10 / 2004 2011 /0257371 A1 10 / 2011 Poulsen et al . wo WO 2004 /097421 11 / 2004 2011 /0305711 Al 10 / 2011 Poulsen et al . WO WO 2005 /009962 2 / 2005 2012 / 0009192 AL 1 / 2012 Zeller et al . WO WO 2005 /041757 5 /2005 2012 / 0225075 AL 9 / 2012 Pios et al. WO WO 2005 / 100360 10 / 2005 2012 / 0294797 AL 11/ 2012 Kovacevich et al . WO WO 2006 / 077212 7 / 2006 2012 / 0294802 Al 11/ 2012 Russo et al . WO WO 2007 / 025212 3 / 2007 2012 /0294822 AL 11/ 2012 Russo et al . WO WO 2007 /025286 3 /2007 2013 / 0216535 A1 8 / 2013 Zeller et al . WO WO 2007 /035906 3 / 2007 2013 / 0295087 AL 11/ 2013 Poulsen et al . WO WO 2007 /048026 4 / 2007 2013 / 0295088 AL 11 / 2013 Poulsen et al . WO WO 2007 / 054809 5 / 2007 2014 /0147438 AL 5 / 2014 Zeller et al . WO WO 2007 /061676 5 / 2007 2014 /0308290 Al 10 / 2014 Pios et al. WO WO 2007 / 076336 7 / 2007 2014 / 0314767 Al 10 / 2014 Pios et al . WO WO 2008 /011190 1 /2008 2015 /0050267 AL 2 / 2015 Zeller et al . WO WO 2008 /097824 8 / 2008 2015 /0259415 AL 9 / 2015 Allan et al. WO WO 2009 /055350 4 / 2009 2015 /0266948 AL 9 / 2015 Bigal et al . WO WO 2009 / 109908 9 / 2009 2015 / 0291690 A1 10 /2015 Zeller et al . WO WO 2009 / 109911 9 / 2009 2015 /0302690 A1 10 / 2015 Poulsen et al. WO WO 2010 /006168 1 / 2010 WO WO 2010 /075238 7 / 2010 2015 / 0307607 A1 11/ 2015 Bigal et al. WO WO 2011 /024113 3 / 2011 2015/ 0322142 Al 12/ 2015 Zeller et al . WO WO 2011/ 156324 12 / 2011 2015 /0361171 Al 12/ 2015 Zeller et al . wo WO 2012 / 162243 11/ 2012 2015 /0361172 Al 12 / 2015 Zeller et al. WO WO 2012 / 162253 11 / 2012 2015 /0361173 A1 12 / 2015 Zeller et al . wo WO 2012 / 162257 11/ 2012 2015 /0376286 A1 12 / 2015 Boone et al. WO WO 2013 /028635 2 / 2013 2016 /0168244 A1 2 / 2016 Zeller et al . WO WO 2014 / 145650 9 / 2014 2016 /0311913 Al 10 / 2016 Sun et al . Wo WO 2014 / 146074 9 / 2014 2017 /0044243 Al 2 / 2017 Poulsen et al . WO WO 2015 /003122 1 / 2015 2017 / 0073403 A1 3 / 2017 Allan et al . WO WO 2016 /044224 3 / 2016 2017 / 0073412 AL 3 / 2017 Pios et al. WO WO 2016 / 171742 10 /2016 2017 / 0081395 A1 3 / 2017 Zeller et al . WO WO 2016 / 205037 12 / 2016 2017/ 0088612 Al 3 / 2017 Bigal et al. OTHER PUBLICATIONS FOREIGN PATENT DOCUMENTS Kussie “ A Single Engineered Amino Acid Substitution Changes CN 1671711 9 / 2005 EP 0212432 3 / 1987 Antibody Fine Specificity ” J immunol 152 ( 1 ) : 146 -52 ( Year : 1994 ). * EP 1031350 8 / 2000 U . S . Appl. No. 13 /621 , 981 , filed Sep . 18 , 2012 , Poulsen et al. EP 1556020 7 / 2005 U .
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