`Acheampong et al.
`
`(10) Patent N0.:
`
`(45) Date of Patent:
`
`US 9,248,191 B2
`*Feb. 2, 2016
`
`US009248191B2
`
`METHODS OF PROVIDING THERAPEUTIC
`EFFECTS USING CYCLOSPORIN
`COMPONENTS
`
`Applicant: Allergan, Inc., Irvine, CA (US)
`
`Inventors: Andrew Acheampong, Irvine, CA (US);
`Diane D. Tang-Liu, Las Vegas, NV
`(US); James N. Chang, Newport Beach,
`CA (US); David F. Power, San
`Clemente, CA (US)
`
`Assignee: Allergan, Inc., Irvine, CA (US)
`
`Notice:
`
`Subject to any disclaimer, the term of this
`patent is extended or adjusted under 35
`U.S.C. l54(b) by 0 days.
`
`This patent is subject to a terminal dis-
`claimer.
`
`14/222,478
`
`Mar. 21, 2014
`
`Prior Publication Data
`
`US 2014/0206626 A1
`
`Jul. 24, 2014
`
`Related U.S. Application Data
`
`Continuation of application No. 13/961,828, filed on
`Aug. 7, 2013, now Pat. No. 8,685,930, which is a
`continuation of application No. 11/897,177, filed on
`Aug. 28, 2007, now Pat. No. 8,618,064, and a
`continuation of application No. 10/927,857, filed on
`Aug. 27, 2004, now abandoned.
`
`Provisional application No. 60/503,137, filed on Sep.
`15, 2003.
`
`Int. Cl.
`A61K 38/13
`A61K 47/02
`A61K 9/00
`A61K 47/44
`A61K 9/107
`A61K 47/10
`A61K 47/22
`A61K 47/32
`U.S. Cl.
`
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`
`cpc ............. .. A61K 47/02 (2013.01); A61K 9/0048
`(2013.01); A61K 9/107 (2013.01); A61K38/13
`(2013.01); A61K47/10 (2013.01); A61K47/22
`(2013.01); A61K47/32 (2013.01); A61K47/44
`(2013.01)
`
`Field of Classification Search
`None
`
`See application file for complete search history.
`
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`(Continued)
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`Primary Examiner — Marcela M Cordero Garcia
`
`(74) Attorney, Agent, or F1'rm—Laura L. Wine; Joel B.
`German; Debra D. Condino
`
`(57)
`
`ABSTRACT
`
`Methods of treating an eye of a human or animal include
`administering to an eye of a human or animal a composition
`in the form of an emulsion including water, a hydrophobic
`component and a cyclo sporin component in a therapeutically
`effective amount of less than 0.1% by weight of the compo-
`sition. The weight ratio of the cyclosporin component to the
`hydrophobic component is less than 0.8.
`
`27 Claims, No Drawings
`
`EXHIBIT 1001
`
` EXHIBIT 1001
`
`
`
`US 9,248,191 B2
`Page 2
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`1 0/2
`3/2
`
`>—->—>—->—>—GGGG>—-L:JI\.)>—>—$©O000O0O0\l\l\l\lUIUIDJDJDJDJDJDJDJDJDJDJL:JLoJLo-)LoJI\J[\JI\JI\JI\JI\JI\)I\)I\)>—->->-{J1
`
`Chang ................ .. A61K 9/0048
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`
`*
`
`D>?>3>D>>D>D>D>D>D>D>D>D>D>D>D>D>>D>>D>>D>>D>>D>>D>>D>>D>>D>>D>>D>D>D>D>UZ1
`
`» »
`
`G©®©®©®©®©®$®©®$®©$©$QGGGQGGGQGGGQGGG
`
`I\—)I\JI\—)I\JI\JI\JI\JI\JI\JI\.>I\JI\JI\.>I\JI\JI\JI\JI\JI\JI\.>I\JI\.>I\JI\.>l\JI\—)l\JI\—>I\JI\—)I\JI\—)I\JI\—)I\JI\—)I\J
`
`9,101,574
`1/0003589
`1/0014665
`1/0036449
`2/0012680
`2/0013272
`2/0016290
`2/0016292
`2/0025927
`2/0045601
`2/0107183
`2/0119190
`2/0165134
`3/0021816
`3/0044452
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`US 9,248,191 B2
`
`1
`METHODS OF PROVIDING THERAPEUTIC
`EFFECTS USING CYCLOSPORIN
`COMPONENTS
`
`RELATED APPLICATION
`
`This application is a continuation of copending U.S. Appli-
`cation Serial No. 13/961828 filed Aug. 7, 2013, which is a
`continuation of U.S. application Ser. No. 11/897,177, filed
`Aug. 28, 2007, now issued as U.S. Pat. No. 8,618,064, which
`is a continuation of U.S. application Ser. No. 10/927,857,
`filed Aug. 27, 2004, now abandoned, which claims the benefit
`ofU.S. Provisional Application No. 60/503,137 filed Sep. 15,
`2003, wl1ich are incorporated in their entirety herein by ref-
`erence.
`
`BACKGROUND OF THE INVENTION
`
`The present invention relates to methods of providing
`desired therapeutic effects to humans or animals using com-
`positions including cyclosporin components. More particu-
`larly, the invention relates to methods including administer-
`ing to an eye of a human or animal a therapeutically effective
`amount of a cyclosporin component to provide a desired
`therapeutic effect, preferably a desired ophthalmic or ocular
`therapeutic effect.
`The use of cyclosporin-A and cyclosporinA derivatives to
`treat ophthalmic conditions has been the subject of various
`patents, for example Ding et al U.S. Pat. No. 5,474,979; Garst
`U.S. Pat. No. 6,254,860; and Garst U.S. Pat. No. 6,350,442,
`this disclosure of each of which is incorporated in its entirely
`herein by reference. In addition, cycl