111111111111111011111 1111#111161111111,1121111111111111111111111111
`
`US008673927B2
`
`(12) United States Patent (cid:9)
`(12) United States Patent
`Dugi et al. (cid:9)
`Dugi et a].
`
`(10) Patent No.: (cid:9)
`(10) Patent N0.:
`(45) Date of Patent: (cid:9)
`(45) Date of Patent:
`
`US 8,673,927 B2
`US 8,673,927 B2
`*Mar. 18, 2014
`*Mar. 18, 2014
`
`(54) USES OF DPP-IV INHIBITORS
`(54) USES OF DPP-IV INHIBITORS
`
`(75) Inventors: Klaus Dugi, Dresden (DE); Frank
`(75) Inventors: Klaus Dugi, Dresden (DE); Frank
`Himmelsbach, Mittelbiberach (DE);
`Himmelsbach, Mittelbiberach (DE);
`Michael Mark, Biberach (DE)
`Michael Mark, Biberach (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 111 days.
`U.S.C. 154(b) by 111 days.
`This patent is subject to a terminal dis-
`This patent is subject to a terminal dis
`claimer.
`claimer.
`
`(21) App1.No.: 12/946,193
`(21) Appl. No.: 12/946,193
`
`(22) Filed:
`(22) Filed: (cid:9)
`
`Nov. 15, 2010
`Nov. 15, 2010
`
`(65)
`(65) (cid:9)
`
`Prior Publication Data
`Prior Publication Data
`
`US 2011/0065731A1
`US 2011/0065731 Al (cid:9)
`
`Mar. 17, 2011
`Mar. 17, 2011
`
`Related U.S. Application Data
`Related US. Application Data
`
`(63) Continuation of application No. 11/744,703, filed on
`(63) Continuation of application No. 11/744,703, ?led on
`May 4, 2007, now Pat. No. 8,232,281.
`May 4, 2007, noW Pat. No. 8,232,281.
`
`(30)
`(30) (cid:9)
`
`Foreign Application Priority Data
`Foreign Application Priority Data
`
` 06009203
`May 4, 2006 (EP) (cid:9)
`May 4, 2006 (EP) ................................... .. 06009203
`
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`
`(51) Int. Cl.
`(51) Int. Cl.
`A 61K 31/52 (cid:9)
`A61K 31/52
`A 61K 31/155 (cid:9)
`A61K 31/155
`(52) U.S. Cl.
`(52) US. Cl.
` 514/263.21; 514/635; 514/868
`USPC (cid:9)
`USPC ..................... .. 514/263.21; 514/635; 514/868
`(58) Field of Classification Search
`(58) Field of Classi?cation Search
`USPC (cid:9)
` 514/263.21, 635, 866
`USPC ................................... .. 514/263.21, 635, 866
`See application ?le for complete search history.
`See application file for complete search history.
`
`(56) (cid:9)
`(56)
`
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`(Continued)
`(Continued)
`
`FOREIGN PATENT DOCUMENTS
`FOREIGN PATENT DOCUMENTS
`
`AU (cid:9)
`AU
`AU (cid:9)
`AU
`
`6/2004
`2003280680 Al (cid:9)
`6/2004
`2003280680 Al
`9/2009
`2009224546 Al (cid:9)
`9/2009
`2009224546 Al
`(Continued)
`(Continued)
`
`OTHER PUBLICATIONS
`OTHER PUBLICATIONS
`
`Bastin, R.J. et al., "Salt Selection and Optimization Procedures for
`Bastin, R]. et al., “Salt Selection and Optimization Procedures for
`Pharmaceutical New Chemical Entities". Organic Process Research
`Pharmaceutical New Chemical Entities”. Organic Process Research
`and Development, 2000, vol. 4, p. 427-435.
`and Development, 2000, vol. 4, p. 427-435.
`Chemical Abstract: No. 21 l5l3-37-0iDalcetrapib. “Propanethioic
`Chemical Abstract: No. 211513-37-0—Dalcetrapib. "Propanethioic
`acid,
`2-methyl-,S-(2-[[[1-(2-ethylbutyl)cyclohexyl}carbonyl}
`acid, (cid:9)
`2-methyl-,S-(2-[[[1-(2-ethylbutyl)cyclohexyl}carbonyl}
`amino Ipheyll ester". Formula: C23 H35 N 02 S. American Chemical
`amino}pheyl}ester”. Formula: C23 H35 N O2 S.American Chemical
`Society. Sep. 20, 1998.
`Society. Sep. 20, 1998.
`875446-37-0iAnacetrapib.
`No.
`Chemical
`Abstract:
`875446-37-0—Anacetrapib.
`No. (cid:9)
`Chemical (cid:9)
`Abstract: (cid:9)
`"2-Oxazolidinone, 5 43,5 -bi s(trifluoromethyl)pheny1]-3 [[4'fluoro -
`“2-OXaZolidinone, 5 - [3 ,5 -bi s(tri?uoromethyl)phenyl] -3 [[4‘?uoro -
`2‘ -methoXy-5 ‘ -( 1 -methylethyl)-4 -(tri?uoromethyl)[ 1, 1‘-biphenyl]
`2'-methoxy-5'-(1 -methylethyl)-4 -(trifluoromethyl)[ 1 ,1'-bipheny1]-
`2-yl]methy1]-4-methyl-,(4S,5R)-" Formula: C30 H25 FIO N 03.
`2-yl]methyl]-4-methyl-,(4S,5R)-” Formula: C30 H25 F10 N O3.
`American Chemical Society, Feb. 28, 2006.
`American Chemical Society, Feb. 28, 2006.
`(Continued)
`(Continued)
`
`Primary Examiner — Kevin E Weddington
`Primary Examiner * Kevin E Weddington
`(74) Attorney, Agent, or Firm — Michael P. Morris; David L.
`(74) Attorney, Agent, orFirm * Michael P. Morris; David L.
`Kershner
`Kershner
`
`(57)
`(57) (cid:9)
`
`ABSTRACT
`ABSTRACT
`
`The specification describes the use of selected DPP IV inhibi-
`The speci?cation describes the use of selected DPP IV inhibi
`tors for the treatment of physiological functional disorders
`tors for the treatment of physiological functional disorders
`and for reducing the risk of the occurrence of such functional
`and for reducing the risk of the occurrence of such functional
`disorders in at-risk patient groups. In addition, the use of the
`disorders in at-risk patient groups. In addition, the use of the
`above-mentioned DPP IV inhibitors in conjunction with
`above-mentioned DPP IV inhibitors in conjunction With
`other active substances is described, by means of which
`other active substances is described, by means of Which
`improved treatment outcomes can be achieved. These appli-
`improved treatment outcomes can be achieved. These appli
`cations may be used to prepare corresponding medicaments.
`cations may be used to prepare corresponding medicaments.
`
`26 Claims, No Drawings
`26 Claims, No Drawings
`
`MYLAN Ex. 1001, Page 1
`
`(cid:9)
`

`
`US 8,673,927 B2
`US 8,673,927 B2
`Page 2
`Page 2
`
`(56)
`(56) (cid:9)
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`MYLAN Ex. 1001, Page 2
`
`

`
`US 8,673,927 B2
`US 8,673,927 B2
`Page 3
`Page 3
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`(56)
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`FOREIGN PATENT DOCUMENTS
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`DE
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`5/1982
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`102004024454 A1 12/2005
`12/2005
`102004024454 Al
`102004044221 Al
`3/2006
`102004044221 A1
`3/2006
`102004054054 Al
`5/2006
`102004054054 A1
`5/2006
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`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
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`2/1991
`0412358 A1
`2/1991
`443983 Al
`8/1991
`443983 A1
`8/ 1991
`0524482 Al
`1/1993
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`1/1993
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`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
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`3/2005
`1514552 A1
`3/2005
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`6/2005
`1537880 A1
`6/2005
`1557165 Al
`7/2005
`1557165 A1
`7/2005
`1586571 Al
`10/2005
`1586571 A1 10/2005
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`1/2007
`1743655 A1
`1/2007
`1760076
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`1760076
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`1829877 Al
`9/2007
`1829877 A1
`9/2007
`1852108 Al
`11/2007
`1852108 A1
`11/2007
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`1/2010
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`1/2010
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`4/1973
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`7/2006
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`7/2006
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`12/2006
`ggggg? 131
`li?ggg
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`2084580 A
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`7/2000
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`6/l962
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`6/1962
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`3/1995
`770120
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`2000502684 A
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`2000502684 A
`3/2000
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`55/2001
`2001213770 A
`8/2001
`2003300977 A
`10/2003
`2003300977 A 10/2003
`2006045156 A
`2/2006
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`2/2006
`2010053576 A
`3/2010
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`3/2010
`20070111099 A
`11/2007
`20070111099 A ll/2007
`9107945 Al
`6/1991
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`4/1992
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`4/1992
`9219227 A2
`11/1992
`9219227 A2 11/1992
`9402150 Al
`2/1994
`9402150 A1
`2/1994
`9403456 A1
`2/1994
`9403456 Al
`2/1994
`9532178 Al
`11/1995
`9532178 A1
`11/1995
`9609045 A1
`3/1996
`9609045 Al
`3/1996
`9636638 A1
`11/1996
`9636638 Al
`11/1996
`9723447 A1
`7/1997
`9723447 Al
`7/1997
`9723473 A1
`7/1997
`9723473 Al
`7/1997
`9746526 Al
`12/1997
`9746526 A1
`12/1997
`9807725
`2/1998
`3337253 Ai
`51333
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`3/1998
`9818770 A1
`5/1998
`9818770 Al
`5/1998
`9822464 A1
`“998
`9822464 Al
`5/1998
`9828007 A1
`7/1998
`9828007 Al
`7/1998
`9840069 A2
`9/1998
`9840069 A2
`9/1998
`9856406 A1 124998
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`12/1998
`9929695 Al
`6/1999
`33333321 $3333
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`10/1999
`0073307 A2
`12/2000
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`0107441 A1
`2/2001
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`2/2001
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`0140180 A2
`81295152 :5
`$5881
`7/2001
`0152825 A2
`7/2001
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`7/2001
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`0177110 Al
`10/2001
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`12/2001
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`1/2002
`0214271 Al
`2/2002
`0214271 A1
`2/2002
`0224698 Al
`3/2002
`0224698 A1
`3/2002
`
`MYLAN Ex. 1001, Page 3
`
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