PTO/SB/08 (09-06)
`Approved for use through 03/31/2007. OMB 0651-0031
`U.S. Patent and Trademark Office: U.S. DEPARTMENT OF COMMERCE
`Under the Paperwork Reduction Act of 1995, no persons are required to respond to a collection of information unless it contains a valid OMB
`control number
`r
`Substitute for form 1449/PTO
`INFORMATION DISCLOSURE
`STATEMENT BY APPLICANT
`
`Date Submitted: March 12, 2012
`
`(use as many sheets as necessary)
`I of 110
`~heet Is
`
`Application Number
`Filing Date
`First Named Inventor
`Art Unit
`Examiner Name
`Attorney Docket Number
`
`Complete if Known
`13/610,580
`September 11, 2012
`Bruce Scharschmidt
`1629
`Sara Elizabeth Townsley
`HOR0027-201-US
`
`~
`
`~
`
`T6
`
`Exami
`ner
`Initials*
`
`Cite
`No. 1
`
`D37
`
`NON PATENT LITERATURE DOCUMENTS
`Include name of the author (in CAPITAL LETTERS), title of the article (when appropriate), title of the
`item (book, magazine, journal, serial, symposium, catalog, etc.) date, page(s), volume-issue
`number(s), publisher, city and/or country where published.
`Gore, S. et al., Impact of the Putative Differentiating Agent Sodium Phenylbutyrate on
`Myelodysplastic Syndromes and Acute Myeloid Leukemia, 7 Clin. Cancer Res. 2330 (2001 ).
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`D38
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`Gropman, A.L. et al., Neurological Implications of Urea Cycle Disorders, 30 J. Inherit Metab Dis. 865
`(2007).
`
`HASSANEIN, T. 1., et al., "Randomized Controlled Study of Extracorporeal Albumin Dialysis for
`Hepatic Encephalopathy in Advanced Cirrhosis," Hepatology 46:1853-1862 (2007).
`
`HASSANEIN, T. 1., et al., "Introduction to the Hepatic Encephalopathy Scoring Algorithm (HESA),"
`Dig. Dis. Sci. 53:529-538 (2008).
`
`HASSANEIN, T., et al., "Performance of the Hepatic Encephalopathy Scoring Algorithm in a Clinical
`Trial of Patients With Cirrhosis and Severe Hepatic Encephalopathy," Am. J. Gastroenterol.
`104:1392-1400 (2009).
`Honda, S. et al., Successful Treatment of Severe Hyperammonemia Using Sodium Phenylacetate
`Power Prepared in Hospital Pharmacy, 25 Bioi. Pharm. Bull. 1244 (2002).
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`D43
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`International Search Report and Written Opinion for PCT/US09/30362, mailed Mar. 2, 2009, 8 pages.
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`D44
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`International Search Report and Written Opinion for PCT/US2009/055256, mailed Dec. 30, 2009, 13
`pages.
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`D45
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`INTER PARTES REVIEW OF U.S. PATENT NO. 8,404,215 Petition Apr. 29,2015
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`D46
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`INTER PARTES REVIEW OF U.S. PATENT NO. 8,642,012 Petition Apr. 29,2015
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`D47
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`Kleppe, S. et al., Urea Cycle Disorders, 5 Current Treatment Options in Neurology 309- 319 (2003).
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`D48
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`Kubota, K. and lshizaki, T., Dose-Dependent Pharmacokinetics of Benzoic Acid Following Oral
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`
`I Examiner
`
`Signature
`
`Date
`Considered
`
`* EXAMINER. ln111allf reference considered, whether or not c11a11on 1s 1n conformance With MPEP 609. Draw lme through c11a11on 1f notm conformance and not
`considered. Include copy of this form with next communication to applicant 1 Applicant's unique citation designation number (optional). 2 See Kinds Codes of
`USPTO Patent Documents at www.uspto.gov or MPEP 901.04. 3 Enter Office that issued the document, by the two-letter code (WI PO Standard ST.3). 4 For
`Japanese patent documents, the indication of the year of the reign of the Emperor must precede the serial number of the patent document 5 Kind of document by the
`appropriate symbols as indicated on the document under WI PO Standard ST.16 if possible. 6 Applicant is to place a check mark here if English language Translation
`is attached.
`This collection of information is required by 37 CFR 1.97 and 1 .98. The information is required to obtain or retain a benefit by the public which is to file (and by the
`USPTO to process) an application. Confidentiality is governed by 35 U.S.C. 122 and 37 CFR 1.14. This collection is estimated to take 2 hours to complete, including
`gathering, preparing, and submitting the completed application form to the USPTO. Time will vary depending upon the individual case. Any comments on the amount
`of time you require to complete this form and/or suggestions for reducing this burden, should be sent to the Chief Information Officer, U.S. Patent and Trademark
`Office, P.O. Box 1450, Alexandria, VA 22313-1450. DO NOT SEND FEES OR COMPLETED FORMS TO THIS ADDRESS. SEND TO: Commissioner for Patents,
`P.O. Box 1450, Alexandria, VA 22313-1450.
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`4835-0776-7055.1
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`If you need assistance in completing the form, call 1-800-PT0-9199 (1-800-786-9199) and select option 2.
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`I
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`Par Pharmaceutical, Inc. Ex. 1009
`Par v. Horizon, IPR of Patent No. 9,561,197
`Page 677 of 1354
`
`

`

`PTO/SB/08 (09-06)
`Approved for use through 03/31/2007. OMB 0651-0031
`U.S. Patent and Trademark Office: U.S. DEPARTMENT OF COMMERCE
`Under the Paperwork Reduction Act of 1995, no persons are required to respond to a collection of information unless it contains a valid OMB
`control number
`r
`Substitute for form 1449/PTO
`INFORMATION DISCLOSURE
`STATEMENT BY APPLICANT
`
`Date Submitted: March 12, 2012
`
`(use as many sheets as necessary)
`I of 110
`
`~heet 16
`
`Application Number
`Filing Date
`First Named Inventor
`Art Unit
`Examiner Name
`Attorney Docket Number
`
`Complete if Known
`13/610,580
`September 11, 2012
`Bruce Scharschmidt
`1629
`Sara Elizabeth Townsley
`HOR0027-201-US
`
`~
`
`~
`
`T6
`
`Exami
`ner
`Initials*
`
`Cite
`No. 1
`
`D49
`
`D50
`
`D51
`
`D52
`
`D53
`
`NON PATENT LITERATURE DOCUMENTS
`Include name of the author (in CAPITAL LETTERS), title of the article (when appropriate), title of the
`item (book, magazine, journal, serial, symposium, catalog, etc.) date, page(s), volume-issue
`number(s), publisher, city and/or country where published.
`Lee, B. and Goss, J., Long-Term Correction of Urea Cycle Disorders, 138 J. Pediatrics S62 (2001 ).
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`Lee, B. et al., Considerations in the Difficult-to-Manage Urea Cycle Disorder Patient, 21 Grit. Care
`Clin. S19 (2005).
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`Lee, B., et al., "Optimizing Ammonia (NH3) Control in Urea Cycle Disorder (UCD) Patients: A
`Predictive Model," Oral Abstract Platform Presentations, Biochemical Genetics, Phoenix, AZ, March
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`Leonard, J.V., Urea Cycle Disorders, 7 Semin. Nenatol. 27 (2002).
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`Lizardi-Cervera, J. et al., Hepatic Encephalopathy: A Review, 2 Annals of Hepatology 122-120
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`Maestri NE, et al., Prospective treatment of urea cycle disorders. J Paediatr 1991 ;119:923-928.
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`Marini, J.C. et al., Phenylbutyrate Improves Nitrogen Disposal via an Alternative Pathway without
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`Mizutani, N. et al., Hyperargininemia: Clinical Course and Treatment with Sodium Benzoate and
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`
`I Examiner
`
`Signature
`
`Date
`Considered
`
`* EXAMINER. ln111allf reference considered, whether or not c11a11on 1s 1n conformance With MPEP 609. Draw lme through c11a11on 1f notm conformance and not
`considered. Include copy of this form with next communication to applicant 1 Applicant's unique citation designation number (optional). 2 See Kinds Codes of
`USPTO Patent Documents at www.uspto.gov or MPEP 901.04. 3 Enter Office that issued the document, by the two-letter code (WI PO Standard ST.3). 4 For
`Japanese patent documents, the indication of the year of the reign of the Emperor must precede the serial number of the patent document 5 Kind of document by the
`appropriate symbols as indicated on the document under WI PO Standard ST.16 if possible. 6 Applicant is to place a check mark here if English language Translation
`is attached.
`This collection of information is required by 37 CFR 1.97 and 1 .98. The information is required to obtain or retain a benefit by the public which is to file (and by the
`USPTO to process) an application. Confidentiality is governed by 35 U.S.C. 122 and 37 CFR 1.14. This collection is estimated to take 2 hours to complete, including
`gathering, preparing, and submitting the completed application form to the USPTO. Time will vary depending upon the individual case. Any comments on the amount
`of time you require to complete this form and/or suggestions for reducing this burden, should be sent to the Chief Information Officer, U.S. Patent and Trademark
`Office, P.O. Box 1450, Alexandria, VA 22313-1450. DO NOT SEND FEES OR COMPLETED FORMS TO THIS ADDRESS. SEND TO: Commissioner for Patents,
`P.O. Box 1450, Alexandria, VA 22313-1450.
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`4835-0776-7055.1
`
`If you need assistance in completing the form, call 1-800-PT0-9199 (1-800-786-9199) and select option 2.
`
`I
`
`Par Pharmaceutical, Inc. Ex. 1009
`Par v. Horizon, IPR of Patent No. 9,561,197
`Page 678 of 1354
`
`

`

`PTO/SB/08 (09-06)
`Approved for use through 03/31/2007. OMB 0651-0031
`U.S. Patent and Trademark Office: U.S. DEPARTMENT OF COMMERCE
`Under the Paperwork Reduction Act of 1995, no persons are required to respond to a collection of information unless it contains a valid OMB
`control number
`r
`Substitute for form 1449/PTO
`INFORMATION DISCLOSURE
`STATEMENT BY APPLICANT
`
`Date Submitted: March 12, 2012
`
`(use as many sheets as necessary)
`I of 110
`
`~heet 17
`
`Application Number
`Filing Date
`First Named Inventor
`Art Unit
`Examiner Name
`Attorney Docket Number
`
`Complete if Known
`13/610,580
`September 11, 2012
`Bruce Scharschmidt
`1629
`Sara Elizabeth Townsley
`HOR0027-201-US
`
`~
`
`~
`
`T6
`
`Exami
`ner
`Initials*
`
`Cite
`No. 1
`
`D61
`
`D62
`
`D63
`
`D64
`
`D65
`
`D66
`
`D67
`
`D68
`
`D69
`
`D70
`
`D71
`
`NON PATENT LITERATURE DOCUMENTS
`Include name of the author (in CAPITAL LETTERS), title of the article (when appropriate), title of the
`item (book, magazine, journal, serial, symposium, catalog, etc.) date, page(s), volume-issue
`number(s), publisher, city and/or country where published.
`MOKHTARANI, M., et al., (2013) "Elevated Phenylacetic Acid Levels Do Not Correlate with Adverse
`Events in Patients with Urea Cycle Disorders o rHepatic Encephalopathy and Can Be Predicted
`Based on the Plasma PAA to PAGN Ratio," Mol Genet Metab 11 0(4):446-453
`MOKHTARANI, M., et al., (2012) "Urinary Phenylacetylglutamine as Dosing Biomarker for Patients
`with Urea Cycle Disorders," Mol Genet Metab 1 07(3):308-314
`
`MONTELEONE, JPR, et al., (2013) "Population Pharmacokinetic Modeling and Dosing Simulations
`of Nitrogen-Scavenging Compounds: Disposition of Glycerol Phenylbutyrate and Sodium
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`MUNOZ, S. J., "Hepatic Encephalopathy," Med. Clin. N. Am. 92:795-812 (2008).
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`Nassogne, M.G., Urea Cycle Defects: Management and Outcome, 28 J. Inherit. Metab. Dis. 407
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`New England Consortium of Metabolic Programs, Acute Illness Protocol: Urea Cycle Disorders: The
`Infant/Child with Argininosuccinate Lyase Deficiency, adapted from Summar, M and Tuchman, M,
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`New England Consortium of Metabolic Programs, Acute Illness Protocol: Urea Cycle Disorders: The
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`
`ORTIZ, M., et al., "Development of a Clinical Hepatic Encephalopathy Staging Scale," Aliment
`Pharmacol Ther 26:859-867 (2007).
`
`PAR PHARMACEUTICAL, INC.'S INITIAL INVALIDITY CONTENTIONS AND NON-INFRINGEMENT
`CONTENTIONS FOR U.S. PATENT NOS. 8,404,215 AND 8,642,012
`
`PARSONS-SMITH, B. G., et al., "The Electroencephalograph in Liver Disease," Lancet 273:867-871
`(1957).
`
`I Examiner
`
`Signature
`
`Date
`Considered
`
`* EXAMINER. ln111allf reference considered, whether or not c11a11on 1s 1n conformance With MPEP 609. Draw lme through c11a11on 1f notm conformance and not
`considered. Include copy of this form with next communication to applicant 1 Applicant's unique citation designation number (optional). 2 See Kinds Codes of
`USPTO Patent Documents at www.uspto.gov or MPEP 901.04. 3 Enter Office that issued the document, by the two-letter code (WI PO Standard ST.3). 4 For
`Japanese patent documents, the indication of the year of the reign of the Emperor must precede the serial number of the patent document 5 Kind of document by the
`appropriate symbols as indicated on the document under WI PO Standard ST.16 if possible. 6 Applicant is to place a check mark here if English language Translation
`is attached.
`This collection of information is required by 37 CFR 1.97 and 1 .98. The information is required to obtain or retain a benefit by the public which is to file (and by the
`USPTO to process) an application. Confidentiality is governed by 35 U.S.C. 122 and 37 CFR 1.14. This collection is estimated to take 2 hours to complete, including
`gathering, preparing, and submitting the completed application form to the USPTO. Time will vary depending upon the individual case. Any comments on the amount
`of time you require to complete this form and/or suggestions for reducing this burden, should be sent to the Chief Information Officer, U.S. Patent and Trademark
`Office, P.O. Box 1450, Alexandria, VA 22313-1450. DO NOT SEND FEES OR COMPLETED FORMS TO THIS ADDRESS. SEND TO: Commissioner for Patents,
`P.O. Box 1450, Alexandria, VA 22313-1450.
`
`4835-0776-7055.1
`
`If you need assistance in completing the form, call 1-800-PT0-9199 (1-800-786-9199) and select option 2.
`
`I
`
`Par Pharmaceutical, Inc. Ex. 1009
`Par v. Horizon, IPR of Patent No. 9,561,197
`Page 679 of 1354
`
`

`

`PTO/SB/08 (09-06)
`Approved for use through 03/31/2007. OMB 0651-0031
`U.S. Patent and Trademark Office: U.S. DEPARTMENT OF COMMERCE
`Under the Paperwork Reduction Act of 1995, no persons are required to respond to a collection of information unless it contains a valid OMB
`control number
`r
`Substitute for form 1449/PTO
`INFORMATION DISCLOSURE
`STATEMENT BY APPLICANT
`
`Date Submitted: March 12, 2012
`
`(use as many sheets as necessary)
`I of 110
`~heet Is
`
`Application Number
`Filing Date
`First Named Inventor
`Art Unit
`Examiner Name
`Attorney Docket Number
`
`Complete if Known
`13/610,580
`September 11, 2012
`Bruce Scharschmidt
`1629
`Sara Elizabeth Townsley
`HOR0027-201-US
`
`~
`
`~
`
`T6
`
`Exami
`ner
`Initials*
`
`Cite
`No. 1
`
`D72
`
`NON PATENT LITERATURE DOCUMENTS
`Include name of the author (in CAPITAL LETTERS), title of the article (when appropriate), title of the
`item (book, magazine, journal, serial, symposium, catalog, etc.) date, page(s), volume-issue
`number(s), publisher, city and/or country where published.
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`
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`Summar, M., Current Strategies for the Management of Neonatal Urea Cycle Disorders, 138 J.
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`
`Summar, M. and Tuchman, M., Proceedings of a Consensus Conference for the Management of
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`D83
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`Summar, M., Urea Cycle Disorders Overview, Gene Reviews, www.genetests.org (Apr. 2003).
`
`I Examiner
`
`Signature
`
`Date
`Considered
`
`* EXAMINER. ln111allf reference considered, whether or not c11a11on 1s 1n conformance With MPEP 609. Draw lme through c11a11on 1f notm conformance and not
`considered. Include copy of this form with next communication to applicant 1 Applicant's unique citation designation number (optional). 2 See Kinds Codes of
`USPTO Patent Documents at www.uspto.gov or MPEP 901.04. 3 Enter Office that issued the document, by the two-letter code (WI PO Standard ST.3). 4 For
`Japanese patent documents, the indication of the year of the reign of the Emperor must precede the serial number of the patent document 5 Kind of document by the
`appropriate symbols as indicated on the document under WI PO Standard ST.16 if possible. 6 Applicant is to place a check mark here if English language Translation
`is attached.
`This collection of information is required by 37 CFR 1.97 and 1 .98. The information is required to obtain or retain a benefit by the public which is to file (and by the
`USPTO to process) an application. Confidentiality is governed by 35 U.S.C. 122 and 37 CFR 1.14. This collection is estimated to take 2 hours to complete, including
`gathering, preparing, and submitting the completed application form to the USPTO. Time will vary depending upon the individual case. Any comments on the amount
`of time you require to complete this form and/or suggestions for reducing this burden, should be sent to the Chief Information Officer, U.S. Patent and Trademark
`Office, P.O. Box 1450, Alexandria, VA 22313-1450. DO NOT SEND FEES OR COMPLETED FORMS TO THIS ADDRESS. SEND TO: Commissioner for Patents,
`P.O. Box 1450, Alexandria, VA 22313-1450.
`
`4835-0776-7055.1
`
`If you need assistance in completing the form, call 1-800-PT0-9199 (1-800-786-9199) and select option 2.
`
`I
`
`Par Pharmaceutical, Inc. Ex. 1009
`Par v. Horizon, IPR of Patent No. 9,561,197
`Page 680 of 1354
`
`

`

`PTO/SB/08 (09-06)
`Approved for use through 03/31/2007. OMB 0651-0031
`U.S. Patent and Trademark Office: U.S. DEPARTMENT OF COMMERCE
`Under the Paperwork Reduction Act of 1995, no persons are required to respond to a collection of information unless it contains a valid OMB
`control number
`r
`Substitute for form 1449/PTO
`INFORMATION DISCLOSURE
`STATEMENT BY APPLICANT
`
`Date Submitted: March 12, 2012
`
`(use as many sheets as necessary)
`I of 110
`
`~heet 19
`
`Application Number
`Filing Date
`First Named Inventor
`Art Unit
`Examiner Name
`Attorney Docket Number
`
`Complete if Known
`13/610,580
`September 11, 2012
`Bruce Scharschmidt
`1629
`Sara Elizabeth Townsley
`HOR0027-201-US
`
`~
`
`~
`
`T6
`
`Exami
`ner
`Initials*
`
`Cite
`No. 1
`
`D84
`
`NON PATENT LITERATURE DOCUMENTS
`Include name of the author (in CAPITAL LETTERS), title of the article (when appropriate), title of the
`item (book, magazine, journal, serial, symposium, catalog, etc.) date, page(s), volume-issue
`number(s), publisher, city and/or country where published.
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`UNITED STATES PATENT AND TRADEMARK OFFICE, International Search Report and Written
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`UNITED STATES PATENT AND TRADEMARK OFFICE, International Search Report and Written
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`Wilson, C.J., et al., Plasma Glutamine and Ammonia Concentrations in Ornithine
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`
`I Examiner
`
`Signature
`
`Date
`Considered
`
`* EXAMINER. ln111allf reference considered, whether or not c11a11on 1s 1n conformance With MPEP 609. Draw lme through c11a11on 1f notm conformance and not
`considered. Include copy of this form with next communication to applicant 1 Applicant's unique citation designation number (optional). 2 See Kinds Codes of
`USPTO Patent Documents at www.uspto.gov or MPEP 901.04. 3 Enter Office that issued the document, by the two-letter code (WI PO Standard ST.3). 4 For
`Japanese patent documents, the indication of the year of the reign of the Emperor must precede the serial number of the patent document 5 Kind of document by the
`appropriate symbols as indicated on the document under WI PO Standard ST.16 if possible. 6 Applicant is to place a check mark here if English language Translation
`is attached.
`This collection of information is required by 37 CFR 1.97 and 1 .98. The information is required to obtain or retain a benefit by the public which is to file (and by the
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`Office, P.O. Box 1450, Alexandria, VA 22313-1450. DO NOT SEND FEES OR COMPLETED FORMS TO THIS ADDRESS. SEND TO: Commissioner for Patents,
`P.O. Box 1450, Alexandria, VA 22313-1450.
`
`4835-0776-7055.1
`
`If you need assistance in completing the form, call 1-800-PT0-9199 (1-800-786-9199) and select option 2.
`
`I
`
`Par Pharmaceutical, Inc. Ex. 1009
`Par v. Horizon, IPR of Patent No. 9,561,197
`Page 681 of 1354
`
`

`

`PTO/SB/08 (09-06)
`Approved for use through 03/31/2007. OMB 0651-0031
`U.S. Patent and Trademark Office: U.S. DEPARTMENT OF COMMERCE
`Under the Paperwork Reduction Act of 1995, no persons are required to respond to a collection of information unless it contains a valid OMB
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`Substitute for form 1449/PTO
`INFORMATION DISCLOSURE
`STATEMENT BY APPLICANT
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`Date Submitted: March 12, 2012
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`(use as many sheets as necessary)
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`Complete if Known
`13/610,580
`September 11, 2012
`Bruce Scharschmidt
`1629
`Sara Elizabeth Townsley
`HOR0027-201-US
`
`~
`
`~
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`T6
`
`Exami
`ner
`Initials*
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`Cite
`No. 1
`
`D96
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`D97
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`D98
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`D99
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`NON PATENT LITERATURE DOCUMENTS
`Include name of the author (in CAPITAL LETTERS), title of the article (when appropriate), title of the
`item (book, magazine, journal, serial, symposium, catalog, etc.) date, page(s), volume-issue
`number(s), publisher, city and/or country where published.
`Wright, P., Review: Nitrogen Excretion: Three End Products, Many Physiological Roles, 198 J.
`Experimental Biology 273 (1995).
`
`Yajima, et al. Diurnal Fluctuations of Blood Ammonia Levels in Adult-Type Citrullinemia, 137 Tokohu
`J. Ex/ Med, 213-220 (1982)
`
`Yu, Ryan and Potter, Murray, Diagnosis of Urea Cycle Disorders in Adulthood: Late- Onset Carbamyl
`Phosphate Synthetase 1 Deficiency, 7 MUMJ 30 (201 0).
`
`Yudkoff, M. et al., In Vivo Nitrogen Metabolism in Ornithine Transcarbamylase Deficiency, 98 J. Clin.
`Invest. 2167 (1996).
`
`D100
`
`Zeitlin, P., Novel Pharmacologic Therapies for Cystic Fibrosis, 103 J. Clinical Investigation 447
`(1999).
`
`D1 01
`
`AHRENS, M. et al. (January 2001 ). "Consensus Statement From a Conference for the Management
`of Patients With Urea Cycle Disorders." Supp. Journal of Pediatrics 138(1 ):S1-S5.
`
`D102
`
`D103
`
`LEE, B. et al. (August 2008). "Preliminary Data on Adult Patients with Urea Cycle Disorders (UCD) in
`An Open-Label, Swirch-Over, Dose Escalation Study Comparing a New Ammonia Scavenger,
`Glyceryl Tri (4-Phenylbutyrate) [HPN-1 00], to Buphenyl® (Sodium Phenylbutyrate [PBA])", abstract
`presented at SSSIEM 2008, Lisbon, Portugal, one page.
`LEE, B. et al. (August 2008). "Preliminary Data on Adult Patients with Urea Cycle Disorders (UCD) in
`An Open-Label, Swirch-Over, Dose Escalation Study Comparing a New Ammonia Scavenger,
`Glyceryl Tri (4-Phenylbutyrate) [HPN-1 00], to Buphenyl® (Sodium Phenylbutyrate [PBA])", presented
`at SSSIEM 2008, Lisbon, Portugal, Poster, one page.
`
`I Examiner
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`Signature
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`Date
`Considered
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`* EXAMINER. ln111allf reference considered, whether or not c11a11on 1s 1n conformance With MPEP 609. Draw lme through c11a11on 1f notm conformance and not
`considered. Include copy of this form with next communication to applicant 1 Applicant's unique citation designation number (optional). 2 See Kinds Codes of
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`This collection of information is required by 37 CFR 1.97 and 1 .98. The information is required to obtain or retain a benefit by the public which is to file (and by the
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`Office, P.O. Box 1450, Alexandria, VA 22313-1450. DO NOT SEND FEES OR COMPLETED FORMS TO THIS ADDRESS. SEND TO: Commissioner for Patents,
`P.O. Box 1450, Alexandria, VA 22313-1450.
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`If you need assistance in completing the form, call 1-800-PT0-9199 (1-800-786-9199) and select option 2.
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`I
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`Par Pharmaceutical, Inc. Ex. 1009
`Par v. Horizon, IPR of Patent No. 9,561,197
`Page 682 of 1354
`
`

`

`PCT
`WORLD INTELLECTUAL PROPERTY ORGANIZATION
`International Bureau
`INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT)
`WO 94/22494
`(51) International Patent Classification 5 :
`(11) International Publication Number:
`A61K 49/02
`
`Al
`
`(43) International Publication Date:
`
`13 October 1994 (13.10.94)
`
`(21) International Application Number:
`
`PCT/US94/03256
`
`(22) International Filing Date:
`
`29 :March 1994 (29.03.94)
`
`(74) Agents: BOUDREAUX,. Gerald, J. et a!.; The du Pont Merck
`Pharmaceutical Company, Legal/Patent Records Center,
`1007 Market Street, Wilmington, DE 19898 (US).
`
`,.-"
`
`t!' s
`
`(30) Priority Data:
`08/040,336
`08/218,861
`
`30 March 1993 (30.03.93)
`28 March 1994 (28.03.94)
`
`us
`us
`
`(71) Applicant: THE DU PONT MERCK PHARMACET.mCAL
`COMPANY [US/US]; 1007 Market Street, Wilmington, DE
`19898 (US).
`
`(72) Inventors: DeGRADO, William, Frank; 502 Bancroft Road,
`Moylan, PA 19063-4207 (US). MOUSA, Shaker, Ahmed;
`4 Linden Circle, Lincoln University, PA 19352-8933 (US).
`SWORIN, Michael; 19 Mary Ella Drive, Newark, DE
`19711-5679 (US). BARRETT, John, Andrew; 46 Folt Run,
`West Groton, MA 01450 (US). EDWARDS, David, Scott;
`123 Farms Drive, Burlington, MA 01803 (US). HARRIS,
`Thomas, David; 56 Zion Hill Road, Salem, NH 03079 (US).
`RAJOPADHYE, Milind; 21 Honeysuckle Road, Westford,
`MA 01886-4038 (US). LIU, Shuang; 17 Judith Road,
`Chelmsford, MA 01824-4742 (US).
`
`(81) Designated States: AU, BB, BG, BR. BY, CA, CN, CZ, F1,
`GE, HU, JP, KG, KP, KR, KZ, LK, LV, MD, MG, MN,
`MW, NO, NZ, PL, RO, RU, SO, SI. SK. TJ, TT. VA. UZ,
`VN, European patent (AT, BE, CH, DE, DK. ES, FR, GB,
`GR, IE, IT, LU, MC, NL, PT, SE), OAPI patent (BF, BJ,
`CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG).
`
`Published
`With international search report.
`
`(54) Title: RADIOLABELED PLATELET GPIIb!IIIa RECEPTOR ANTAGONISTS AS IMAGING AGENTS FOR TiiE DIAGNOSIS
`OF TIIROMBOEMBOLIC DISORDERS
`
`(57) Abstract
`
`This invention provides novel radiopharma(cid:173)
`ceuticals that are radiolabeled cyclic compounds
`containing carbocyclic or heterocyclic ring systems
`which act as antagonists of the platelet glycoprotein ·
`Ilb/IIIa complex; to methods of using said radio(cid:173)
`pharmaceuticals as imaging agents for the diagnosis
`of arterial and venous thrombi; to novel reagents for
`the preparation of said radiophannaceuticals; and to
`kits comprising said reagents.
`
`Par Pharmaceutical, Inc. Ex. 1009
`Par v. Horizon, IPR of Patent No. 9,561,197
`Page 683 of 1354
`
`

`

`·-
`
`•
`
`FOR THE PURPOSES OF INFORMATION ONLY
`
`Codes used to identify States party to the PCT on the front pages of pamphlets publishing international
`applications under the PCT.
`
`AT
`AU
`BB
`BE
`BF
`BG
`BJ
`BR
`BY
`CA
`CF
`CG
`CB
`Cl
`CM
`CN
`cs
`cz
`DE
`DK
`ES
`Fl
`FR
`GA
`
`Auotria
`AUSiralia
`BarbadOII
`Belgium
`BumnaFuo
`Bu.lgsria
`Benin
`Brazil
`Belanls
`Canada
`Central African R.epubfu:
`Congo
`Switz:erlaod
`a.te d'hoin:
`OuDcroon
`China
`Czedloslovatia
`Czecll Republic:
`Germany
`Deomarlr;
`Spain
`FiDlaDd
`l"raalce
`Gabon
`
`GB
`GE
`GN
`GR
`HU
`IE
`IT
`JP
`KE
`KG
`KP
`
`KR
`KZ
`Ll
`LK
`LU
`LV
`MC
`MD
`MG
`ML
`MN
`
`United Kingdom
`Georgia
`Guino<:&
`On:o::e
`Hllllgary
`l.rela.od
`Italy
`Japaa
`Kenya
`Kyrgystan
`Democrllic People's Republic
`ofKo=
`Republic of Korea
`KazakbiiWl
`Liedltcuotcio
`Srt l.u*a
`LID.embou7;,
`l..otv1a
`MOOIICO
`Republic of Moldova
`Mad&g.....-
`M&li
`Mongolia
`
`MR
`MW
`NE
`NL
`NO
`NZ
`PL
`PT
`RO
`RU
`SD
`SE
`Sl
`SK
`SN
`TD
`TG
`TJ
`TT
`UA
`us
`uz
`
`'\~N
`
`Mauritania
`Malawi
`Niga:
`Nelhcrlallds
`Norway
`NewZealaod
`Poland
`Portugal
`Romonia
`Russian Fccla'alioo
`Sudan
`Swecleo
`Sto-na
`Slovakia
`Senegal
`Qad
`Toso
`Taj~
`1'rt1lidad aDd TobagO
`Vlaaine
`United Staleo of Am«toa
`Uzbeldltall
`VietNam
`
`\
`
`I
`
`Par Pharmaceutical, Inc. Ex. 1009
`Par v. Horizon, IPR of Patent No. 9,561,197
`Page 684 of 1354
`
`

`

`wo 94/22494
`
`PCT /US94/03256
`
`•
`
`I
`
`5
`
`10
`
`15
`
`20
`
`·-
`
`TITLE
`Radiolabeled Platelet GPIIb/IIIa Receptor Antagonists
`As Imaging Agents For The Diagnosis Of Thromboembolic
`Disorders
`
`•
`
`CROSS-REFERENCE TO RELATED APPLICATIONS
`The present application is a co