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`535 72B2
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`USO112
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`(12) United States Patent
`US 11,253,572 B2
`(10) Patent No.:
`*Feb. 22, 2022
`(45) Date of Patent:
`Yancopoulos
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`USE OF A VEGF ANTAGONIST TO TREAT
`ANGIOGENIC EYE DISORDERS
`
`Applicant: REGENERON
`PHARMACEUTICALS, INC.,
`Tarrytown, NY (US)
`
`Inventor: George Yancopoulos, Yorktown
`Heights, NY (US)
`
`Assignee: REGENERON
`PHARMACEUTICALS, INC.,
`‘Tarrytown, NY (US)
`
`(*)
`
`Notice:
`
`Subject to any disclaimer, the term of this
`patent is extended or adjusted under 35
`U.S.C. 154(b) by 0 days.
`
`This patent is subject to a terminal dis-
`claimer.
`
`(21)
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`(22)
`
`(65)
`
`Appl. No.: 17/352,892
`
`Filed:
`
`Jun. 21, 2021
`
`Prior Publication Data
`
`US 2021/0308217 Al
`
`Oct. 7, 2021
`
`Related U.S. Application Data
`
`(2013.01); A6IK 2039/5035 (2013.01); CO7K
`2319/30 (2013.01), CO7K 2319/32 (2013.01)
`Field of Classification Search
`None
`See applicationfile for complete searchhistory.
`
`References Cited
`U.S. PATENT DOCUMENTS
`
`6,171,586 Bl
`6,833,349 B2
`6,879,294 B2
`6,897,294 B2
`7,070,959 BI
`7,303,746 B2
`7,303,747 B2
`7,303,748 B2
`7,306,799 B2
`7,374,757 B2
`7,374,758 B2
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`7,482,002 B2
`7,521,049 B2
`7,531,173 B2
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`
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`Papadopoulos
`12/2007 Wiegand
`12/2007 Wiegandetal.
`12/2007 Wiegand
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`5/2008
`
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`Wiegandetal.
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`(Continued)
`
`FOREIGN PATENT DOCUMENTS
`
`(63)
`
`Continuation of application No. 17/350,958, filed on
`dun. 17, 2021, which is a continuation of application
`No. 17/112,404, filed on Dec. 4, 2020, which is a
`continuation ofapplication No. 17/072.417, filed on
`Oct. 16, 2020, which is a continuation ofapplication
`No. 16/055,847, filed on Aug. 6, 2018, now Pat. No.
`10,857,205, and a continuation of application No.
`16/397,267, filed on Apr. 29, 2019, now Pat. No.
`10,888,601, which is a continuation of application
`No. 16/159,282, filed on Oct. 12, 2018, nowPat. No.
`10,828,345, which is a continuation of application
`No. 15/471,506, filed on Mar. 28, 2017, now Pat. No.
`Christine J Saoud
`Primary Examiner-
`10,130,681, which is a continuation of application
`Assistant Examiner—Jon M Lockard
`No. 14/972,560, filed on Dec. 17, 2015, now Pat. No.
`
`9,669,069, whichis a continuation of application No. (74) Attorney, Agent, or Firm—‘Thomas Triolo; Karl
`Bozicevic
`13/940,370,
`filed on Jul. 12, 2013, now Pat. No.
`9,254.338, which is
`a
`continuation-in-part of
`application No. PCT/US2012/020855, filed on Jan.
`11, 2012.
`
`CN
`CN
`
`1304427 C
`100502945 C
`
`3/2007
`6/2009
`
`(Continued)
`
`OTHER PUBLICATIONS
`
`U.S. Appl. No. 16/055,847—Third Party Submissions dated May1,
`2019.
`
`(Continued)
`
`(57)
`
`ABSTRACT
`
`(60)
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`(31)
`
`(52)
`
`Provisional application No. 61/432,245, filed on Jan.
`13, 2011, provisional application No. 61/434,836,
`filed on Jan. 21, 2011, provisional application No.
`61/561,957, filed on Nov. 21, 2011.
`
`Int. Cl.
`AGIK 38/17
`CO7K 14/71
`CO7K 19/00
`CO7K 16/22
`AGIK 9/00
`A6IK 39/00
`U.S. Cl.
`CPE sauuys AGIK 38/179 (2013.01); A6IK 9/0048
`(2013.01); CO7K 14/71 (2013.01); CO7K 16/22
`
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`(2006.01)
`
`The present invention provides methods for treating angio-
`genic eye disorders by sequentially administering multiple
`doses of a VEGFantagonist to a patient. The methods ofthe
`present
`invention include the administration of multiple
`doses of a VEGF antagonist to a patient at a frequency of
`once every 8 or more weeks. The methods of the present
`invention are useful
`for the treatment of angiogenic eye
`disorders such as age related macular degeneration, diabetic
`retinopathy, diabetic macular edema, central retinal vein
`occlusion, branch retinal vein occlusion, and corneal neo-
`vascularization.
`
`30 Claims, 1 Drawing Sheet
`
`Specification includes a Sequence Listing.
`
`Apotex Exhibit 1001
`Apotex Exhibit 1001
`Page 1 of 25
`Page 1 of 25
`
`

`

`US 11,253,572 B2
`Page 2
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`(56)
`
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`OTHER PUBLICATIONS
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`Apotex Exhibit 1001
`Apotex Exhibit 1001
`Page 2 of 25
`Page 2 of 25
`
`

`

`US 11,253,572 B2
`Page 3
`
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`
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`Macular Degeneration” 70 pages, Latest version submitted Jun. 8,
`2011 on ClinicalTrials.gov (NCT00320775_ 2006-2011).
`Information from ClinicalTrials.gov archive History of Changes for
`Study: NCT00320775 “Safety and Tolerability of Intravitreal Admin-
`istration of VEGF Trap in Patients With Neovascular Age-Related
`Macular Degeneration” 10 pages, Latest version submitted Mar. 16,
`2015 on ClinicalTrials.gov (NCT00320775_2015).
`Information from ClinicalTrials.gov archive History of Changes for
`Study: NCT00320788 “Safety and Efficacy of Repeated Intravitreal
`Administration of Vascular Endothelial Growth Factor (VEGF)
`Trap in Patients With Wet Age-Related Macular Degeneration
`(AMD)” 71 pages, Latest version submitted Dec.
`1, 2011 on
`ClinicalTrials.gov (NCTO0320788_2006-2011).
`Information from ClinicalTrials.gov archive History of Changes for
`Study: NCT00320788 “Safety and Efficacy of RepeatedIntravitreal
`Administration of Vascular Endothelial Growth Factor (VEGF)
`Trap in Patients With Wet Age-Related Macular Degeneration
`(AMD)” 31 pages, Latest version submitted Jan, 27, 2012 on
`ClinicalTrials.gov (NCT00320788_ 2012).
`Information from ClinicalTrials.gov archive History of Changes for
`Study: NCT00320814 “Phase | Study of VEGF Trap in Patients
`With Diabetic Macular Edema” 30 pages, Latest version submitted
`Jun. 8, 2011 on Clinical Trials.gov (NCTO0320814_ 2006-2011).
`Information from ClinicalTrials.gov archive History of Changes for
`Study: NCT00509795 “Double-Masked Study of Efficacy and Safety
`of IVT VEGFTrap-Eye in Subjects With Wet AMD (VIEW 1)" 318
`pages, Latest version submitted Dec. 1, 2011 on ClinicalTrials.gov
`(NCTO05097952007-2011).
`Information from ClinicalTrials.gov archive History of Changes for
`Study: NCT00509795 “Double-Masked Study of Efficacy and Safety
`of IVT VEGF Trap-Eye in Subjects With Wet AMD (VIEW 1)" 200
`pages, Latest version submitted Dec. 20, 2012 on ClinicalTrials.gov
`(NCT00509795 2012).
`Information from ClinicalTrials.gov archive History of Changes for
`Study: NCT00527423 “Randomized, Single-Masked, Long-Term,
`
`Apotex Exhibit 1001
`Apotex Exhibit 1001
`Page 3 of 25
`Page 3 of 25
`
`

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`US 11,253,572 B2
`Page 4
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`(56)
`
`References Cited
`OTHER PUBLICATIONS
`
`Safety and Tolerability Study of VEGF Trap-Eye in AMD” 64
`pages, Latest version submitted Nov.
`|, 2011 on ClinicalTrials.gov
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`Study: NCT00527423 “Randomized, Single-Masked, Long-Term,
`Safety and Tolerability Study of VEGF Trap-Eye in AMD” 42
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`Study: NCT00637377 “Vascular Endothelial Growth Factor (WEGF)
`Trap-Eye: Investigation of Efficacy and Safety in Wet Age-Related
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`2008-2011).
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`Study: NCT00637377 “Vascular Endothelial Growth Factor (WEGF)
`Trap-Eye: Investigation of Efficacy and Safety in Wet Age-Related
`Macular Degeneration (AMD) (VIEW 2)” 289 pages, Latest version
`submitted Nov. 28, 2014 on ClinicalTrials.gov (NCTOO637377_
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`Aflibercept Injection (IAILEYLEA®:BAY86-5321L)] [Nvestigation
`ofClinical Impact (DA VINCI)” 135 pages, Latest version submit-
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`Information from ClinicalTrials.gov archive History of Changes for
`Study: NCT00789477 “DME And VEGF Trap-Eye [Intravitreal
`Aflibercept Injection (IAL EYLEA®;BAY86-5321)] [Nvestigation
`of Clinical Impact (DA VINCI)” 53 pages, Latest version submitted
`Aug. 28, 2014 on ClinicalTrials.gov (NCT00789477_2013-2014).
`Information from ClinicalTrials.gov archive History of Changes for
`Study: NCT00943072 “Vascular Endothelial Growth Factor (WEGF)
`Trap-Eye: Investigation of Efficacy and Safety in Central Retinal
`Vein Occlusion (CRVO)" 98 pages, Latest version submitted May
`9, 2011 on ClinicalTrials.gov (NCT00943072_2009-2011).
`Information from ClinicalTrials.gov archive History of Changes for
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`
`1,
`
`Apotex Exhibit 1001
`Apotex Exhibit 1001
`Page 4 of 25
`Page 4 of 25
`
`

`

`US 11,253,572 B2
`Page 5
`
`(56)
`
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