Materials Considered by S. David Kimball, Ph.D.
`
`Case: IPR2015-01836
`Patent No. 7,932,268
`
`Nickname
`CFAD Pet.
`
`Description
`Petition for Inter Partes Review of U.S. Patent No.
`8,618,135, dated August, 28, 2015.
`Institution of Inter Partes Review, IPR2015-01835,
`Institution
`dated March 7, 2016.
`Decision
`’268 Patent U.S. Patent No. 7,932,268
`’135 Patent U.S. Patent No. 8,618,135
`Zusman Dec. Declaration of Randall J. Zusman, M.D.
`Mayersohn
`Declaration of Michael Mayersohn, Ph.D.
`Dec.
`’915
`Provisional
`Pink Sheet
`2004
`
`Doc. No.
`Paper 1
`
`Paper 7
`
`Ex. 1001
`Ex. 10011
`Ex. 1002
`Ex. 1003
`
`Ex. 1006
`
`Ex. 1013
`
`U.S. Provisional Patent Application No. 60/550,915
`
`“Bayer/PPD Implitapide Development Follows
`Zetia Model”, THE PINK SHEET, Vol. 66, No. 7, p. 17
`(2004)
`Evan Stein, “Microsomal Triglyceride Transfer
`Protein (MTP) Inhibitor (implitapide) program”,
`Presentation Given at PPD’s Analyst Day (February
`5, 2004)
`Chang, et al., “Microsomal triglyceride transfer
`protein (MTP) inhibitors: Discovery of clinically
`active inhibitors using high-throughput screening
`and parallel synthesis paradigms”, CURRENT
`OPINION IN DRUG DISCOVERY & DEV., Vol. 5, No. 4,
`pp. 562-570 (2002)
`Chandler, et. al, “CP-346086: an MTP inhibitor that
`lowers plasma cholesterol,” JOURNAL OF LIPID
`RESEARCH, Vol. 44, pp.1887-1901 (2003)
`NDA No. 203858, Sponsor’s Background Package
`(October 17, 2012)
`“MTP inhibitor research discontinued”, THE PINK
`
`Ex. 1014
`
`Stein
`
`Ex. 1015
`
`Chang
`
`Ex. 1016
`
`Chandler
`
`Ex. 2002
`
`Ex. 2011
`
`Lomitapide
`NDA
`Pink Sheet
`
`
`1 This exhibit appears in the docket for related case IPR2015-01835.
`
`1
`
`
`
`
`
`
`
`
`
`PENN EX. 2033
`CFAD v. PENN
`IPR2015-01836
`
`
`
`Case: IPR2015-01836
`Patent No. 7,932,268
`
`Nickname
`CFAD Pet.
`
`Description
`Petition for Inter Partes Review of U.S. Patent No.
`8,618,135, dated August, 28, 2015.
`Institution of Inter Partes Review, IPR2015-01835,
`Institution
`dated March 7, 2016.
`Decision
`’268 Patent U.S. Patent No. 7,932,268
`’135 Patent U.S. Patent No. 8,618,135
`Zusman Dec. Declaration of Randall J. Zusman, M.D.
`Mayersohn
`Declaration of Michael Mayersohn, Ph.D.
`Dec.
`’915
`Provisional
`Pink Sheet
`2004
`
`Doc. No.
`Paper 1
`
`Paper 7
`
`Ex. 1001
`Ex. 10011
`Ex. 1002
`Ex. 1003
`
`Ex. 1006
`
`Ex. 1013
`
`U.S. Provisional Patent Application No. 60/550,915
`
`“Bayer/PPD Implitapide Development Follows
`Zetia Model”, THE PINK SHEET, Vol. 66, No. 7, p. 17
`(2004)
`Evan Stein, “Microsomal Triglyceride Transfer
`Protein (MTP) Inhibitor (implitapide) program”,
`Presentation Given at PPD’s Analyst Day (February
`5, 2004)
`Chang, et al., “Microsomal triglyceride transfer
`protein (MTP) inhibitors: Discovery of clinically
`active inhibitors using high-throughput screening
`and parallel synthesis paradigms”, CURRENT
`OPINION IN DRUG DISCOVERY & DEV., Vol. 5, No. 4,
`pp. 562-570 (2002)
`Chandler, et. al, “CP-346086: an MTP inhibitor that
`lowers plasma cholesterol,” JOURNAL OF LIPID
`RESEARCH, Vol. 44, pp.1887-1901 (2003)
`NDA No. 203858, Sponsor’s Background Package
`(October 17, 2012)
`“MTP inhibitor research discontinued”, THE PINK
`
`Ex. 1014
`
`Stein
`
`Ex. 1015
`
`Chang
`
`Ex. 1016
`
`Chandler
`
`Ex. 2002
`
`Ex. 2011
`
`Lomitapide
`NDA
`Pink Sheet
`
`
`1 This exhibit appears in the docket for related case IPR2015-01835.
`
`1
`
`
`
`
`
`
`
`
`
`PENN EX. 2033
`CFAD v. PENN
`IPR2015-01836
`
`
`
`Doc. No.
`
`Ex. 2018
`
`Ex. 2019
`
`Ex. 2020
`
`Ex. 2029
`Ex. 2036
`
`Ex. 2037
`
`Ex. 2038
`
`Ex. 2042
`
`Ex. 2059
`
`Ex. 2060
`
`Ex. 2061
`
`
`
`
`
`
`
`Description
`
`Nickname
`2000
`Mayersohn
`1980
`Jones
`
`SHEET (2000)
`Mayersohn, “Designing a dosing regimen,” DRUG
`THERAPY, Vol. 10, No. 10, pp. 99-102 (1980)
`Jones, et. al, “Comparative Dose Efficacy Study of
`Atorvastatin Versus Simvastatin, Pravastatin,
`Lovastatin, and Fluvastatin in Patients With
`Hypercholesterolemia (The CURVES Study),” THE
`AMERICAN JOURNAL OF CARDIOLOGY, Vol. 81, pp.
`582-87 (1998)
`Robl, et. al, “A Novel Series of Highly Potent
`Benzimidazole-Based Microsomal Triglyceride
`Transfer Protein Inhibitors,” JOURNAL OF
`MEDICINAL CHEMISTRY, Vol. 44, pp. 851-56 (2001)
`Curriculum Vitae for S. David Kimball, Ph.D.
`Lüllmann, et. al, “Lipidosis Induced by
`Amphiphillic Cationic Drugs”, BIOCHEMICAL
`PHARMACOLOGY, Vol. 27, pp. 1103-08 (1978)
`Ploemen, et. al, “Use of physiochemical calculation
`of pKa and CLogP to predict phospholipidosis-
`inducing potential: A case study with structurally
`related piperazines,” EXPERIMENTAL AND TOXIC
`PATHOLOGY, Vol. 55, pp. 347-55 (2004)
`Cavalli, et. al, “Toward a pharmacophore for drugs
`inducing the long QT syndrome: insights from a
`CoMFA study of HERG K(+) channel blockers,”
`JOURNAL OF MEDICINAL CHEMISTRY, Vol. 45, pp.
`3844-53 (2002) (Penn Ex. 2038, “Cavalli”)
`Pharmaceutical Product Development, Inc., Annual
`Report for the Fiscal Year Ending December 31,
`2005, SEC Form 10-K (2006)
`Albert, Xenobiosis: Food, Drugs and Poisons in the
`Human Body, Chapman & Hall (1987)
`Goodman Goodman, et. al., Goodman & Gilman’s The
`Pharmacological Basis of Therapeutics, MacMillan
`(1985) (Penn Ex. 2060, “Goodman”)
`van de Waterbeemd & Gifford “ADMET in silico
`modelling: towards prediction paradise?”, NATURE
`2
`
`Robl
`
`n/a
`Lüllmann
`
`Ploemen
`
`Cavalli
`
`PPD 10-K
`
`Albert
`
`van de
`Waterbeemd
`
`
`
`
`
`PENN EX. 2033
`CFAD v. PENN
`IPR2015-01836
`
`
`
`Doc. No.
`
`Ex. 2062
`
`Ex. 2063
`
`Ex. 2064
`
`Ex. 2065
`
`Ex. 2066
`
`Ex. 2067
`
`Ex. 2068
`
`Ex. 2069
`
`Ex. 2070
`
`
`
`
`
`
`
`Nickname
`
`Halliwell
`
`Fischer
`
`Mason
`
`Tristiani-
`Firouzi
`
`Curran
`
`Fermini
`
`Crumb
`
`Lo
`
`Description
`REVIEWS DRUG DISCOVERY, Vol 2, No. 3, pp. 192-
`204 (2003)
`Failed Drugs “35 FDA-Approved Prescription Drugs Later Pulled
`from the Market”, http://prescriptiondrugs.procon.
`org/view.resource.php?resourceID=005528, Last
`updated January 30, 2014
`Halliwell, “Cationic Amphiphilic Drug-Induced
`Phospholipidosis,” TOXICOLOGIC PATHOLOGY, Vol.
`25, pp. 53-60 (1997)
`Fischer et. al, “CAFCA: A Novel Tool for the
`Calculation of Amphiphilic Properties of Charged
`Drug Molecules,” CHIMIA, Vol. 54, pp. 640-45
`(2000)
`Mason, et. al, “Reevaluating Equilibrium and
`Kinetic Binding Parameters for Lipophilic Drugs
`Based on a Structural Model for Drug Interaction
`with Biological Membranes,” JOURNAL OF
`MEDICINAL CHEMISTRY, Vol. 34, pp. 869-77 (1991)
`Tristani-Firouzi, et. al, “Molecular Biology of K+
`Channels and Their Role in Cardiac Arrhythmias,”
`AMERICAN JOURNAL OF MEDICINE, Vol. 110, pp. 50-
`59 (2001)
`Curran, et. al, “A Molecular Basis for Cardiac
`Arrhythmia: HERG Mutations Cause Long QT
`Syndrome,” CELL, Vol. 80, pp. 795-803 (1995)
`Fermini & Fossa, “Pre-Clinical Assessment of
`Drug-Induced QT Interval Prolongation, Current
`Issues and Impact on Drug Discovery,” ANNUAL
`REPORTS IN MEDICINAL CHEMISTRY, Vol. 39, pp.
`323-33 (2004)
`Crumb & Cavero, “QT Interval Prolongation by
`Non-cardiovascular Drugs: Issues and Solutions for
`Novel Drug Development,” PHARMACEUTICAL
`SCIENCE & TECHNOLOGY TODAY, Vol. 2, pp. 270-80
`(1999)
`Lo, et. al, “Pharmacokinetics of losartan, an
`angiotensin II receptor antagonist, and its active
`3
`
`
`
`
`
`PENN EX. 2033
`CFAD v. PENN
`IPR2015-01836
`
`
`
`Doc. No.
`
`Nickname
`
`Ex. 2071
`
`Wilson
`
`Description
`metabolite EXP3174 in humans,” CLINICAL
`PHARMACOLOGY & THERAPEUTICS, Vol. 58, No. 6,
`pp. 641-49 (1995)
`Block & Beale, eds., Wilson and Grisvold’s
`Textbook of Organic Medicinal and Pharmaceutical
`chemistry, 11th Ed., Lippincott Williams & Wilkins,
`pp. 65-66 (2004)
`
`
`
`
`
`
`
`
`4
`
`
`
`
`
`PENN EX. 2033
`CFAD v. PENN
`IPR2015-01836
`
`
Accessing this document will incur an additional charge of $.
After purchase, you can access this document again without charge.
Accept $ Charge
Still Working On It
This document is taking longer than usual to download. This can happen if we need to contact the court directly to obtain the document and their servers are running slowly.
Give it another minute or two to complete, and then try the refresh button.
A few More Minutes ... Still Working
It can take up to 5 minutes for us to download a document if the court servers are running slowly.
Thank you for your continued patience.
This document could not be displayed.
We could not find this document within its docket. Please go back to the docket page and check the link. If that does not work, go back to the docket and refresh it to pull the newest information.
Your account does not support viewing this document.
You need a Paid Account to view this document. Click here to change your account type.
Your account does not support viewing this document.
Set your membership
status to view this document.
With a Docket Alarm membership, you'll
get a whole lot more, including:
- Up-to-date information for this case.
- Email alerts whenever there is an update.
- Full text search for other cases.
- Get email alerts whenever a new case matches your search.
One Moment Please
The filing “” is large (MB) and is being downloaded.
Please refresh this page in a few minutes to see if the filing has been downloaded. The filing will also be emailed to you when the download completes.
Your document is on its way!
If you do not receive the document in five minutes, contact support at support@docketalarm.com.
Sealed Document
We are unable to display this document, it may be under a court ordered seal.
If you have proper credentials to access the file, you may proceed directly to the court's system using your government issued username and password.
Access Government Site
