11111111111111111111111111f1JIIIR1111111111111111111111111
`
`US008846695B2
`
`(12) United States Patent (cid:9)
`(12) United States Patent
`Dugi
`Dugi
`
`(10) Patent No.: (cid:9)
`(10) Patent N0.:
`(45) Date of Patent: (cid:9)
`(45) Date of Patent:
`
`US 8,846,695 B2
`US 8,846,695 B2
`Sep. 30, 2014
`Sep. 30, 2014
`
`(54) TREATMENT FOR DIABETES IN PATIENTS
`(54) TREATMENT FOR DIABETES IN PATIENTS
`WITH INADEQUATE GLYCEMIC CONTROL
`WITH INADEQUATE GLYCEMIC CONTROL
`DESPITE METFORMIN THERAPY
`DESPITE METFORMIN THERAPY
`COMPRISING A DPP-IV INHIBITOR
`COMPRISING A DPP-IV INHIBITOR
`
`(75) Inventor: Klaus Dugi, Dresden (DE)
`(75) Inventor: Klaus Dugi, Dresden (DE)
`
`(73) Assignee: Boehringer Ingelheim International
`(73) Assignee: Boehringer Ingelheim International
`GmbH, Ingelheim am Rhein (DE)
`GmbH, Ingelheim am Rhein (DE)
`
`( * ) Notice:
`( * ) Notice:
`
`Subject to any disclaimer, the term of this
`Subject to any disclaimer, the term of this
`patent is extended or adjusted under 35
`patent is extended or adjusted under 35
`U.S.C. 154(b) by 148 days.
`U.S.C. 154(b) by 148 days.
`
`(21) App1.No.:
`(21) Appl. No.:
`
`13/143,370
`13/143,370
`
`(22) PCT Filed:
`(22) PCT Filed:
`
`Jan. 7, 2010
`Jan. 7, 2010
`
`(86) PCT No.:
`(86) PCT No.:
`§ 371 (0X1)’
`§ 371 (c)(1),
`(2), (4) Date:
`(2), (4) Date: (cid:9)
`
`PCT/EP2010/050103
`PCT/EP2010/050103
`
`Aug. 18, 2011
`Aug. 18, 2011
`
`(87) PCT Pub. No.: W02010/079197
`(87) PCT Pub. No.: WO2010/079197
`
`PCT Pub. Date: Jul. 15, 2010
`PCT Pub. Date: Jul. 15, 2010
`
`(65)
`(65) (cid:9)
`
`(30)
`(30) (cid:9)
`
`Prior Publication Data
`Prior Publication Data
`
`US 2011/0301182 Al (cid:9)
`US 2011/0301182 A1
`
`Dec. 8, 2011
`Dec. 8,2011
`
`Foreign Application Priority Data
`Foreign Application Priority Data
`
` 09150159
`Jan. 7, 2009 (EP) (cid:9)
`Jan. 7, 2009 (EP) ................................... .. 09150159
`
`(2006.01)
`(2006.01)
`
`(51) Int. Cl.
`(51) Int. Cl.
`A61K 31/52 (cid:9)
`A61K 31/52
`(52) U.S. Cl.
`(52) US. Cl.
` 514/263.21
`USPC (cid:9)
`USPC ................................................... .. 514/263.21
`(58) Field of Classification Search
`(58) Field of Classi?cation Search
`USPC (cid:9)
` 514/263.21
`USPC ................................................... .. 514/263.21
`See application ?le for complete search history.
`See application file for complete search history.
`
`(56) (cid:9)
`(56)
`
`References Cited
`References Cited
`
`U.S. PATENT DOCUMENTS
`U.S. PATENT DOCUMENTS
`
`2,056,046
`Fourneau
`9/1936
`2,056,046 A
`9/1936 Fourneau
`2,375,138
`5/1945
`Victors
`2,375,138 A
`5/1945 Victors
`2,629,736
`2/1953
`Krimmel
`2,629,736 A
`2/1953 Krimmel
`2,730,544
`1/1956
`Sahyun
`2,730,544 A
`1/1956 Sahyun
`2,750,387
`6/1956
`Krimmel
`2,750,387 A
`6/1956 Krimmel
`2,928,833
`3/1960
`Leake et al.
`2,928,833 A
`3/1960 Leake et a1.
`3,174,901
`3/1965
`Sterne
`3,174,901 A
`3/1965 Sterne
`3,236,891
`2/1966
`Seemuller
`3,236,891 A
`2/1966 Seemuller
`3,454,635
`7/1969
`Muth
`3,454,635 A
`7/1969 Muth
`3,673,241
`6/1972
`Marxer
`3,673,241 A
`6/1972 Marxer
`3,925,357
`12/1975
`Okada et al.
`3,925,357 A 12/1975 Okadaet a1.
`1/1977
`Bender et al.
`4,005,208
`1/1977 Bender et al.
`4,005,208 A
`12/1977
`Bodor et al.
`4,061,753
`4,061,753 A 12/1977 Bodor et a1.
`5/1983
`Benjamin et al.
`4,382,091
`5/1983 Benjamin etal.
`4,382,091 A
`7/1986
`Regnier et al.
`4,599,338
`7/1986 Regnieret a1.
`4,599,338 A
`1/1987
`Junge et al.
`4,639,436
`1/1987 Junge et al.
`4,639,436 A
`8/1987
`Meguro et al.
`4,687,777
`8/1987 Meguro et a1.
`4,687,777 A
`5/1988
`Harris et al.
`4,743,450
`5/1988 Harris et a1.
`4,743,450 A
`3/1989
`Schickaneder et al.
`4,816,455
`3/1989 Schickaneder et al.
`4,816,455 A
`10/1989
`Lindholm
`4,873,330
`4,873,330 A 10/1989 Lindholm
`11/1990
`Jacobson et al.
`4,968,672
`4,968,672 A 11/1990 Jacobson et al.
`8/1991
`Janssens et al.
`5,041,448
`5,041,448
`8/1991 Janssens et al.
`A
`9/1991
`Findeisen et al.
`5,051,517
`5,051,517
`9/1991 Findeisen et al.
`A
`
`Munson, Jr. et al.
`1/1992
`5,084,460 A (cid:9)
`1/1992 Munson, Jr. et al.
`5,084,460 A
`7/1992
`5,130,244 A (cid:9)
`Nishimaki et al.
`7/1992 Nishimaki et a1.
`5,130,244 A
`6/1993
`5,219,870 A (cid:9)
`Kim
`6/1993 Kim
`5,219,870 A
`6/1993
`5,223,499 A (cid:9)
`Greenlee et al.
`6/1993 Greenlee et a1.
`5,223,499 A
`8/1993
`5,234,897 A (cid:9)
`Findeisen et al.
`8/1993 Findeisen et al.
`5,234,897 A
`11/1993
`5,258,380 A (cid:9)
`Janssens et al.
`5,258,380 A 11/1993 Janssens et al.
`5,266,555 A (cid:9)
`11/1993
`Findeisen et al.
`5,266,555 A 11/1993 Findeisen et al.
`5,273,995 A (cid:9)
`12/1993
`Roth
`5,273,995 A 12/1993 Roth
`5,284,967 A (cid:9)
`2/1994
`Macher
`5,284,967 A
`2/1994 Macher
`5,300,298 A (cid:9)
`4/1994
`Lalloue
`5,300,298 A
`4/1994 LaNoue
`5,329,025 A (cid:9)
`7/1994
`Wong et al.
`5,329,025 A
`7/1994 Wong et a1.
`5,332,744 A (cid:9)
`7/1994
`Chakravarty et al.
`5,332,744 A
`7/1994 Chakravarty et a1.
`5,389,642 A (cid:9)
`2/1995
`Dorsch et al.
`5,389,642 A
`2/1995 Dorsch et a1.
`5,399,578 A (cid:9)
`3/1995
`Buhlmayer et al.
`5,399,578 A
`3/1995 Buhlmayer et al.
`5,407,929 A (cid:9)
`4/1995
`Takahashi et al.
`5,407,929 A
`4/1995 Takahashi et a1.
`5,470,579 A (cid:9)
`11/1995
`Bonte et al.
`5,470,579 A 11/1995 Bonte et a1.
`5,591,762 A (cid:9)
`1/1997
`Hauel et al.
`5,591,762 A
`1/1997 Hauel et a1.
`5,594,003 A (cid:9)
`1/1997
`Hauel et al.
`5,594,003 A
`1/1997 Hauel et a1.
`5,602,127 A (cid:9)
`2/1997
`Hauel et al.
`5,602,127 A
`2/1997 Hauel et a1.
`5,614,519 A (cid:9)
`3/1997
`Hauel et al.
`5,614,519 A
`3/1997 Hauel et a1.
`5,719,279 A (cid:9)
`2/1998
`Kufner-Muhl et al.
`5,719,279 A
`2/1998 Kufner-Muhl et al.
`5,728,849 A (cid:9)
`3/1998
`Bouchard et al.
`5,728,849 A
`3/1998 Bouchard et al.
`5,753,635 A (cid:9)
`5/1998
`Buckman et al.
`5,753,635 A
`5/1998 Buckman et a1.
`5,830,908 A (cid:9)
`11/1998
`Grunenberg et al.
`5,830,908 A 11/1998 Grunenberg et al.
`(Continued)
`(Continued)
`
`FOREIGN PATENT DOCUMENTS
`FOREIGN PATENT DOCUMENTS
`
`AU
`AU
`AU
`AU
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`
`6/2004
`2003280680 Al
`6/2004
`2003280680 A1
`9/2009
`2009224546 Al
`9/2009
`2009224546 A1
`5/1982
`1123437 Al
`5/1982
`1123437 A1
`5/1995
`2136288 Al
`5/1995
`2136288 A1
`2/2002
`2418656 Al
`2/2002
`2418656 A1
`3/2004
`2496249 Al
`3/2004
`2496249 A1
`3/2004
`2496325 Al
`3/2004
`2496325 A1
`4/2004
`2498423 Al
`4/2004
`2498423 A1
`5/2004
`2505389 Al
`5/2004
`2505389 A1
`6/2004
`2508233 Al
`6/2004
`2508233 A1
`(Continued)
`(Continued)
`
`OTHER PUBLICATIONS
`OTHER PUBLICATIONS
`
`Eckhardt et al., Journal of Med. Chem., 2007, 50:6450-6453.*
`Eckhardt et al., Journal of Med. Chem., 2007, 50:6450-6453.*
`Graefe-Mody et al. publication, Current Medical Research and Opin
`Graefe-Mody et al. publication, Current Medical Research and Opin-
`ion, 2009, 25(8): 1963-1972.*
`ion, 2009, 25(8): 1963-1972.*
`International Search Report and Written Opinion for PCT/EP2010/
`International Search Report and Written Opinion for PCT/EP2010/
`050103 mailed Mar. 22, 2010.
`050103 mailed Mar. 22, 2010.
`International Search Report and Written Opinion for PCT/EP2011/
`International Search Report and Written Opinion for PCT/EP2011/
`057163 mailed Jun. 27, 2011.
`057163 mailed Jun. 27, 2011.
`International Search Report for PCT/EP2008/060740 mailed Mar.
`International Search Report for PCT/EP2008/060740 mailed Mar.
`30, 2009.
`30, 2009.
`International Search Report for PCT/EP2010/051093 mailed Jul. 14,
`International Search Report for PCT/EP2010/051093 mailed Jul. 14,
`2010.
`2010.
`
`(Continued)
`(Continued)
`
`Primary Examiner — Rei-tsang Shiao
`Primary Examiner * Rei-tsang Shiao
`(74) Attorney, Agent, or Firm — Michael P. Morris; David L.
`(74) Attorney, Agent, 0rFirm * Michael P. Morris; David L.
`Kershner
`Kershner
`
`(57)
`(57) (cid:9)
`
`ABSTRACT
`ABSTRACT
`
`The present invention relates to the finding that certain DPP-4
`The present invention relates to the ?nding that certain DPP-4
`inhibitors are particularly suitable for improving glycemic
`inhibitors are particularly suitable for improving glycemic
`control in type 2 diabetes patients With inadequate glycemic
`control in type 2 diabetes patients with inadequate glycemic
`control despite metformin therapy.
`control despite metformin therapy.
`
`4 Claims, No Drawings
`4 Claims, No Drawings
`
`Mylan EX 1001, Page 1
`
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`(cid:9)
`

`
`US 8,846,695 B2
`US 8,846,695 B2
`Page 2
`Page 2
`
`(56)
`(56) (cid:9)
`
`References Cited
`References Cited (cid:9)
`
`U_g_ PATENT DOCUMENTS
`U.S. PATENT DOCUMENTS (cid:9)
`
`5 879 708 A
`3/1999 Makino et al‘
`5,879,708 A
`Makino et al. (cid:9)
`3/1999
`5’958’951 A
`9/1999 Ahmdt et 31‘
`5,958,951 A
`Ahrndt et al. (cid:9)
`9/1999
`5’965’555 A 10/1999 Gebert etal,
`Gebert et al. (cid:9)
`5,965,555 A
`10/1999
`5:965:59; A 10/1999 Buhlmayeretal,
`Buhlmayer et al. (cid:9)
`5,965,592 A
`10/1999
`1/2000 Whitcomb
`6011049 A
`Whitcomb (cid:9)
`6,011,049 A
`1/2000
`80000 Carter et 31‘
`6’107’302 A
`Carter et al. (cid:9)
`6,107,302 A
`8/2000
`6’166’063 A 12/2000 Villhauer
`Villhauer (cid:9)
`6,166,063 A
`12/2000
`@2001 Klokkers et 31‘
`6’248’758 B1
`Klokkers et al. (cid:9)
`6,248,758 B1
`6/2001
`10/2001 Demuth et 31‘
`633033661 B1
`Demuth et al. (cid:9)
`6,303,661 B1
`10/2001
`1/2002 Bantick et a1,
`6342 601 B1
`Bantick et al. (cid:9)
`6,342,601 B1
`1/2002
`4/2002 (3mm
`6’372’940 B1
`Cavazza (cid:9)
`6,372,940 B1
`4/2002
`4/2003 Demuth et 31‘
`6’548’481 B1
`Demuth et al. (cid:9)
`6,548,481 B1
`4/2003
`600% Asano etal‘
`6’579’868 B1
`Asano et al. (cid:9)
`6,579,868 B1
`6/2003
`4/2004 Gobbi et 31‘
`6’727’261 B2
`Gobbi et al. (cid:9)
`6,727,261 B2
`4/2004
`8/2004 Hale and,
`6’784’195 B2
`Hale et al. (cid:9)
`6,784,195 B2
`8/2004
`6’821’978 B2 11/2004 Chackalamannil et 31‘
`Chackalamann 1 et al. (cid:9)
`6,821,978 B2
`11/2004
`3/2005 Kmth and,
`638693947 B2
`Kanstrup et al. (cid:9)
`6,869,947 B2
`3/2005
`2/2006 Hamann etal‘
`6,995,183 B2
`Hamann et al. (cid:9)
`6,995,183 B2
`2/2006
`6/2006 Kitajima et a1,
`7,060,722 B2
`Kitajima et al. (cid:9)
`7,060,722 B2
`6/2006
`7/2006 Kitajima et a1,
`7,074,794 B2
`Kitajima et al. (cid:9)
`7,074,794 B2
`7/2006
`7/2006 Yoshikawa et al‘
`7074 798 B2
`Yoshikawa et al. (cid:9)
`7,074,798 B2
`7/2006
`7/2006 Dahanukar etal‘
`7’074’923 B2
`Dahanukar et al. (cid:9)
`7,074,923 B2
`7/2006
`9/2006 Hauel et 31‘
`7’109’192 B2
`Hauel et al. (cid:9)
`7,109,192 B2
`9/2006
`2/2007 Eckhardt et al‘
`7,179,809 B2
`Eckhardt et al. (cid:9)
`7,179,809 B2
`2/2007
`2/2007 Himmelsbach etal‘
`7’183’280 B2
`Himmelsbach et al. (cid:9)
`7,183,280 B2
`2/2007
`3/2007 Kanstmp etal‘
`731922952 B2
`Kanstrup et al. (cid:9)
`7,192,952 B2
`3/2007
`5/2007 Eckhardt et al‘
`7217711 B2
`Eckhardt et al. (cid:9)
`7,217,711 B2
`5/2007
`6/2007 Kmth and,
`732352538 B2
`Kanstrup et al. (cid:9)
`7,235,538 B2
`6/2007
`7/2007 Eberhardt et a1,
`7,247,478 B2
`Eberhardt et al. (cid:9)
`7,247,478 B2
`7/2007
`7,291,642 B2 11/2007 Kauffmann_Hefner et a1,
`Kauffmann-Hefner et al. (cid:9)
`7,291,642 B2
`11/2007
`4/2008 Barth et 31‘
`7361687 B2
`Barth et al. (cid:9)
`7,361,687 B2
`4/2008
`7/2008 Eckhardtet 31‘
`733932847 B2
`Eckhardt et al. (cid:9)
`7,393,847 B2
`7/2008
`8/2008 Himmelsbach etal.
`7,407,955 B2
`Himmelsbach et al. (cid:9)
`7,407,955 B2
`8/2008
`7432 262 B2 10/2008 Eckhardt et al‘
`Eckhardt et al. (cid:9)
`7,432,262 B2
`10/2008
`7’439’370 B2 10/2008 Eckhardt
`Eckhardt (cid:9)
`7,439,370 B2
`10/2008
`7’470’716 B2 @2008 Eckhardt et 31‘
`Eckhardt et al. (cid:9)
`7,470,716 B2
`12/2008
`1/2009 Eckhardt et 31‘
`734763671 B2
`Eckhardt et al. (cid:9)
`7,476,671 B2
`1/2009
`1/2009 Himmelsbach etal.
`7,482,337 B2
`Himmelsbach et al. (cid:9)
`7,482,337 B2
`1/2009
`2/2009 Langkopfet 31‘
`7,495,002 B2
`Langkopf et al. (cid:9)
`7,495,002 B2
`2/2009
`2/2009 Eckhardt et a1,
`7495 003 B2
`Eckhardt et al. (cid:9)
`7,495,003 B2
`2/2009
`2/2009 Himmelsbach et 31‘
`7,495,005 B2
`Himmelsbach et al. (cid:9)
`7,495,005 B2
`2/2009
`3/2009 Himmelsbach et 31‘
`735013426 B2
`Himmelsbach et al. (cid:9)
`7,501,426 B2
`3/2009
`6/2009 Himmelsbach etal.
`7,550,455 B2
`Himmelsbach et al. (cid:9)
`7,550,455 B2
`6/2009
`7/2009 Eckhardt et al‘
`7 560 450 B2
`Eckhardt et al. (cid:9)
`7,560,450 B2
`7/2009
`7/2009 Eckhardt et 31‘
`7’566’707 B2
`Eckhardt et al. (cid:9)
`7,566,707 B2
`7/2009
`8/2009 Mal-er et 31‘
`7’569’574 B2
`Maier et al. (cid:9)
`7,569,574 B2
`8/2009
`8/2009 Eckhardt et 31‘
`7’579’449 B2
`Eckhardt et al. (cid:9)
`7,579,449 B2
`8/2009
`736103153 B2 10/2009 Carter, hem,
`Carter, Jr. et al. (cid:9)
`7,610,153 B2
`10/2009
`1/2010 Himmelsbach etal.
`7,645,763 B2
`Himmelsbach et al. (cid:9)
`7,645,763 B2
`1/2010
`5/2010 Boehringer et a1,
`7,718,666 B2
`Boehringer et al. (cid:9)
`7,718,666 B2
`5/2010
`9/2010 Munson et al‘
`7,799,782 B2
`Munson et al. (cid:9)
`7,799,782 B2
`9/2010
`7,820,815 B2 10/2010 Pfrengle et a1.
`Pfrengle et al. (cid:9)
`7,820,815 B2
`10/2010
`7 838 529 B2 11/2010 Himmelsbach et 31‘
`Himmelsbach et al. (cid:9)
`7,838,529 B2
`11/2010
`8,039,477 B2 10/2011 Hendrix et al‘
`Hendrix et al. (cid:9)
`8,039,477 B2
`10/2011
`8’071’583 B2 12/2011 Himmelsbach
`Himmelsbach (cid:9)
`8,071,583 B2
`12/2011
`1001; Pfrengle et 31‘
`831062060 B2
`Pfrengle et al. (cid:9)
`8,106,060 B2
`1/2012
`2/2012 Himmelsbach et 31‘
`8119648 B2
`Himmelsbach et al. (cid:9)
`8,119,648 B2
`2/2012
`4/2012 Hendrix et 31‘
`8’158’633 B2
`Hendrix et al. (cid:9)
`8,158,633 B2
`4/2012
`5/2012 Himmelsbach et 31‘
`8,178,541 B2
`Himmelsbach et al. (cid:9)
`8,178,541 B2
`5/2012
`7/2012 Dugietal,
`832323281 B2
`Dugi et al. (cid:9)
`8,232,281 B2
`7/2012
`9/2001 Demuth et a1.
`2001/0020006 A1
`Demuth et al. (cid:9)
`2001/0020006 Al
`9/2001
`2001/0051646 A1 12/2001 Demuth et a1.
`Demuth et al. (cid:9)
`2001/0051646 Al
`12/2001
`2/2002 Robletal'
`2002/0019411 A1
`Robl et al. (cid:9)
`2002/0019411 Al
`2/2002
`9/2002 Ellsworth et a1.
`2002/0137903 A1
`Ellsworth et al. (cid:9)
`2002/0137903 Al
`9/2002
`2002/0161001 A1 10/2002 Kanstrup etal.
`Kanstrup et al. (cid:9)
`2002/0161001 Al
`10/2002
`2002/0169174 A1 11/2002 Chackalamannil et a1.
`Chackalamannil et al. (cid:9)
`2002/0169174 Al
`11/2002
`2002/0198205 A1 12/2002 Himmelsbach etal.
`Himmelsbach et al. (cid:9)
`2002/0198205 Al
`12/2002
`Pearson et al. (cid:9)
`2003/0078269 Al
`4/2003
`4/2003 Pearson et a1.
`2003/0078269 A1
`Edmondson et al. (cid:9)
`2003/0100563 Al
`5/2003
`5/2003 Edmondson etal.
`2003/0100563 A1
`6/2003 Kanstrup etal.
`2003/0105077 A1
`Kanstrup et al. (cid:9)
`2003/0105077 Al
`6/2003
`Washburn et al. (cid:9)
`2003/0114390 Al
`6/2003
`6/2003 Washburn et a1.
`2003/0114390 A1
`Fujino et al. (cid:9)
`2003/0130313 Al
`7/2003
`7/2003 Fujino etal.
`2003/0130313 A1
`Gobbi et al. (cid:9)
`2003/0149071 Al
`8/2003
`8/2003 Gobbi et a1.
`2003/0149071 A1
`Arch et al. (cid:9)
`2003/0166578 Al
`9/2003
`9/2003 Arch et a1.
`2003/0166578 A1
`2003/0199528 A1 10/2003 Kanstrup etal.
`Kanstrup et al. (cid:9)
`2003/0199528 Al
`10/2003
`
`2003/0224043 A1 12/2003 Appelet a1.
`2003/0224043 Al 12/2003 Appel et al.
`2003/0232987 Al (cid:9)
`12/2003 Dahanukar et al.
`2003/0232987 A1 12/2003 Dahanukar etal.
`2003/0236272 Al 12/2003 Carr
`2003/0236272 A1 12/2003 Can
`2004/0023981 Al (cid:9)
`2/2004 Ren et al.
`2004/0023981 A1
`2/2004 Ren etal.
`2004/0034014 Al (cid:9)
`2/2004 Kanstrup et al.
`2004/0034014 A1
`2/2004 Kanstrup et al.
`2004/0063725 Al (cid:9)
`4/2004 Barth et al.
`2004/0063725 A1
`4/2004 Banh etal.
`2004/0077645 Al (cid:9)
`4/2004 Himmelsbach et al.
`2004/0077645 A1
`4/2004 Himmelsbach etal.
`2004/0082570 Al (cid:9)
`4/2004 Yoshikawa et al.
`2004/0082570 A1
`4/2004 Yoshikawaet al.
`2004/0087587 Al (cid:9)
`5/2004 Himmelsbach et al.
`2004/0087587 A1
`5/2004 Himmelsbach et a1.
`2004/0097510 Al (cid:9)
`5/2004 Himmelsbach et al.
`2004/0097510 A1
`5/2004 Himmelsbach etal.
`2004/0116328 Al (cid:9)
`6/2004 Yoshikawa et al.
`2004/0116328 A1
`6/2004 Yoshikawaet a1.
`2004/0122048 Al (cid:9)
`6/2004 Benjamin et al.
`2004/0122048 A1
`6/2004 Benjamin et a1.
`2004/0122228 Al (cid:9)
`6/2004 Maier et al.
`2004/0122228 A1
`6/2004 Maier et a1.
`2004/0126358 Al (cid:9)
`7/2004 Warne et al.
`2004/0126358 A1
`7/2004 Warne et al.
`2004/0138214 Al (cid:9)
`7/2004 Himmelsbach et al.
`2004/0138214 A1
`7/2004 Himmelsbach et a1.
`2004/0138215 Al (cid:9)
`7/2004 Eckhardt et al.
`2004/0138215 A1
`7/2004 Eckhardtetal.
`2004/0166125 Al (cid:9)
`8/2004 Himmelsbach et al.
`2004/0166125 A1
`8/2004 Himmelsbach et a1.
`2004/0171836 Al (cid:9)
`9/2004 Fujino et al.
`2004/0171836 A1
`9/2004 Fujino et a1.
`2004/0180925 Al (cid:9)
`9/2004 Matsuno et al.
`2004/0180925 A1
`9/2004 Matsuno et a1.
`2004/0259903 Al (cid:9)
`12/2004 Boehringer et al.
`2004/0259903 A1 12/2004 Boehringer et a1.
`2005/0020574 Al (cid:9)
`1/2005 Hauel et al.
`2005/0020574 A1
`1/2005 Hanel et a1.
`2005/0026921 Al (cid:9)
`2/2005 Eckhardt et al.
`2005/0026921 A1
`2/2005 Eckhardtet 31.
`2005/0032804 Al (cid:9)
`2/2005 Cypes et al.
`2005/0032804 A1
`2/2005 Cypes et a1.
`2005/0065145 Al (cid:9)
`3/2005 Cao et al.
`2005/0065145 A1
`3/2005 Cao et a1.
`2005/0070562 Al (cid:9)
`3/2005 Jones et al.
`2005/0070562 A1
`3/2005 Jones et a1.
`2005/0070594 Al (cid:9)
`3/2005 Kauschke et al.
`2005/0070594 A1
`3/2005 Kauschke et a1.
`2005/0130985 Al (cid:9)
`6/2005 Himmelsbach et al.
`2005/0130985 A1
`6/2005 Himmelsbach et a1.
`2005/0143377 Al (cid:9)
`6/2005 Himmelsbach et al.
`2005/0143377 A1
`6/2005 Himmelsbach et a1.
`2005/0171093 Al (cid:9)
`8/2005 Eckhardt et al.
`2005/0171093 A1
`8/2005 Eckhardtetal.
`2005/0187227 Al (cid:9)
`8/2005 Himmelsbach et al.
`2005/0187227 A1
`8/2005 Himmelsbach et al.
`2005/0203095 Al (cid:9)
`9/2005 Eckhardt et al.
`2005/0203095 A1
`9/2005 Eckhardt et 31.
`2005/0234108 Al (cid:9)
`10/2005 Himmelsbach et al.
`2005/0234108 A1 10/2005 Himmelsbach et a1.
`2005/0234235 Al (cid:9)
`10/2005 Eckhardt et al.
`2005/0234235 A1 10/2005 Eckhardt et 31.
`2005/0239778 Al (cid:9)
`10/2005 Konetzki et al.
`2005/0239778 A1 10/2005 KonetZki et al.
`2005/0256310 Al (cid:9)
`11/2005 Hulin et al.
`2005/0256310 A1 11/2005 Hulin et a1.
`2005/0261271 Al (cid:9)
`11/2005 Feng et al.
`2005/0261271 A1 11/2005 Feng etal.
`2005/0261352 Al (cid:9)
`11/2005 Eckhardt
`2005/0261352 A1 11/2005 150141th
`2005/0266080 Al (cid:9)
`12/2005 Desai et al.
`2005/0266080 A1 12/2005 D6831 et a1.
`2005/0276794 Al (cid:9)
`12/2005 Papas et al.
`2005/0276794 A1 12/2005 Papas etal.
`2006/0004074 Al (cid:9)
`1/2006 Eckhardt et al.
`2006/0004074 A1
`1/2006 Eckhardtetal.
`2006/0034922 Al (cid:9)
`2/2006 Cheng et al.
`2006/0034922 A1
`2/2006 Cheng et a1.
`2006/0039974 Al (cid:9)
`2/2006 Akiyama et al.
`2006/0039974 A1
`2/2006 Akiyama etal
`2006/0047125 Al (cid:9)
`3/2006 Leonardi et al.
`2006/0047125 A1
`3/2006 Leonardlet al.
`2006/0058323 Al (cid:9)
`3/2006 Eckhardt et al.
`2006/0058323 A1
`3/2006 Eckhardt et 31.
`2006/0063787 Al (cid:9)
`3/2006 Yoshikawa et al.
`2006/0063787 A1
`3/2006 Yoshikawa et a1.
`2006/0074058 Al (cid:9)
`4/2006 Holmes et al.
`2006/0074058 A1
`4/2006 Holmes et a1.
`2006/0079541 Al (cid:9)
`4/2006 Langkopf et al.
`2006/0079541 A1
`4/2006 Langkopfetal
`2006/0094722 Al (cid:9)
`5/2006 Yasuda et al.
`2006/0094722 A1
`5/2006 Yasuda et a1.
`2006/0100199 Al (cid:9)
`5/2006 Yoshikawa et al.
`2006/0100199 A1
`5/2006 Yoshikawa et a1.
`2006/0106035 Al (cid:9)
`5/2006 Hendrix et al.
`2006/0106035 A1
`5/2006 Hendrix etal.
`2006/0111372 Al (cid:9)
`5/2006 Hendrix et al.
`2006/0111372 A1
`5/2006 Hendrix etal.
`2006/0111379 Al (cid:9)
`5/2006 Guillemont et al.
`2006/0111379 A1
`5/2006 Guillemont et a1.
`2006/0134206 Al (cid:9)
`6/2006 Iyer et al.
`2006/0134206 A1
`6/2006 Iyeretal
`2006/0142310 Al (cid:9)
`6/2006 Pfrengle et al.
`2006/0142310 A1
`6/2006 Pfrengle et a1.
`2006/0154866 Al (cid:9)
`7/2006 Chu et al.
`2006/0154866 A1
`7/2006 Chu et a1.
`2006/0159746 Al (cid:9)
`7/2006 Troup et al.
`2006/0159746 A1
`7/2006 Tr_<>u_p etal
`2006/0173056 Al (cid:9)
`8/2006 Kitajima et al.
`2006/0173056 A1
`55/2006 K1ta]1maet a1.
`2006/0205711 Al (cid:9)
`9/2006 Himmelsbach et al.
`2006/0205711 A1
`9/2006 Himmelsbach et a1.
`2006/0205943 Al (cid:9)
`9/2006 Dahanukar et al.
`2006/0205943 A1
`9/2006 Dahanukar etal.
`2006/0247226 Al (cid:9)
`11/2006 Himmelsbach et al.
`2006/0247226 A1 11/2006 Himmelsbach et al.
`2006/0270668 Al (cid:9)
`11/2006 Chew et al.
`2006/0270668 A1 11/2006 Chew et a1.
`2006/0270701 Al (cid:9)
`11/2006 Kroth et al.
`2006/0270701 A1 11/2006 Kroth etal.
`2007/0027168 Al (cid:9)
`2/2007 Pfrengle et al.
`2007/0027168 A1
`2/2007 Pfrengle et a1.
`2007/0060530 Al (cid:9)
`3/2007 Christopher et al.
`2007/0060530 A1
`3/2007 Christopheretal.
`2007/0072803 Al (cid:9)
`3/2007 Chu et al.
`2007/0072803 A1
`3/2007 Chu etal~
`2007/0072810 Al (cid:9)
`3/2007 Asakawa
`2007/0072810 A1
`3/2007 Asakawa
`2007/0088038 Al (cid:9)
`4/2007 Eckhardt et al.
`2007/0088038 A1
`4/2007 Eckhardtet al.
`2007/0093659 Al (cid:9)
`4/2007 Bonfanti et al.
`2007/0093659 A1
`4/2007 Bonfantletal
`2007/0142383 Al (cid:9)
`6/2007 Eckhardt et al.
`2007/0142383 A1
`6/2007 E8khardtetal~
`2007/0185091 Al (cid:9)
`8/2007 Himmelsbach et al.
`2007/0185091 A1
`8/2007 Hlmmelsbach etal~
`2007/0196472 Al (cid:9)
`8/2007 Kiel et al.
`2007/0196472 A1
`55/2007 Kiel er a1.
`2007/0197522 Al (cid:9)
`8/2007 Edwards et al.
`2007/0197522 A1
`8/2007 Edwards etal.
`2007/0219178 Al (cid:9)
`9/2007 Muramoto
`2007/0219178 A1
`9/2007 Muramoto
`2007/0259900 Al (cid:9)
`11/2007 Sieger et al.
`2007/0259900 A1 11/2007 Sieger et a1.
`2007/0259925 Al (cid:9)
`11/2007 Boehringer et al.
`2007/0259925 A1 11/2007 Boehringer et a1.
`2007/0259927 Al (cid:9)
`11/2007 Suzuki et al.
`2007/0259927 A1 11/2007 Suzuki et a1.
`2007/0281940 Al (cid:9)
`12/2007 Dugi et al.
`2007/0281940 A1 12/2007 Dugietal.
`2007/0299076 Al (cid:9)
`12/2007 Piotrowski et al.
`2007/0299076 A1 12/2007 Piotrowski et a1.
`2008/0039427 Al (cid:9)
`2/2008 Ray et al.
`2008/0039427 A1
`2/2008 Ray et a1.
`
`Mylan EX 1001, Page 2
`
`

`
`US 8,846,695 B2
`US 8,846,695 B2
`Page 3
`Page 3
`
`(56)
`(56) (cid:9)
`
`References Cited
`References Cited
`
`U.S. PATENT DOCUMENTS
`U.S. PATENT DOCUMENTS
`
`5/2008 Kohlrausch et a1.
`2008/0107731 A1
`5/2008 (cid:9) Kohlrausch et al.
`2008/0107731 Al (cid:9)
`5/2008 Znnei
`2008/0108816 A1
`5/2008 (cid:9) Zutter
`2008/0108816 Al (cid:9)
`2008/0249089 A1 10/2008 Himmelsbach etal.
`2008/0249089 Al (cid:9)
`10/2008 (cid:9) Himmelsbach et al.
`2008/0255159 A1 10/2008 Himmelsbach etal.
`2008/0255159 Al (cid:9)
`10/2008 (cid:9) Himmelsbach et al.
`2008/0312243 A1 12/2008 Eckhardt et a1.
`2008/0312243 Al (cid:9)
`12/2008 (cid:9) Eckhardt et al.
`2008/0318922 A1 12/2008 Nakahira etal.
`2008/0318922 Al (cid:9)
`12/2008 (cid:9) Nakahira et al.
`2009/0023920 A1
`1/2009 Eckhardt
`2009/0023920 Al (cid:9)
`1/2009 Eckhardt
`2009/0088408 A1
`4/2009 Meade et a1.
`2009/0088408 Al (cid:9)
`4/2009 (cid:9) Meade et al.
`2009/0088569 A1
`4/2009 Eckhardt et a1.
`2009/0088569 Al (cid:9)
`4/2009 (cid:9) Eckhardt et al.
`2009/0093457 A1
`4/2009 Himmelsbach etal.
`2009/0093457 Al (cid:9)
`4/2009 Himmelsbach et al.
`2009/0131432 A1
`5/2009 Himmelsbach etal.
`2009/0131432 Al (cid:9)
`5/2009 (cid:9) Himmelsbach et al.
`2009/0136596 A1
`5/2009 Munson et a1.
`2009/0136596 Al (cid:9)
`5/2009 (cid:9) Munson et al.
`2009/0137801 A1
`5/2009 Himmelsbach etal.
`2009/0137801 Al (cid:9)
`5/2009 (cid:9) Himmelsbach et al.
`2009/0149483 A1
`6/2009 Nakahira etal.
`2009/0149483 Al (cid:9)
`6/2009 (cid:9) Nakahira et al.
`2009/0186086 A1
`7/2009 Shankar et a1.
`2009/0186086 Al (cid:9)
`7/2009 (cid:9) Shankar et al.
`2009/0192314 A1
`7/2009 Pfrengle et a1.
`2009/0192314 Al (cid:9)
`7/2009 (cid:9) Pfrengle et al.
`2009/0297470 A1 12/2009 Franz
`2009/0297470 Al (cid:9)
`12/2009 Franz
`2009/0301105 A1 12/2009 Leening
`2009/0301105 Al (cid:9)
`12/2009 (cid:9) Loerting
`2009/0325926 A1 12/2009 Himmelsbach
`2009/0325926 Al (cid:9)
`12/2009 Himmelsbach
`2010/0074950 A1
`3/2010 Sesha
`2010/0074950 Al (cid:9)
`3/2010 (cid:9) Sesha
`2010/0092551 A1
`4/2010 Nakamura et a1.
`2010/0092551 Al (cid:9)
`4/2010 Nakamura et al.
`2010/0173916 A1
`7/2010 Himmelsbach etal.
`2010/0173916 Al (cid:9)
`7/2010 (cid:9) Himmelsbach et al.
`2010/0179191 A1
`7/2010 Himmelsbach etal.
`2010/0179191 Al (cid:9)
`7/2010 (cid:9) Himmelsbach et al.
`2010/0183531 A1
`7/2010 Johncock et a1.
`2010/0183531 Al (cid:9)
`7/2010 (cid:9)
`Johncock et al.
`2010/0204250 A1
`8/2010 Himmelsbach etal.
`2010/0204250 Al (cid:9)
`8/2010 (cid:9) Himmelsbach et al.
`2010/0209506 A1
`8/2010 Eisenreich
`2010/0209506 Al (cid:9)
`8/2010 (cid:9) Eisenreich
`2010/0310664 A1 12/2010 Watson etal.
`2010/0310664 Al (cid:9)
`12/2010 (cid:9) Watson et al.
`2011/0009391 A1
`1/2011 Braun et a1.
`2011/0009391 Al (cid:9)
`1/2011 (cid:9) Braun et al.
`2011/0046076 A1
`2/2011 Eickelmann et a1.
`2011/0046076 Al (cid:9)
`2/2011 (cid:9) Eickelmann et al.
`2011/0065731 A1
`3/2011 Dugi et a1.
`2011/0065731 Al (cid:9)
`3/2011 (cid:9) Dugi et al.
`2011/0092510 A1
`4/2011 Klein etal.
`2011/0092510 Al (cid:9)
`4/2011 (cid:9) Klein et al.
`2011/0098240 A1
`4/2011 Dugi et a1.
`2011/0098240 Al (cid:9)
`4/2011 (cid:9) Dugi et al.
`2011/0112069 A1
`5/2011 Himmelsbach etal.
`2011/0112069 Al (cid:9)
`5/2011 (cid:9) Himmelsbach et al.
`2011/0144083 A1
`6/2011 Himmelsbach etal.
`2011/0144083 Al (cid:9)
`6/2011 (cid:9) Himmelsbach et al.
`2011/0144095 A1
`6/2011 Himmelsbach etal.
`2011/0144095 Al (cid:9)
`6/2011 (cid:9) Himmelsbach et al.
`2011/0190322 A1
`8/2011 Klein etal.
`2011/0190322 Al (cid:9)
`8/2011 (cid:9) Klein et al.
`2011/0195917 A1
`8/2011 Dugi et a1.
`2011/0195917 Al (cid:9)
`8/2011 (cid:9) Dugi et al.
`2011/0206766 A1
`8/2011 Friedl et a1.
`2011/0206766 Al (cid:9)
`8/2011 (cid:9) Friedl et al.
`2011/0263493 A1 10/2011 Dugietal.
`2011/0263493 Al (cid:9)
`10/2011 (cid:9) Dugi et al.
`2011/0263617 A1 10/2011 Market a1.
`2011/0263617 Al (cid:9)
`10/2011 (cid:9) Mark et al.
`2011/0275561 A1 11/2011 Graefe-Modyet a1.
`2011/0275561 Al (cid:9)
`11/2011 (cid:9) Graefe-Mody et al.
`2011/0301182 A1 12/2011 Dugi
`2011/0301182 Al (cid:9)
`12/2011 (cid:9) Dugi
`2012/0003313 A1
`1/2012 Kohlrausch et a1.
`2012/0003313 Al (cid:9)
`1/2012 (cid:9) Kohlrausch et al.
`2012/0035158 A1
`2/2012 Himmelsbach etal.
`2012/0035158 Al (cid:9)
`2/2012 (cid:9) Himmelsbach et al.
`2012/0040982 A1
`2/2012 Himmelsbach etal.
`2012/0040982 Al (cid:9)
`2/2012 (cid:9) Himmelsbach et al.
`2012/0053173 A1
`3/2012 Banno etal.
`2012/0053173 Al (cid:9)
`3/2012 (cid:9) Banno et al.
`2012/0094894 A1
`4/2012 Graefe-Mody et a1.
`2012/0094894 Al (cid:9)
`4/2012 (cid:9) Graefe-Mody et al.
`2012/0107398 A1
`5/2012 Schneider et a1.
`2012/0107398 Al (cid:9)
`5/2012 (cid:9) Schneider et al.
`2012/0121530 A1
`5/2012 Klein etal.
`2012/0121530 Al (cid:9)
`5/2012 (cid:9) Klein et al.
`2012/0122776 A1
`5/2012 Graefe-Mody et a1.
`2012/0122776 Al (cid:9)
`
`5/2012 (cid:9) Graefe-Mody et al.
`2012/0129874 A1
`5/2012 Sieger et a1.
`2012/0129874 Al (cid:9)
`
`5/2012 (cid:9) Sieger et al.
`2012/0142712 A1
`6/2012 Pfren le et a1.
`2012/0142712 Al (cid:9)
`6/2012 (cid:9) Pfrengle et al.
`. g
`2012/0165251 Al (cid:9)
`6/2012 (cid:9) Klein et al.
`2012/0165251 A1
`6/2012 Klein etal.
`2012/0208831 Al (cid:9)
`8/2012 (cid:9) Himmelsbach et al.
`2012/0208831 A1
`8/2012 Hlmmelsbach et 31.
`2012/0219622 Al (cid:9)
`8/2012 (cid:9) Kohlrausch et al.
`2012/0219622 A1
`8/2012 KohlPausch 6t {11.
`2012/0219623 Al (cid:9)
`8/2012 (cid:9) Meinicke
`2012/0219623 A1
`8/2012 Meinieke
`2012/0252782 Al (cid:9)
`10/2012 (cid:9) Himmelsbach et al.
`2012/0252782 A1 10/2012 Hlmmelsbach et al.
`2012/0252783 Al (cid:9)
`10/2012 (cid:9) Himmelsbach et al.
`2012/0252783 A1 10/2012 Himmelsbach etal.
`2012/0296091 Al (cid:9)
`11/2012 (cid:9) Sieger et al.
`2012/0296091 A1 11/2012 Sieger et a1.
`2013/0122089 Al (cid:9)
`5/2013 (cid:9) Kohlrausch et al.
`2013/0122089 A1
`5/2013 Kohlrausch et a1.
`2013/0172244 Al (cid:9)
`7/2013 (cid:9) Klein et al.
`2013/0172244 A1
`7/2013 Klein etal.
`2013/0184204 A1
`7/2013 Pfrengle et a1.
`2013/0184204 Al (cid:9)
`7/2013 (cid:9) Pfrengle et al.
`2013/0196898 A1
`8/2013 Dugi et a1.
`2013/0196898 Al (cid:9)
`8/2013 (cid:9) Dugi et al.
`2013/0236543 A1
`9/2013 Ito etal.
`2013/0236543 Al (cid:9)
`9/2013 (cid:9)
`Ito et al.
`FOREIGN PATENT DOCUMENTS
`FOREIGN PATENT DOCUMENTS
`
`CA
`CA (cid:9)
`CA
`CA (cid:9)
`CA
`CA (cid:9)
`CA
`CA (cid:9)
`CA
`CA (cid:9)
`CA (cid:9)
`CA
`CA (cid:9)
`CA
`
`2529729 A1 12/2004
`2529729 Al (cid:9)
`
`12/2004
`2543074 A1
`600%
`2543074 Al (cid:9)
`6/2005
`2555050 Al
`9/2005
`2555050 Al (cid:9)
`9/2005
`2556064 A1
`9/2005
`2556064 Al (cid:9)
`9/2005
`2558067 A1 10/2005
`2558067 Al (cid:9)
`10/2005
`2561210 Al (cid:9)
`10/2005
`2561210 A1 10/2005
`2562859 Al (cid:9)
`11/2005
`2562859 A1 11/2005
`
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CA
`CN
`(3N
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`DE
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`EP
`ES
`ES
`ES
`ES
`ES
`ES
`FR
`FR
`GB
`GB
`HU
`HU
`HU
`HU
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`JP
`KR
`KR
`WO
`$8
`WO
`WO
`wo
`W0
`WO
`WO
`W0
`WO
`wo
`WO
`WO
`WO
`WO
`WO
`WO
`WO
`W0
`WO
`wo
`
`3/2006
`2576294 Al
`3/2006
`2576294 A1
`6/2006
`2590912 Al
`6/2006
`2590912 A1
`11/2007
`2651019 Al
`2651019 A1 11/2007
`2651089 Al
`11/2007
`2651089 A1
`11/2007
`101234105 A
`8/2008
`101234105 A
`8/2008
`2205815 Al
`8/1973
`2205815 A1
`8/1973
`2758025 Al
`7/1979
`2758025 A1
`7/ 1979
`10109021 Al
`9/2002
`10109021 A1
`9/2002
`10117803 Al
`10/2002
`10117803 A1 10/2002
`10238243 Al
`3/2004
`10238243 A1
`3/2004
`102004019540 Al
`11/2005
`102004019540 A1
`11/2005
`102004024454 Al
`12/2005
`102004024454 A1 12/2005
`102004044221 Al
`3/2006
`102004044221 A1
`3/2006
`102004054054 Al
`5/2006
`102004054054 A1
`5/2006
`0023032 Al
`1/1981
`0023032 A1
`1/1981
`0149578 A2
`7/1985
`0149578 A2
`7/1985
`0223403 A2
`5/1987
`0223403 A2
`5/1987
`0237608 Al
`9/1987
`0237608 A1
`9/1987
`0248634 A2
`12/1987
`0248634 A2 12/1987
`0389282 A2
`9/1990
`0389282 A2
`9/1990
`0399285 Al
`11/1990
`0399285 A1
`11/1990
`0400974 A2
`12/1990
`0400974 A2 12/1990
`409281 Al
`1/1991
`409281 A1
`1/1991
`0412358 Al
`2/1991
`0412358 A1
`2/1991
`443983 Al
`8/1991
`443983 A1
`8/1991
`0475482 Al
`3/1992
`0475482 A1
`3/1992
`0524482 Al
`1/1993
`0524482 A1
`1/1993
`0657454 Al
`6/1995
`0657454 A1
`6/1995
`0775704 Al
`5/1997
`0775704 A1
`5/1997
`0950658 Al
`10/1999
`0950658 A1 10/ 1999
`1054012 Al
`11/2000
`1054012 A1 11/2000
`1066265 Al
`1/2001
`1066265 A1
`1/2001
`1333033
`8/2003
`1333033
`8/2003
`1338595 A2
`8/2003
`1338595 A2
`8/2003
`1406873 A2
`4/2004
`1406873 A2
`4/2004
`1500403 Al
`1/2005
`1500403 A1
`1/2005
`1514552 Al
`3/2005
`1514552 A1
`3/2005
`1535906 Al
`6/2005
`1535906 A1
`6/2005
`1537880 Al
`6/2005
`1537880 A1
`6/2005
`1557165 Al
`7/2005
`1557165 A1
`7/2005
`1586571 Al
`10/2005
`1586571 A1 10/2005
`1743655 Al
`1/2007
`1743655 A1
`1/2007
`1760076
`3/2007
`1760076
`3/2007
`1829877 Al
`9/2007
`1829877 A1
`9/2007
`1852108 Al
`11/2007
`1852108 A1 11/2007
`1897892 A2
`3/2008
`1897892 A2
`3/2008
`2143443 Al
`1/2010
`2143443 A1
`1/2010
`385302 Al
`4/1973
`385302 A1
`4/1973
`2256797 T3
`7/2006
`2256797 T3
`7/2006
`2263057 T3
`12/2006
`2263057 T3
`12/2006
`2707641 Al
`1/1995
`2707641 A1
`1/1995
`2084580 A
`4/1982
`2084580 A
`4/1982
`9003243
`5/1990
`9003243
`5/1990
`9902308 A2
`7/2000
`9902308 AZ
`70000
`S374895 A
`6/1962
`5374895 A
`6/1962
`3/1995
`770120
`“995
`770120
`8333339
`12/1996
`8333339
`12/1996
`11193270
`M999
`11193270
`7/1999
`2000502684 A
`30000
`2000502684 A
`3/2000
`2001213770 A
`8/2001
`2001213770 A
`8/2001
`2002348279 A 00002
`2002348279 A
`12/2002
`2003286287 A 10/2003
`2003286287 A
`10/2003
`2003300977 A 10/2003
`2003300977 A
`10/2003
`2004161749 A
`6/2004
`2004161749 A
`6/2004
`2006045156 A
`2/2006
`2006045156 A
`2/2006
`2010053576 A
`3/2010
`2010053576 A
`3/2010
`2010524580 A
`7/2010
`2010524580 A
`7/2010
`20070111099 A
`11/2007
`20070111099 A 11/2007
`9107945 Al
`6/1991
`35826712 :1
`$133;
`9205175 Al
`4/1992
`9219227 A2
`11/1992
`9219227 A2 11/1992
`9402150 Al
`2/1994
`9402150 Al
`2/1994
`9403456 Al
`2/1994
`9403456 A1
`“994
`11/1995
`9532178 Al
`11/1995
`9532178 A1
`9609045 Al
`3/1996
`9609045 Al
`3/1996
`9611917 Al
`4/1996
`9611917 A1
`4/1996
`9636638 Al
`11/1996
`9636638 A1
`11/1996
`9723447 Al
`7/1997
`9723447 A1
`7/1997
`9723473 Al
`7/1997
`9723473 A1
`7/1997
`
`Mylan EX 1001, Page 3
`
`

`
`US 8,846,695 B2
`US 8,846,695 B2
`Page 4
`Page 4
`
`(56)
`(56)
`
`WO
`WO
`WO
`WO
`W0
`WO
`WO
`WO
`WO
`WO
`W0
`WO
`WO
`WO
`WO
`WO
`W0
`WO
`W0
`WO
`WO
`WO
`WO
`WO
`W0
`WO
`WO
`WO
`WO
`WO
`W0
`WO
`WO
`WO
`WO
`WO
`W0
`WO
`W0
`WO
`WO
`WO
`WO
`WO
`W0
`WO
`WO
`WO
`WO
`WO
`W0
`WO
`WO
`WO